Target General Infomation
Target ID
T77913
Former ID
TTDS00086
Target Name
Histamine H1 receptor
Gene Name
HRH1
Synonyms
H1 Histamine receptor; Histamine receptor 1; HRH1
Target Type
Successful
Disease Allergic skin disorders [ICD10: L00-L99]
Allergic rhinitis [ICD9: 472.0, 477, 995.3; ICD10: J00, J30, J31.0, T78.4]
Anxiety disorder [ICD9: 300, 311; ICD10: F32, F40-F42]
Allergic conjunctivitis [ICD9: 204.0, 372.0, 372.14, 995.3; ICD10: C91.0, H10, H10.45, T78.4]
Allergic disorders; Itching; Nausea [ICD9: 698, 787, 787.0, 995.3; ICD10: L29, R11, T78.4]
Allergic rhinitis; Urticaria [ICD9: 477, 708; ICD10: J30, L50]
Allergy [ICD9: 995.3; ICD10: T78.4]
Asthma [ICD10: J45]
Anxiety disorder; Morning sickness [ICD9: 300, 643.0; ICD10: F40-F42, O21.0]
Allergic rhinitis; Urticaria; Pruritus [ICD9: 477, 708; ICD10: J30, L50]
Anesthesia [ICD9: 338; ICD10: R20.0]
Common cold; Allergies [ICD9: 460, 995.3; ICD10: J00, T78.4]
Depression [ICD9: 311; ICD10: F30-F39]
Dry cough [ICD10: R05]
Hypersensitivity reactions; Coughs; Common colds [ICD10: R05]
Hay fever [ICD9: 477; ICD10: J30]
Hay fever; Allergic rhinitis [ICD9:477, 472.0, 995.3; ICD10: J30, J00, J31.0, T78.4]
Hay fever; Cough [ICD9:477, 786.2; ICD10: J30, R05]
Insomnia [ICD9: 307.41, 307.42, 327.0, 780.51, 780.52; ICD10: F51.0, G47.0]
Insomnia; Anxiety disorder [ICD9:307.41, 307.42, 327.0, 780.51, 780.52, 300, 311; ICD10: F51.0, G47.0, F32, F40-F42]
Nasal congestion [ICD9: 478.19; ICD10: J34.89]
Nausea; Vomiting [ICD9: 787, 787.0; ICD10: R11]
Obesity [ICD9: 278; ICD10: E66]
Ocular allergy [ICD9: 360-379; ICD10: H00-H59]
Pruritus [ICD9: 698; ICD10: L29]
Pain [ICD9: 338, 356.0, 356.8,780; ICD10: G64, G90.0, R52, G89]
Parkinson's disease [ICD9: 332; ICD10: G20]
Perennial and seasonal allergic rhinitis; Vasomotor rhinitis; Allergic conjunctivitis [ICD10: H10]
Respiratory allergies; Allergic rhinitis [ICD9:460-519, 472.0, 477, 995.3; ICD10: J00-J99, J00, J30, J31.0, T78.4]
Respiratory allergies; Cancer [ICD9:460-519, 140-229; ICD10: J00-J99, C00-C96]
Rhinitis [ICD9: 472.0, 477; ICD10: J00, J30, J31.0]
Respiratory disease [ICD10: J00-J99]
Rhinitis; Urticaria; Allergy [ICD10: J00, J30, J31.0, L50, T78.4]
Seasonal and perennial allergic rhinitis and vasomotor rhinitis [ICD10: J30]
Sleep disorders [ICD9: 307.4, 327, 780.5; ICD10: F51, G47]
Vertigo meniere's disease [ICD9: 386.0, 438.85, 780.4; ICD10: H81, H81.0, R42]
Vertigo's disease; Meniere's disease [ICD10: H81.09]
Unspecified [ICD code not available]
Function
In peripheral tissues, the H1 subclass of histamine receptors mediates the contraction of smooth muscles, increase in capillary permeability due to contraction of terminal venules, and catecholamine release from adrenal medulla, as well as mediating neurotransmission in the central nervous system.
BioChemical Class
GPCR rhodopsin
Target Validation
T77913
UniProt ID
Sequence
MSLPNSSCLLEDKMCEGNKTTMASPQLMPLVVVLSTICLVTVGLNLLVLYAVRSERKLHT
VGNLYIVSLSVADLIVGAVVMPMNILYLLMSKWSLGRPLCLFWLSMDYVASTASIFSVFI
LCIDRYRSVQQPLRYLKYRTKTRASATILGAWFLSFLWVIPILGWNHFMQQTSVRREDKC
ETDFYDVTWFKVMTAIINFYLPTLLMLWFYAKIYKAVRQHCQHRELINRSLPSFSEIKLR
PENPKGDAKKPGKESPWEVLKRKPKDAGGGSVLKSPSQTPKEMKSPVVFSQEDDREVDKL
YCFPLDIVHMQAAAEGSSRDYVAVNRSHGQLKTDEQGLNTHGASEISEDQMLGDSQSFSR
TDSDTTTETAPGKGKLRSGSNTGLDYIKFTWKRLRSHSRQYVSGLHMNRERKAAKQLGFI
MAAFILCWIPYFIFFMVIAFCKNCCNEHLHMFTIWLGYINSTLNPLIYPLCNENFKKTFK
RILHIRS
Drugs and Mode of Action
Drug(s) (S)-(+)-Dimethindene maleate Drug Info Approved Pruritus [1]
Aceprometazine Drug Info Approved Sleep disorders [2]
Acrivastine Drug Info Approved Allergic rhinitis [3]
Alcaftadine Drug Info Approved Allergic conjunctivitis [4], [5]
Antazoline Drug Info Approved Nasal congestion [6], [7]
Azatadine Drug Info Approved Allergic rhinitis [8], [9]
Azelastine Drug Info Approved Allergic conjunctivitis [10], [11]
Bepotastine Drug Info Approved Allergic rhinitis; Urticaria; Pruritus [10], [12]
Bromodiphenhydramine Drug Info Approved Hay fever; Cough [13], [14], [15]
Brompheniramine Drug Info Approved Allergic rhinitis [16], [17]
Buclizine Drug Info Approved Nausea; Vomiting [18], [19]
Carbinoxamine Drug Info Approved Seasonal and perennial allergic rhinitis and vasomotor rhinitis [15]
Cetirizine Drug Info Approved Allergic rhinitis [3], [20]
Chlophedianol Drug Info Approved Dry cough [15]
Chlorpheniramine Drug Info Approved Allergic rhinitis; Urticaria [21], [22]
Cinnarizine Drug Info Approved Vertigo meniere's disease [23]
Clemastine Drug Info Approved Allergic rhinitis [24], [25]
Cyclizine Drug Info Approved Nausea; Vomiting [26], [27]
Cyproheptadine Drug Info Approved Perennial and seasonal allergic rhinitis; Vasomotor rhinitis; Allergic conjunctivitis [15]
Desloratadine Drug Info Approved Allergic rhinitis [28], [29]
Dexbrompheniramine Drug Info Approved Hay fever; Allergic rhinitis [30], [31], [15]
Dexchlorpheniramine Maleate Drug Info Approved Rhinitis; Urticaria; Allergy [15]
Dimenhydrinate Drug Info Approved Nausea; Vomiting [32]
Dimethindene Drug Info Approved Respiratory allergies; Allergic rhinitis [1], [15]
Diphenhydramine Drug Info Approved Vertigo's disease; Meniere's disease [15]
Diphenylpyraline Drug Info Approved Allergic rhinitis [33], [34]
Doxepin Drug Info Approved Depression [35], [36]
Doxylamine Drug Info Approved Anxiety disorder; Morning sickness [37], [38]
Emedastine Drug Info Approved Allergic conjunctivitis [10], [39]
Epinastine Drug Info Approved Allergic conjunctivitis [10], [40]
Ergotidine Drug Info Approved Respiratory allergies; Cancer [41], [42], [15]
Ethopropazine Drug Info Approved Parkinson's disease [43], [44]
Fexofenadine Drug Info Approved Allergic rhinitis [45], [3]
Hydroxyzine Drug Info Approved Anxiety disorder [46], [47]
Ketotifen Drug Info Approved Allergic conjunctivitis [10], [48]
Levocabastine Drug Info Approved Allergic conjunctivitis [10], [49]
Levocetirizine dihydrochloride Drug Info Approved Allergic rhinitis [50], [51]
Loratadine Drug Info Approved Allergy [28], [52]
Mepyramine Drug Info Approved Allergy [53], [54]
Mepyramine maleate Drug Info Approved Allergy [53]
Mequitazine Drug Info Approved Allergic rhinitis [55]
Methdilazine Drug Info Approved Allergic rhinitis [56], [57]
Mizolastine Drug Info Approved Allergic rhinitis [58]
Olopatadine Drug Info Approved Allergic conjunctivitis [10], [59]
Oxatomide Drug Info Approved Hay fever [60]
Pemirolast Drug Info Approved Allergic conjunctivitis [10], [61], [15]
Phenindamine Drug Info Approved Common cold; Allergies [62]
Pheniramine Drug Info Approved Hay fever [10], [63]
Promethazine Drug Info Approved Allergic disorders; Itching; Nausea [64], [65]
Propiomazine Drug Info Approved Insomnia; Anxiety disorder [66], [67], [15]
Pyrilamine Maleate Drug Info Approved Headache [60], [68]
Tranilast Drug Info Approved Ocular allergy [10], [69]
Trimeprazine Drug Info Approved Allergic rhinitis [70], [71]
Tripelennamine Drug Info Approved Hypersensitivity reactions; Coughs; Common colds [15]
Triprolidine Drug Info Approved Hay fever [72], [73]
RUPATADINE Drug Info Phase 4 Discovery agent [74]
AC-170 Drug Info Phase 3 Allergic conjunctivitis [75]
Carebastine Drug Info Phase 3 Ocular allergy [10]
Olopatadine Drug Info Phase 3 Ocular allergy [10], [59]
E-4716 Drug Info Phase 2 Respiratory disease [76]
LY-2624803 Drug Info Phase 2 Insomnia [77]
Noberastine Drug Info Phase 2 Asthma [78]
OBE-101 Drug Info Phase 2 Obesity [79]
UCB-35440 Drug Info Phase 2 Rhinitis [80]
Vapitadine Drug Info Phase 2 Allergic skin disorders [81]
Astemizole Drug Info Withdrawn from market Allergic rhinitis [3], [82]
Chlophedianol Drug Info Withdrawn from market Anesthesia [83], [84]
Terfenadine Drug Info Withdrawn from market Allergy [3], [85]
Norastemizole Drug Info Discontinued in Preregistration Discovery agent [86]
GSK835726 Drug Info Discontinued in Phase 2 Allergic rhinitis [87]
HSR-609 Drug Info Discontinued in Phase 2 Rhinitis [88]
Loratadine Drug Info Discontinued in Phase 2 Allergic rhinitis [89]
Mequitamium iodide Drug Info Discontinued in Phase 2 Asthma [90]
ReN-1869 Drug Info Discontinued in Phase 2 Pain [91]
SUN-1334H Drug Info Discontinued in Phase 2 Allergic rhinitis [92]
AZD-1744 Drug Info Discontinued in Phase 1 Asthma [93]
GSK1004723 Drug Info Discontinued in Phase 1 Allergic rhinitis [94]
KA-398 Drug Info Terminated Asthma [95]
Selenotifen Drug Info Terminated Asthma [96]
SUN-1334H Drug Info Investigative Unspecified [97]
Antagonist (+)-cis-H2-PAT Drug Info [98]
(+)-trans-H2-PAT Drug Info [98]
(+/-)-cis-H2-PAT Drug Info [98]
(+/-)-trans-H2-PAT Drug Info [98]
(-)-trans-H2-PAT Drug Info [98]
(S)-(+)-Dimethindene maleate Drug Info [99], [1], [100], [68]
(S)-cetirizine Drug Info [101]
9-OH-risperidone Drug Info [102]
AC-170 Drug Info [103]
Aceprometazine Drug Info [104]
Acrivastine Drug Info [105], [106]
Alcaftadine Drug Info [4]
Antazoline Drug Info [107], [108], [109], [106]
arpromidine Drug Info [110]
Astemizole Drug Info [109], [111]
Azatadine Drug Info [112]
Azelastine Drug Info [60], [113]
Bepotastine Drug Info [114]
Bromodiphenhydramine Drug Info [115]
Brompheniramine Drug Info [116]
BU-E 47 Drug Info [110]
Buclizine Drug Info [117]
Carbinoxamine Drug Info [118]
Carebastine Drug Info [10]
Cetirizine Drug Info [119], [120]
Chlophedianol Drug Info [121]
Chlorpheniramine Drug Info [122], [60], [68]
Cinnarizine Drug Info [123], [124]
Clemastine Drug Info [125], [126]
Cyclizine Drug Info [127], [128], [129]
Cyproheptadine Drug Info [130], [131]
Desloratadine Drug Info [132], [133]
Dexbrompheniramine Drug Info [134]
Dimenhydrinate Drug Info [135], [136]
Dimethindene Drug Info [99], [1], [100], [68]
Diphenhydramine Drug Info [137], [60]
Diphenylpyraline Drug Info [138]
Doxylamine Drug Info [139], [140]
Emedastine Drug Info [141]
Epinastine Drug Info [142]
Fexofenadine Drug Info [119], [132]
GSK1004723 Drug Info [143]
GSK835726 Drug Info [143]
HSR-609 Drug Info [144], [15]
Hydroxyclemastine Drug Info [125], [126]
Hydroxyzine Drug Info [145], [146]
impromidine Drug Info [147]
Ketotifen Drug Info [148], [60]
Levocabastine Drug Info [149], [150]
Levocetirizine dihydrochloride Drug Info [148], [60], [132]
Loratadine Drug Info [151], [152], [153]
Mepyramine Drug Info [120], [154], [53]
Mepyramine maleate Drug Info [120], [154], [53]
Mequitazine Drug Info [155]
Methdilazine Drug Info [156]
Mizolastine Drug Info [157]
Noberastine Drug Info [158]
Olopatadine Drug Info [10]
Oxatomide Drug Info [149], [60]
Pemirolast Drug Info [159]
Phenindamine Drug Info [160]
Pheniramine Drug Info [161]
Promethazine Drug Info [60], [68]
Propiomazine Drug Info [162]
Pyrilamine Maleate Drug Info [60], [68]
ReN-1869 Drug Info [163]
SUN-1334H Drug Info [97]
Terfenadine Drug Info [164], [153]
Tranilast Drug Info [10]
Trimeprazine Drug Info [165]
Tripelennamine Drug Info [166], [167], [168], [169]
Triprolidine Drug Info [170]
Vapitadine Drug Info [171]
[11C]doxepin Drug Info [172]
[11C]pyrilamine Drug Info [173]
Inhibitor 1-(4-p-Tolyl-butyl)-piperidine Drug Info [174]
1-[(Furan-2(5H)-one)-4-methyl]-desloratadine Drug Info [175]
2-(9,10-dihydroanthracen-9-yl)-N-methylethanamine Drug Info [176]
3,3-diphenylpropan-1-amine Drug Info [176]
4,4-Diphenylbutan-1-amine Drug Info [176]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one Drug Info [177]
9-(2-aminoethyl)-9,10-dihydroanthracene Drug Info [176]
9-(2-aminopropyl)-9,10-dihydroanthracene Drug Info [176]
9-(Aminomethyl)-9,10-dihydroanthracene Drug Info [176]
9-Phenyl-2,3-dihydro-1H-indeno[2,1-c]pyridine Drug Info [178]
DIMEBOLIN Drug Info [179]
Diphenyl(piperidin-4-yl)methanol Drug Info [174]
Doxepin Drug Info [180]
KF-A6 Drug Info [181]
MDL-28163 Drug Info [182]
N,N-dimethyl-2,2-diphenylethanamine Drug Info [176]
N,N-Dimethyl-3,3-diphenylpropan-1-amine Drug Info [176]
N,N-dimethyl-4,4-diphenylbutan-1-amine Drug Info [176]
N-hydroxycarbamate derivative Drug Info [183]
N-methyl-3,3-diphenylpropan-1-amine Drug Info [176]
N-methyl-4,4-diphenylbutan-1-amine Drug Info [176]
OCTOCLOTHEPIN Drug Info [184]
R-226161 Drug Info [185]
R-dimethindene Drug Info [186]
RUPATADINE Drug Info [182]
VUF-10148 Drug Info [187]
Agonist 2-(2-thiazolyl)ethanamine Drug Info [110]
2-(3-bromophenyl)histamine Drug Info [110]
2-(3-chlorophenyl)histamine Drug Info [110]
2-(3-iodophenyl)histamine Drug Info [110]
2-pyridylethylamine Drug Info [101]
8R-Lisuride Drug Info [188]
dimethylhistaprodifen Drug Info [110]
Ergotidine Drug Info [41]
histaprodifen Drug Info [189]
methylhistaprodifen Drug Info [110]
oxo-arpromidine Drug Info [147]
S-(-)-Lisuride Drug Info [188]
UR-PG131A Drug Info [147]
UR-PG146 Drug Info [147]
UR-PG153 Drug Info [147]
UR-PG55B Drug Info [147]
Modulator AZD-1744 Drug Info [190]
Dexchlorpheniramine Maleate Drug Info [191]
E-4716 Drug Info [76]
Ethopropazine Drug Info [191]
KA-398 Drug Info [173]
LY-2624803 Drug Info [192]
Mequitamium iodide Drug Info [193]
Norastemizole Drug Info
OBE-101 Drug Info [194]
Selenotifen Drug Info [195]
UCB-35440 Drug Info [196]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway Calcium signaling pathway
Neuroactive ligand-receptor interaction
Inflammatory mediator regulation of TRP channels
PANTHER Pathway Histamine H1 receptor mediated signaling pathway
Reactome Histamine receptors
G alpha (q) signalling events
WikiPathways Monoamine GPCRs
GPCRs, Class A Rhodopsin-like
IL-4 Signaling Pathway
Gastrin-CREB signalling pathway via PKC and MAPK
GPCR ligand binding
GPCR downstream signaling
References
REF 1Prescription and safety of dimethindene maleate micropellet capsules in Hungary. Orv Hetil. 2004 Feb 15;145(7):327-9.
REF 2Drug information of Aceprometazine, 2008. eduDrugs.
REF 3Comparative tolerability of second generation antihistamines. Drug Saf. 1999 May;20(5):385-401.
REF 4Mullard A: 2010 FDA drug approvals. Nat Rev Drug Discov. 2011 Feb;10(2):82-5.
REF 5(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7587).
REF 6FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 018746.
REF 7(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7116).
REF 8FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 017601.
REF 9(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7119).
REF 10Emerging drugs for ocular allergy. Expert Opin Emerg Drugs. 2005 Aug;10(3):505-20.
REF 11(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7121).
REF 12(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7466).
REF 13FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 009319.
REF 14(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7132).
REF 15Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
REF 16FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 083821.
REF 17(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7133).
REF 18(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7134).
REF 19Drug information of Buclizine, 2008. eduDrugs.
REF 20(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 1222).
REF 21FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 070797.
REF 22(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6976).
REF 23Drug information of Cinnarizine, 2008. eduDrugs.
REF 24FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 073283.
REF 25(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6063).
REF 26FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 009495.
REF 27(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7151).
REF 28Desloratadine treatment for intermittent and persistent allergic rhinitis: a review. Clin Ther. 2007 Sep;29(9):1795-802.
REF 29(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7157).
REF 30FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 089116.
REF 31(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7588).
REF 32FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 040519.
REF 33(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7165).
REF 34Drug information of Diphenylpyraline, 2008. eduDrugs.
REF 35Emerging treatments for depression. Expert Opin Pharmacother. 2006 Dec;7(17):2323-39.
REF 36(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 1225).
REF 37FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 040167.
REF 38(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7171).
REF 39(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7174).
REF 40(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7176).
REF 41Cloning and pharmacological characterization of a fourth histamine receptor (H(4)) expressed in bone marrow. Mol Pharmacol. 2001 Mar;59(3):420-6.
REF 42(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 1247).
REF 43Drugs used to treat Parkinson's disease, present status and future directions. CNS Neurol Disord Drug Targets. 2008 Oct;7(4):321-42.
REF 44(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7181).
REF 45(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 4819).
REF 46FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 085551.
REF 47(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7199).
REF 48(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7206).
REF 49(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 1586).
REF 50FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 022064.
REF 51(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 1214).
REF 52(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7216).
REF 53Antinociception induced by central administration of histamine in the formalin test in rats. Indian J Physiol Pharmacol. 2008 Jul-Sep;52(3):249-54.
REF 54(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 1220).
REF 55Drug information of Mequitazine, 2008. eduDrugs.
REF 56(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7231).
REF 57Drug information of Methdilazine, 2008. eduDrugs.
REF 58Population pharmacokinetic analysis and optimization of the experimental design for mizolastine solution in children. J Pharmacokinet Pharmacodyn. 2001 Jun;28(3):299-319.
REF 59(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7249).
REF 60Intact cell binding for in vitro prediction of sedative and non-sedative histamine H1-receptor antagonists based on receptor internalization. J Pharmacol Sci. 2008 May;107(1):66-79. Epub 2008 Apr 29.
REF 61(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7329).
REF 62Drug information of Phenindamine, 2008. eduDrugs.
REF 63(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7267).
REF 64FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 089013.
REF 65(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7282).
REF 66FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 012382.
REF 67(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7284).
REF 68Inhibition by histamine H1 receptor antagonists of endogenous glibenclamide-sensitive K+ channels in follicle-enclosed Xenopus oocytes. Eur J Pharmacol. 1994 Jan 1;266(1):99-102.
REF 69(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6326).
REF 70(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7237).
REF 71Drug information of Trimeprazine, 2008. eduDrugs.
REF 72Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77. Epub 2007 Feb 20.
REF 73(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 1228).
REF 74ClinicalTrials.gov (NCT00258141) Study With Rupatadine in Mosquito-Bite Allergic Adult Subjects. U.S. National Institutes of Health.
REF 75ClinicalTrials.gov (NCT02132169) A Multi-Center Study Evaluating the Safety of AC-170 0.24%. U.S. National Institutes of Health.
REF 76Population pharmacokinetics of epinastine, a histamine H1 receptor antagonist, in adults and children. Br J Clin Pharmacol. 2005 Jan;59(1):43-53.
REF 77ClinicalTrials.gov (NCT00784875) An Efficacy Study of Compound LY2624803 in the Treatment of Patients With Chronic Insomnia. U.S. National Institutes of Health.
REF 78Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001178)
REF 79ClinicalTrials.gov (NCT00409305) The Effect of Betahistine on Body Weight in Obese Subjects. U.S. National Institutes of Health.
REF 80Clinical pipeline report, company report or official report of UCB.
REF 81Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800020866)
REF 82(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 2603).
REF 83(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7324).
REF 84Drug information of Chlophedianol, 2008. eduDrugs.
REF 85(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 2608).
REF 86Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007228)
REF 87Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800028154)
REF 88Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005369)
REF 89Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800015252)
REF 90Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000086)
REF 91Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800014046)
REF 92Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800026836)
REF 93Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800025772)
REF 94Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800028155)
REF 95Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007218)
REF 96Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001341)
REF 97Preclinical efficacy and safety pharmacology of SUN-1334H, a potent orally active antihistamine agent. Drugs R D. 2008;9(2):93-112.
REF 98J Pharmacol Exp Ther. 2002 Jul;302(1):328-36.A novel phenylaminotetralin radioligand reveals a subpopulation of histamine H(1) receptors.
REF 99Effects of dimethindene maleate nasal spray on the quality of life in seasonal allergic rhinitis. Rhinology. 2003 Sep;41(3):159-66.
REF 100Analytical method for simultaneously measuring ex vivo drug receptor occupancy and dissociation rate: application to (R)-dimethindene occupancy of central histamine H1 receptors. J Recept Signal Transduct Res. 2009;29(2):84-93.
REF 101Large-scale overproduction, functional purification and ligand affinities of the His-tagged human histamine H1 receptor. Eur J Biochem. 2004 Jul;271(13):2636-46.
REF 102Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding. Psychopharmacology (Berl). 1996 Mar;124(1-2):57-73.
REF 103Clinical pipeline report, company report or official report of NicOx SA.
REF 104Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34.
REF 105Clinical pharmacology of new histamine H1 receptor antagonists. Clin Pharmacokinet. 1999 May;36(5):329-52.
REF 106Nonsedating histamine H1-receptor antagonists. Clin Pharm. 1989 May;8(5):331-44.
REF 107A current appreciation of sites for pharmacological intervention in allergic conjunctivitis: effects of new topical ocular drugs. Acta Ophthalmol Scand Suppl. 1999;(228):33-7.
REF 108Influence of antazoline and ketotifen on the anticonvulsant activity of conventional antiepileptics against maximal electroshock in mice. Eur Neuropsychopharmacol. 2004 Aug;14(4):307-18.
REF 109Histamine and the convulsive threshold or effectiveness of antiepileptic drugs. Przegl Lek. 2008;65(11):803-6.
REF 110Multiple differences in agonist and antagonist pharmacology between human and guinea pig histamine H1-receptor. J Pharmacol Exp Ther. 2003 Jun;305(3):1104-15. Epub 2003 Mar 6.
REF 111Histamine H1 receptor induces cytosolic calcium increase and aquaporin translocation in human salivary gland cells. J Pharmacol Exp Ther. 2009 Aug;330(2):403-12. Epub 2009 May 14.
REF 112Comparative effects of loratadine and azatadine in the treatment of seasonal allergic rhinitis. Asian Pac J Allergy Immunol. 1990 Dec;8(2):103-7.
REF 113The in vivo potency and selectivity of azelastine as an H1 histamine-receptor antagonist in human airways and skin. J Allergy Clin Immunol. 1988 Dec;82(6):1113-8.
REF 114Mast cells play a critical role in the pathogenesis of viral myocarditis. Circulation. 2008 Jul 22;118(4):363-72. Epub 2008 Jul 7.
REF 115Studies on synergism between penicillins and ambodryl (bromodiphenhydramine HCl), an antihistamine with antimicrobial property. Indian J Exp Biol. 1990 Mar;28(3):253-8.
REF 116Histamine-induced venodilation in human beings involves both H1 and H2 receptor subtypes. J Allergy Clin Immunol. 1994 Mar;93(3):606-14.
REF 117Toxicologic and clinical appraisal of buclizine, a new antihistaminic compound. J Allergy. 1956 Jan;27(1):63-7.
REF 118Comparison of the effects of eleven histamine H1-receptor antagonists on monoamine turnover in the mouse brain. Naunyn Schmiedebergs Arch Pharmacol. 1994 Feb;349(2):140-4.
REF 119Knockouts model the 100 best-selling drugs--will they model the next 100? Nat Rev Drug Discov. 2003 Jan;2(1):38-51.
REF 120Design, synthesis and histamine H1-receptor antagonistic activity of some novel 4-amino-2-(substituted)-5-(substituted) aryl-6-[(substituted aryl) amino] pyrimidines. Arzneimittelforschung. 2009;59(5):243-7.
REF 121Identification and differentiation of alkylamine antihistamines and their metabolites in urine by computerized gas chromatography-mass spectrometry. J Chromatogr. 1988 Aug 19;430(1):31-41.
REF 122Combined histamine H1 and H3 receptor blockade produces nasal decongestion in an experimental model of nasal congestion. Am J Rhinol. 1999 Sep-Oct;13(5):391-9.
REF 123Effects of calcium-antagonistic drugs on the stimulation by carbamoylcholine and histamine of phosphatidylinositol turnover in longitudinal smooth muscle of guinea-pig ileum. Biochem J. 1976 Nov 15;160(2):163-9.
REF 124Central effects of cinnarizine: restricted use in aircrew. Aviat Space Environ Med. 2002 Jun;73(6):570-4.
REF 125Stereoselective synthesis of (-)-hydroxyclemastine as a versatile intermediate for the H1 receptor antagonist clemastine. Arch Pharm Res. 2007 Dec;30(12):1521-5.
REF 126Histamine upregulates keratinocyte MMP-9 production via the histamine H1 receptor. J Invest Dermatol. 2008 Dec;128(12):2783-91. Epub 2008 Jun 12.
REF 127Comparison of cyclizine and ondansetron for the prevention of postoperative nausea and vomiting in laparoscopic day-case gynaecological surgery. Anaesthesia. 2002 Jan;57(1):61-5.
REF 128Histamine H1-receptor antagonists, promethazine and homochlorcyclizine, increase the steady-state plasma concentrations of haloperidol and reduced haloperidol. Ther Drug Monit. 2003 Apr;25(2):192-6.
REF 129Synthesis and combined H1-/H2 antagonist activity of mepyramine, pheniramine and cyclizine derivatives with cyanoguanidine, urea and nitroethenediamine partial structures. Arch Pharm (Weinheim). 1994Jul;327(7):455-62.
REF 130Antihistamines in the treatment of dermatitis. J Cutan Med Surg. 2003 Nov-Dec;7(6):467-73.
REF 131Cyproheptadine displays preclinical activity in myeloma and leukemia. Blood. 2008 Aug 1;112(3):760-9. Epub 2008 May 23.
REF 132Update on prescription and over-the-counter histamine inverse agonists in rhinitis therapy. Curr Allergy Asthma Rep. 2009 Mar;9(2):140-8.
REF 133Examining the tolerability of the non-sedating antihistamine desloratadine: a prescription-event monitoring study in England. Drug Saf. 2009;32(2):169-79. doi: 10.2165/00002018-200932020-00009.
REF 134H2 histaminergic control of inhibition of eating induced by intragastric NaCl in rats. Physiol Behav. 1998 Aug;65(1):105-13.
REF 135Mechanisms and abuse liability of the anti-histamine dimenhydrinate. Neurosci Biobehav Rev. 2002 Jan;26(1):61-7.
REF 136Histamine 1 receptor antagonist in symptomatic treatment of renal colic accompanied by nausea: two birds with one stone? Urology. 2009 Jan;73(1):32-6. Epub 2008 Oct 11.
REF 137Histamine as an autocrine regulator of leukemic cell proliferation. Leuk Lymphoma. 2000 Jan;36(3-4):367-73.
REF 138Transport mechanism of an H1-antagonist at the blood-brain barrier: transport mechanism of mepyramine using the carotid injection technique. Biol Pharm Bull. 1994 May;17(5):676-9.
REF 139Steady-state brain concentrations of antihistamines in rats: interplay of membrane permeability, P-glycoprotein efflux and plasma protein binding. Pharmacology. 2004 Oct;72(2):92-8.
REF 140First-generation H1 antihistamines found in pilot fatalities of civil aviation accidents, 1990-2005. Aviat Space Environ Med. 2007 May;78(5):514-22.
REF 141Emedastine difumarate: a review of its potential ameliorating effect for tissue remodeling in allergic diseases. Expert Opin Pharmacother. 2009 Aug;10(11):1859-67.
REF 142Influence of epinastine hydrochloride, an H1-receptor antagonist, on the function of mite allergen-pulsed murine bone marrow-derived dendritic cells in vitro and in vivo. Mediators Inflamm. 2009;2009:738038. Epub 2009 Apr 9.
REF 143Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).
REF 144Studies on the novel antiallergic agent HSR-609: its penetration into the central nervous system in mice and guinea pigs and its selectivity for the histamine H1-receptor. Jpn J Pharmacol. 1997 Apr;73(4):291-8.
REF 145Physicochemical, pharmacological and pharmacokinetic properties of the zwitterionic antihistamines cetirizine and levocetirizine. Curr Med Chem. 2008;15(21):2173-91.
REF 146Hydroxyzine, a first generation H(1)-receptor antagonist, inhibits human ether-a-go-go-related gene (HERG) current and causes syncope in a patient with the HERG mutation. J Pharmacol Sci. 2008 Dec;108(4):462-71. Epub 2008 Dec 5.
REF 147Probing ligand-specific histamine H1- and H2-receptor conformations with NG-acylated Imidazolylpropylguanidines. J Pharmacol Exp Ther. 2006 Apr;317(1):139-46. Epub 2006 Jan 4.
REF 148Influence of chronic treatment with H1 receptor antagonists on the anticonvulsant activity of antiepileptic drugs. Pol J Pharmacol. 2001 Jan-Feb;53(1):93-6.
REF 149Effects of fexofenadine and other antihistamines on components of the allergic response: adhesion molecules. J Allergy Clin Immunol. 2003 Oct;112(4 Suppl):S78-82.
REF 150Contribution of alpha4beta1 integrin to the antiallergic effect of levocabastine. Biochem Pharmacol. 2008 Sep 15;76(6):751-62. Epub 2008 Jul 15.
REF 151Clinical research of Ibudilast on treating the steroid resistant allergic rhinitis. Lin Chung Er Bi Yan Hou Tou Jing Wai Ke Za Zhi. 2009 Jan;23(2):63-6.
REF 152Effect of descarboethoxyloratadine, the major metabolite of loratadine, on the human cardiac potassium channel Kv1.5. Br J Pharmacol. 1997 Nov;122(5):796-8.
REF 153Second-generation antihistamines: a comparative review. Drugs. 1999 Jan;57(1):31-47.
REF 154Receptor mediation and nociceptin inhibition of bradykinin-induced plasma extravasation in the knee joint of the rat. Inflamm Res. 2009 Jun 21.
REF 155Efficiency of mequitazine in the treatment of allergic rhinitis and chronic urticaria in children. A bibliographic systematic review. Rev Alerg Mex. 2008 Jan-Feb;55(1):3-9.
REF 156Effect of H1 blockers alone and in combination with morphine to produce antinociception in mice. Neuropharmacology. 1985 Jan;24(1):1-4.
REF 157Histamine H1-receptor antagonists inhibit nuclear factor-kappaB and activator protein-1 activities via H1-receptor-dependent and -independent mechanisms. Clin Exp Allergy. 2008 Jun;38(6):947-56.
REF 158A double-blind placebo controlled dose response study of noberastine on histamine induced weal and flare. Eur J Clin Pharmacol. 1991;40(1):83-5.
REF 159The effect of a combined therapy with a histamine H1 antagonist and a chemical mediator release inhibitor on allergic conjunctivitis. Ophthalmologica. 2008;222(4):232-9. Epub 2008 May 8.
REF 160The histamine H1-receptor antagonist binding site. A stereoselective pharmacophoric model based upon (semi-)rigid H1-antagonists and including a known interaction site on the receptor. J Med Chem. 1995 Aug 18;38(17):3351-60.
REF 161Role of central histaminergic system in lorazepam withdrawal syndrome in rats. Pharmacol Biochem Behav. 2001 Apr;68(4):777-82.
REF 162How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
REF 163ReN 1869, a novel tricyclic antihistamine, is active against neurogenic pain and inflammation. Eur J Pharmacol. 2002 Jan 18;435(1):43-57.
REF 164Small mouse cholangiocytes proliferate in response to H1 histamine receptor stimulation by activation of the IP3/CaMK I/CREB pathway. Am J Physiol Cell Physiol. 2008 Aug;295(2):C499-513. Epub 2008 May 28.
REF 165Effectiveness of alimemazine in controlling retching after Nissen fundoplication. J Pediatr Surg. 2005 Nov;40(11):1737-40.
REF 166Histamine H1 and H2 receptor antagonists accelerate skin barrier repair and prevent epidermal hyperplasia induced by barrier disruption in a dry environment. J Invest Dermatol. 2001 Feb;116(2):261-5.
REF 167Prostaglandin E2 aggravates gastric mucosal injury induced by histamine in rats through EP1 receptors. Life Sci. 2003 Dec 19;74(5):629-41.
REF 168Role of N-methyl-D-aspartate receptors in gastric mucosal blood flow induced by histamine. J Neurosci Res. 2004 Sep 1;77(5):730-8.
REF 169Involvement of histamine H1 and H2 receptors in the regulation of STAT-1 phosphorylation: inverse agonism exhibited by the receptor antagonists. Int Immunopharmacol. 2005 Jul;5(7-8):1299-309.
REF 170Histamine excites rat lateral vestibular nuclear neurons through activation of post-synaptic H2 receptors. Neurosci Lett. 2008 Dec 19;448(1):15-9. Epub 2008 Oct 14.
REF 171Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800020866)
REF 172Evaluation of in vivo selective binding of [11C]doxepin to histamine H1 receptors in five animal species. Nucl Med Biol. 2004 May;31(4):493-502.
REF 173(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 262).
REF 174Bioorg Med Chem Lett. 2009 Sep 1;19(17):5043-7. Epub 2009 Aug 5.Structural determinants for histamine H(1) affinity, hERG affinity and QTc prolongation in a series of terfenadine analogs.
REF 175Bioorg Med Chem. 2010 Feb 15;18(4):1626-32. Epub 2010 Jan 4.Stereoselective synthesis of desloratadine derivatives as antagonist of histamine.
REF 176Bioorg Med Chem. 2009 Sep 15;17(18):6496-504. Epub 2009 Aug 13.Synthesis, structure-affinity relationships, and modeling of AMDA analogs at 5-HT2A and H1 receptors: structural factors contributing to selectivity.
REF 177J Med Chem. 2010 Sep 9;53(17):6386-97.Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 receptor agonist with unprecedented selectivity and procognitive potential.
REF 178Bioorg Med Chem Lett. 2000 Jun 5;10(11):1277-9.Conformationally-restricted ligands for the histamine H1 receptor.
REF 179Bioorg Med Chem Lett. 2010 Jan 1;20(1):78-82. Epub 2009 Nov 14.Synthesis and biological activity of 5-styryl and 5-phenethyl-substituted 2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indoles.
REF 180Novel therapeutic usage of low-dose doxepin hydrochloride. Expert Opin Investig Drugs. 2007 Aug;16(8):1295-305.
REF 181Antimicrob Agents Chemother. 2007 Nov;51(11):4133-40. Epub 2007 Sep 10.Design, synthesis, and evaluation of 10-N-substituted acridones as novel chemosensitizers in Plasmodium falciparum.
REF 182J Med Chem. 2005 Oct 20;48(21):6523-43.Designed multiple ligands. An emerging drug discovery paradigm.
REF 183Bioorg Med Chem Lett. 2005 Feb 15;15(4):1083-5.5-Lipoxygenase inhibition by N-hydroxycarbamates in dual-function compounds.
REF 184J Med Chem. 2010 Oct 14;53(19):7021-34.Exploring the neuroleptic substituent in octoclothepin: potential ligands for positron emission tomography with subnanomolar affinity for |A(1)-adrenoceptors.
REF 185Bioorg Med Chem. 2007 Jun 1;15(11):3649-60. Epub 2007 Mar 21.Tricyclic isoxazolines: identification of R226161 as a potential new antidepressant that combines potent serotonin reuptake inhibition and alpha2-adrenoceptor antagonism.
REF 186J Med Chem. 2009 Sep 10;52(17):5307-10.Characterization of novel selective H1-antihistamines for clinical evaluation in the treatment of insomnia.
REF 187J Med Chem. 2008 Apr 24;51(8):2457-67. Epub 2008 Mar 22.Fragment based design of new H4 receptor-ligands with anti-inflammatory properties in vivo.
REF 1888R-lisuride is a potent stereospecific histamine H1-receptor partial agonist. Mol Pharmacol. 2004 Mar;65(3):538-49.
REF 189Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist. J Pharmacol Exp Ther. 2005 Sep;314(3):1310-21. Epub 2005 Jun 9.
REF 190Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
REF 191Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
REF 192Current Phase II investigational therapies for insomnia. Expert Opin Investig Drugs. 2015 Mar;24(3):401-11.
REF 193High-affinity binding of mequitamium iodide (LG 30435) to muscarinic and histamine H1 receptors. Eur J Pharmacol. 1990 Jul 17;182(3):413-20.
REF 194Betahistine in the treatment of M?ni?re's disease. Neuropsychiatr Dis Treat. 2007 August; 3(4): 429-440.
REF 195Effect of BN 52256 and other mediator antagonists on ouabain-induced cardiac arrhythmia in a model of anaphylaxis in guinea-pigs. Pharmacol Res. 1992 Feb-Mar;25(2):173-80.
REF 196The effect of a novel, dual function histamine H1 receptor antagonist/5-lipoxygenase enzyme inhibitor on in vivo dermal inflammation and extravasation. Eur J Pharmacol. 2005 Jan 4;506(3):265-71. Epub 2004 Dec 1.

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