Target Information
Target General Infomation | |||||
---|---|---|---|---|---|
Target ID |
T47094
|
||||
Former ID |
TTDS00194
|
||||
Target Name |
Substance-P receptor
|
||||
Gene Name |
TACR1
|
||||
Synonyms |
NK-1 receptor; NK-1R; Neurokinin 1 receptor; SPR; Substance P receptor; Tachykinin 1 receptor; Tachykinin neurokinin 1 receptor; Tachykinin receptor 1; TACR1
|
||||
Target Type |
Successful
|
||||
Disease | Alcohol use disorders [ICD9: 303; ICD10: F10.2] | ||||
Asthma [ICD10: J45] | |||||
Brain injury [ICD10: S09.90] | |||||
Chronic obstructive pulmonary disease [ICD9: 490-492, 494-496; ICD10: J40-J44, J47] | |||||
Cough [ICD9: 786.2; ICD10: R05] | |||||
Chemotherapy-induced nausea [ICD9: 787, 787.0; ICD10: R11] | |||||
Cancer pain [ICD9: 140-229, 338,780; ICD10: R52, G89] | |||||
Diabetes [ICD9: 253.5, 588.1; ICD10: E23.2, N25.1] | |||||
Depression; Anxiety [ICD9: 300, 311; ICD10: F30-F39, F40-F42] | |||||
Depression [ICD9: 311; ICD10: F30-F39] | |||||
Emesis; Irritable bowel syndrome [ICD9: 564.1, 787; ICD10: K58, R11] | |||||
Emesis [ICD9: 787; ICD10: R11] | |||||
Eczema [ICD10: L20-L30] | |||||
Incontinence; Anxiety disorder; Chemotherapyinduced emesis; Major depressive disorder [ICD9: 296.2, 296.3, 300, 787, 787.6, 788.3; ICD10: F32, F33, F40-F42, N39.3-N39.4] | |||||
Influenza virus [ICD10: J11.1] | |||||
Irritable bowel syndrome with diarrhoea [ICD9: 493, 564.1, 787.91; ICD10: A09, J45, K58, K59.1] | |||||
Irritable bowel syndrome; Chemo therapy induced emesis; Gastric motility disorder [ICD9: 536.8, 564.1, 787; ICD10: K30, K58, R11] | |||||
Mood disorder [ICD10: F30-F39] | |||||
Migraine [ICD9: 346; ICD10: G43] | |||||
Major depressive disorder [ICD9: 296.2, 296.3, 710.0; ICD10: F32, F33, M32] | |||||
Nausea; Vomiting [ICD9: 787, 787.0; ICD10: R11] | |||||
Overactive bladder disorder [ICD9: 188, 596.51; ICD10: C67, N32.81] | |||||
Pain [ICD9: 338, 356.0, 356.8,780; ICD10: G64, G90.0, R52, G89] | |||||
Respiratory tract inflammation [ICD10: J00-J99] | |||||
Severe mood disorders; Depression [ICD9: 296, 311; ICD10: F30-F39, F32] | |||||
Schizophrenia [ICD9: 295; ICD10: F20] | |||||
Urinary incontinence [ICD9: 788.3; ICD10: N39.3, N39.4, R32] | |||||
Unspecified [ICD code not available] | |||||
Function |
This is a receptor for the tachykinin neuropeptide substance P. It is probably associated with G proteins that activate a phosphatidylinositol-calcium second messenger system. The rank order of affinity of this receptor to tachykinins is: substance P > substance K > neuromedin-K.
|
||||
BioChemical Class |
GPCR rhodopsin
|
||||
Target Validation |
T47094
|
||||
UniProt ID | |||||
Sequence |
MDNVLPVDSDLSPNISTNTSEPNQFVQPAWQIVLWAAAYTVIVVTSVVGNVVVMWIILAH
KRMRTVTNYFLVNLAFAEASMAAFNTVVNFTYAVHNEWYYGLFYCKFHNFFPIAAVFASI YSMTAVAFDRYMAIIHPLQPRLSATATKVVICVIWVLALLLAFPQGYYSTTETMPSRVVC MIEWPEHPNKIYEKVYHICVTVLIYFLPLLVIGYAYTVVGITLWASEIPGDSSDRYHEQV SAKRKVVKMMIVVVCTFAICWLPFHIFFLLPYINPDLYLKKFIQQVYLAIMWLAMSSTMY NPIIYCCLNDRFRLGFKHAFRCCPFISAGDYEGLEMKSTRYLQTQGSVYKVSRLETTIST VVGAHEEEPEDGPKATPSSLDLTSNCSSRSDSKTMTESFSFSSNVLS |
||||
Drugs and Mode of Action | |||||
Drug(s) | Aprepitant | Drug Info | Approved | Nausea; Vomiting | [536361], [540429] |
MK-869 | Drug Info | Approved | Depression | [546681], [551871] | |
Rolapitant | Drug Info | Approved | Chemotherapy-induced nausea | [523745], [541084] | |
Netupitant | Drug Info | Phase 3 | Chemotherapy-induced nausea | [523441], [541077] | |
CP-122721 | Drug Info | Phase 2 | Major depressive disorder | [546318] | |
DAPITANT | Drug Info | Phase 2 | Pain | [525747] | |
GW 597599 | Drug Info | Phase 2 | Mood disorder | [547359] | |
LANEPITANT | Drug Info | Phase 2 | Pain | [540448], [546075] | |
LY-2590443 | Drug Info | Phase 2 | Migraine | [522513] | |
LY-686017 | Drug Info | Phase 2 | Alcohol use disorders | [521696] | |
NKP 608 | Drug Info | Phase 2 | Mood disorder | [531755] | |
Orvepitant | Drug Info | Phase 2 | Depression; Anxiety | [547887] | |
SCH-900978 | Drug Info | Phase 2 | Cough | [551472] | |
SSR240600 | Drug Info | Phase 2 | Urinary incontinence | [521692] | |
TKA-731 | Drug Info | Phase 2 | Pain | [527779] | |
VESTIPITANT MESYLATE | Drug Info | Phase 2 | Major depressive disorder | [523755] | |
VOFOPITANT HYDROCHLORIDE | Drug Info | Phase 2 | Emesis | [522215], [541087] | |
CJ-12255 | Drug Info | Phase 1 | Eczema | [550083] | |
Figopitant | Drug Info | Phase 1 | Diabetes | [524845] | |
Casopitant | Drug Info | Withdrawn from market | Chemotherapy-induced nausea | [536580], [541092] | |
BL-1832 | Drug Info | Discontinued in Phase 3 | Pain | [547403] | |
L-759274 | Drug Info | Discontinued in Phase 3 | Severe mood disorders; Depression | [536580] | |
Zunrisa/Rezonic | Drug Info | Discontinued in Phase 3 | Chemotherapy-induced nausea | [550098] | |
CGP-49823 | Drug Info | Discontinued in Phase 2 | Pain | [545737] | |
CS-003 | Drug Info | Discontinued in Phase 2 | Chronic obstructive pulmonary disease | [536223] | |
DNK-333 | Drug Info | Discontinued in Phase 2 | Irritable bowel syndrome with diarrhoea | [536223] | |
Ezlopitant | Drug Info | Discontinued in Phase 2 | Emesis; Irritable bowel syndrome | [536188], [541086] | |
FK-224 | Drug Info | Discontinued in Phase 2 | Asthma | [539332], [544903] | |
FK-888 | Drug Info | Discontinued in Phase 2 | Migraine | [539339], [545042] | |
GSK 679769 | Drug Info | Discontinued in Phase 2 | Incontinence; Anxiety disorder; Chemotherapyinduced emesis; Major depressive disorder | [536188] | |
Nolpitantium besilate | Drug Info | Discontinued in Phase 2 | Asthma | [539335], [545622] | |
TA-5538 | Drug Info | Discontinued in Phase 2 | Overactive bladder disorder | [548065] | |
TAK-637 | Drug Info | Discontinued in Phase 2 | Depression | [536580] | |
AVE-5883 | Drug Info | Discontinued in Phase 1/2 | Asthma | [548050] | |
GSK1144814 | Drug Info | Discontinued in Phase 1 | Schizophrenia | [522978] | |
GSK424887 | Drug Info | Discontinued in Phase 1 | Depression; Anxiety | [548690] | |
SDZ-NKT-343 | Drug Info | Discontinued in Phase 1 | Pain | [546834] | |
SLV-323 | Drug Info | Discontinued in Phase 1 | Irritable bowel syndrome; Chemo therapy induced emesis; Gastric motility disorder | [536188] | |
CI-1021 | Drug Info | Terminated | Discovery agent | [546490] | |
CP-96345 | Drug Info | Terminated | Discovery agent | [544830] | |
FK-355 | Drug Info | Terminated | Asthma | [547257] | |
FR-113680 | Drug Info | Terminated | Asthma | [544862] | |
GR-82334 | Drug Info | Terminated | Emesis | [546010] | |
L-732138 | Drug Info | Terminated | Discovery agent | [546118] | |
L-733060 | Drug Info | Terminated | Discovery agent | [546077] | |
L-741671 | Drug Info | Terminated | Emesis | [546715] | |
MEN-11149 | Drug Info | Terminated | Asthma | [546726] | |
MEN-11467 | Drug Info | Terminated | Respiratory tract inflammation | [546840] | |
RP-67580 | Drug Info | Terminated | Pain | [540457], [545049] | |
WIN-64821 | Drug Info | Terminated | Asthma | [546013] | |
Inhibitor | (D)-Phe-(D)-Phe-NH2 | Drug Info | [530745] | ||
(D)-Phe-(L)-Phe-NH2 | Drug Info | [530745] | |||
(L)-Phe-(D)-Phe-NH2 | Drug Info | [530745] | |||
2-Phenyl-3-(1-phenyl-ethoxy)-piperidine | Drug Info | [551332] | |||
3,6-Diphenyl-1-oxa-7-aza-spiro[4.5]decane | Drug Info | [526420] | |||
3-Benzyloxy-2-phenyl-piperidine | Drug Info | [551332] | |||
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one | Drug Info | [531079] | |||
7-METHYL-8-OXO-5-P-TOLYL-7,8-DIHYDRO-[1,7]NAPHTHYRIDINE-6-CARBOXYLIC ACID (3,5-BIS-TRIFLUOROMETHYL-BENZYL)-METHYL-AMIDE (STRUCTURAL MIX) | Drug Info | [534725] | |||
7-METHYL-8-OXO-5-P-TOLYL-7,8-DIHYDRO-[1,7]NAPHTHYRIDINE-6-CARBOXYLIC ACID (S)-[(R)-1-(3,5-BIS-TRIFLUOROMETHYL-PHENYL)-ETHYL]-METHYL-AMIDE (ENANTIOMERIC MIX) | Drug Info | [534725] | |||
7-METHYL-8-OXO-5-P-TOLYL-7,8-DIHYDRO-[1,7]NAPHTHYRIDINE-6-CARBOXYLIC ACID (S)-[(S)-1-(3,5-BIS-TRIFLUOROMETHYL-PHENYL)-ETHYL]-METHYL-AMIDE (ENANTIOMERIC MIX) | Drug Info | [534725] | |||
Ac-Phe-Phe-NH2 | Drug Info | [530745] | |||
Arg-Pro-Lys-Pro-Ala-Gln-Phe-Phe-Gly-Leu-Met-NH2 | Drug Info | [529205] | |||
Arg-Pro-Lys-Pro-Ala-Ser-Phe-Phe-Gly-Leu-Met-NH2 | Drug Info | [529205] | |||
Arg-Pro-Lys-Pro-Gln-Ser-Phe-Phe-Gly-Leu-Met-NH2 | Drug Info | [529205] | |||
CP-96345 | Drug Info | [551274] | |||
ENDOMORPHIN 2 | Drug Info | [530745] | |||
FR-113680 | Drug Info | [526802] | |||
H-Ala-Pro-Phe-Phe-NH2 | Drug Info | [530745] | |||
H-Arg-Pro-Lys-Pro-Gln-Gln-Phe-OH | Drug Info | [530745] | |||
H-Leu-Phe-NH2 | Drug Info | [530745] | |||
H-Phe-NH2 | Drug Info | [530745] | |||
H-Phe-Phe-NH2 | Drug Info | [530745] | |||
H-Pro-Phe-Phe-NH2 | Drug Info | [530745] | |||
H-Tyr(OMe)-Phe(2-Me)-NH2 | Drug Info | [530745] | |||
H-Tyr-Ala-Phe-Phe-NH2 | Drug Info | [530745] | |||
H-Tyr-D-Ala-Gly Phe-Pro-Leu-Trp-O-3,5-Bzl(CF3)2 | Drug Info | [529306] | |||
H-Tyr-D-Ala-Gly-Phe-Pro-Leu-Trp-NH-3,5-Bzl(CF3)2 | Drug Info | [529306] | |||
H-Tyr-D-Ala-Gly-Phe-Pro-Leu-Trp-NH-Bzl | Drug Info | [529306] | |||
H-Tyr-D-Ala-Gly-Phe-Pro-Leu-Trp-NMe-3,5-Bzl(CF3)2 | Drug Info | [529306] | |||
H-Tyr-D-Ala-Gly-Phe-Pro-Leu-Trp-NMe-Bzl | Drug Info | [529306] | |||
H-Tyr-D-Ala-Gly-Phe-Pro-Leu-Trp-O-Bzl | Drug Info | [529306] | |||
H-Tyr-Pro-Ala-Phe-NH2 | Drug Info | [530745] | |||
H-Tyr-Pro-Phe-Ala-NH2 | Drug Info | [530745] | |||
H-Tyr-Pro-Phe-Phe-OH | Drug Info | [530745] | |||
L-708568 | Drug Info | [534017] | |||
L-732138 | Drug Info | [530392] | |||
L-733060 | Drug Info | [551332] | |||
L-736281 | Drug Info | [534156] | |||
L-741671 | Drug Info | [534156] | |||
MDL-28163 | Drug Info | [527799] | |||
Pro-Lys-Pro-Gln-Gln-Phe-Phe-Gly-Leu-Met-NH2 | Drug Info | [529205] | |||
R-226161 | Drug Info | [528772] | |||
SP-SAP | Drug Info | [543792] | |||
SPANTIDE | Drug Info | [526793] | |||
Substance P | Drug Info | [534785] | |||
Tyr-D-Ala-Gly-Phe-Met-Pro-Leu-Trp-NH-Bzl | Drug Info | [529724] | |||
[Sar9,Met(O2)11]-SP | Drug Info | [529789] | |||
Antagonist | Aprepitant | Drug Info | [537211] | ||
befetupitant | Drug Info | [527912] | |||
BL-1832 | Drug Info | [550124] | |||
Casopitant | Drug Info | [536580] | |||
CGP-49823 | Drug Info | [534604] | |||
CI-1021 | Drug Info | [535587] | |||
CJ 11,974-01 | Drug Info | [537538] | |||
CJ-12255 | Drug Info | [532409], [551871] | |||
CP-100263 | Drug Info | [536188] | |||
CP-122721 | Drug Info | [536307] | |||
CP-99,994 | Drug Info | [535587] | |||
CS-003 | Drug Info | [536223] | |||
DAPITANT | Drug Info | [545693], [551871] | |||
Ezlopitant | Drug Info | [536188] | |||
Figopitant | Drug Info | [531741] | |||
FK-355 | Drug Info | [526798] | |||
FK-888 | Drug Info | [526652] | |||
GR-82334 | Drug Info | [526764] | |||
GSK 679769 | Drug Info | [536188] | |||
GSK424887 | Drug Info | [550963] | |||
GW 597599 | Drug Info | [530964] | |||
L-703,606 | Drug Info | [534153] | |||
L-759274 | Drug Info | [536580] | |||
LANEPITANT | Drug Info | [532961], [551871] | |||
LY-2590443 | Drug Info | [543792] | |||
LY-686017 | Drug Info | [544119] | |||
MEN-11149 | Drug Info | [534597] | |||
MEN-11467 | Drug Info | [525953] | |||
MK-869 | Drug Info | [536307] | |||
Netupitant | Drug Info | [532860] | |||
NKP 608 | Drug Info | [531755] | |||
Nolpitantium besilate | Drug Info | [533608] | |||
Orvepitant | Drug Info | [550963] | |||
R116031 | Drug Info | [526382] | |||
Rolapitant | Drug Info | [532860] | |||
RP-67580 | Drug Info | [533623] | |||
S-41744 | Drug Info | [543792] | |||
SCH 206272 | Drug Info | [526412] | |||
SCH-900978 | Drug Info | [549868] | |||
SDZ-NKT-343 | Drug Info | [534708] | |||
spantide II | Drug Info | [528399] | |||
SSR240600 | Drug Info | [535610] | |||
T2328 | Drug Info | [529254] | |||
TA-5538 | Drug Info | [548066] | |||
TAK-637 | Drug Info | [536580] | |||
TKA-731 | Drug Info | [527779] | |||
VESTIPITANT MESYLATE | Drug Info | [530964], [551871] | |||
VOFOPITANT HYDROCHLORIDE | Drug Info | [530121], [551871] | |||
WIN-64821 | Drug Info | [533611] | |||
Zunrisa/Rezonic | Drug Info | [550963] | |||
[125I]L703,606 | Drug Info | [533970] | |||
[18F]SPA-RQ | Drug Info | [543792] | |||
Modulator | AVE-5883 | Drug Info | [528579] | ||
DNK-333 | Drug Info | ||||
EU-C-001 | Drug Info | [543792] | |||
FK-224 | Drug Info | [526798] | |||
GSK1144814 | Drug Info | ||||
SLV-323 | Drug Info | [536188] | |||
WIN-64745 | Drug Info | ||||
WIN-66306 | Drug Info | ||||
WIN-68577 | Drug Info | ||||
ZD-6021 | Drug Info | ||||
Agonist | eledoisin | Drug Info | [534153] | ||
Homspera | Drug Info | [543792] | |||
kassinin | Drug Info | [534153] | |||
neurokinin A | Drug Info | [534404] | |||
physalaemin | Drug Info | [534153] | |||
Septide | Drug Info | [537828] | |||
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
TEP | EXP Info | ||||
Pathways | |||||
KEGG Pathway | Calcium signaling pathway | ||||
Neuroactive ligand-receptor interaction | |||||
Measles | |||||
PANTHER Pathway | CCKR signaling map ST | ||||
Reactome | G alpha (q) signalling events | ||||
WikiPathways | SIDS Susceptibility Pathways | ||||
Gastrin-CREB signalling pathway via PKC and MAPK | |||||
Spinal Cord Injury | |||||
Peptide GPCRs | |||||
GPCR ligand binding | |||||
GPCR downstream signaling | |||||
References | |||||
Ref 521692 | ClinicalTrials.gov (NCT00174798) MILADY: A Randomized, Placebo-controlled Safety and Efficacy Trial of SSR240600C in Treatment of Overactive Bladder or Urge Urinary Incontinence.. U.S. National Institutes of Health. | ||||
Ref 521696 | ClinicalTrials.gov (NCT00191022) Comparison of LY686017 With a Marketed Drug in the Treatment of Social Anxiety Disorder. U.S. National Institutes of Health. | ||||
Ref 522215 | ClinicalTrials.gov (NCT00606697) A Study With GW597599 And GR205171: Potential New Drugs For The Treatment Of Primary Insomnia. U.S. National Institutes of Health. | ||||
Ref 522513 | ClinicalTrials.gov (NCT00804973) Study in Subjects With Acute Migraines Headaches.. U.S. National Institutes of Health. | ||||
Ref 522978 | ClinicalTrials.gov (NCT01090440) Pharmacokinetics, Effect of Food, Safety and Tolerability of a New Tablet Formulation of GSK1144814 in Healthy Subjects. U.S. National Institutes of Health. | ||||
Ref 523441 | ClinicalTrials.gov (NCT01339260) An Efficacy and Safety Study of Oral Netupitant and Palonosetron for the Prevention of Nausea and Vomiting. U.S. National Institutes of Health. | ||||
Ref 523745 | ClinicalTrials.gov (NCT01500213) A Safety and Efficacy Study of Rolapitant for the Prevention of Chemotherapy-Induced Nausea and Vomiting (CINV) in Subjects Receiving Highly Emetogenic Chemotherapy. U.S. National Institutes of Health. | ||||
Ref 523755 | ClinicalTrials.gov (NCT01507194) A Study of Vestipitant (GW597599) in the Treatment of Breakthrough Postoperative Nausea and Vomiting (PONV). U.S. National Institutes of Health. | ||||
Ref 524845 | ClinicalTrials.gov (NCT02199899) Safety, Tolerability and Pharmacodynamics of BIIF 1149 BS in Healthy Young Male Volunteers. U.S. National Institutes of Health. | ||||
Ref 527779 | The NK1-receptor antagonist TKA731 in painful diabetic neuropathy: a randomised, controlled trial. Eur J Pain. 2006 Aug;10(6):567-71. Epub 2005 Sep 30. | ||||
Ref 531755 | Neurokinin-1-receptor antagonism decreases anxiety and emotional arousal circuit response to noxious visceral distension in women with irritable bowel syndrome: a pilot study. Aliment Pharmacol Ther.2012 Feb;35(3):360-7. | ||||
Ref 536188 | Emerging drugs for chemotherapy-induced emesis. Expert Opin Emerg Drugs. 2006 Mar;11(1):137-51. | ||||
Ref 536223 | Emerging drugs for the treatment of chronic obstructive pulmonary disease. Expert Opin Emerg Drugs. 2006 May;11(2):275-91. | ||||
Ref 536361 | Natural 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 536580 | Novel drugs and therapeutic targets for severe mood disorders. Neuropsychopharmacology. 2008 Aug;33(9):2080-92. Epub 2008 Jan 2. | ||||
Ref 539332 | (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: 2103). | ||||
Ref 539335 | (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: 2107). | ||||
Ref 539339 | (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: 2114). | ||||
Ref 540429 | (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: 3490). | ||||
Ref 540448 | (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: 3510). | ||||
Ref 540457 | (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: 3522). | ||||
Ref 541077 | (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: 5742). | ||||
Ref 541084 | (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: 5749). | ||||
Ref 541086 | (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: 5751). | ||||
Ref 541087 | (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: 5752). | ||||
Ref 541092 | (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: 5758). | ||||
Ref 544830 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001257) | ||||
Ref 544862 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001352) | ||||
Ref 544903 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001455) | ||||
Ref 545042 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001953) | ||||
Ref 545049 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001969) | ||||
Ref 545622 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003930) | ||||
Ref 545737 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004456) | ||||
Ref 546010 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005872) | ||||
Ref 546013 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005879) | ||||
Ref 546075 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006197) | ||||
Ref 546077 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006210) | ||||
Ref 546118 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006439) | ||||
Ref 546318 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007429) | ||||
Ref 546490 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008532) | ||||
Ref 546681 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009602) | ||||
Ref 546715 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009849) | ||||
Ref 546726 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009948) | ||||
Ref 546834 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010524) | ||||
Ref 546840 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010564) | ||||
Ref 547257 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800014508) | ||||
Ref 547359 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800015473) | ||||
Ref 547403 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800015961) | ||||
Ref 547887 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800020168) | ||||
Ref 548050 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800021516) | ||||
Ref 548065 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800021639) | ||||
Ref 548690 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800027682) | ||||
Ref 525953 | Effect of the long-acting tachykinin NK(1) receptor antagonist MEN 11467 on tracheal mucus secretion in allergic ferrets. Br J Pharmacol. 2001 Jan;132(1):189-96. | ||||
Ref 526382 | Pharmacological profile of (2R-trans)-4-[1-[3,5-bis(trifluoromethyl)benzoyl]-2-(phenylmethyl)-4-piperidinyl]-N-(2,6-dimethylphenyl)-1-acetamide (S)-Hydroxybutanedioate (R116301), an orally and centrally active neurokinin-1 receptor antagonist. J Pharmacol Exp Ther. 2002 Aug;302(2):696-709. | ||||
Ref 526412 | SCH 206272: a potent, orally active tachykinin NK(1), NK(2), and NK(3) receptor antagonist. Eur J Pharmacol. 2002 Aug 23;450(2):191-202. | ||||
Ref 526420 | Bioorg Med Chem Lett. 2002 Oct 7;12(19):2719-22.Spirocyclic NK(1) antagonists II: [4.5]-spiroethers. | ||||
Ref 526652 | Pharmacological profile of a high affinity dipeptide NK1 receptor antagonist, FK888. Br J Pharmacol. 1992 Nov;107(3):785-9. | ||||
Ref 526764 | Effect of the NK-1 receptor antagonist GR 82,334 on reflexly-induced bladder contractions. Life Sci. 1992;51(26):PL277-80. | ||||
Ref 526793 | J Med Chem. 1992 Apr 3;35(7):1273-9.Synthesis and substance P antagonist activity of naphthimidazolium derivatives. | ||||
Ref 526798 | FK 224, a novel cyclopeptide substance P antagonist with NK1 and NK2 receptor selectivity. J Pharmacol Exp Ther. 1992 Jul;262(1):398-402. | ||||
Ref 526802 | FR 113680: a novel tripeptide substance P antagonist with NK1 receptor selectivity. Br J Pharmacol. 1992 May;106(1):123-6. | ||||
Ref 527779 | The NK1-receptor antagonist TKA731 in painful diabetic neuropathy: a randomised, controlled trial. Eur J Pain. 2006 Aug;10(6):567-71. Epub 2005 Sep 30. | ||||
Ref 527799 | J Med Chem. 2005 Oct 20;48(21):6523-43.Designed multiple ligands. An emerging drug discovery paradigm. | ||||
Ref 527912 | Design and synthesis of a novel, achiral class of highly potent and selective, orally active neurokinin-1 receptor antagonists. Bioorg Med Chem Lett. 2006 Mar 1;16(5):1362-5. Epub 2005 Dec 5. | ||||
Ref 528399 | Spantide II, an effective tachykinin antagonist having high potency and negligible neurotoxicity. Proc Natl Acad Sci U S A. 1990 Jun;87(12):4833-5. | ||||
Ref 528579 | Effect of an NK1/NK2 receptor antagonist on airway responses and inflammation to allergen in asthma. Am J Respir Crit Care Med. 2007 Mar 1;175(5):450-7. Epub 2006 Dec 14. | ||||
Ref 528772 | Bioorg 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 529205 | J Med Chem. 2007 Dec 27;50(26):6501-6. Epub 2007 Dec 8.Conformational comparisons of a series of tachykinin peptide analogs. | ||||
Ref 529254 | Pharmacological characterization of T-2328, 2-fluoro-4'-methoxy-3'-[[[(2S,3S)-2-phenyl-3-piperidinyl]amino]methyl]-[1,1'-biphenyl]-4-carbonitrile dihydrochloride, as a brain-penetrating antagonist oftachykinin NK1 receptor. J Pharmacol Sci. 2008 Jan;106(1):121-7. Epub 2008 Jan 11. | ||||
Ref 529306 | J Med Chem. 2008 Mar 13;51(5):1369-76. Epub 2008 Feb 12.A structure-activity relationship study and combinatorial synthetic approach of C-terminal modified bifunctional peptides that are delta/mu opioid receptor agonists and neurokinin 1 receptor antagonists. | ||||
Ref 529724 | J Med Chem. 2008 Oct 23;51(20):6334-47. Epub 2008 Sep 27.The importance of micelle-bound states for the bioactivities of bifunctional peptide derivatives for delta/mu opioid receptor agonists and neurokinin 1 receptor antagonists. | ||||
Ref 529789 | J Med Chem. 2008 Nov 27;51(22):7094-8.cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), a new histamine H4R antagonist that blocks pain responses against carrageenan-induced hyperalgesia. | ||||
Ref 530121 | Efficacy and safety of casopitant mesylate, a neurokinin 1 (NK1)-receptor antagonist, in prevention of chemotherapy-induced nausea and vomiting in patients receiving cisplatin-based highly emetogenicchemotherapy: a randomised, double-blind, placebo-controlled trial. Lancet Oncol. 2009 Jun;10(6):549-58. | ||||
Ref 530392 | Bioorg Med Chem. 2009 Oct 15;17(20):7337-43. Epub 2009 Aug 21.The biological activity and metabolic stability of peptidic bifunctional compounds that are opioid receptor agonists and neurokinin-1 receptor antagonists with a cystine moiety. | ||||
Ref 530745 | J Med Chem. 2010 Mar 25;53(6):2383-9.Discovery of dipeptides with high affinity to the specific binding site for substance P1-7. | ||||
Ref 530964 | Application of LC-NMR to the identification of bulk drug impurities in NK1 antagonist GW597599 (vestipitant). Magn Reson Chem. 2010 Jul;48(7):523-30. | ||||
Ref 531079 | J 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 531741 | Investigation of figopitant and its metabolites in rat tissue by combining whole-body autoradiography with liquid extraction surface analysis mass spectrometry. Drug Metab Dispos. 2012 Mar;40(3):419-25. | ||||
Ref 531755 | Neurokinin-1-receptor antagonism decreases anxiety and emotional arousal circuit response to noxious visceral distension in women with irritable bowel syndrome: a pilot study. Aliment Pharmacol Ther.2012 Feb;35(3):360-7. | ||||
Ref 532409 | Neurokinin-1 receptor, a new modulator of lymphangiogenesis in obese-asthma phenotype. Life Sci. 2013 Aug 6;93(4):169-77. | ||||
Ref 532860 | Netupitant and palonosetron trigger NK1 receptor internalization in NG108-15 cells. Exp Brain Res. 2014 Aug;232(8):2637-44. | ||||
Ref 532961 | NK1 receptor antagonists as a new treatment for corneal neovascularization. Invest Ophthalmol Vis Sci. 2014 Sep 16;55(10):6783-94. | ||||
Ref 533608 | SR 140333, a novel, selective, and potent nonpeptide antagonist of the NK1 tachykinin receptor: characterization on the U373MG cell line. J Neurochem. 1994 Apr;62(4):1399-407. | ||||
Ref 533611 | WIN 64821, a novel neurokinin antagonist produced by an Aspergillus sp. II. Biological activity. J Antibiot (Tokyo). 1994 Apr;47(4):399-410. | ||||
Ref 533623 | Effects of RP 67580, a tachykinin NK1 receptor antagonist, on a primary afferent-evoked response of ventral roots in the neonatal rat spinal cord. Br J Pharmacol. 1994 Dec;113(4):1141-6. | ||||
Ref 533970 | Radioiodinated L-703,606: a potent, selective antagonist to the human NK1 receptor. Appl Radiat Isot. 1994 Jan;45(1):97-103. | ||||
Ref 534017 | J Med Chem. 1993 Jul 9;36(14):2044-5.N-acyl-L-tryptophan benzyl esters: potent substance P receptor antagonists. | ||||
Ref 534153 | The unpredicted high affinities of a large number of naturally occurring tachykinins for chimeric NK1/NK3 receptors suggest a role for an inhibitory domain in determining receptor specificity. J BiolChem. 1996 Aug 23;271(34):20250-7. | ||||
Ref 534156 | J Med Chem. 1996 Jul 19;39(15):2907-14.N-heteroaryl-2-phenyl-3-(benzyloxy)piperidines: a novel class of potent orally active human NK1 antagonists. | ||||
Ref 534404 | Nonpeptide tachykinin receptor antagonists: I. Pharmacological and pharmacokinetic characterization of SB 223412, a novel, potent and selective neurokinin-3 receptor antagonist. J Pharmacol Exp Ther.1997 Jun;281(3):1303-11. | ||||
Ref 534597 | Pharmacology of the peptidomimetic, MEN 11149, a new potent, selective and orally effective tachykinin NK1 receptor antagonist. Eur J Pharmacol. 1998 Jan 12;341(2-3):201-9. | ||||
Ref 534604 | The potency of the novel tachykinin receptor antagonist CGP49823 at rat and gerbil motoneurones in vitro. Eur J Pharmacol. 1998 Jan 26;342(2-3):203-8. | ||||
Ref 534708 | The effects of SDZ NKT 343, a potent NK1 receptor antagonist, on cutaneous responses of primate spinothalamic tract neurones sensitized by intradermal capsaicin injection. Exp Brain Res. 1998 Aug;121(3):355-8. | ||||
Ref 534725 | J Med Chem. 1998 Oct 22;41(22):4232-9.Axially chiral N-benzyl-N,7-dimethyl-5-phenyl-1, 7-naphthyridine-6-carboxamide derivatives as tachykinin NK1 receptor antagonists: determination of the absolute stereochemical requirements. | ||||
Ref 534785 | Bioorg Med Chem Lett. 1998 Feb 3;8(3):281-4.Synthesis and structure-activity relationships of CP-122,721, a second-generation NK-1 receptor antagonist. | ||||
Ref 535587 | Gabapentin and the neurokinin(1) receptor antagonist CI-1021 act synergistically in two rat models of neuropathic pain. J Pharmacol Exp Ther. 2002 Nov;303(2):730-5. | ||||
Ref 535610 | SSR240600 [(R)-2-(1-[2-[4-[2-[3,5-bis(trifluoromethyl)phenyl]acetyl]-2-(3,4-dichlorophenyl)-2-morpholinyl]ethyl]- 4-piperidinyl)-2-methylpropanamide], a centrally active nonpeptide antagonist of the tachykinin neurokinin-1 receptor: I. biochemical and pharmacological characterization. J Pharmacol Exp Ther. 2002 Dec;303(3):1171-9. | ||||
Ref 536188 | Emerging drugs for chemotherapy-induced emesis. Expert Opin Emerg Drugs. 2006 Mar;11(1):137-51. | ||||
Ref 536223 | Emerging drugs for the treatment of chronic obstructive pulmonary disease. Expert Opin Emerg Drugs. 2006 May;11(2):275-91. | ||||
Ref 536307 | A review of drug options in age-related macular degeneration therapy and potential new agents. Expert Opin Pharmacother. 2006 Dec;7(17):2355-68. | ||||
Ref 536580 | Novel drugs and therapeutic targets for severe mood disorders. Neuropsychopharmacology. 2008 Aug;33(9):2080-92. Epub 2008 Jan 2. | ||||
Ref 537211 | Potent, brain-penetrant, hydroisoindoline-based human neurokinin-1 receptor antagonists. J Med Chem. 2009 May 14;52(9):3039-46. | ||||
Ref 537538 | Targeting pain-depressed behaviors in preclinical assays of pain and analgesia: drug effects on acetic acid-depressed locomotor activity in ICR mice. Life Sci. 2009 Aug 12;85(7-8):309-15. | ||||
Ref 537828 | Septide: an agonist for the NK1 receptor acting at a site distinct from substance P. Mol Pharmacol. 1994 Feb;45(2):287-93. | ||||
Ref 543792 | (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: 360). | ||||
Ref 544119 | Stress-related neuropeptides and alcoholism: CRH, NPY and beyond. Alcohol. 2009 November; 43(7): 491-498. | ||||
Ref 545693 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004225) | ||||
Ref 548066 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800021639) | ||||
Ref 550124 | WO patent application no. 2006,0132,05, Neurokinin-1 receptor antagonists for the treatment of conditions responsive to testosterone elevation. | ||||
Ref 551274 | 2-Aryl-1-azabicyclo[2.2.2]octanes as novel nonpeptide substance P antagonists, Bioorg. Med. Chem. Lett. 4(6):839-842 (1994). |
If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.