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 521692ClinicalTrials.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 521696ClinicalTrials.gov (NCT00191022) Comparison of LY686017 With a Marketed Drug in the Treatment of Social Anxiety Disorder. U.S. National Institutes of Health.
Ref 522215ClinicalTrials.gov (NCT00606697) A Study With GW597599 And GR205171: Potential New Drugs For The Treatment Of Primary Insomnia. U.S. National Institutes of Health.
Ref 522513ClinicalTrials.gov (NCT00804973) Study in Subjects With Acute Migraines Headaches.. U.S. National Institutes of Health.
Ref 522978ClinicalTrials.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 523441ClinicalTrials.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 523745ClinicalTrials.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 523755ClinicalTrials.gov (NCT01507194) A Study of Vestipitant (GW597599) in the Treatment of Breakthrough Postoperative Nausea and Vomiting (PONV). U.S. National Institutes of Health.
Ref 524845ClinicalTrials.gov (NCT02199899) Safety, Tolerability and Pharmacodynamics of BIIF 1149 BS in Healthy Young Male Volunteers. U.S. National Institutes of Health.
Ref 525747Dapitant. RPR 100893. Drugs R D. 1999 Dec;2(6):383-4.
Ref 527779The 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 531755Neurokinin-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 536188Emerging drugs for chemotherapy-induced emesis. Expert Opin Emerg Drugs. 2006 Mar;11(1):137-51.
Ref 536223Emerging drugs for the treatment of chronic obstructive pulmonary disease. Expert Opin Emerg Drugs. 2006 May;11(2):275-91.
Ref 536361Natural 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 536580Novel 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 544830Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001257)
Ref 544862Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001352)
Ref 544903Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001455)
Ref 545042Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001953)
Ref 545049Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001969)
Ref 545622Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003930)
Ref 545737Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004456)
Ref 546010Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005872)
Ref 546013Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005879)
Ref 546075Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006197)
Ref 546077Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006210)
Ref 546118Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006439)
Ref 546318Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007429)
Ref 546490Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008532)
Ref 546681Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009602)
Ref 546715Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009849)
Ref 546726Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009948)
Ref 546834Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010524)
Ref 546840Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010564)
Ref 547257Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800014508)
Ref 547359Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800015473)
Ref 547403Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800015961)
Ref 547887Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800020168)
Ref 548050Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800021516)
Ref 548065Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800021639)
Ref 548690Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800027682)
Ref 550083HIV ANTIRETROVIRAL DRUG SUSCEPTIBILITY AND DRUG INTERACTIONS (DIRECTOR: MARK MANAK). The Children's Hospital of Philadelphia.
Ref 550098Clinical pipeline report, company report or official report of GlaxoSmithKline.
Ref 551472Clinical pipeline report, company report or official report of OPKO Health Inc.
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
Ref 525953Effect 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 526382Pharmacological 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 526412SCH 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 526420Bioorg Med Chem Lett. 2002 Oct 7;12(19):2719-22.Spirocyclic NK(1) antagonists II: [4.5]-spiroethers.
Ref 526652Pharmacological profile of a high affinity dipeptide NK1 receptor antagonist, FK888. Br J Pharmacol. 1992 Nov;107(3):785-9.
Ref 526764Effect of the NK-1 receptor antagonist GR 82,334 on reflexly-induced bladder contractions. Life Sci. 1992;51(26):PL277-80.
Ref 526793J Med Chem. 1992 Apr 3;35(7):1273-9.Synthesis and substance P antagonist activity of naphthimidazolium derivatives.
Ref 526798FK 224, a novel cyclopeptide substance P antagonist with NK1 and NK2 receptor selectivity. J Pharmacol Exp Ther. 1992 Jul;262(1):398-402.
Ref 526802FR 113680: a novel tripeptide substance P antagonist with NK1 receptor selectivity. Br J Pharmacol. 1992 May;106(1):123-6.
Ref 527779The 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 527799J Med Chem. 2005 Oct 20;48(21):6523-43.Designed multiple ligands. An emerging drug discovery paradigm.
Ref 527912Design 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 528399Spantide 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 528579Effect 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 528772Bioorg 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 529205J Med Chem. 2007 Dec 27;50(26):6501-6. Epub 2007 Dec 8.Conformational comparisons of a series of tachykinin peptide analogs.
Ref 529254Pharmacological 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 529306J 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 529724J 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 529789J 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 530121Efficacy 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 530392Bioorg 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 530745J 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 530964Application 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 531079J 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 531741Investigation 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 531755Neurokinin-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 532409Neurokinin-1 receptor, a new modulator of lymphangiogenesis in obese-asthma phenotype. Life Sci. 2013 Aug 6;93(4):169-77.
Ref 532860Netupitant and palonosetron trigger NK1 receptor internalization in NG108-15 cells. Exp Brain Res. 2014 Aug;232(8):2637-44.
Ref 532961NK1 receptor antagonists as a new treatment for corneal neovascularization. Invest Ophthalmol Vis Sci. 2014 Sep 16;55(10):6783-94.
Ref 533608SR 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 533611WIN 64821, a novel neurokinin antagonist produced by an Aspergillus sp. II. Biological activity. J Antibiot (Tokyo). 1994 Apr;47(4):399-410.
Ref 533623Effects 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 533970Radioiodinated L-703,606: a potent, selective antagonist to the human NK1 receptor. Appl Radiat Isot. 1994 Jan;45(1):97-103.
Ref 534017J Med Chem. 1993 Jul 9;36(14):2044-5.N-acyl-L-tryptophan benzyl esters: potent substance P receptor antagonists.
Ref 534153The 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 534156J 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 534404Nonpeptide 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 534597Pharmacology 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 534604The 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 534708The 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 534725J 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 534785Bioorg 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 535587Gabapentin 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 535610SSR240600 [(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 536188Emerging drugs for chemotherapy-induced emesis. Expert Opin Emerg Drugs. 2006 Mar;11(1):137-51.
Ref 536223Emerging drugs for the treatment of chronic obstructive pulmonary disease. Expert Opin Emerg Drugs. 2006 May;11(2):275-91.
Ref 536307A review of drug options in age-related macular degeneration therapy and potential new agents. Expert Opin Pharmacother. 2006 Dec;7(17):2355-68.
Ref 536580Novel drugs and therapeutic targets for severe mood disorders. Neuropsychopharmacology. 2008 Aug;33(9):2080-92. Epub 2008 Jan 2.
Ref 537211Potent, brain-penetrant, hydroisoindoline-based human neurokinin-1 receptor antagonists. J Med Chem. 2009 May 14;52(9):3039-46.
Ref 537538Targeting 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 537828Septide: 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 544119Stress-related neuropeptides and alcoholism: CRH, NPY and beyond. Alcohol. 2009 November; 43(7): 491-498.
Ref 545693Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004225)
Ref 548066Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800021639)
Ref 549868Clinical pipeline report, company report or official report of OPKO Health, Inc.
Ref 550124WO patent application no. 2006,0132,05, Neurokinin-1 receptor antagonists for the treatment of conditions responsive to testosterone elevation.
Ref 550963Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).
Ref 5512742-Aryl-1-azabicyclo[2.2.2]octanes as novel nonpeptide substance P antagonists, Bioorg. Med. Chem. Lett. 4(6):839-842 (1994).
Ref 5513323-Benzyloxy-2-phenylpiperidine NK1 antagonists: the influence of alpha methyl substitution, Bioorg. Med. Chem. Lett. 7(23):2959-2962 (1997).
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015

If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.