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Receptors, Neurokinin-1

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Definition: A class of cell surface receptors for tachykinins with a preference for substance P. Neurokinin-1 (NK-1) receptors have been cloned and are members of the G protein coupled receptor superfamily. They are found on many cell types including central and peripheral neurons, smooth muscle cells, acinar cells, endothelial cells, fibroblasts, and immune cells.  tachykinin receptors; DF: RECEPT NEUROKININ 1    Other names Substance P Receptors; SP-P Receptors; Receptors, Substance P; Neurokinin-1 Receptors; NK-1 Receptors; SP P Receptors; SP P Receptor; Receptors, SP P; Receptors, Neurokinin 1; Receptors, NK 1; Receptor, Substance P; Receptor, SP-P; Receptor, Neurokinin-1; Receptor, NK-1; P Receptors, Substance; Neurokinin 1 Receptors; P Receptor, Substance; Neurokinin 1 Receptor; NK 1 Receptors; NK 1 Receptor
 
SubstanceCAS Registry & nameCategoriesSourceDrugs*
1-(amino(oxo)acetyl)-N-(1-(3,5-bis(trifluoromethyl)phenyl)ethyl)-3-(4-fluoro-2-methylphenyl)-N-methylpiperidine-4-carboxamide  0   *Piperidines Receptors, Neurokinin-1/antagonists & inhibitors. Bioorg Med Chem. 2012 Jan 15;20(2):962-77.
AZD 2738  0   *Azetidines *Benzamides Receptors, Neurokinin-1/antagonists & inhibitors Receptors, Neurokinin-2/antagonists & inhibitors. Drug Dev Ind Pharm 2011 Jun;37(6):719-26
AZD 8081  0   *Azetidines *Benzamides Receptors, Neurokinin-1/antagonists & inhibitors Receptors, Neurokinin-2/antagonists & inhibitors. Drug Dev Ind Pharm 2011 Jun;37(6):702-13
2-piperazin-1-ylindan-2-carboxylic acid (3-chloro-5-fluorobenzyl)methylamide  0   *Indans *Piperazines Receptors, Neurokinin-1/antagonists & inhibitors. Eur Neuropsychopharmacol 2010 Sep;20(9):599-621
tyrosyl-cyclo(penicillamine-glycyl-phenylalanyl-penicillamine)-prolyl-leucyl-tryptophyl-NH-(3',5'-(CF3)2-Bzl)  0   *Peptides, Cyclic Receptors, Opioid/agonists Receptors, Neurokinin-1/antagonists & inhibitors. J Med Chem 2010 Aug 12;53(15):5491-501
serlopitant  0   *Isoindoles Receptors, Neurokinin-1/antagonists & inhibitors. J Urol 2010 Aug;184(2):616-22
Sch 425078  0   *Imidazoles Receptors, Neurokinin-1/antagonists & inhibitors. Org Lett 2009 Jun 4;11(11):2365-8
vestipitant  0   *Piperidines Receptors, Neurokinin-1/antagonists & inhibitors. Eur Neuropsychopharmacol 2008 Oct;18(10):729-50
3-(6-methoxy-1-methyl-1-trifluoromethylisochroman-7-yl)methylamino-2-phenylpiperidine  0   *Benzopyrans *Piperidines Receptors, Neurokinin-1/antagonists & inhibitors. Bioorg Med Chem 2008 Aug 1;16(15):7193-205
N-((2-cyclopropoxy-5-(5-trifluomethyl)tetrazol-1-yl)benzyl)-2-phenylpiperidin-3-amine  0   *Piperidines Receptors, Neurokinin-1/antagonists & inhibitors. J Neurochem 2008 Sep;106(6):2476-88
casopitant  0   *Piperazines *Piperidines Receptors, Neurokinin-1/antagonists & inhibitors. Curr Opin Investig Drugs 2008 Jul;9(7):774-85
tyrosyl-alanyl-glycyl-phenylalanyl-norleucyl-prolyl-leucyl-tryptophyl-O-3,5-benzyl(CF3)2  0   *Oligopeptides Receptors, Opioid, mu/agonists Receptors, Opioid, delta/agonists Receptors, Neurokinin-1/antagonists & inhibitors. J Med Chem 2007 Jun 14;50(12):2779-86
tyrosyl-alanyl-glycyl-phenylalanyl-methionyl-prolyl-leucyl-tryptophyl-O-3,5-benzyl(CF3)2  0   *Oligopeptides Receptors, Opioid, mu/agonists Receptors, Opioid, delta/agonists Receptors, Neurokinin-1/antagonists & inhibitors. J Med Chem 2007 Jun 14;50(12):2779-86
(2-fluoromethoxy-5-(5-trifluoromethyltetrazol-1-yl)benzyl)(2-phenylpiperidin-3-yl)amine  0   *Piperidines *Tetrazoles Fluorine Radioisotopes Receptors, Neurokinin-1/antagonists & inhibitors. J Nucl Med 2007 Jan;48(1):100-7
3-(2-methoxy-5-trifluoromethoxybenzyl)amino-1-methyl-2-phenylpiperidine  0   *Piperidines Carbon Radioisotopes Receptors, Neurokinin-1/antagonists & inhibitors. Nucl Med Biol 2004 Aug;31(6):699-704
ASN 1377642  0   *Aniline Compounds *Triazoles Receptors, Neurokinin-1/antagonists & inhibitors. J Med Chem 2004 Oct 21;47(22):5381-92
6-diphenylmethyl-5-(5-isopropyl-2-methoxybenzylamino)-1-azabicyclo(2.2.2)octane-3-carboxylic acid  0   *Bicyclo Compounds, Heterocyclic Receptors, Neurokinin-1/antagonists & inhibitors. Am J Physiol Gastrointest Liver Physiol 2003 Dec;285(6):G1259-67
6-phenyl-1-oxa-7-azaspiro(4,5)decane  0   *Aza Compounds *Spiro Compounds Receptors, Neurokinin-1/antagonists & inhibitors. J Org Chem 2002 Feb 22;67(4):1093-101
1-(5-((2-((1-(3,5-bis(trifluoromethyl)phenyl)ethyl)oxy)-3-(4-fluorophenyl)morpholin-4-yl)methyl)-2H-1,2,3-triazol-4-yl)-N,N-dimethylmethanamine  0   *Morpholines *Triazoles Receptors, Neurokinin-1/antagonists & inhibitors. J Med Chem 2001 Nov 22;44(24):4296-9
PD 174424  0   *Carbamates *Indoles Receptors, Neurokinin-1/antagonists & inhibitors. J Med Chem 2001 Jul 5;44(14):2276-85
1-oxo-7-azaspirodecane  0   *Aza Compounds *Spiro Compounds Receptors, Neurokinin-1/antagonists & inhibitors. Org Lett 2001 Mar 8;3(5):671-4
3-aryl-6-phenyl-1-oxa-7-azaspiro(4.5)decane  0   *Aza Compounds *Spiro Compounds Receptors, Neurokinin-1/antagonists & inhibitors. Org Lett 2001 Mar 8;3(5):667-70
quinoline-4-carboxylic acid (1-(3,5-bis-trifluoromethylbenzoyl)-2-(4-chlorobenzyl)piperidin-4-yl)amide  0   *Piperidines *Quinolines Receptors, Neurokinin-1/antagonists & inhibitors. Behav Brain Res 2000 Oct;115(1):19-23
ezlopitant  147116-64-1 (2S,3S)-2-(Diphenylmethyl)-3-((5-isopropyl-2-methoxy- benzyl)amino)quinuclidine  *Benzylamines *Bicyclo Compounds, Heterocyclic Receptors, Neurokinin-1/analogs & derivatives. Drug Metab Dispos 2000 Sep;28(9):1069-76
2-(1-(3,5-bis(trifluoromethyl)phenyl)ethoxy)-3-(4-fluoro)phenyl-4-(5-(2-phosphoryl-3-oxo-4H,-1,2,4-triazolo))methylmorpholine, bis(N-methylglucamine) salt  0   *Acetals *Morpholines Receptors, Neurokinin-1/antagonists & inhibitors. J Med Chem 2000 Mar 23;43(6):1234-41
MDL 103392  0   *Pyrroles *Pyrrolidines Receptors, Neurokinin-1/antagonists & inhibitors Receptors, Neurokinin-2/antagonists & inhibitors. Bioorg Med Chem 1999 Dec;7(12):2867-76
R116301  0   *Butanols Receptors, Neurokinin-1/antagonists & inhibitors. Clin Pharmacol Ther 1999 Nov;66(5):522-7
CJ 11974  0   *Benzene Derivatives Receptors, Neurokinin-1. J Clin Oncol 1999 Jan;17(1):338-43
HSP 117  0   *Benzofurans *Piperidines Receptors, Neurokinin-1/antagonists & inhibitors. Neuroscience Lett 1998 Oct 2;254(3):169-72
phenylglycinol  0   Glycine/*analogs & derivatives Receptors, Neurokinin-1/antagonists & inhibitors. Bioorg Med Chem Lett 1998 Jan 6;8(1):51-6
4-(3,5-bis(trifluoromethyl)benzyloxymethyl)-1-(2-methylthiazol-5-ylmethyl)-4-phenylpiperidine  0   *Piperidines *Thiazoles Receptors, Neurokinin-1/antagonists & inhibitors. J Med Chem 1998 Nov 5;41(23):4623-35
1-(4-(3,5-bis(trifluoromethyl)benzyloxymethyl)-4-phenylpiperidin-1-yl)-2-pyrrolidineacetamide  0   *Piperidines *Pyrrolidines Receptors, Neurokinin-1/antagonists & inhibitors. J Med Chem 1998 Nov 5;41(23):4623-35
L 754030  0   *Acetals *Morpholines Receptors, Neurokinin-1/antagonists & inhibitors. J Med Chem 1998 Nov 5;41(23):4607-14
N-(1-(3,5-bis(trifluoromethyl)phenyl)ethyl)-7,8-dihydro-N,7-dimethyl-5-(4-methylphenyl)-8-oxo-1,7-naphthyridine-6-carboxamide  0   *Naphthyridines Receptors, Neurokinin-1/antagonists & inhibitors. J Med Chem 1998 Oct 22;41(22):4232-9
N-(3,5-bis(trifluoromethyl)benzyl)-7,8-dihydro-N,7-dimethyl-5-(4-methylphenyl)-8-oxo-1,7-naphthyridine-6-carboxamide  0   *Naphthyridines Receptors, Neurokinin-1/antagonists & inhibitors. J Med Chem 1998 Oct 22;41(22):4232-9
aprepitant  0   *Morpholines Antidepressive Agents Receptors, Neurokinin-1.
Pharma Action Antiemetics 		Science 1998 Sep 11;281(5383):1640-5EMEND
substance P, Cys(3,6)-Tyr(8)-Pro(9)  0   Substance P/*analogs & derivatives Receptors, Neurokinin-1/agonists. J Neurophysiol 1998 Jul;80(1):218-29
SDZ NKT 343  0   *Naphthalenes Proline/*analogs & derivatives Receptors, Neurokinin-1/antagonists & inhibitors. Br J Pharmacol 1998 May;124(1):83-92
CI 1021  0   *Benzofurans *Carbamates Receptors, Neurokinin-1/antagonists & inhibitors. J Pharmacol Exp Ther 1998 Jun;285(3):1226-32
substance P, Arg(1)-Pro(2)-Phe(7)-His(9)  0   Substance P/*analogs & derivatives Receptors, Neurokinin-1/antagonists & inhibitors. J Med Chem 1998 Apr 23;41(9):1497-506
YM 35375  0   *Piperidines *Spiro Compounds Receptors, Neurokinin-1/antagonists & inhibitors Receptors, Neurokinin-2/antagonists & inhibitors. Chem Pharm Bull (Tokyo) 1998 Feb;46(2):242-54
MDL 108,207DA  0   *Pyrrolidines *Benzimidazoles Receptors, Neurokinin-1/antagonists & inhibitors. Int Arch Allergy Immunol 1998 Feb;115(2):169-78
MEN 10930  0   *Indoles Alanine/*analogs & derivatives Receptors, Neurokinin-1/antagonists & inhibitors. Neuropeptides 1997 Aug;31(4):373-9
L 743310  0   *Indoles Receptors, Neurokinin-1/antagonists & inhibitors. Neuropharmacology 1996;35(8):1121-9
L 741671  0   *Triazoles Receptors, Neurokinin-1/antagonists & inhibitors. Neuropharmacology 1996;35(8):1121-9
L 733060  148700-85-0   *Piperidines Stereoisomerism Receptors, Neurokinin-1/antagonists & inhibitors. Pain 1996 Sep;67(1):189-95
CAM 4750  0   *Benzofurans *Carbamates Receptors, Neurokinin-1/antagonists & inhibitors. J Pharm Biomed anal 1996 Sep;14(12):1709-16
CAM 4515  0   *Benzofurans *Carbamates Receptors, Neurokinin-1/antagonists & inhibitors. J Pharm Biomed Anal 1996 Sep;14(12):1709-16
GR 205171  168266-90-8   *Piperidines *Tetrazoles Stereoisomerism Receptors, Neurokinin-1/antagonists & inhibitors.
Pharma Action Antiemetics 		Regul Pept 1996 Aug 27;65(1):45-53
S 18523  0   *Dipeptides *Tetrazoles Receptors, Neurokinin-1/antagonists & inhibitors. Eur J Pharmacol 1996 Aug 22;310(1):37-46
LY 306740  0   *Acetamides Stereoisomerism Receptors, Neurokinin-1/antagonists & inhibitors. Mol Pharmacol 1996 Nov;50(5):1189-99
cyclo((2-naphthyl)alanyl-tryptophyl-(4-fluoro)phenylalanyl-threonyl-phenylalanyl-prolyl)  0   *Peptides, Cyclic Receptors, Neurokinin-1/antagonists & inhibitors. J Med Chem 1996 Jun 21;39(13):2441-8
MDL 105212A  0   *Piperidines *Pyrrolidines Stereoisomerism Receptors, Neurokinin-1/antagonists & inhibitors Receptors, Neurokinin-2/antagonists & inhibitors. J Pharmacol Exp Ther 1996 May;277(2):840
CP 122721  0   *Piperidines Stereoisomerism Receptors, Neurokinin-1/antagonists & inhibitors. J Pharmacol Exp Ther 1996 May;277(2):900
S 16474  0   *Oligopeptides Receptors, Neurokinin-1/antagonists & inhibitors Receptors, Neurokinin-2/antagonists & inhibitors. Eur J Pharmacol 1995 Dec 29;294(2-3):677-84
GR 203040  168398-02-5   *Piperidines *Tetrazoles Receptors, Neurokinin-1/antagonists & inhibitors. J Med Chem 1995 Dec 22;38(26):4985-92
LY 303870  0   *Indoles *Piperidines Stereoisomerism Receptors, Neurokinin-1/antagonists & inhibitors. J Pharmacol Exp Ther 1995 Nov;275(2):737-44
substance P (5-11), Glp(5)-Glu(O-benzyl)(11)  0   *Peptide Fragments Pyrrolidonecarboxylic Acid/*analogs & derivatives Substance P/*analogs & derivatives Receptors, Neurokinin-1/agonists. Int J Pept Protein Res 1995 Jun;45(6):508-13
substance P (6-11), Glp(6)-Glu(O-benzyl)(11)  0   *Peptide Fragments Pyrrolidonecarboxylic Acid/*analogs & derivatives Substance P/*analogs & derivatives Receptors, Neurokinin-1/agonists. Int J Pept Protein Res 1995 Jun;45(6):508-13
LY 297911  0   Receptors, Neurokinin-1/*antagonists & inhibitors. Am J Physiol 1995 Jun;268(6 Pt 1):L957-65
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Sources: NLM Medical Subject Headings, NIH UMLS, Drugs@FDA, FDA AERS original data copyright United States Government. No endorsement implied. Last modified 6/6/2012
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