Target Information
Target General Infomation | |||||
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Target ID |
T89213
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Former ID |
TTDC00193
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Target Name |
Neuropeptide Y receptor type 1
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Gene Name |
NPY1R
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Synonyms |
NPY1-R; Neuropeptide Y Y(1) receptor; Neuropeptide Y receptor Y1; Neuropeptide Y-Y1 receptor; NPY1R
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Target Type |
Clinical Trial
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Disease | Cardiovascular disorder [ICD10: I00-I99] | ||||
Eating disorders reduction in food intake obesity anxiety [ICD9: 307.5; ICD10: F50] | |||||
Eating disorders reduction in food intake [ICD9: 307.5; ICD10: F50] | |||||
Eating disorder [ICD9: 278, 307.5, 401, 428.0; ICD10: E66, F50, I10-I16, I50] | |||||
Hypertension [ICD9: 401; ICD10: I10-I16] | |||||
Hypertension; Obesity; Heart disease [ICD9: 278, 390-429; ICD10: E66, I00-I52] | |||||
Obesity [ICD9: 278; ICD10: E66] | |||||
Function |
Receptor for neuropeptide Y and peptide YY. The rank order of affinity of this receptor for pancreatic polypeptides is NPY > [Pro-34] PYY, PYY and [Leu-31, Pro-34] NPY > NPY (2-36) > [Ile-31, Gln-34] PP and PYY (3-36) > PP > NPY free acid.
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BioChemical Class |
GPCR rhodopsin
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Target Validation |
T89213
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UniProt ID | |||||
Sequence |
MNSTLFSQVENHSVHSNFSEKNAQLLAFENDDCHLPLAMIFTLALAYGAVIILGVSGNLA
LIIIILKQKEMRNVTNILIVNLSFSDLLVAIMCLPFTFVYTLMDHWVFGEAMCKLNPFVQ CVSITVSIFSLVLIAVERHQLIINPRGWRPNNRHAYVGIAVIWVLAVASSLPFLIYQVMT DEPFQNVTLDAYKDKYVCFDQFPSDSHRLSYTTLLLVLQYFGPLCFIFICYFKIYIRLKR RNNMMDKMRDNKYRSSETKRINIMLLSIVVAFAVCWLPLTIFNTVFDWNHQIIATCNHNL LFLLCHLTAMISTCVNPIFYGFLNKNFQRDLQFFFNFCDFRSRDDDYETIAMSTMHTDVS KTSLKQASPVAFKKINNNDDNEKI |
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Drugs and Mode of Action | |||||
Drug(s) | GI-264879A | Drug Info | Preclinical | Obesity | [536122] |
PD-160170 | Drug Info | Preclinical | Hypertension; Obesity; Heart disease | [536122] | |
H-409/22 | Drug Info | Discontinued in Phase 2 | Cardiovascular disorder | [547165] | |
NEUROPEPTIDE-Y | Drug Info | Discontinued in Phase 2 | Discovery agent | [522433] | |
BIBP 3226 | Drug Info | Terminated | Hypertension | [534151], [538935] | |
Neuropeptide Y | Drug Info | Terminated | Discovery agent | [538940], [546411] | |
SR 120819A | Drug Info | Terminated | Eating disorder | [534212], [538943] | |
Inhibitor | 4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one | Drug Info | [531079] | ||
AcPYY(22-36) | Drug Info | [528484] | |||
Adp[-Trp-Arg-Nva-Arg-Tyr-NH2]2 | Drug Info | [528136] | |||
BMS-189323 | Drug Info | [527291] | |||
BMS-245782 | Drug Info | [527291] | |||
H-[Trp-Arg-Nva-Arg-Tyr]2-NH2 | Drug Info | [528136] | |||
H-[Trp-Arg-Nva-Arg-Tyr]3-NH2 | Drug Info | [528136] | |||
LRHYLNLLTRQRY-NH2 | Drug Info | [528667] | |||
N-arylpiperazine derivative | Drug Info | [527291] | |||
Neuropeptide Y | Drug Info | [530519] | |||
NEUROPEPTIDE-Y | Drug Info | [529844] | |||
Pim[-Trp-Arg-Nva-Arg-Tyr-NH2]2 | Drug Info | [528136] | |||
PYY(22-36) | Drug Info | [528484] | |||
Sub[-Trp-Arg-Nva-Arg-Tyr-NH2]2 | Drug Info | [528136] | |||
Sub[-Tyr-Arg-Leu-Arg-Tyr-NH2]2 | Drug Info | [528136] | |||
[Cys-Trp-Arg-Nva-Arg-Tyr-NH2]2 | Drug Info | [528136] | |||
Antagonist | BIBO3304 | Drug Info | [536091] | ||
BIBP 3226 | Drug Info | [535020], [535675] | |||
BMS-193885 | Drug Info | [535359] | |||
GI-264879A | Drug Info | [536122] | |||
H-409/22 | Drug Info | [525884] | |||
J-104870 | Drug Info | [534933] | |||
NPY-1 antagonist | Drug Info | [536225] | |||
PD-160170 | Drug Info | [536122] | |||
S-19528 | Drug Info | [536225] | |||
S-25585 | Drug Info | [536225] | |||
SR 120819A | Drug Info | [537861] | |||
[125I]GR231118 | Drug Info | [525704] | |||
[3H]BIBP3226 | Drug Info | [543756] | |||
Pathways | |||||
KEGG Pathway | cAMP signaling pathway | ||||
Neuroactive ligand-receptor interaction | |||||
NetPath Pathway | FSH Signaling Pathway | ||||
Reactome | Peptide ligand-binding receptors | ||||
G alpha (i) signalling events | |||||
WikiPathways | GPCRs, Class A Rhodopsin-like | ||||
Peptide GPCRs | |||||
Endothelin Pathways | |||||
GPCR ligand binding | |||||
GPCR downstream signaling | |||||
References | |||||
Ref 522433 | ClinicalTrials.gov (NCT00748956) Intranasal Administration of Neuropeptide Y in Healthy Male Volunteers. U.S. National Institutes of Health. | ||||
Ref 534151 | Neuropeptide Y and the nonpeptide antagonist BIBP 3226 share an overlapping binding site at the human Y1 receptor. Mol Pharmacol. 1996 Aug;50(2):285-92. | ||||
Ref 534212 | SR 120107A antagonizes neuropeptide Y Y1 receptor mediated sympathetic vasoconstriction in pigs in vivo. Eur J Pharmacol. 1996 Jun 3;305(1-3):145-54. | ||||
Ref 536122 | Emerging drugs for obesity: linking novel biological mechanisms to pharmaceutical pipelines. Expert Opin Emerg Drugs. 2005 Aug;10(3):643-60. | ||||
Ref 538935 | (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: 1485). | ||||
Ref 538940 | (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: 1504). | ||||
Ref 538943 | (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: 1530). | ||||
Ref 525704 | [(125)I]-GR231118: a high affinity radioligand to investigate neuropeptide Y Y(1) and Y(4) receptors. Br J Pharmacol. 2000 Jan;129(1):37-46. | ||||
Ref 525884 | In vivo characterization of the novel neuropeptide Y Y1 receptor antagonist H 409/22. J Cardiovasc Pharmacol. 2000 Oct;36(4):516-25. | ||||
Ref 527291 | Bioorg Med Chem Lett. 2004 Dec 20;14(24):5975-8.Isosteric N-arylpiperazine replacements in a series of dihydropyridine NPY1 receptor antagonists. | ||||
Ref 528136 | J Med Chem. 2006 Apr 20;49(8):2661-5.Neuropeptide Y (NPY) Y4 receptor selective agonists based on NPY(32-36): development of an anorectic Y4 receptor selective agonist with picomolar affinity. | ||||
Ref 528484 | Bioorg Med Chem Lett. 2007 Jan 15;17(2):538-41. Epub 2006 Oct 7.Identification of selective neuropeptide Y2 peptide agonists. | ||||
Ref 528667 | Bioorg Med Chem Lett. 2007 Apr 1;17(7):1916-9. Epub 2007 Jan 24.A long-acting selective neuropeptide Y2 receptor PEGylated peptide agonist reduces food intake in mice. | ||||
Ref 529844 | J Med Chem. 2008 Dec 25;51(24):8168-72.Guanidine-acylguanidine bioisosteric approach in the design of radioligands: synthesis of a tritium-labeled N(G)-propionylargininamide ([3H]-UR-MK114) as a highly potent and selective neuropeptide Y Y1 receptor antagonist. | ||||
Ref 530519 | J Nat Prod. 2009 Dec;72(12):2172-6.5-OHKF and NorKA, depsipeptides from a Hawaiian collection of Bryopsis pennata: binding properties for NorKA to the human neuropeptide Y Y1 receptor. | ||||
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 534933 | The novel neuropeptide Y Y(1) receptor antagonist J-104870: a potent feeding suppressant with oral bioavailability. Biochem Biophys Res Commun. 1999 Dec 9;266(1):88-91. | ||||
Ref 535020 | Effects of a selective neuropeptide Y Y(1) receptor antagonist BIBP 3226 on double peaked vasoconstrictor responses to periarterial nerve stimulation in canine splenic arteries. Br J Pharmacol. 2000 Aug;130(7):1699-705. | ||||
Ref 535359 | Dihydropyridine neuropeptide Y Y(1) receptor antagonists. Bioorg Med Chem Lett. 2002 Feb 11;12(3):379-82. | ||||
Ref 535675 | Intracerebroventricular injection of a neuropeptide Y-Y1 receptor agonist increases while BIBP3226, a Y1 antagonist, reduces the infarct volume following transient middle cerebral artery occlusion inrats. Neuroscience. 2003;116(1):119-26. | ||||
Ref 536091 | Neuropeptide Y induced modulation of dopamine synthesis in the striatum. Regul Pept. 2005 Jul 15;129(1-3):73-8. | ||||
Ref 536122 | Emerging drugs for obesity: linking novel biological mechanisms to pharmaceutical pipelines. Expert Opin Emerg Drugs. 2005 Aug;10(3):643-60. | ||||
Ref 536225 | Emerging drugs for eating disorder treatment. Expert Opin Emerg Drugs. 2006 May;11(2):315-36. |
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