Target Information

Target General Infomation
Target ID
T89213
Former ID
TTDC00193
Target Name
Neuropeptide Y receptor type 1
Gene Name
NPY1R
Synonyms
NPY1-R; Neuropeptide Y Y(1) receptor; Neuropeptide Y receptor Y1; Neuropeptide Y-Y1 receptor; NPY1R
Target Type
Clinical Trial
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.
BioChemical Class
GPCR rhodopsin
Target Validation
T89213
UniProt ID
P25929
Sequence
MNSTLFSQVENHSVHSNFSEKNAQLLAFENDDCHLPLAMIFTLALAYGAVIILGVSGNLA
LIIIILKQKEMRNVTNILIVNLSFSDLLVAIMCLPFTFVYTLMDHWVFGEAMCKLNPFVQ
CVSITVSIFSLVLIAVERHQLIINPRGWRPNNRHAYVGIAVIWVLAVASSLPFLIYQVMT
DEPFQNVTLDAYKDKYVCFDQFPSDSHRLSYTTLLLVLQYFGPLCFIFICYFKIYIRLKR
RNNMMDKMRDNKYRSSETKRINIMLLSIVVAFAVCWLPLTIFNTVFDWNHQIIATCNHNL
LFLLCHLTAMISTCVNPIFYGFLNKNFQRDLQFFFNFCDFRSRDDDYETIAMSTMHTDVS
KTSLKQASPVAFKKINNNDDNEKI
Drugs and Mode of Action
Drug(s) GI-264879A Drug Info Preclinical Obesity [1]
PD-160170 Drug Info Preclinical Hypertension; Obesity; Heart disease [1]
H-409/22 Drug Info Discontinued in Phase 2 Cardiovascular disorder [2]
NEUROPEPTIDE-Y Drug Info Discontinued in Phase 2 Discovery agent [3]
BIBP 3226 Drug Info Terminated Hypertension [4], [5]
Neuropeptide Y Drug Info Terminated Discovery agent [6], [7]
SR 120819A Drug Info Terminated Eating disorder [8], [9]
Inhibitor 4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one Drug Info [10]
AcPYY(22-36) Drug Info [11]
Adp[-Trp-Arg-Nva-Arg-Tyr-NH2]2 Drug Info [12]
BMS-189323 Drug Info [13]
BMS-245782 Drug Info [13]
H-[Trp-Arg-Nva-Arg-Tyr]2-NH2 Drug Info [12]
H-[Trp-Arg-Nva-Arg-Tyr]3-NH2 Drug Info [12]
LRHYLNLLTRQRY-NH2 Drug Info [14]
N-arylpiperazine derivative Drug Info [13]
Neuropeptide Y Drug Info [15]
NEUROPEPTIDE-Y Drug Info [16]
Pim[-Trp-Arg-Nva-Arg-Tyr-NH2]2 Drug Info [12]
PYY(22-36) Drug Info [11]
Sub[-Trp-Arg-Nva-Arg-Tyr-NH2]2 Drug Info [12]
Sub[-Tyr-Arg-Leu-Arg-Tyr-NH2]2 Drug Info [12]
[Cys-Trp-Arg-Nva-Arg-Tyr-NH2]2 Drug Info [12]
Antagonist BIBO3304 Drug Info [17]
BIBP 3226 Drug Info [18], [19]
BMS-193885 Drug Info [20]
GI-264879A Drug Info [1]
H-409/22 Drug Info [21]
J-104870 Drug Info [22]
NPY-1 antagonist Drug Info [23]
PD-160170 Drug Info [1]
S-19528 Drug Info [23]
S-25585 Drug Info [23]
SR 120819A Drug Info [24]
[125I]GR231118 Drug Info [25]
[3H]BIBP3226 Drug Info [26]
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 1Emerging drugs for obesity: linking novel biological mechanisms to pharmaceutical pipelines. Expert Opin Emerg Drugs. 2005 Aug;10(3):643-60.
REF 2Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800013561)
REF 3ClinicalTrials.gov (NCT00748956) Intranasal Administration of Neuropeptide Y in Healthy Male Volunteers. U.S. National Institutes of Health.
REF 4Neuropeptide 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 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: 1485).
REF 6(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 7Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007971)
REF 8SR 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 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: 1530).
REF 10J 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 11Bioorg Med Chem Lett. 2007 Jan 15;17(2):538-41. Epub 2006 Oct 7.Identification of selective neuropeptide Y2 peptide agonists.
REF 12J 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 13Bioorg Med Chem Lett. 2004 Dec 20;14(24):5975-8.Isosteric N-arylpiperazine replacements in a series of dihydropyridine NPY1 receptor antagonists.
REF 14Bioorg 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 15J 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 16J 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 17Neuropeptide Y induced modulation of dopamine synthesis in the striatum. Regul Pept. 2005 Jul 15;129(1-3):73-8.
REF 18Effects 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 19Intracerebroventricular 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 20Dihydropyridine neuropeptide Y Y(1) receptor antagonists. Bioorg Med Chem Lett. 2002 Feb 11;12(3):379-82.
REF 21In vivo characterization of the novel neuropeptide Y Y1 receptor antagonist H 409/22. J Cardiovasc Pharmacol. 2000 Oct;36(4):516-25.
REF 22The 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 23Emerging drugs for eating disorder treatment. Expert Opin Emerg Drugs. 2006 May;11(2):315-36.
REF 24SR 120819A, an orally-active and selective neuropeptide Y Y1 receptor antagonist. FEBS Lett. 1995 Apr 3;362(2):192-6.
REF 25[(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 26(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: 305).

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