Neuromedin U receptor explained

neuromedin U receptor 1
Hgncid:	4518
Symbol:	NMUR1
Altsymbols:	GPR66
Entrezgene:	10316
Omim:	604153
Refseq:	NM_006056
Uniprot:	Q9HB89
Chromosome:	2
Arm:	q
Band:	37.1

neuromedin U receptor 2
Hgncid:	16454
Symbol:	NMUR2
Altsymbols:	NMU2R
Entrezgene:	56923
Omim:	605108
Refseq:	NM_020167
Uniprot:	Q9GZQ4
Chromosome:	5
Arm:	q
Band:	33.1

The neuromedin U receptors are two G-protein coupled receptors which bind the neuropeptide hormones neuromedin U and neuromedin S.^[1] There are two subtypes of the neuromedin U receptor, each encoded by a separate gene .

Selective Ligands

Neuromedin U is an agonist at both the NMU₁ and NMU₂ subtypes, while neuromedin S is selective for NMU₂, and is a more potent agonist at this subtype than neuromedin U.^{[2] [3]} Several other peptide and non-peptide ligands are also available for the NMU receptors.

Agonists

Non-selective

• Neuromedin U
• non-peptide NMU modulators ^{[4] [5]}

NMU₂ selective

• Neuromedin S

Antagonists

NMU₂ selective

• R-PSOP ^[6]

External links

• Web site: Neuromedin U Receptors . IUPHAR Database of Receptors and Ion Channels . International Union of Basic and Clinical Pharmacology . 2007-10-25 . 2016-03-03 . https://web.archive.org/web/20160303184108/http://www.iuphar-db.org/GPCR/ChapterMenuForward?chapterID=1312 . dead .

Notes and References

1. Brighton PJ, Szekeres PG, Willars GB . Neuromedin U and its receptors: structure, function, and physiological roles . . 56 . 2 . 231–48 . June 2004 . 15169928 . 10.1124/pr.56.2.3 . 884735 .
2. Mitchell J, Maguire J, Davenport A . Emerging pharmacology and physiology of neuromedin U and the structurally related peptide neuromedin S . British Journal of Pharmacology . 158. 1. 87–103. June 2009 . 19519756 . 10.1111/j.1476-5381.2009.00252.x . 2795236.
3. Peier A, Kosinski J, Cox-York K, Qian Y, Desai K, Feng Y, Trivedi P, Hastings N, Marsh DJ . The antiobesity effects of centrally administered neuromedin U and neuromedin S are mediated predominantly by the neuromedin U receptor 2 (NMUR2) . Endocrinology . 150 . 7 . 3101–9 . July 2009 . 19324999 . 10.1210/en.2008-1772 . 2703546.
4. Meng T, Su HR, Binkert C, Fischli W, Zhou L, Shen JK, Wang MW . Identification of non-peptidic neuromedin U receptor modulators by a robust homogeneous screening assay . Acta Pharmacologica Sinica . 29 . 4 . 517–27 . April 2008 . 18358099 . 10.1111/j.1745-7254.2008.00769.x. free .
5. Kajino M, Hinuma S, Tarui N, Yamashita T, Nakayama Y. Receptor regulators. European Patent EP 1559428 A1. Published 03.08.2005
6. Liu JJ, Payza K, Huang J, Liu R, Chen T, Coupal M, Laird JM, Cao CQ, Butterworth J, Lapointe S, Bayrakdarian M, Trivedi S, Bostwick JR . Discovery and pharmacological characterization of a small-molecule antagonist at neuromedin U receptor NMUR2 . The Journal of Pharmacology and Experimental Therapeutics . 330 . 1 . 268–75 . July 2009 . 19369576 . 10.1124/jpet.109.152967 . 7366636 .