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 (NMUR1, NMUR2).
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
Antagonists
- NMU2 selective
- R-PSOP [6]
References
- ^ Brighton PJ, Szekeres PG, Willars GB (June 2004). "Neuromedin U and its receptors: structure, function, and physiological roles". Pharmacological Reviews. 56 (2): 231–48. doi:10.1124/pr.56.2.3. PMID 15169928. S2CID 884735.
- ^ Mitchell J, Maguire J, Davenport A (June 2009). "Emerging pharmacology and physiology of neuromedin U and the structurally related peptide neuromedin S". British Journal of Pharmacology. 158 (1): 87–103. doi:10.1111/j.1476-5381.2009.00252.x. PMC 2795236. PMID 19519756.
- ^ Peier A, Kosinski J, Cox-York K, Qian Y, Desai K, Feng Y, Trivedi P, Hastings N, Marsh DJ (July 2009). "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. doi:10.1210/en.2008-1772. PMC 2703546. PMID 19324999.
- ^ Meng T, Su HR, Binkert C, Fischli W, Zhou L, Shen JK, Wang MW (April 2008). "Identification of non-peptidic neuromedin U receptor modulators by a robust homogeneous screening assay". Acta Pharmacologica Sinica. 29 (4): 517–27. doi:10.1111/j.1745-7254.2008.00769.x. PMID 18358099.
- ^ Kajino M, Hinuma S, Tarui N, Yamashita T, Nakayama Y. Receptor regulators. European Patent EP 1559428 A1. Published 03.08.2005
- ^ 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 (July 2009). "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. doi:10.1124/jpet.109.152967. PMID 19369576. S2CID 7366636.
External links
- "Neuromedin U Receptors". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. Archived from the original on 2016-03-03. Retrieved 2007-10-25.
- Neuromedin+U+Receptor at the U.S. National Library of Medicine Medical Subject Headings (MeSH)
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This page was last edited on 10 March 2024, at 11:14