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Neuromedin U receptor: Wikis

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neuromedin U receptor 1
Identifiers
Symbol NMUR1
Alt. symbols GPR66
Entrez 10316
HUGO 4518
OMIM 604153
RefSeq NM_006056
UniProt Q9HB89
Other data
Locus Chr. 2 q37.1
neuromedin U receptor 2
Identifiers
Symbol NMUR2
Alt. symbols NMU2R
Entrez 56923
HUGO 16454
OMIM 605108
RefSeq NM_020167
UniProt Q9GZQ4
Other data
Locus Chr. 5 q33.1

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 (NMUR1, NMUR2).

Contents

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.

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Agonists

Non-selective
NMU2 selective

Antagonists

NMU2 selective

References

  1. ^ 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.  
  2. ^ 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. doi:10.1111/j.1476-5381.2009.00252.x. PMID 19519756.  
  3. ^ 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. PMID 19324999.  
  4. ^ 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. PMID 18358099.  
  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 (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.  

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