BMS-470,539

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BMS-470,539
BMS 470539.svg
Systematic (IUPAC) name
(2S)-2-amino-N-[(1R)-2-(4-butanoyl-4-phenyl-1-piperidyl)-1-[(4-methoxyphenyl)methyl]-2-oxo-ethyl]-3-(3-methylimidazol-4-yl)propanamide dihydrochloride
Clinical data
Legal status
  • Non-regulated
Routes S.C.[1]
Pharmacokinetic data
Bioavailability 100% (with S.C. administration)[1]
Half-life 1.7 hours[1]
Identifiers
CAS number 457893-92-4 N
ATC code None
ChemSpider 26232155 YesY
Chemical data
Formula C32H41N5O4 
Molecular mass 559.70 g/mol
 N (what is this?)  (verify)

BMS-470,539 is a synthetic, small molecule drug which acts as a potent and highly selective full agonist of the MC1 receptor.[2][1] It was discovered in 2003 as part of an effort to understand the role of the MC1 receptor in immunomodulation, and has since been used in scientific research to determine its role in inflammatory processes.[2][1][3] The compound was designed with the intention of mimicking the central His-Phe-Arg-Trp pharmacophore of the melanocortins,[1][2] and this proved to be successful based on its favorable pharmacodynamic profile.

See also[edit]

References[edit]

  1. ^ a b c d e f Kang L, McIntyre KW, Gillooly KM, et al. (October 2006). "A selective small molecule agonist of the melanocortin-1 receptor inhibits lipopolysaccharide-induced cytokine accumulation and leukocyte infiltration in mice". Journal of Leukocyte Biology 80 (4): 897–904. doi:10.1189/jlb.1204748. PMID 16888084. 
  2. ^ a b c Herpin TF, Yu G, Carlson KE, et al. (March 2003). "Discovery of tyrosine-based potent and selective melanocortin-1 receptor small-molecule agonists with anti-inflammatory properties". Journal of Medicinal Chemistry 46 (7): 1123–6. doi:10.1021/jm025600i. PMID 12646021. 
  3. ^ Leoni G, Voisin MB, Carlson K, Getting S, Nourshargh S, Perretti M (May 2010). "The melanocortin MC(1) receptor agonist BMS-470539 inhibits leucocyte trafficking in the inflamed vasculature". British Journal of Pharmacology 160 (1): 171–80. doi:10.1111/j.1476-5381.2010.00688.x. PMC 2860217. PMID 20331604.