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YM-348

From Wikipedia, the free encyclopedia
Chemical compound
Pharmaceutical compound
YM-348
Identifiers
  • (2S)-1-(7-ethyl-1H-furo[2,3-g]indazol-1-yl)propan-2-amine
CAS Number
PubChemCID
IUPHAR/BPS
ChemSpider
UNII
CompTox Dashboard(EPA)
Chemical and physical data
FormulaC14H17N3O
Molar mass243.310 g·mol−1
3D model (JSmol)
  • n3cc2ccc1oc(cc1c2n3C[C@@H](N)C)CC
  • InChI=1S/C14H17N3O/c1-3-11-6-12-13(18-11)5-4-10-7-16-17(14(10)12)8-9(2)15/h4-7,9H,3,8,15H2,1-2H3/t9-/m0/s1
  • Key:QLOOWOVVZLBYHU-VIFPVBQESA-N
  (verify)

YM-348 is anindazolethylamine derivative drug which acts as a potent and selective5-HT2Creceptoragonist, with an EC50 of 1nM and 15x selectivity over5-HT2A, although it only has moderate selectivity of 3x over the closely related5-HT2B receptor.[1][2] It hasthermogenic andanorectic effects in animal studies, making it potentially useful for the treatment ofobesity.[3][4][5][6]

See also

[edit]

References

[edit]
  1. ^Kimura Y, Hatanaka K, Naitou Y, Maeno K, Shimada I, Koakutsu A, et al. (January 2004). "Pharmacological profile of YM348, a novel, potent and orally active 5-HT2C receptor agonist".European Journal of Pharmacology.483 (1):37–43.doi:10.1016/j.ejphar.2003.10.004.PMID 14709324.
  2. ^Shimada I, Maeno K, Kazuta K, Kubota H, Kimizuka T, Kimura Y, et al. (February 2008). "Synthesis and structure-activity relationships of a series of substituted 2-(1H-furo[2,3-g]indazol-1-yl)ethylamine derivatives as 5-HT2C receptor agonists".Bioorganic & Medicinal Chemistry.16 (4):1966–82.doi:10.1016/j.bmc.2007.10.100.PMID 18035544.
  3. ^Hayashi A, Sonoda R, Kimura Y, Takasu T, Suzuki M, Sasamata M, Miyata K (June 2004). "Antiobesity effect of YM348, a novel 5-HT2C receptor agonist, in Zucker rats".Brain Research.1011 (2):221–7.doi:10.1016/j.brainres.2004.03.032.PMID 15157808.S2CID 23199460.
  4. ^Smith BM, Thomsen WJ, Grottick AJ (March 2006). "The potential use of selective 5-HT2C agonists in treating obesity".Expert Opinion on Investigational Drugs.15 (3):257–66.doi:10.1517/13543784.15.3.257.PMID 16503763.S2CID 22100586.
  5. ^Nilsson BM (July 2006). "5-Hydroxytryptamine 2C (5-HT2C) receptor agonists as potential antiobesity agents".Journal of Medicinal Chemistry.49 (14):4023–34.doi:10.1021/jm058240i.PMID 16821762.
  6. ^Wacker DA, Miller KJ (July 2008). "Agonists of the serotonin 5-HT2C receptor: preclinical and clinical progression in multiple diseases".Current Opinion in Drug Discovery & Development.11 (4):438–45.PMID 18600561.
5-HT1
5-HT1A
5-HT1B
5-HT1D
5-HT1E
5-HT1F
5-HT2
5-HT2A
5-HT2B
5-HT2C
5-HT37
5-HT3
5-HT4
5-HT5A
5-HT6
5-HT7
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