YM-348

YM-348
Identifiers
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
Chemical and physical data
Formula C14H17N3O
Molar mass 243.31 g·mol−1
3D model (JSmol)
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YM-348 is an indazole derivative drug which acts as a potent and selective 5-HT2C receptor agonist, with an EC50 of 1nM and 15x selectivity over 5-HT2A, although it only has moderate selectivity of 3x over the closely related 5-HT2B receptor.[1][2] It has thermogenic and anorectic effects in animal studies, making it potentially useful for the treatment of obesity.[3][4][5][6]

See also

References

  1. ↑ Kimura, Y; Hatanaka, K; Naitou, Y; Maeno, K; Shimada, I; Koakutsu, A; Wanibuchi, F; Yamaguchi, T (2004). "Pharmacological profile of YM348, a novel, potent and orally active 5-HT2C receptor agonist". European Journal of Pharmacology. 483 (1): 37–43. PMID 14709324. doi:10.1016/j.ejphar.2003.10.004.
  2. ↑ Shimada, I; Maeno, K; Kazuta, K; Kubota, H; Kimizuka, T; Kimura, Y; Hatanaka, K; Naitou, Y; et al. (2008). "Synthesis and structure-activity relationships of a series of substituted 2-(1H-furo2,3-gindazol-1-yl)ethylamine derivatives as 5-HT2C receptor agonists". Bioorganic & Medicinal Chemistry. 16 (4): 1966–82. PMID 18035544. doi:10.1016/j.bmc.2007.10.100.
  3. ↑ Hayashi, A; Sonoda, R; Kimura, Y; Takasu, T; Suzuki, M; Sasamata, M; Miyata, K (2004). "Antiobesity effect of YM348, a novel 5-HT2C receptor agonist, in Zucker rats". Brain Research. 1011 (2): 221–7. PMID 15157808. doi:10.1016/j.brainres.2004.03.032.
  4. ↑ Smith, BM; Thomsen, WJ; Grottick, AJ (2006). "The potential use of selective 5-HT2C agonists in treating obesity". Expert Opinion on Investigational Drugs. 15 (3): 257–66. PMID 16503763. doi:10.1517/13543784.15.3.257.
  5. ↑ Nilsson, BM (2006). "5-Hydroxytryptamine 2C (5-HT2C) receptor agonists as potential antiobesity agents". Journal of Medicinal Chemistry. 49 (14): 4023–34. PMID 16821762. doi:10.1021/jm058240i.
  6. ↑ Wacker, DA; Miller, KJ (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.


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