YM-348
YM-348 je lek sa indazolnim osnovom koji deluje kao potentan i selektivan agonist 5-HT2C receptor, sa EC50 vrednošću od 1 nM i 15x selektivnošću u odnosu na 5-HT2A. On je umereno selektivan 3x u odnosu na blisko srodni 5-HT2B receptor.[1][2] On ispoljava termogeno i anoreksično dejsto u životinjskim studijama, što ga čini potencijalno korisnim u lečenju gojaznosti.[3][4][5][6]
IUPAC ime | |
---|---|
(2S)-1-(7-ethyl-1H-furo[2,3-g]indazol-1-il)propan-2-amin | |
Hemijski podaci | |
Formula | C14H17N3O |
Molarna masa | 243,304 g/mol |
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Vidi još
уредиReference
уреди- ^ 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.
- ^ Shimada, I; Maeno, K; Kazuta, K; Kubota, H; Kimizuka, T; Kimura, Y; Hatanaka, K; Naitou, Y; Wanibuchi, F (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.
- ^ 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.
- ^ 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.
- ^ 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.
- ^ 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.
Spoljašnje veze
уреди
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