YM-348

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YM-348
(IUPAC) ime
(2S)-​1-​(7-​ethyl-​1H-​furo[2,3-g]indazol-​1-​il)propan-​2-​amin
Klinički podaci
Identifikatori
ATC kod  ?
Hemijski podaci
Formula C14H17N3O 
Mol. masa 243,304 g/mol
SMILES eMolekuli & PubHem
Farmakoinformacioni podaci
Trudnoća  ?
Pravni status

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]

Vidi još[uredi - уреди | uredi izvor]

Reference[uredi - уреди | uredi izvor]

  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. 
  2. 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. 
  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. 

Spoljašnje veze[uredi - уреди | uredi izvor]


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