YM-348

YM-348
YM-348
YM-348 structure.png
식별자
  • (2S)-1-(7-에틸-1H-푸로[2,3-g]indazol-1-yl)프로판-2-아민
CAS 번호
펍켐 CID
IUPHAR/BPS
켐스파이더
CompTox 대시보드 (EPA)
화학 및 물리적 데이터
공식C14H17N3O
어금질량243.1987 g·properties−1
3D 모델(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(14-12)8-9-9(2)15/7,9H,3,8,15H2,1-2H3/t9/m0/m01
  • 키:QLOWOVVZLBYHU-VIFPVBQESA-N
(iii)

YM-348인다졸 파생 의약품으로2B, 밀접하게 연관된 5-HT 수용체보다 3배 정도 선택성이 있지만 EC는50 1nM, 선택성은 15배인 5-HT2A 걸쳐 강력한 선택적 5-HT2C 수용체 작용제로 작용한다.[1][2] 동물 연구에서 열성식이성 효과가 있어 비만 치료에 잠재적으로 유용하다.[3][4][5][6]

참고 항목

참조

  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.