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YM-348
Systematic (IUPAC) name
(2S)-​1-​(7-​ethyl-​1H-​furo[2,3- g]indazol-​1-​yl)propan-​2-​amine
Identifiers
CAS number  ?
ATC code  ?
PubChem  ?
Chemical data
Formula C 14H17N3O 
Mol. mass 243.304 g/mol
SMILES eMolecules & PubChem
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life  ?
Excretion  ?
Therapeutic considerations
Pregnancy cat.  ?
Legal status
Routes  ?

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. Pharmacological profile of YM348, a novel, potent and orally active 5-HT2C receptor agonist. European Journal of Pharmacology. 2004 Jan 1;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, Sakamoto S, Tsukamoto S. 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 and Medicinal Chemistry. 2008 Feb 15;16(4):1966-82. PMID 18035544
  3. ^ Hayashi A, Sonoda R, Kimura Y, Takasu T, Suzuki M, Sasamata M, Miyata K. Antiobesity effect of YM348, a novel 5-HT2C receptor agonist, in Zucker rats. Brain Research. 2004 Jun 18;1011(2):221-7. PMID 15157808
  4. ^ Smith BM, Thomsen WJ, Grottick AJ. The potential use of selective 5-HT2C agonists in treating obesity. Expert Opinion on Investigational Drugs. 2006 Mar;15(3):257-66. PMID 16503763
  5. ^ Nilsson BM. 5-Hydroxytryptamine 2C (5-HT2C) receptor agonists as potential antiobesity agents. Journal of Medicinal Chemistry. 2006 Jul 13;49(14):4023-34. PMID 16821762
  6. ^ Wacker DA, Miller KJ. Agonists of the serotonin 5-HT2C receptor: preclinical and clinical progression in multiple diseases. Current Opinion in Drug Discovery and Development. 2008 Jul;11(4):438-45. PMID 18600561
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