WAY-161503

Summary

WAY-161503 is a full agonist of 5-HT2C receptors (Ki = 3.3 nM for displacement of DOI), ~6-fold less potent at 5-HT2A receptors (Ki = 18 nM) and 20-fold less potent at 5-HT2B receptors (Ki = 60 nM).[1] In functional studies, it stimulates calcium mobilization coupled to 5-HT2C, 5-HT2B, and 5-HT2A receptors with EC50 values of 0.8, 1.8, and 7 nM, respectively.[1] WAY-161503 has been reported to produce dose-dependent decreases in food intake in 24-hour fasted normal Sprague-Dawley rats, diet-induced obese mice, and obese Zucker rats with ED50 values of 1.9, 6.8, and 0.73 mg/kg, respectively.[1]

WAY-161503
Identifiers
  • 8,9-dichloro-2,3,4,4a-tetrahydro-1H-pyrazino[1,2-a]quinoxalin-5(6H)-one
CAS Number
  • 75704-24-4
PubChem CID
  • 3906894
ChemSpider
  • 3130042
Chemical and physical data
FormulaC11H11Cl2N3O
Molar mass272.13 g·mol−1
3D model (JSmol)
  • Interactive image
  • Clc1cc2NC(=O)C3CNCCN3c2cc1Cl
  • InChI=1S/C11H11Cl2N3O/c12-6-3-8-9(4-7(6)13)16-2-1-14-5-10(16)11(17)15-8/h3-4,10,14H,1-2,5H2,(H,15,17)
  • Key:PHGWDAICBXUJDU-UHFFFAOYSA-N

WAY-161503 has been used to examine the role of 5-HT2C receptors in rodent models of depression, locomotion, reinforcement, or motivated behaviors.[2][3]

References edit

  1. ^ a b c Rosenzweig-Lipson S, Zhang J, Mazandarani H, Harrison BL, Sabb A, Sabalski J, et al. (February 2006). "Antiobesity-like effects of the 5-HT2C receptor agonist WAY-161503". Brain Research. 1073–1074: 240–51. doi:10.1016/j.brainres.2005.12.052. PMID 16430874. S2CID 23160473.
  2. ^ Cryan JF, Lucki I (December 2000). "Antidepressant-like behavioral effects mediated by 5-Hydroxytryptamine(2C) receptors". The Journal of Pharmacology and Experimental Therapeutics. 295 (3): 1120–6. PMID 11082448.
  3. ^ Hayes DJ, Mosher TM, Greenshaw AJ (February 2009). "Differential effects of 5-HT2C receptor activation by WAY 161503 on nicotine-induced place conditioning and locomotor activity in rats". Behavioural Brain Research. 197 (2): 323–30. doi:10.1016/j.bbr.2008.08.034. PMID 18805442. S2CID 16911749.