WAY-161503

WAY-161503
Identifiers
	IUPAC name 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
Formula	C11H11Cl2N3O
Molar mass	272.13 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES Clc1cc2NC(=O)C3CNCCN3c2cc1Cl;
	InChI 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 is a full agonist of 5-HT_2C receptors (Ki = 3.3 nM for displacement of DOI), ~6-fold less potent at 5-HT_2A receptors (Ki = 18 nM) and 20-fold less potent at 5-HT_2B receptors (Ki = 60 nM).^[1] In functional studies, it stimulates calcium mobilization coupled to 5-HT_2C, 5-HT_2B, and 5-HT_2A 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 has been used to examine the role of 5-HT_2C receptors in rodent models of depression, locomotion, reinforcement, or motivated behaviors.^[2]^[3]

References

^ ^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.
^ 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.
^ 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.

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[Sharon-1] 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.

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