(Rac)-WAY-161503

(Rac)-WAY-161503 is a potent, selective, highly affinity 5-HT2C receptor agonist with a Ki of 4 nM and an EC50 of 12 nM. (Rac)-WAY-161503 displays higher affinity for 5-HT2C than 5-HT2A and 5-HT2B receptors. (Rac)-WAY-161503 has anti-obesity and antidepressant effects[1][2].

Research Areas >> Metabolic Disease

Research Areas >> Neurological Disease

Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor

Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor

5-HT2C Receptor:4 nM (Ki)

5-HT2C Receptor:12 nM (EC50)

(Rac)-WAY-161503 (3-30 mg/kg; intraperitoneal injection; male C57BL/6J mice) treatment dose-dependently decreases locomotor activity, an effect that is blocked by the 5-HT2C/2B antagonist SER-082. Additionally, the decreased locomotor activity produced by 10 mg/kg DOI is potentiated in the 5-HT2A KO mice[1]. Animal Model: Male C57BL/6J mice with hallucinogen 1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane (DOI)[1] Dosage: 3 mg/kg, 10 mg/kg, 30 mg/kg Administration: Intraperitoneal injection Result: Dose-dependently decreased locomotor activity, an effect that was blocked by the 5-HT2C/2B antagonist SER-082.

[1]. Halberstadt AL, et al. 5-HT(2A) and 5-HT(2C) receptors exert opposing effects on locomotor activity in mice. Neuropsychopharmacology. 2009 Jul;34(8):1958-67.

[2]. Welmaker GS, et al. Synthesis and 5-hydroxytryptamine (5-HT) activity of 2,3,4,4a-tetrahydro-1H-pyrazino[1,2-a]quinoxalin-5-(6H)ones and 2,3,4,4a,5,6-hexahydro-1H-pyrazino[1,2-a]quinoxalines. Bioorg Med Chem Lett. 2000 Sep 4;10(17):1991-4.