Uses
WAY-163909 hydrochloride is a potent 5-hydroxytryptamine receptor 2C (5-HT2C) agonist with an EC50 of 8 nM and a maximum efficacy of 90%, while displaying minimal activity at 5-HT2A receptors. Its selectivity is further demonstrated by Ki values of 10.5 nM for 5-HT2C, alongside higher Ki values for 5-HT2A (212 nM), 5-HT7 (343 nM), and 5-HT2B (485 nM), and it lacks significant activity at various other receptors.
Biochem/physiol Actions
WAY-163909 is a 5-hydroxytryptamine receptor 2C (5-HT2C) agonist (EC50/Emax = 8 nM/90% vs. 185 nM/40%/5-HT2B; Ki = 10.5 nM/5-HT2C, 212 nM/5-HT2A, 343 nM/5-HT7, 485 nM/5-HT2B, 245 nM/D4, 665 nM/rat α-1, >1 μM/5-HT1A, D2, D3, rat 5-HT-T) with no 5-HT2A-stimulatory potency. WAY-163909 exhibits anorectic (ED50 in mg/kg via i.p. = 1.4/DIO mice and 5.19/Zucker rats), antipsychotic (morphine-induced mouse climbing ID50 = 10.69 mg/kg i.p.; rat avoidance responding reduction ED50 = 1.27 mg/kg i.p. and 6.50 mg/kg p.o.) and antidepressant (10 mg/kg, i.p. or s.c. in forced rat swimming test ; 3 mg/kg/day i.p. in reducing olfactory bulbectomy/BULB-induced hyperactivity in rats) efficacy in vivo.
