Acetophenazine is a typical antipsychotic that binds to the serotonin (5-HT) receptor subtypes 5-HT6 and 5-HT7 and the androgen receptor (Kis = 72, 2.4, and 800 nM, respectively).1,2 Acetophenazine also inhibits the binding of the sigma receptor agonist SKF 10047 (Ki = 36 nM) and the dopamine D2-selective antagonist spiperone (IC50 = 17 nM) to guinea pig brain membranes.3 It increases the duration of fighting and the latency to submission in mice.4
1.Roth, B.L., Craigo, S.C., Choudhary, M.S., et al.Binding of typical and atypical antipsychotic agents to 5-hydroxytryptamine-6 and 5-hydroxytryptamine-7 receptorsJ. Pharmacol. Exp. Ther.268(3)1403-1410(1994) 2.Bisson, W.H., Cheltsov, A.V., Bruey-Sedano, N., et al.Discovery of antiandrogen activity of nonsteroidal scaffolds of marketed drugsProc. Natl. Acad. Sci. USA104(29)11927-11932(2007) 3.Tam, S.W., and Cook, L.σ opiates and certain antipsychotic drugs mutually inhibit (+)-[3H] SKF 10,047 and [3H]haloperidol binding in guinea pig brain membranesProc. Natl. Acad. Sci. USA81(17)5618-5621(1984) 4.Knight, W.R., Holtz, J.R., and Sprogis, G.R.Acetophenazine and fighting behavior in miceScience141(3583)830-831(1963)