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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
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1. Binding of typical and atypical antipsychotic agents to 5-
2. Discovery of antiandrogen activity of nonsteroidal scaffolds of marketed drugs. Proc. Natl. Acad. Sci. USA 104(29), 11927-11932 (2007).
3. σ opiates and certain antipsychotic drugs mutually inhibit (+)-
4. Acetophenazine and fighting behavior in mice. Science 141(3583), 830-831 (1963).