ISOCLOZAPINE is typical antipsychotic that acts by blocking the receptors in the brain’s dopamine pathways. Isoclozapine has high affinities at both DA (D1 and D2) and serotonin (5-HT2A and 5-HT2C) receptors. Isoclozapine shows the greatest antipsychotic potential on inhibition of apomorphine-induced climbing in mice at quite low doses under sc or po administrations. However, Isoclozapine also produces catalepsy at low doses.

PF-03246799 (PF-3246799) is a potent 5-HT2C receptor agonist. PF-3246799 had minimal activation at either the 5-HT2A or 5-HT2B receptors, combined with robust efficacy in a preclinical canine model of SUI and attractive pharmacokinetic and safety properties. It is a candidate for clinical development for the treatment of SUI.

WAY 208466 dihydrochloride is a high affinity, selective SR-6 (5-HT6) receptor agonist. WAY-208466 produced both antidepressant-like and anxiolytic-like effects. Direct infusion of WAY-208466 into the dorsal raphe nucleus, locus coeruleus, basal forebrain (horizontal limb of the diagonal band of Broca) or laterodorsal tegmental nucleus specifically decreased REM sleep without significantly altering wakefulness or slow wave sleep.

P-88-8991 (Hydroxy Iloperidone, 4-[3-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl] propoxy]- 3-methoxy-methylbenzenemethanol) is the major active metabolite of Iloperidone an atypical antipsychotic that used for the acute treatment of schizophrenia in adults. Metabolic reduction of Iloperidone carbonyl group leads to P-88-8991 in rats, dogs, and humans. The receptor affinity profile of P-88-8991 is comparable to that of iloperidone: this metabolite binds to the serotonin 5-HT2A receptors, adrenergic alpha1 and alpha2C receptors, and D2A receptors and with lower affinity to other monoamine (dopamine, serotonin, and histamine H1 ) receptors. The comparable receptor binding profile of P-88-8991 indicates that it is likely to contribute to the clinical profile of iloperidone. Preclinical experiments, such as the mouse apomorphine climbing test, the rat self-stimulation, and the pole climb avoidance task, indicate antipsychotic activity of P88-8991 and confirm that this metabolite crosses the blood–brain barrier