Paliperidone palmitate

Paliperidone palmitate is an orally effective competitive antagonist of dopamine D2 receptors and 5-hydroxytryptamine 2A (5-HT2A) receptors that can cross the blood-brain barrier. Paliperidone palmitate competitively inhibits the effects of dopamine and 5-hydroxytryptamine by binding to dopamine D2 receptors and 5-HT2A receptors, regulating the balance of the neurotransmitter system and thus exerting antipsychotic activity. Paliperidone palmitate is mainly used in the research field of schizophrenia^[1][2][3]. In Vivo:Co-administration of paliperidone palmitate (62.4 mg/kg in mice and 20 mg/kg in rats; intramuscular injection; single dose) with hyaluronidase (HY-172442) altered the depot release of paliperidone palmitate in the first 4 days after injection and increased plasma exposure in both BALB/c mice and Sprague Dawley rat models, but did not affect the long-acting release characteristics of paliperidone palmitate. In mice, hyaluronidase altered the tissue morphology at the injection site, resulting in infiltration of macrophages between myocytes, and in rats, granulomas with central cavities and necrosis formed at the injection site[2].