Prochlorperazine maleate (84-02-6) inhibits dynamin and clathrin-mediated endocytosis (CME) with an IC50=5.8 μM for CME.1?Increases tumor cell antigen presentation enhancing the efficacy of anti-tumor mAbs.2?A clinically useful antipsychotic agent3?with antimigraine4?and antiemetic activity5.
Antiemetic;Dopamine antagonist
Compazine (GlaxoSmithKline).
Prochlorperazinemaleate, 2-chloro-10-[3-(4-methyl-1-piperazinyl)propyl]phenothiazinemaleate (Compazine), is in the piperazine subgroupof the phenothiazines, characterized by high-milligramantipsychotic potency, a high prevalence of EPS, and lowsedative and autonomic effects. Prochlorperazine is more potenton a milligram basis than its alkylamino counterpart,chlorpromazine. Because of the high prevalence of EPS, however,it is used mainly for its antiemetic effect, not for its antipsychoticeffect.
D 2 receptor antagonist. Also interacts with 5-HT 3 and nAChR. Displays antipsychotic, antispasmodic, antiemetic and antinociceptive activity in vivo .
Phenothiazine antipsychotic; D2 dopamine receptor antagonist; antispasmodic
References/Citations
1) Daniel?et al.?(2015),?Phenothiazine-derived antipsychotic drugs inhibit dynamin and clathrin-mediated endocytosis; Traffic,?16?635
2) Chew?et al.?(2020),?Endocytosis Inhibition in Humans to Improve Responses to ADCC-Mediating Antibodies; Cell,?180?895
3) Hollister?et al.?(1969),?Clinical use of psychotherapeutic drugs: current status;?Clin. Pharmacol. Ther.,?10?170
4) Cook and Newberry (2018),?Emergency Department Use of Intravenous Prochlorperazine for Acute Migraine; Adv. Emerg. Nurs. J.,?40?148
5) Van den Berg?et al.?(1996),?The prophylactic antiemetic efficacy of prochlorperazine and ondansetron in nasal septal surgery: a randomized double-blind comparison; Anaesth. Intensive Care,?24?538
