A mutual prodrug ester of GABA and perphenazine exhibits antischizophrenic efficacy with diminished extrapyramidal effects.

@article{Nudelman2008AMP,
  title={A mutual prodrug ester of GABA and perphenazine exhibits antischizophrenic efficacy with diminished extrapyramidal effects.},
  author={Abraham Nudelman and Irit Gil-ad and Nava Shpaisman and Igor Terasenko and Hanna Ron and K. V. Savitsky and Yona Geffen and Abraham Weizman and Ada Rephaeli},
  journal={Journal of medicinal chemistry},
  year={2008},
  volume={51 9},
  pages={2858-62}
}
The perphenazine and fluphenazine GABA esters 3 and 4 evaluated in rat models for antipsychotic activity displayed a significant decrease of catalepsy associated with increased prolactin blood levels. Efficacy was evaluated in the d-amphetamine-induced hyperactivity model, where perphenazine abolished hyperactivity and induced sedation and catalepsy, whereas 3 reduced hyperactivity without sedation or catalepsy. Thus, 3 (BL-1020) constitutes a prototype of novel antipsychotics possessing… CONTINUE READING