1973•Acta Pharmacologica et ToxicologicaRequires access

The Comparative Pharmacology of Flupenthixol and some Reference Neuroleptics

I. Møller Nielsen, V. Pedersen, Mogens Nymark, K. F. Franck, Vita Boeck, Bjarne Fjalland, Anne Vibeke Christensen

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Abstract

Abstract:Flupenthixol, a thioxanthene derivative may exist in two isomeric forms, α and β. Flupenthixol contains 45‐55 % α‐flupenthixol. The pharmacological effects of flupenthixol, α‐ and β‐flupenthixol have been compared with those of clopenthixol, chlorprothixene, fluphenazine, perphenazine, chlorpromazine and haloperidol. In most pharmacological screening tests α‐flupenthixol was equipotent with fluphenazine. β‐Flupenthixol showed very low pharmacological activity. As expected the potency of flupenthixol was about one half that of α‐flupenthixol. Flupenthixol was considerably more potent than clopenthixol and chlorprothixene in the inhibition of conditioned avoidance response. The influence on temperature regulation and the peripheral α‐adrenolytic effect was considerably weaker than that of chlorprothixene.

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Abstract:Flupenthixol, a thioxanthene derivative may exist in two isomeric forms, α and β. Flupenthixol contains 45‐55 % α‐flupenthixol. The pharmacological effects of flupenthixol, α‐ and β‐flupenthixol have been compared with those of clopenthixol, chlorprothixene, fluphenazine, perphenazine, chlorpromazine and haloperidol. In most pharmacological screening tests α‐flupenthixol was equipotent with fluphenazine. β‐Flupenthixol showed very low pharmacological activity. As expected the potency of flupenthixol was about one half that of α‐flupenthixol. Flupenthixol was considerably more potent than clopenthixol and chlorprothixene in the inhibition of conditioned avoidance response. The influence on temperature regulation and the peripheral α‐adrenolytic effect was considerably weaker than that of chlorprothixene.

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Available abstract

Abstract:Flupenthixol, a thioxanthene derivative may exist in two isomeric forms, α and β. Flupenthixol contains 45‐55 % α‐flupenthixol. The pharmacological effects of flupenthixol, α‐ and β‐flupenthixol have been compared with those of clopenthixol, chlorprothixene, fluphenazine, perphenazine, chlorpromazine and haloperidol. In most pharmacological screening tests α‐flupenthixol was equipotent with fluphenazine. β‐Flupenthixol showed very low pharmacological activity. As expected the potency of flupenthixol was about one half that of α‐flupenthixol. Flupenthixol was considerably more potent than clopenthixol and chlorprothixene in the inhibition of conditioned avoidance response. The influence on temperature regulation and the peripheral α‐adrenolytic effect was considerably weaker than that of chlorprothixene.

Key concepts: Fluphenazine, Pharmacology, Haloperidol, Perphenazine, Chemistry, Chlorpromazine, Potency, Medicine

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