[Biochemistry and pharmacology of benzamides].
The pharmacologic characteristics of the action of benzamide derivatives on the central nervous system are discussed, with sulpiride as the reference agent. The pharmacologic study of sulpiride includes the study of its effects on animal behaviour and of the biochemical modifications in the central monoaminergic systems. In animals, sulpiride has a strikingly atypical action, with no cataleptigen effects except at high dosages, a dissociated antagonism towards the effects of apomorphine and activating effects at low dosages. A dissociated antagonism towards the effects of sulpiride on the central monoaminergic receptors results in a typical neuroleptic pattern at high dosages, with a predominating action on mesolimbic structures at low dosages. As for its action on central dopaminergic receptors, sulpiride shows a high affinity for mesolimbic structures and for structures which are not included in the blood-brain barrier: it has no effect on DA receptors bound to adenyl-cyclase; it activates at low dosages (by blocking inhibiting receptors) and inhibits at high dosages (by blocking activating receptors); it has no extrapyramidal effects; according to Schwartz, Costentin et al., it would block D2 and especially D4 receptors in the mesolimbus and striatum at low dosages and striatal D2 receptors at high dosages. In the last chapter, the other benzamide derivatives are discussed relatively to sulpiride.
D000818:Animals; D001522:Behavior, Animal / Q000187:drug effects; D001549:Benzamides / Q000494:pharmacology*; D001921:Brain / Q000187:drug effects*; D002415:Cats; D004285:Dogs; D004305:Dose-Response Relationship, Drug; D051379:Mice; D051381:Rats; D011954:Receptors, Dopamine / Q000187:drug effects; D013469:Sulpiride / Q000494:pharmacology*
D001549:Benzamides; D011954:Receptors, Dopamine; D013469:Sulpiride
Biochimie et pharmacologie des benzamides.