Effects of neuroleptics on 3H-haloperidol and 3H-CIS (Z)-flupenthixol binding and on adenylate cyclase activity in vitro
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TL;DR
It is suggested that 3 H-FPT binding and AC activity represent agonistic DA receptors situated postsynaptically.
Abstract
The binding of 3H-haloperidol (3H-Hal) and 3H-cis(Z)-flupenthixol (3H-FPT) and the dopamine (DA) stimulated adenylate cyclase (AC) activity in rat striatal tissue were investigated in vitro. 3H-Hal and 3H-FPT bind to striatal membranes in a saturable manner with dissociation constants of 3.1 and 3.8nM, respectively. The number of binding sites for 3H-FPT was 3 times higher than for 3H-Hal. Specific binding of the two ligands was highest in corpus striatum followed by olfactory tubercles and frontal cortex. A significant binding of 3H-FPT was observed in thalmus. Neuroleptics inhibited DA stimulated AC activity and the binding of 3H-Hal and 3H-FPT. Butyrophenones and diphenylbutylpiperidines were weak inhibitors of both 3H-FPT binding and AC activity. A very close correlation between the effects in 3H-FPT binding and AC activity was found, whereas the correlations 3H-Hal vs 3H-FPT and 3H-Hal vs AC were much weaker. It is suggested that 3H-FPT binding and AC activity represent agonistic DA receptors situated postsynaptically.