Effects of a series of substituted benzamides on rat prolactin secretion and 3H-spiperone binding to bovine anterior pituitary membranes |
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Authors: | Herbert Y Meltzer Miljana Simonovic Rebecca So |
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Institution: | 1. Department of Psychiatry, University of Chicago Pritzker School of Medicine, USA;2. Illinois State Psychiatric Institute, USA |
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Abstract: | The potency of seven substituted benzamine drugs (AHR-5531B, AHR-5645B, AHR-6092, AHR-8764, bromopride, sultopride and tiapride) to stimulate rat prolactin (PRL) secretion was found to be three orders of magnitude greater than that of non-benzamide neuroleptic drugs relative to their respective abilities to inhibit 3H-spiperone binding to bovine anterior pituitary membranes. Nevertheless, the IC50 values for the inhibition of 3H-spiperone binding by the seven substituted benzamide drugs was significantly correlated with their high potency to stimulate rat PRL secretion . Further, the slope of the regression line for these substituted benzamides paralleled that of a series of butyrophenone, phenothiazine, morphanthridine and dibenzodiazepine neuroleptic drugs. Two benzamide (sulpiride and metoclopramide) and three non-benzamide neuroleptic drugs gave intermediate results. This data suggests that blockade of different subgroups of dopamine receptors in the anterior pituitary gland labeled by 3H-spiperone may be responsible for the stimulation of PRL secretion by the benzamide and non-benzamide neuroleptioc drugs. |
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