Abstract
Radioligand binding studies were used to analyze the interactions of two novel anxiolytics, buspirone and TVX Q 7821, with a series of 10 neuronal membrane receptor sites. Buspirone ( IC 50 = 24 n m ) and TVX Q 7821 ( IC 50 = 9.5 n m ) display the highest affinity for 5-hydroxytryptamine 1A (5-HT 1A) binding sites labeled by 3H-8-hydroxy-2-(di- n-propylamino) tetralin (DPAT). By contrast, buspirone is 16-fold weaker at dopamine (D 2) receptors ( IC 50 = 380 n m ), whereas TVX Q 7821 is 6-fold less potent at alpha-adrenergic 1 sites ( IC 50 = 58 n m ). At the other receptors studied, buspirone and TVX Q 7821 had similar pharmacological profiles. Both agents display moderate affinity for histamine (H 1), alpha-adrenergic 2, and 5-HT 2 binding sites. The drugs are essentially inactive at 5-HT 1B, calcium channel antagonist, muscarinic cholinergic, and benzodiazepine receptors. These results suggest that the anxiolytic effects of buspirone and TVX Q 7821 may be mediated by central 5-HT 1A receptors.
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