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. 1984 Jun 1;101(3-4):289-93.
doi: 10.1016/0014-2999(84)90173-0.

Stereoselective blockade at [3H]5-HT binding sites and at the 5-HT autoreceptor by propranolol

Stereoselective blockade at [3H]5-HT binding sites and at the 5-HT autoreceptor by propranolol

D N Middlemiss. Eur J Pharmacol. .

Abstract

(-)-Propranolol displaced 5-HT1 and 5-HT1B receptor binding (pIC50 6.76 and 6.31 respectively) and antagonized the inhibitory effect of 5-HT on continuous K+ (25 mM) evoked release of [3H]5-HT from superfused rat frontal cortex slices (apparent pA2 6.67). (+)-Propranolol was essentially inactive in all tests. The results support the claim that the 5-HT autoreceptor has a pharmacological resemblance to the 5-HT1 recognition site and in particular to the low affinity 5-HT1B subtype of this site.

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