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

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

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.

MeSH terms

  • Animals
  • Cerebral Cortex / metabolism
  • In Vitro Techniques
  • Male
  • Potassium / metabolism
  • Propranolol / pharmacology*
  • Rats
  • Rats, Inbred Strains
  • Receptors, Serotonin / drug effects*
  • Receptors, Serotonin / metabolism
  • Stereoisomerism

Substances

  • Receptors, Serotonin
  • Propranolol
  • Potassium