Stereoselective blockade at [3H]5-HT binding sites and at the 5-HT autoreceptor by propranolol.
(-)-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.
D000818:Animals; D002540:Cerebral Cortex / Q000378:metabolism; D066298:In Vitro Techniques; D008297:Male; D011188:Potassium / Q000378:metabolism; D011433:Propranolol / Q000494:pharmacology*; D051381:Rats; D011919:Rats, Inbred Strains; D011985:Receptors, Serotonin / Q000187:drug effects* / Q000378:metabolism; D013237:Stereoisomerism
D011985:Receptors, Serotonin; D011433:Propranolol; D011188:Potassium