Isoproterenol and propranolol: ability to cross the blood-brain barrier and effects on cerebral circulation in man.
Using the "double indicator" technique the ability of 3H-isoproterenol and 14C-propranolol to cross the blood-brain barrier was studied in man. In 3 subjects extraction of isoproterenol was 3.8% in a single passage and the PS product was 2.0 ml/100g/min. In 4 patients extraction of propranolol was 63% and PS was 46.7 ml/100/min. Regional cerebral blood flow (rCBF) was studied in man with the 133Xe-intraarterial injection method. Intracarotid isoproterenol (3 migrogram/min., 6 patients) caused a significant reduction in rCBF, but after correction for a concomitant decrease in arterial PCO2 the alteration was no longer significant (59.8 -51.7/57.4 ml/100g/min.). Intracarotid propranolol (0.15 mg/kg, 11 patients) caused no significant change in rCBF, but after correction for arterial PCO2 change the lateration although on 4% was just significant, p less than 0.05. (56.3 -55.8/54.1 ml/100g/min). After propranolol the rCBF changes caused by alterations in the arterial PCO2 were normal and the focal flow increase during hand work could not be changed by simultaneous intracarotid propranolol.
D000328:Adult; D000368:Aged; D001794:Blood Pressure / Q000187:drug effects; D001812:Blood-Brain Barrier / Q000187:drug effects; D002245:Carbon Dioxide / Q000097:blood; D002560:Cerebrovascular Circulation / Q000187:drug effects*; D005260:Female; D006339:Heart Rate / Q000187:drug effects; D006801:Humans; D007545:Isoproterenol / Q000097:blood* / Q000494:pharmacology; D008297:Male; D008875:Middle Aged; D011433:Propranolol / Q000097:blood* / Q000494:pharmacology; D011943:Receptors, Adrenergic, beta / Q000187:drug effects
D011943:Receptors, Adrenergic, beta; D002245:Carbon Dioxide; D011433:Propranolol; D007545:Isoproterenol