Studies on inhibition of TSH stimulation of adenyl cyclase activity in thyroid plasma membrane preparations by propranolol.
Propranolol (1 mM) was found to inhibit TSH stimulation of adenyl cyclase activity in a subcellular fraction from bovine thyroid enriched in plasma membranes. However, stimulation due to PGE1 or NaF was not similarly inhibited. Since (i) and inhibition was observed at concentrations of propranolol between 10-minus 4 and 10- minus 3M, and appeared to be noncompetitive (ii) the optical isomers of propranolol were equipotent, (iii) inhibition was specific for propranolol since it was not observed with the closely related drug practolol (1 mM), and (iv) quinidine (1 mM) and the local anaesthetics lignocaine and aptocaine also proved inhibitory, we concluded that propranolol inhibition of TSH stimulation was due to its "quinidine-like" properties (i.e., relatively specific and characteristic membrane-active properties) and not to its action as a beta-adrenergic antagonist.
D000251:Adenosine Triphosphatases / Q000378:metabolism; D000262:Adenylyl Cyclases / Q000378:metabolism*; D000779:Anesthetics, Local / Q000494:pharmacology; D000818:Animals; D002417:Cattle; D002462:Cell Membrane / Q000187:drug effects / Q000201:enzymology; D004789:Enzyme Activation / Q000187:drug effects; D005459:Fluorides / Q000494:pharmacology; D066298:In Vitro Techniques; D008012:Lidocaine / Q000494:pharmacology; D008274:Magnesium / Q000494:pharmacology; D010744:Phosphoric Monoester Hydrolases / Q000378:metabolism; D011188:Potassium / Q000494:pharmacology; D011217:Practolol / Q000494:pharmacology; D011433:Propranolol / Q000494:pharmacology*; D011458:Prostaglandins E / Q000494:pharmacology; D011802:Quinidine / Q000494:pharmacology; D012964:Sodium / Q000494:pharmacology; D013237:Stereoisomerism; D013961:Thyroid Gland / Q000201:enzymology*; D013972:Thyrotropin / Q000494:pharmacology / Q000502:physiology*
D000779:Anesthetics, Local; D011458:Prostaglandins E; D013972:Thyrotropin; D008012:Lidocaine; D012964:Sodium; D011433:Propranolol; D010744:Phosphoric Monoester Hydrolases; D000251:Adenosine Triphosphatases; D000262:Adenylyl Cyclases; D008274:Magnesium; D011802:Quinidine; D005459:Fluorides; D011188:Potassium; D011217:Practolol