Effect of some antiarrhythmics on [3H]clonidine binding to alpha 2-adrenergic receptors.
The effects of the antiarrhythmics quinidine, propranolol, procainamide and lidocaine were determined on the specific binding of [3H]clonidine to the alpha 2-adrenergic receptor. Quinidine is effective in decreasing specific [3H]clonidine binding to the alpha 2 receptor within the range of therapeutic blood levels (Ki = 6 x 10 (-8) M). The effectiveness of all compounds tested, with the exception of quinidine and procainamide, correlate with the membrane/buffer partition coefficient, suggesting a relationship with the local anesthetic activity.
D000818:Animals; D000889:Anti-Arrhythmia Agents / Q000494:pharmacology*; D001921:Brain / Q000378:metabolism; D002395:Catecholamines / Q000494:pharmacology; D002417:Cattle; D003000:Clonidine / Q000378:metabolism*; D066298:In Vitro Techniques; D011802:Quinidine / Q000494:pharmacology; D011941:Receptors, Adrenergic / Q000378:metabolism*; D011942:Receptors, Adrenergic, alpha / Q000187:drug effects / Q000378:metabolism*
D000889:Anti-Arrhythmia Agents; D002395:Catecholamines; D011941:Receptors, Adrenergic; D011942:Receptors, Adrenergic, alpha; D011802:Quinidine; D003000:Clonidine