The effects of lidocaine and procainamide on the sarcolemmal membrane high affinity cyclic AMP phosphodiesterase of rat myocardium.
The incubation of rat myocardial sarcolemmal membranes with 10(-4)M lidocaine or procainamide results in a decreased fluorescence polarization of the extrinsic probes (diphenylhexatriene and 12-anthroylstearate) and in the stimulation of the membrane-bound high affinity cyclic AMP phosphodiesterase activity (PDE). Lidocaine or procainamide do not contrast, but facilitate the aminophylline inhibitory action on the PDE activity, without modifying the basic molecular mechanism of the inhibitory action. The amplitudes of the effects described are inversely correlated to the temperature, being greater at the lower tested temperature (25 degrees greater than 30 degrees greater than 37 degrees C).
Illiano
G
G
Galderisi
R
R
Di Donato
A
A
Paolisso
G
G
Draetta
G F
GF
D015105:3',5'-Cyclic-AMP Phosphodiesterases / Q000378:metabolism*; D000818:Animals; D005454:Fluorescence Polarization; D066298:In Vitro Techniques; D007425:Intracellular Membranes / Q000201:enzymology; D008012:Lidocaine / Q000494:pharmacology*; D008297:Male; D008560:Membrane Fluidity / Q000187:drug effects; D009206:Myocardium / Q000201:enzymology*; D011342:Procainamide / Q000494:pharmacology*; D051381:Rats; D011919:Rats, Inbred Strains; D012508:Sarcolemma / Q000201:enzymology*
D008012:Lidocaine; D015105:3',5'-Cyclic-AMP Phosphodiesterases; D011342:Procainamide