Cholinergic stimulation modulates the negative inotropic effect of cocaine on ferret ventricular myocardium. Miao, Lin, Zhihua Qiu, and James P. Morgan. Charles A. Dana Research Institute and the Harvard-Thorndike Laboratory of Beth Israel Hospital and Cardiovascular Division, Department of Medicine, Beth Israel Hospital and Harvard Medical School, Boston, Massachusetts
APStracts 2:0359H, 1995.
We tested the hypothesis that the negative inotropic effect (NIE) of cocaine is mediated, at least in part, by cholinergic stimulation and can be correlated with the degree of cyclic AMP dependency of the inotropic state. Cardiac myocytes were isolated from the left ventricles of ferrets and loaded with the fluorescent Ca2- indicator, indo-1. Cells were placed in physiologic solution containing 2.0 mM Ca2-, stimulated at 0.5 Hz; 30 degrees C. Cocaine decreased peak cell shortening and peak intracellular Ca2- in a concentration-dependent manner (10-8 M - 10-4 M). The concentration/response curve of cocaine was shifted significantly downward compared with those of lidocaine and procaine in the same range of concentrations. Atropine 10-6 M shifted the concentration/response curve of cocaine, but not those of lidocaine and procaine, rightward with a pA2 value (7.66) similar to that obtained with carbachol (7.99). With prior addition of isoproterenol (ISO)10-8 M or increased Ca2- (4.0 mM) to increase cell shortening to the same degree (around 60%), cocaine and carbachol decreased contractility to a significantly greater extent in the ISO stimulated myocytes. To clarify if these treatments changed responsiveness of the contractile elements to Ca2-, the effect of 2,3-butanedione monoxime (BDM), an agent that interferes with the interaction of myosin and actin, was tested with previous addition of ISO or increased Ca2- and no differential effect occurred. Therefore, we postulate that (1) the NIE of cocaine on myocytes is caused by decreased Ca2- availability; (2) this effect is due to specific stimulation of cholinergic receptors in addition to other direct myocardial (probably local anesthetic) effects; and (3) the NIE correlates with the level of cyclic AMP dependence of the inotropic state.

Received 10 January 1995; accepted in final form 11 August 1995.
APS Manuscript Number H20-5.
Article publication pending Am. J. Physiol. (Heart Circ. Physiology).
ISSN 1080-4757 Copyright 1995 The American Physiological Society.
Published in APStracts on 24 August 1995.