Evidence that high affinity (3H)clonidine binding cooperates with H2-receptors in the canine coronary smooth muscle membrane.

We have investigated the effects of myocardial ischemia and exogenous histamine and 4-methylhistamine on the regulation of membrane bound alpha 2- and beta-adrenoreceptors (ARs) in the canine coronary artery smooth muscle (CAS). The results indicate that exposure of CAS to ischemia and histamine is associated with the stimulation of adenylate cyclase and with a down-regulation of alpha 2-ARs which is accompanied by the sequestration of alpha 2-AR sites into light membrane particles. The increased number of beta-AR sites in CAS represents a c-AMP mediated adaptational pathway in compromised CAS.