Mechanisms of the internalization of ß-adrenergic receptor recognition sites
Since the regulation of transmitter and co-transmitter receptors appears to have a fundamental role in the modulation of neuronal communication, current research trends in receptor pharmacology emphasize the necessity to learn more about the molecular mechanisms that participate in such regulation. Many models have been proposed to obtain information on receptor function. Among these frog erythrocytes have been extensively used to study β-adrenergic receptor regulation (Lefkowitz et al., 1976). One of the phenomena that appears to possess heuristic value in β-adrenergic receptor studies is the receptor subsensitivity or desensitization elicited by persistent stimulation. Such a persistent stimulation of β-adrenergic receptors located in the frog erythrocyte membrane attenuates the receptor capability to respond to successive stimuli. Presently it is believed that this desensitization is due to a decrease in the number of recognition sites of β-adrenergic receptors (Mickey et al., 1976). Since transmitter receptors are currently viewed as composed by three functional units: 1) recognition site; 2) coupling device; 3) amplifying system, it is important to decide whether all three mechanisms participate in the desensitization caused by persistent stimulation.
KeywordsAdenylate Cyclase Recognition Site Receptor Binding Site Current Research Trend Persistent Stimulation
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