α-Adrenoceptor subclassification

Presynaptic α-autoreceptors

The discovery of postsynaptic alpha 2-adrenoreceptors with the drug specificities of presynaptic alpha 2-adrenoreceptors has contributed to a refinement of the classification of alpha-adrenoreceptors. postsynaptic alpha 2-adrenoreceptors have been identified by pharmacological means and with the aid of direct radioligand-receptor binding studies. The evidence for the existence of this class of alpha 2-adrenoreceptors in the brain and in vascular smooth muscle is particularly strong. Central postsynaptic alpha 2-adrenoreceptors play a major part in the hypotensive action of centrally acting antihypertensive drugs such as clonidine and alpha-methyl-DOPA. Vascular smooth muscle cells contain postsynaptic alpha 2-adrenoreceptors which mediate vasoconstriction, like the more classical alpha 1-adrenoreceptors. The simultaneous occurrence of contractile alpha 1- and alpha 2-adrenoreceptors in vascular smooth muscle offers a simple model for the characterization of alpha-adrenoreceptor agonists and antagonists. At present, highly selective agonists of alpha 2-adrenoreceptors have been found. These new compounds may be useful for the classification of other alpha-adrenoreceptor populations. It has been suggested that the vascular postsynaptic alpha 2-adrenoreceptor might be located at extrasynaptic sites. Accordingly, adrenaline released by the adrenal medulla would be the endogenous stimulant. Finally, observations have been made in vivo indicating that a transmembrane influx of calcium ions is necessary for linking the drug-induced activation of these alpha 2-adrenoreceptors to vasoconstriction.

Mini-review. The postsynaptic alpha 2-adrenoreceptor

Clonidine raises blood pressure in severe idiopathic orthostatic hypotension

alpha-Adrenoceptors may be subdivided based on their anatomical distribution within the synapse. Presynaptic alpha-adrenoceptors are generally of the alpha 2-subtype and modulate neurotransmitter liberation via a negative feedback mechanism. Postsynaptic alpha-adrenoceptors are usually of the alpha 1-subtype and mediate the response of the effector organ. Although this "anatomical" subclassification is generally applicable, many exceptions exist. A more useful classification of alpha-adrenoceptor subtypes is based on a pharmacological characterization in which selective agonists and antagonists are used. Peripheral alpha-adrenoceptors are critical in the regulation of the cardiovascular system. Postsynaptic alpha-adrenoceptors in arteries and veins represent a mixed population of alpha 1/alpha 2-adrenoceptors, with both subtypes mediating vasoconstriction. In the peripheral arterial circulation, postsynaptic vascular alpha 1-adrenoceptors are found in the adrenergic neuroeffector junction, whereas postsynaptic vascular alpha 2-adrenoceptors are located extrajunctionally. In the venous circulation, it appears that alpha 2-adrenoceptors may be predominantly junctional, whereas alpha 1-adrenoceptors may be predominantly extrajunctional. It has been proposed that junctional alpha-adrenoceptors will respond predominantly to norepinephrine liberated from sympathetic neurons, whereas extrajunctional alpha-adrenoceptors likely respond to circulating catecholamines. The functional role of extrajunctional alpha-adrenoceptors may be more important in disease states such as hypertension and congestive heart failure where circulating levels of catecholamines may be high and contribute to the maintenance of elevated vascular resistance. alpha 2-Adrenoceptors are also associated with the intima and may play a role in the release of an endogenous relaxing factor from the endothelium.(ABSTRACT TRUNCATED AT 250 WORDS)

Distribution and function of peripheral alpha-adrenoceptors in the cardiovascular system.

α2- and α2-vasular adrenoceptors in the dog

Blockade of central alpha 2-adrenoceptors enhances the carotid occlusion response in dogs.

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α2- and α2-vasular adrenoceptors in the dog

Blockade of central alpha 2-adrenoceptors enhances the carotid occlusion response in dogs.