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Mini-review. The postsynaptic alpha 2-adrenoreceptor.

P B Timmermans, P A van Zwieten

    Journal of Autonomic Pharmacology
    |March 1, 1981
    PubMed
    Summary
    This summary is machine-generated.

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    Postsynaptic alpha 2-adrenoreceptors, similar to presynaptic ones, refine receptor classification. These receptors in the brain and blood vessels are key to understanding blood pressure regulation and vasoconstriction.

    Area of Science:

    • Pharmacology
    • Adrenergic Receptor Research
    • Cardiovascular Physiology

    Background:

    • The classification of alpha-adrenoreceptors is being refined by the discovery of postsynaptic alpha 2-adrenoreceptors.
    • These receptors share drug specificities with presynaptic alpha 2-adrenoreceptors.

    Purpose of the Study:

    • To present evidence for the existence and function of postsynaptic alpha 2-adrenoreceptors.
    • To explore their role in the central nervous system and vascular smooth muscle.
    • To discuss their implications for drug classification and cardiovascular regulation.

    Main Methods:

    • Pharmacological identification of postsynaptic alpha 2-adrenoreceptors.
    • Direct radioligand-receptor binding studies.
    • In vivo observations of calcium ion influx.

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    Main Results:

    • Postsynaptic alpha 2-adrenoreceptors are strongly evidenced in the brain and vascular smooth muscle.
    • Central postsynaptic alpha 2-adrenoreceptors are crucial for the hypotensive effects of drugs like clonidine.
    • Vascular smooth muscle contains both alpha 1- and alpha 2-adrenoreceptors mediating vasoconstriction.
    • Highly selective alpha 2-adrenoreceptor agonists have been developed.
    • Transmembrane calcium influx is necessary for alpha 2-adrenoreceptor-mediated vasoconstriction.

    Conclusions:

    • The discovery of postsynaptic alpha 2-adrenoreceptors refines alpha-adrenoreceptor classification.
    • These receptors play significant roles in blood pressure control and vasoconstriction.
    • The presence of both alpha 1 and alpha 2 receptors in vascular smooth muscle provides a model for drug characterization.
    • New selective agonists may aid in classifying other alpha-adrenoreceptor populations.
    • Extrasynaptic localization of vascular postsynaptic alpha 2-adrenoreceptors is suggested, with adrenaline as the endogenous stimulant.