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Vasoconstriction mediated by postsynaptic alpha 2-adrenoceptor stimulation.

P B Timmermans, P A van Zwieten

    Naunyn-Schmiedeberg'S Archives of Pharmacology
    |August 1, 1980
    PubMed
    Summary
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    B-HT 933 activates a specific type of alpha 2-adrenoceptor in blood vessels, distinct from alpha 1-adrenoceptors. This finding helps characterize the alpha-adrenoceptors involved in vasoconstriction.

    Area of Science:

    • Pharmacology
    • Cardiovascular Physiology

    Background:

    • Postsynaptic alpha-adrenoceptors mediate vasoconstriction.
    • B-HT 933 is a compound administered intravenously to rats.
    • Understanding adrenoceptor subtypes is crucial for cardiovascular drug development.

    Purpose of the Study:

    • To characterize the postsynaptic alpha-adrenoceptors responsible for B-HT 933-induced vasoconstriction.
    • To differentiate the adrenoceptor subtype activated by B-HT 933 from alpha 1-adrenoceptors.

    Main Methods:

    • Administration of B-HT 933 to pithed, normotensive rats.
    • Quantification of antagonism by alpha-adrenoceptor blocking drugs (rauwolscine, yohimbine, corynanthine).
    • Comparison of B-HT 933's hypertensive response onset with (-)-phenylephrine.

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    Main Results:

    • B-HT 933 induced a slower hypertensive response compared to (-)-phenylephrine.
    • Rauwolscine and yohimbine were effective antagonists of B-HT 933's effects.
    • Corynanthine showed significantly less antagonism, indicating alpha 2-adrenoceptor involvement.

    Conclusions:

    • The postsynaptic alpha-adrenoceptors activated by B-HT 933 are of the alpha 2-subtype.
    • B-HT 933 identifies a distinct subclass of postsynaptic alpha 2-adrenoceptors in vascular smooth muscle.
    • Both alpha 1- and alpha 2-adrenoceptors likely contribute to mediating vasoconstriction.