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A potent new beta2-adrenoceptor blocking agent.

J L Imbs, F Miesch, J Schwartz

    British Journal of Pharmacology
    |July 1, 1977
    PubMed
    Summary
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    A novel beta2-adrenoceptor blocking agent was identified. This agent induces hypertension in normal rats but does not prevent it in SHR rats, yet it inhibits renin secretion.

    Area of Science:

    • Pharmacology
    • Cardiovascular Research

    Background:

    • Beta2-adrenoceptors play a role in regulating blood pressure and renin secretion.
    • Developing selective beta2-adrenoceptor antagonists is crucial for understanding cardiovascular regulation.

    Purpose of the Study:

    • To characterize a new beta2-adrenoceptor blocking agent, (t-Butyl-amino-3-ol-2-propyl) oximino-9 fluorene.
    • To investigate its effects on blood pressure and renin secretion in different rat models.

    Main Methods:

    • In vitro assessment of beta2-adrenoceptor blockade using isolated trachea.
    • In vivo studies in normotensive and spontaneously hypertensive rats (SHR).
    • Measurement of blood pressure and evaluation of renin secretion following isoprenaline infusion.

    Main Results:

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    • The compound demonstrated significant beta2-adrenoceptor blocking activity with a pA2 of 9.23+/-0.25.
    • It induced hypertension in normotensive rats.
    • It did not prevent arterial hypertension in SHR rats.
    • It successfully inhibited isoprenaline-induced renin secretion.

    Conclusions:

    • The new fluorene derivative is a potent beta2-adrenoceptor antagonist.
    • Its effects on blood pressure are complex, inducing hypertension in normotensive states but not preventing it in established hypertension.
    • The compound selectively inhibits renin secretion, suggesting potential applications in managing renin-angiotensin system-related disorders.