Feb 1, 1976

Dual effect of alpha-adrenoceptor antagonists in rat isolated vas deferens

British Journal of Pharmacology
A Jurkiewicz, Neide Hyppolito Jurkiewicz

Abstract

1 In rat isolated vas deferens, the isotonic contractile responses to low doses of noradrenaline or adrenaline were antagonized, and those to high doses were potentiated, by yohimbine, piperoxan, phentolamine and tolazoline. Effects due to intermediate doses were not affected, or were potentiated within about 30 min, following an initial inhibition. 2 The alpha-adrenoceptor blockers thus caused a shift to the right and an increase of the maximum height of log dose-response curves of alpha-adrenoceptor stimulants. For a given dose of antagonist, the onset was slower for the potentiating than for the blocking effect. 3 The shift to the right induced by piperoxan and yohimbine on dose-response curves of noradrenaline and adrenaline was analysed with the Schild plot, and the slopes obtained, around 0.3, were lower than expected from receptor theory. When cocaine was used to block neuronal uptake, the slopes were close to 1.0. 4 The increase in maximum response to noradrenaline and adrenaline induced by alpha-adrenoceptor blockers was dependent on the time of incubation, on the dose of antagonist, and on the initial height of responses to the agonist. A less pronounced potentiation was also obtained when acetylcholine was used as ag...Continue Reading

Mentioned in this Paper

Yohimbin Spiegel
Tolazoline
Antagonist Muscle Action
Uptake
Adrenergic alpha-Antagonists
Cocaine
Epinephrine Measurement
Medihaler-Epi
Neuronal
Adrenergic Receptor

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