PHARMACOLOGICAL PROPERTIES OF SOME ALPHA-ADRENOCEPTOR BLOCKING-DRUGS

  • 1 January 1980
    • journal article
    • research article
    • Vol. 290  (24) , 1553-1555
Abstract
Six .alpha.-adrenoceptor blocking agents were investigated in dogs and rats. The most potent agents were 170 150 [dl-(imidazolyl-2)-2benzodioxane 1-4] and 170 153 [dl (cyclopropylmethylaminomethyl)2-benzodioxane 1-4] . At low doses (0.1 .mu.g/kg) they reversed the pressor response to low doses of adrenaline [epinephrine, A] (0.1 and 0.3 .mu.g/kg) and suppressed the response to high doses of A. They reduced the pressor response to noradrenaline [norepinephrine]. In addition, in dogs 170 150 increased the tachycardia due to stimulation of the cardiac nerve. The compound prevented and reversed the inhibition due to clonidine on the effects of cardiac nerve stimulation. Compound 170 153 did not increase the tachycardia due to cardiac nerve stimulatin, but it prevented and reversed the inhibitory effects of clonidine on this stimulation. Both 170 150 and 170 153 are potent .alpha.-adrenoceptor blocking agents acting on both pre and post-synaptic .alpha.-adrenoceptors which could be interesting pharmacological tools.

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