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• W2045006977 abstract "1 The increase in diastolic pressure of pithed, normotensive rats was determined after i.v. administration of the α-adrenoreceptor agonists L-phenylephrine and B-HT 933. 2 α-Adrenoreceptor antagonists varied widely in their relative inhibitory effects towards either L-phenylephrine- or B-HT 933-induced vasoconstrictor responses. Prazosin displayed the highest affinity for the postsynaptic α-adrenoreceptor triggered by L-phenylephrine. The rank order of potency was further: phentolamine > dihydroergotamine > clozapine > corynanthine > azapetine > yohimbine > piperoxan > tolazoline > mianserin > rauwolscine. On the other hand, the rank order of potency towards B-HT 933 was: dihydroergotamine > rauwolscine > yohimbine > phentolamine > piperoxan > prazosin > tolazoline > mianserin > corynanthine > azapetine > clozapine. These data are in general agreement with the classification for α1-(triggered by L-phenylephrine) and α2-(triggered by B-HT 933) adrenoreceptors. Both populations are present postsynaptically in vascular smooth muscle of the pithed rat and are involved in vasoconstriction. 3 The ratio of KB post α2/KB post α1 was calculated as a measure of selectivity for either α-adrenoreceptor site. The α-adrenoreceptor antagonists used cover a 20,000-fold range of activity ratios. The antagonists most selective for either type were prazosin (α1) and rauwolscine (α2). The selectivity of the α-adrenoreceptor antagonists for postsynaptic α1- and α2-adrenoreceptors in the intact circulatory system of the pithed rat is comparable with the reported selectivity of these blocking agents for α1 (postsynaptic)- and α2 (presynaptic)-adrenoreceptors in the rabbit isolated pulmonary artery. 4 It is concluded that two distinct types of postsynaptic α-adrenoreceptors participate in vasoconstriction in the pithed rat. Apart from the classical α1-adrenoreceptor, vascular smooth muscle of the pithed rat contains postsynaptic α2-adrenoreceptors resembling those previously found mainly presynaptically. The presence of separate classes of postsynaptic α1- and α2-adrenoreceptors in the intact circulatory system of the pithed rat offers the possibility to use this relatively simple animal model as an in vivo test system for the pharmacological characterization of α-adrenoreceptor agonists and antagonists." @default.
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• W2045006977 title "EVALUATION OF THE SELECTIVITY OF α-ADRENORECEPTOR BLOCKING DRUGS FOR POSTSYNAPTIC α1- AND α2-ADRENORECEPTORS IN A SIMPLE ANIMAL MODEL" @default.
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• W2045006977 doi "https://doi.org/10.1111/j.1474-8673.1980.tb00441.x" @default.
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