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- W1968082942 abstract "In β-blocked pithed rats various α-adrenoceptor agonists increased mean blood pressure. Dose-response curves were determined for the agonists in the absence and in the presence of the two selective antagonists, rauwolscine (α2) and prazosin (α1). Doses of these antagonists which shifted the dose response curves for an agonist 10-fold to the right along the abscissa D10 rauwolscine = D10R; D10 prazosin = D10P) were then calculated. The ratio D10R/D10P varied greatly within the 10 drugs tested and is concentrated as a measure of an agonist's selectivity ratio α1/α2. In pithed rats B-HT 920 (most selective α2) and methoxamine (most selective α1) concentrated the nictitating membrane dose-dependently. The selective antagonists yohimbine and prazosin shifted the cumulative dose-response curves of the two agonists to the right to different extents, indicating two different α-receptor populations, similar to those at postsynaptic vascular sites. In any given tissue, the ratio of equieffective doses, B-HT 920/methoxamine, is considered as a measure of the ratio of α1/α2 adrenoceptor ‘importance’ in that tissue. This ratio was high (4.0) in the nictitating membrane as compared with those at postsynaptic vascular sites (0.8) and at presynaptic cardiac sites (0.04). It is concluded that the effect of an α-adrenoceptor agonist will depend on (1) its α1/α2 selectively and (2) the ‘importance’ of α1/α2 adrenoceptors in the target organ." @default.
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- W1968082942 date "1981-08-01" @default.
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- W1968082942 title "α1- and α2-adrenoceptor subtypes: Selectively of various agonists and relative distribution of receptors as determined in rats" @default.
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- W1968082942 doi "https://doi.org/10.1016/0014-2999(81)90232-6" @default.
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