Abstract
In this study we investigated the actions of SDZ NVI-085 ((−)-(4 aR, 10 aR)-3,4,4 a,5,10,10 a-hexahydro-6-methoxy-4-methyl-9-(methylthio)-2 H-naphth[2,3- b)-1,4-oxazine hydrogen malonate), previously classified and employed as a selective α 1-adrenoceptor agonist, in the rat isolated aorta assay. It was shown that, in addition to its α 1-adrenoceptor agonistic action, SDZ NVI-085 behaves as a competitive antagonist of 5-hydroxytryptamine (5-HT)-induced contraction of rat aorta (p K B = 8.13 ± 0.08). The structurally related α 1-adrenoceptor agonist, SK&F 89748-A ( l-1,2,3,4-tetrahydro-8-methoxy-5-(methylthio)-2-naphthalenamine hydrochloride), produced inhibition of the 5-HT response only at the highest concentration tested (1 μM) with an associated pA 2 value of 6.0 ± 0.1. These findings suggest that the affinity of SDZ NVI-085 for 5-HT 2 receptors is considerably higher than for α 1-adrenoceptors, which may have implications for its use as a pharmacological tool.
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