Abstract

This preliminary study has analyzed the potential ability of the 5-HT 1A ligand spiroxatrine to interact with vascular α 1-adrenoceptors. Norepinephrine and the selective α 1-adrenoceptor agonist, methoxamine, elicited concentration-dependent contractions of rat aortic rings. In contrast, (±)-spiroxatrine (from 10 −8 to 3.1×10 −7 M) was devoid of any effect on vascular tone per se, but shifted the concentration-response curves of norepinephrine and methoxamine to the right in a concentration-dependent manner with pA 2 values of 8.48±0.22 and 8.93±0.33, respectively. Endothelium removal did not significantly affect the above pA 2 values of (±)-spiroxatrine. These data, taken in concert, support the contention that (±)-spiroxatrine displays α 1-adrenoceptor blocking properties in rat aortic rings.

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