α1-adrenoceptor blocking properties of SPIROXATRINE (cas 1054-88-2) in rat aorta

Add time:07/24/2019    Source:sciencedirect.com

This preliminary study has analyzed the potential ability of the 5-HT1A ligand SPIROXATRINE (cas 1054-88-2) to interact with vascular α1-adrenoceptors. Norepinephrine and the selective α1-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 pA2 values of 8.48±0.22 and 8.93±0.33, respectively. Endothelium removal did not significantly affect the above pA2 values of (±)-spiroxatrine. These data, taken in concert, support the contention that (±)-spiroxatrine displays α1-adrenoceptor blocking properties in rat aortic rings.

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