Centrally acting hypotensive agents with affinity for 5‐HT1A binding sites inhibit forskolin‐stimulated adenylate cyclase activity in calf hippocampus

Abstract

A number of centrally acting hypotensive agents and other ligands with high affinity for 5‐hydroxytryptamine1A (5‐HT1A) recognition sites have been tested on forskolin‐stimulated adenylate cyclase activity in calf hippocampus, a functional model for 5‐HT1A‐receptors. Concentration‐dependent inhibition of forskolin‐stimulated adenylate cyclase activity was elicited by the reference 5‐HT1‐receptor agonists (mean EC50 value, nm): 5‐HT (22), 5‐carboxamidotryptamine (5‐CT, 3.2), 8‐hydroxy‐2‐(di‐n‐propylamino)‐tetralin (8‐OH‐DPAT, 8.6), N,N‐dipropyl‐5‐carboxamidotryptamine (DP‐5‐CT, 2.3), l‐[2‐(4‐aminophenyl)ethyl]‐4‐(3‐trifluoromethylphenyl)‐piperazine (PAPP or LY 165163, 20), 5‐methoxy‐3‐(l,2,3,..