标题：Inhibitory Effects of a Newly Synthesized 5-HT2 Receptor Antagonist, AT-1015 (N-[2-[4-(5H-Dibenzo[a, d]cyclohepten-5-ylidene)piperidino]-ethyl]-1-formyl-4-piperidinecarboxamide Monohydrochloride Monohydrate), on Contraction and Relaxation of Pig Coronary Arteries Induced by 5-HT and α-Methylserotonin : Comparison with Ketanserin
摘要：Inhibitory effects of a newly synthesized 5-HT2 receptor antagonist, AT-1015 (N-[2-[4-(5H-dibenzo[a, d]cyclohepten-5-ylidene)piperidino]ethyl]-1-formyl-4-piperidinecarboxamide monohydrochloride monohydrate) on contraction and relaxation of coronary arteries of pig hearts mediated by 5-HT2 subtypes were evaluated and these results were compared with those of ketanserin. Contraction and relaxation were determined by adding 5-HT or α-methylserotonin (α-Me-5-HT) as agonists. Although ketanserin induced rightward shifts of contraction, AT-1015 inhibited the maximal response. In addition, ketanserin inhibited relaxation induced by high concentration of agonists, but there were no inhibitory effects of AT-1015 on relaxation. Thus, these results suggest that AT-1015 is a strong non-competitive 5-HT2 antagonist in porcine coronary arteries and that this drug clearly exhibited different effects on the contraction and relaxation of coronary arteries of pig hearts from those of ketanserin.
