Novel antagonists of 5-HT3 receptors. Synthesis and biological evaluation of piperazinylquinoxaline derivatives

…, JA Palop, JC Del Castillo, JM Caldero…

Index: Monge, A.; Palop, J. A.; Castillo, J. C. Del; Caldero, J. M.; Roca, J.; et al. Journal of Medicinal Chemistry, 1993 , vol. 36, # 19 p. 2745 - 2750

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Citation Number: 58

Abstract

A series of piperazinylquinoxalines has been synthesized and studied as 5-HT3 receptor antagonists in different preparations. Antagonism to 5-HT in the longitudinal muscle of the guinea pig ileum was particularly prominent in cyanoquinoxaline derivatives with an alkyl substitutuent on the piperazine moiety. The pA2 of some selected compounds against the 5- HT3 agonist 2-methyl-5HT in the guinea pig ileum was in the range of tropisetron or ...