Final Thoughts on Chemistry for 49679-45-0

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Novel Antagonists of 5-HT3 Receptors. Synthesis and Biological Evaluation of Piperazinylquinoxaline Derivatives

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 substituent 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 ondansetron, and one of them, 7e, was more potent than these reference compounds by approximately 2 or 3 orders of magnitude.However, these compounds were markedly less potent than either tropisetron or ondansetron as displacers of 3H-BRL 43694 binding to rat cortical membranes or as antagonists of the Bezold-Jarisch reflex in rats.Piperazinylcyanoquinoxalines represent a new class of 5-HT3 antagonists with a selective effect on guinea pig peripheral receptors.

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Reference£º
Quinoxaline – Wikipedia,
Quinoxaline | C8H6N1904 | ChemSpider