Antinociceptive (aminoalkyl) indoles

…, TE D'Ambra, V Kumar, MA Eissenstat…

Index: Bell, Malcolm R.; D'Ambra, Thomas E.; Kumar, Virendra; Eissenstat, Michael A.; Herrmann, John L.; et al. Journal of Medicinal Chemistry, 1991 , vol. 34, # 3 p. 1099 - 1110

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Citation Number: 161

Abstract

The (aminoa1kyl) indole (AAI) derivative pravadoline (la) inhibited prostaglandin (PG) synthesis in mouse brain microsomes in vitro and ex vivo and exhibited antinociceptive activity in several rodent assays. In vitro structure-activity relationship studies of this new class of PG synthesis inhibitors revealed a correspondence in three respects to those reported for the arylacetic acids:(1)“a-methylation” caused an increase in PG inhibitory ...