Author/Authors :
Virendra Kumar Mishra، نويسنده , , Michael D. Alexander، نويسنده , , Malcolm R. Bell، نويسنده , , Michael A. Eissenstat، نويسنده , , Frances M. Casiano، نويسنده , , Susan M. Chippari، نويسنده , , Dean A. Haycock، نويسنده , , Daniel A. Luttinger، نويسنده , , Joan E. Kuster، نويسنده , , Matthew S. Miller، نويسنده , , Joan I. Stevenson، نويسنده , , Susan J. Ward، نويسنده ,
Abstract :
Indence analogs of pravadoline exhibited antinociceptive activity in several animal models. The inhibition of prostaglandin (PG) synthesis in mouse brain microsomes was diminished in these pravadoline analogs, but they were potent in inhibiting electrically stimulated contractions in the mouse vas deferens (MVD) preparations. Binding studies with ligand WIN 55212-2 have aided to demonstrate that the morpholinoalkyl-indene binding site is functionally equivalent with cannabinoid binding site. The antinociceptive activity of the indene derivatives appears to be mediated by increased affinity for the cannabinoid receptor.