hydrolysis. However, the maximum increase in the PI hydrolysis was significantly (P < 0.01) less than oxotremorine and RS 86. lntraperitoneal administration of U-80816 dose-dependently increased striatal acetylcholine (ACh) concentration, and the effect was significant ( P < 0.01) at 30 mg/kg. In the presence of hemicholinium-3 (HC-3), U-80816 inhibited the release of (3H)-ACh from hippocarnpal slices. On the other hand, in the presence of eserine, U-80816 increased the release of (3H)-ACh. In in vivo pharmacological tests, U-80816 produced hypothermia and tremors in mice. This compound failed to produce lacrimation or salivation in mice when administered up to 100 mg/kg. U-80816 antagonized oxotremorineinduced salivation. It is bioavailable to the brain in a significant amount after oral adminis- tration and has a sufficiently long duration of action. The in vitro and in vivo pharmacological investigations indicate that U-80816 is a partial agonist of muscarinic receptors.
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