Abstract
New derivatives of 2-(carboxycyclopropyl)glycine (CCG), (2 S,1′ S,21′ R,31′ S)- and (2 S,1′ S,2′ R,3′ R)-2-(2-carboxy-3 -methoxymethylcyclopropyl)glycine ( trans- and cis-MCG-I), effectively inhibited forskolinstimulated cyclic AMP formation in a concentration dependent manner in cultured spinal neurones of rats. They effectively depressed monosynaptic excitation in the spinal reflex of newborn rats with IC 50 values of 0.3 and 3 μM, respectively, which was sensitive to (+)-MCPG. They did not cause any depolarization even when the concentration was increased up to 0.3 mM. However, after treatment with quisqualate, cis-MCG-I caused a depolarization of motoneurones in the newborn rat spinal cord in a concentration dependent manner with a threshold concentration of 1 μM (quisqualate effect). The depolarizing activity developed after quisqualate treatment gradually decreased but lasted for more than 2 hr. The depolarization induced by cis-MCG-I seemed pharmacologically similar to that of phosphonate-containing analogues of glutamate such as L-AP4 or L-AP6 under the “quisqualate effect”. These novel CCG derivatives would be expected to provide useful probes for elucidating the physiological function of mGluRs.
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