Add time:08/29/2019         Source:sciencedirect.com

The action of PHACLOFEN (cas 114012-12-3), the phosphonic acid derivative of baclofen, on baclofen-induced suppression of spinal reflex transmission was tested in anaesthetized rats. Intrathecal (i.th.) injection of phaclofen, 100 nmol, antagonized the depressant effect of baclofen, 2 nmol, on spinal Hoffmann (H)-reflexes and polysynaptic flexor reflexes but had no effect on the action of muscimol, 20 nmol. The antagonistic effect of phaclofen on baclofen-induced depression of H-reflexes was dose-dependent in doses ranging from 1 to 100 nmol. When administered alone, phaclofen, 100 nmol, was devoid of stimulatory or depressant effects on spinal reflexes. These results indicate that phaclofen specifically antagonizes the reflex suppressant action of baclofen. The lack of intrinsic action of phaclofen suggests that there is no endogenous tonic inhibition mediated by GABAB receptors under the present experimental conditions.

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