Pharmacological and Pharmacokinetic Studies on Anti-spastic Drugs

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Antispastic drugs have been used for the relief of elevated muscle tone in spastic paralysis and spinal cord injury. In the present research, the precise mechanisms of action of antispastic drugs have been studied.1. Using spinal cord slices isolated from adult rats,alpha_1-agonistic action has been shown to enhance the spinal motorneuron activity.2.alpha_2-Agonists reduced noradrenaline release from descending noradrenergic terminals in the spinal cord. These results suggest that alpha_1-agonistic action elevates muscle tone and that muscle relaxation caused by alpha_2-agonists is due to the decrease in noradrenaline release in the spinal cord.3. The method which can be used for evaluation of the site of action (spinal or supraspinal level) of antispastic drugs was developed.4. The mechanism of antispastic drugs was studied using nystagmus in rabbits.5. 2-Deoxyglucose method was improved using [^3H]-3-O-methylglucose and [^<14>C]-2-deoxyglucose. The time required for measurement of glucose utilization was shortened to 5-10 min from 45 min. This method can be used for study of site of action of antispastic drugs.