Abstract

Publisher Summary This chapter highlights the effects of 6-hydroxydopa. 6-Hydroxydopa (2,4,5-trihydroxyphenylalanine) (6-OHDOPA), the carboxyl analog of 6-hydroxydopamine, is a drug whose usefulness lies in its ability to enter the brain after peripheral injection, and cause a selective destruction of noradrenergic terminals. The effects of various drugs on the NE-depleting action of 6-OHDOPA were studied. The action of 6-OHDOPA in depleting the NE content of the brain, and of the heart could be prevented by d -amphetamine and L-amphetamine, desipramine, and chlorpromazine. These agents were inhibitors of the membrane pump for uptake of catecholamines. It is found that because amino acids such as tyrosine and dopa are not inhibited by blockers of the amine uptake mechanism, it would seem that 6-OHDOPA, an amino acid, is converted extraneuronally to 6-hydroxydopamine, which is then inhibited from uptake into adrenergic nerves by the above blocking agents. Tranylcypromine, a monoamine oxidase inhibitor, failed to alter the effect of 6-OHDOPA on the NE content in the ventricle, and in the brain as compared with saline-injected controls.

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