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Journal of Pharmacology And Experimental Therapeutics, Vol. 179, Issue 2, 250-258, 1971
Copyright © 1971 by American Society for Pharmacology and Experimental Therapeutics

TETRAHYDROISOQUINOLINE ALKALOIDS: UPTAKE BY RAT BRAIN HOMOGENATES AND INHIBITION OF CATECHOLAMINE UPTAKE

RICHARD HEIKKILA 1, GERALD COHEN 1, and DOROTHY DEMBIEC 1

1 Departments of Psychiatry, Neurology and Biochemistry, Columbia University College of Physicians and Surgeons and The New York State Psychiatric Institute, New York, New York

We have studied the uptake of 3H-dopamine, 3H-norepinephrine and the 3H-tetrahydroisoquinoline alkaloids derived from these 3H-catecholamines by condensation with acetaldehyde. The alkaloids and the catecholamines accumulated in the tissue to several times their concentrations in the medium. Alkaloid uptake was much less than catecholamine uptake when these substances were compared at 10-6 M; differences were less marked at 10-6 M as a result of saturation of the catecholamine uptake mechanism. We have also studied the effect of a nonradioactive, dopamine-derived tetrahydroisoquinoline alkaloid (salsolinol) on the uptake of 3H-catecholamines. Salsolinol inhibited the accumulation of catecholamines. This inhibition was concentration dependent over the range 10-5 to 10-8 M; inhibition was less than that observed with reserpine or desmethylimipramine. When salsolinol was added after 3H-catecholamines had accumulated in the tissue, there was release of 3H-catecholamines into the medium. These observations are consistent with the point of view that tetrahydroisoquinoline alkaloids may play an important role in alcoholism.

Submitted on November 24, 1970
Accepted on June 28, 1971




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Copyright © 1971 by the American Society for Pharmacology and Experimental Therapeutics.