Potential inhibitors of tyrosine hydroxylase and dopamine-beta-hydroxylase.
A series of methyl-substituted 1,2,3,4-tetrahydrocarbazoles was synthesized and screened for in vitro activity against tyrosine hydroxylase and dopamine-beta-hydroxylase. The most potent compounds were evaluated for inhibition of norepinephrine biosynthesis in rats. The results indicated no significant decrease in norepinephrine levels at three dosage levels.
D000818:Animals; D002227:Carbazoles / Q000138:chemical synthesis / Q000494:pharmacology*; D055598:Chemical Phenomena; D002621:Chemistry; D004299:Dopamine beta-Hydroxylase / Q000037:antagonists & inhibitors*; D066298:In Vitro Techniques; D008297:Male; D009638:Norepinephrine / Q000096:biosynthesis; D051381:Rats; D011919:Rats, Inbred Strains; D014446:Tyrosine 3-Monooxygenase / Q000037:antagonists & inhibitors*
D002227:Carbazoles; D014446:Tyrosine 3-Monooxygenase; D004299:Dopamine beta-Hydroxylase; D009638:Norepinephrine