Possible biologically active metabolites of 5-hydroxy-6-methyl-2-di-n-propylaminotetralin.
5-Hydroxy-6-methyl-2-di-n- propylaminotetralin 1b exhibits prominent peripheral presynaptic and central dopaminergic effects, and pharmacological test data suggest that this compound is metabolically activated in vivo. It was speculated that the 6-methyl group is oxidized. To evaluate this possibility and as a prelude to a metabolism study, 5-hydroxy-6-formyl 5 and 5-hydroxy-6-hydroxymethyl-2-di-n- propylaminotetralin 2b were synthesized. Both compounds exhibited marked potency/activity in a cat cardioaccelerator nerve preparation. The biological data on these compounds are consistent with the possibility of their being pharmacologically active metabolites of compound 1b.
D000818:Animals; D002415:Cats; D055598:Chemical Phenomena; D002621:Chemistry; D003864:Depression, Chemical; D004305:Dose-Response Relationship, Drug; D004347:Drug Interactions; D004558:Electric Stimulation; D005260:Female; D005728:Ganglia, Sympathetic / Q000187:drug effects / Q000502:physiology*; D006321:Heart / Q000294:innervation; D006339:Heart Rate / Q000187:drug effects*; D008297:Male; D009281:Naphthalenes / Q000494:pharmacology*; D013469:Sulpiride / Q000494:pharmacology; D013764:Tetrahydronaphthalenes / Q000138:chemical synthesis / Q000378:metabolism / Q000494:pharmacology*
D009281:Naphthalenes; D013764:Tetrahydronaphthalenes; D013469:Sulpiride; C031457:DK 118