2-Amino-4,7-dimethoxyindan derivatives: synthesis and assessment of dopaminergic and cardiovascular actions.
N-Alkylated derivatives of 2-amino-4,7-dimethoxyindan were prepared for evaluation of central and peripheral dopaminergic activity using biochemical and behavioral tests in the rat and cardiovascular responses in the cat. 2-(Di-n-propylamino)-4,7-dimethoxyindan (4e) demonstrated equal activity with apomorphine to activate peripheral presynaptic dopamine receptors. Central pre- and postsynaptic dopamine receptors were also activated with 4e. In contrast to the intense long-acting sympathomimetic actions previously reported for the 2-amino-5,8-dimethoxytetralins, these compounds produced weak, transient effects in heart rate and blood pressure. The majority of 2-amino-4,7-dimethoxyindan derivatives tested are weak or inactive pre- and postsynaptic dopamine receptor agonists.
D000818:Animals; D001667:Binding, Competitive; D002415:Cats; D002417:Cattle; D002490:Central Nervous System / Q000187:drug effects; D055598:Chemical Phenomena; D002621:Chemistry; D004298:Dopamine / Q000502:physiology*; D004558:Electric Stimulation; D006439:Hemodynamics / Q000187:drug effects*; D006801:Humans; D066298:In Vitro Techniques; D007189:Indans / Q000138:chemical synthesis* / Q000494:pharmacology; D007192:Indenes / Q000138:chemical synthesis*; D008297:Male; D051379:Mice; D009043:Motor Activity / Q000187:drug effects; D018377:Neurotransmitter Agents / Q000096:biosynthesis; D051381:Rats; D011919:Rats, Inbred Strains; D013134:Spiperone / Q000378:metabolism; D013239:Stereotyped Behavior / Q000187:drug effects
D007189:Indans; D007192:Indenes; D018377:Neurotransmitter Agents; D013134:Spiperone; D004298:Dopamine