Cerebral dopamine agonist properties of some 2-aminotetralin derivatives after peripheral and intracerebral administration
- 1 September 1977
- journal article
- research article
- Published by American Chemical Society (ACS) in Journal of Medicinal Chemistry
- Vol. 20 (9) , 1111-1116
- https://doi.org/10.1021/jm00219a001
Abstract
A series of variously N-substituted 2-aminotetralins having OH groups at 5 and 6 and at 6 and 7 positions, as well as nonoxygenated systems, was evaluated in rats for central dopaminergic effects. Stereotypical behavioral effects (sniffing, compulsive gnawing and hyperactivity) produced by direct intracerebral administration of some of the agents differed strikingly from responses resulting from peripheral administration. The centrally mediated responses of hyperactivity and stereotypical gnawing-biting head and limb movements were separable in some test compounds. An improved route to 2-aminotetralin systems was utilized for some of the compounds; it involved Pummerer rearrangement and cyclization of .beta.-keto sulfoxides and reductive amination of .beta.-tetralones with a NaBH4-carboxylic acid complex.This publication has 1 reference indexed in Scilit:
- The conformation of dopamine at its uptake site; further studies with rigid analoguesJournal of Pharmacy and Pharmacology, 1974