Aminotetralins as narcotic antagonists. 2. Synthesis and opiate-related activity of 1-phenyl-3-aminotetralins

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Abstract
The synthesis and analgesic agonist and antagonist activities of several 3-[N-(cyclopropylmethyl)-N-methylamino]-1-phenyltetralins are reported. The design of these agents was based partially on the possibility of 2 aryl receptor binding sites on the opiate receptor. The agents lack the phenolic hydroxyl and quaternary C functionalities generally associated with opiate activity; yet both the cis- and trans-1-phenyl-3-aminotetralins displayed significant agonist and antagonist activity. The trans isomer neither suppressed nor precipitated withdrawal signs in addicted monkeys.