2-substituted tetralin derivatives as conformationally restricted butyrophenone analogs.
Five related derivatives of 2-(2-piperidinoethyl)tetralin have been synthesized as partially rigid analogs of the neuroleptic butyrophenones. Their in vitro dopamine receptor binding properties and in vivo inhibition of dexamphetamine-induced locomotor activity are described. 1-Phenyl-2-(2-piperidinoethyl)-3,4-dihydronaphthalene hydrochloride (8) is about 1% as potent as haloperidol.
D000818:Animals; D014150:Antipsychotic Agents / Q000138:chemical synthesis*; D001667:Binding, Competitive / Q000187:drug effects; D001923:Brain Chemistry / Q000187:drug effects; D055598:Chemical Phenomena; D002621:Chemistry; D003913:Dextroamphetamine / Q000037:antagonists & inhibitors; D066298:In Vitro Techniques; D008297:Male; D051379:Mice; D009043:Motor Activity / Q000187:drug effects; D009281:Naphthalenes / Q000138:chemical synthesis*; D051381:Rats; D011919:Rats, Inbred Strains; D011954:Receptors, Dopamine / Q000187:drug effects; D013134:Spiperone / Q000378:metabolism; D013764:Tetrahydronaphthalenes / Q000138:chemical synthesis* / Q000494:pharmacology
D014150:Antipsychotic Agents; D009281:Naphthalenes; D011954:Receptors, Dopamine; D013764:Tetrahydronaphthalenes; D013134:Spiperone; D003913:Dextroamphetamine