Journal of Medicinal Chemistry · 1987 · 33 citations · 0 references
MedicineMedicinal ChemistryPharmacologyNeurochemistryNeuropharmacologyPsychopharmacologyCholinergic PharmacologyLigand BindingReceptor PharmacologySerotonergic Pharmacology5-Hydroxytryptamine Receptor PharmacologyDopamine Receptor AgonistsSerotonin AgonistsSerotonin Receptor Pharmacology
C1-Methylated derivatives of the potent 5-hydroxytryptamine (5-HT) receptor agonist 8-hydroxy-2-(di-n-propylamino)tetralin (8-OH-DPAT, 1) were synthesized and tested for central 5-HT and dopamine receptor activity by use of a biochemical test method in rats. cis-8-Hydroxy-1-methyl-2-(di-n-propylamino)tetralin (8) was found to be a 5-HT receptor agonist. The (+)-enantiomer of 8 had a potency equal to that of 1, whereas (-)-8 and the trans isomer (+/-)-9 were inactive.