8-hydroxy-2-(di-n-propylamino)tetralin, 8-OH-DPAT, a potent and selective simplified ergot congener with central 5-HT-receptor stimulating activity
Journal of Neural Transmission September 1, 1982 S. Hjorth, A. Carlsson, P. Lindberg et al.
The simplified ergot congener 8-hydroxy-2-(di-n-propylamino)tetralin (8-OH-DPAT) elicits pronounced biochemical and behavioral changes indicative of central serotoninomimetic activity. These effects are resistant to prior monoamine depletion or synthesis inhibition, suggesting direct serotonin-receptor agonism. 8-OH-DPAT increases 5-HT levels, decreases 5-HIAA levels, 5-HT-synthesis rate and 5-HT utilization, and inhibits 5-HT neuronal firing, with potency comparable to lisuride or LSD. Unlike those compounds, 8-OH-DPAT lacks appreciable effects on central catecholamine receptors, making it the most potent and selective centrally acting 5-HT agonist described.