Phenethylamine hallucinogens in the locus coeruleus: potency of action correlates with rank order of 5-HT2binding affinity

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Abstract

The rank order of potency for the physiological effects of three phenethylamine hallucinogens in the locus coeruleus (LC) was identical to that previously shown for their 5-HT2binding affinity ((-) DOB > DOM > (+)DOB). The behaviorally inactive positional isomer of DOB, SL-7161, did not significantly affect LC unit activity. These results offer insight into structure-activity relationships at 5-HT2receptors and support earlier findings that the actions of hallucinogens displayed in the LC are mediated via 5-HT2receptors. © 1986.

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Rasmussen, K., Glennon, R. A., & Aghajanian, G. K. (1986). Phenethylamine hallucinogens in the locus coeruleus: potency of action correlates with rank order of 5-HT2binding affinity. European Journal of Pharmacology, 132(1), 79–82. https://doi.org/10.1016/0014-2999(86)90014-2

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