Psychotomimesis Mediated by κ Opiate Receptors

作者：Andreas F. H. Pfeiffer, Victor Brantl, Albert Herz, H. M. Emrich · 发表于：Science · 年份：1986 · DOI：10.1126/science.3016896 · 被引用次数：865 · 研究领域：Pharmacological Receptor Mechanisms and Effects、Receptor Mechanisms and Signaling、Neuropeptides and Animal Physiology

The kappa opioid agonists are analgesics that seem to be free of undesired morphine-like effects. Their dysphoric actions observed with the kappa agonist cyclazocine are thought to be mediated by an action at sigma-phencyclidine receptors. The benzomorphan kappa agonist MR 2033 is inactive at sigma-phencyclidine receptors. In male subjects, the opiate-active (-)-isomer, but not the (+)-isomer, elicited dose-dependent dysphoric and psychotomimetic effects that were antagonized by naloxone. Thus, kappa opiate receptors seem to mediate psychotomimetic effects. In view of the euphorigenic properties of mu agonists, our results imply the existence of opposed opioid systems affecting emotional and perceptual experiences.