Effects of phencyclidine metabolites on serotonin uptake in rat brain.
T Hori, T Suzuki, A Baba, S Abe, T Yamamoto, T Moroji, H Shiraishi
Neuroscience Letters May 17, 1996 DOI: 10.1016/0304-3940(96)11617-7 (opens in new tab)
Study at a glance
AI-extracted from the abstract| Characteristics | In vitro binding and uptake study Peer reviewed |
|---|---|
| Population | Rat brain tissue |
| Intervention | Phencyclidine (PCP) |
| Measures | [3H]5-HT uptake, [3H]paroxetine binding, [3H]5-HT binding to 5-HT1 receptors, [3H]ketanserin binding to 5-HT2 receptors |
| Topics | Serotonin |
| Key points | PCP and its metabolites inhibited serotonin uptake and paroxetine binding in rat brain but did not inhibit binding to 5-HT1 or 5-HT2 receptors. The major metabolite trans-4-PPC was the most potent inhibitor of serotonin uptake. The authors suggest that some serotonergic effects of PCP may be mediated by its metabolites acting on serotonin uptake. |
Abstract
The effects of phencyclidine (PCP) and its metabolites on serotonin (5-hydroxytryptamine, 5-HT) receptors were studied. PCP and its metabolites inhibited the uptake of [3H]5-HT and the binding of [3H]paroxetine in rat brain, while they failed to inhibit either [3H]5-HT binding to 5-HT1 receptors or [3H]ketanserin binding to 5-HT2 receptors. The trans-isomer of 4-phenyl-4-(I-piperidinyl)cyclo-hexanol (trans-4-PPC), the major metabolite of PCP, rather than PCP itself, inhibited [3H]5-HT uptake most potently. These results suggest that the serotonergic effects of PCP, in part, may be based on the effects of PCP metabolites on 5-HT uptake.
Comparable studies
Other preclinical and animal studies on serotonin, most cited first.
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| Psilocybin induces rapid and persistent growth of dendritic spines in frontal cortex in vivo Mice | 2021 | Observational cohort | |
| Neurotoxicity of the psychedelic amphetamine, methylenedioxymethamphetamine. Rats (implied by typical neurochemical study context) | 1987 | Experimental study | |
| Psychedelics promote neuroplasticity through the activation of intracellular 5-HT2A receptors In vitro and in vivo (rodent) models | 2023 | Experimental study | |
| 3,4-Methylenedioxymethamphetamine and 3,4-methylenedioxyamphetamine destroy serotonin terminals in rat brain: quantification of neurodegeneration by measurement of [3H]paroxetine-labeled serotonin uptake sites. Rat brain | 1987 | Animal experiment | |
| Comparison of the monoamine transporters from human and mouse in their sensitivities to psychostimulant drugs Human and mouse dopamine, norepinephrine, and serotonin transporters expressed in cells | 2006 | In vitro laboratory study |
Citations in the library
Cited by 5
- Effect fingerprinting of new psychoactive substances (NPS): What can we learn from in vitro data? Pharmacology & Therapeutics February 1, 2018
- Hippocampal serotonin depletion unmasks differences in the hyperlocomotor effects of phencyclidine and MK-801: quantitative versus qualitative analyses Frontiers in Pharmacology 2013
- Safety and Efficacy of Monoamine Oxidase Inhibitors in Patients Who Use Psychoactive Substances: Potential Drug Interactions and Substance Use Disorder Treatment Data. CNS Drugs January 17, 2026
- Phencyclidine-Based New Psychoactive Substances. Handbook of experimental pharmacology 2018
- Effects of repeated phencyclidine treatment on serotonin transporter in rat brain. Neuroscience Letters February 11, 2000
Cites 3
- Recent advances in the phencyclidine model of schizophrenia American Journal of Psychiatry October 1, 1991
- Behavioral effects of phencyclidine and its major metabolite, (trans)4-phenyl-4-(1-piperidinyl)cyclohexanol, in mice. Behavioural Brain Research November 16, 1994
- Serotonergic involvement in phencyclidine-induced behaviors. Pharmacology, Biochemistry, and Behavior September 1984