PMID- 1696701 OWN - NLM STAT- MEDLINE DCOM- 19900918 LR - 20190726 IS - 0028-3908 (Print) IS - 0028-3908 (Linking) VI - 29 IP - 7 DP - 1990 Jul TI - Reduction of in vivo binding of [3H]paroxetine in mouse brain by 3,4-methylenedioxymethamphetamine. PG - 633-9 AB - The effects of 3,4-methylenedioxymethamphetamine (MDMA) on the in vivo binding of [3H]paroxetine, a potent and selective 5-hydroxytryptamine (5-HT; serotonin) uptake inhibitor, in the brain of the mouse were studied. The distribution of radioactivity in the brain of the mouse, after intravenous administration of [3H]paroxetine, was significantly altered by pretreatment with MDMA (15 mg/kg, i.p., 3 hr before). The hypothalamus/cerebellum and cerebral cortex/cerebellum ratios, as a function of time, were significantly decreased after the pretreatment with MDMA, indicating that the in vivo binding of [3H]paroxetine to uptake sites for 5-HT in the brain of the mouse was significantly decreased by MDMA. These ratios could reflect those of the total binding, to the non-specific binding and free ligand, since the cerebellum has very low levels of binding for [3H]paroxetine. Furthermore, these ratios decreased after pretreatment with MDMA, in a dose-dependent manner. However, the binding of [3H]paroxetine to membranes from the brain of the mouse in vitro was not altered by treatment with MDMA. The discrepancy between the in vivo binding and in vitro binding of [3H]paroxetine in the brain of the mouse is discussed. FAU - Hashimoto, K AU - Hashimoto K AD - Department of Radiopharmaceutical Chemistry, Faculty of Pharmacy and Pharmaceutical Sciences, University of Fukuyama, Japan. FAU - Goromaru, T AU - Goromaru T LA - eng PT - Journal Article PT - Research Support, Non-U.S. Gov't PL - England TA - Neuropharmacology JT - Neuropharmacology JID - 0236217 RN - 0 (Amphetamines) RN - 0 (Piperidines) RN - 0 (Serotonin Antagonists) RN - 333DO1RDJY (Serotonin) RN - 41VRH5220H (Paroxetine) RN - 4764-17-4 (3,4-Methylenedioxyamphetamine) RN - 54-16-0 (Hydroxyindoleacetic Acid) RN - KE1SEN21RM (N-Methyl-3,4-methylenedioxyamphetamine) SB - IM MH - 3,4-Methylenedioxyamphetamine/analogs & derivatives/*pharmacology MH - Amphetamines/*pharmacology MH - Analysis of Variance MH - Animals MH - Brain/*metabolism MH - Chromatography, High Pressure Liquid MH - Chromatography, Thin Layer MH - Hydroxyindoleacetic Acid/analysis MH - Injections, Intravenous MH - Male MH - Mice MH - N-Methyl-3,4-methylenedioxyamphetamine MH - Paroxetine MH - Piperidines/*metabolism/pharmacology MH - Serotonin/analysis MH - Serotonin Antagonists/*metabolism/pharmacology EDAT- 1990/07/01 00:00 MHDA- 1990/07/01 00:01 CRDT- 1990/07/01 00:00 PHST- 1990/07/01 00:00 [pubmed] PHST- 1990/07/01 00:01 [medline] PHST- 1990/07/01 00:00 [entrez] AID - 10.1016/0028-3908(90)90024-l [doi] PST - ppublish SO - Neuropharmacology. 1990 Jul;29(7):633-9. doi: 10.1016/0028-3908(90)90024-l.