PMID- 1702633 OWN - NLM STAT- MEDLINE DCOM- 19910208 LR - 20190623 IS - 0006-2952 (Print) IS - 0006-2952 (Linking) VI - 41 IP - 1 DP - 1991 Jan 1 TI - Effect of 3,4-methylenedioxymethamphetamine on [3H]paroxetine binding in the frontal cortex and blood platelets of rats. PG - 79-84 AB - The effects of single or repeated administration of the racemic mixture of 3,4-methylenedioxymethamphetamine (MDMA; 20 mg/kg, s.c.) on the number (Bmax) of serotonin (5-HT) uptake sites as determined by [3H]paroxetine binding and the concentration of 5-HT and its major metabolite, 5-hydroxyindoleacetic acid (5-HIAA), were measured in the frontal cortex and blood platelets of rats 1 and 7 days following its administration. A single injection of MDMA significantly (P less than 0.05) decreased the number of [3H]paroxetine binding sites as well as the concentrations of 5-HT and 5-HIAA in the frontal cortex but not in platelets 7 days following administration. Repeated injections of MDMA (twice daily for 4 days) significantly (P less than 0.05) decreased the number of 5-HT uptake sites and the concentration of 5-HT and 5-HIAA in the frontal cortex but not in platelets 7 days following administration. Pretreatment with the 5-HT2/5-HT1C antagonist, ketanserin, inhibited the MDMA-induced decrease in 5-HT and 5-HIAA concentrations and the number of [3H]paroxetine binding sites in the frontal cortex 7 days following a single administration. These data are suggestive that blood platelets are less sensitive than brain tissue to the 5-HT-depleting effects of MDMA. The ability of ketanserin pretreatment to block MDMA-induced decreases in [3H]paroxetine binding sites in the frontal cortex is suggestive that 5-HT2/5-HT1C receptors may be involved in the neurotoxic effects of MDMA. FAU - Nash, J F AU - Nash JF AD - Department of Psychiatry, School of Medicine, Case Western Reserve University, Cleveland, OH 44106. FAU - Arora, R C AU - Arora RC FAU - Schreiber, M A AU - Schreiber MA FAU - Meltzer, H Y AU - Meltzer HY LA - eng GR - M01RR00080/RR/NCRR NIH HHS/United States GR - MH41594/MH/NIMH NIH HHS/United States GR - MH41684/MH/NIMH NIH HHS/United States GR - etc. PT - Comparative Study PT - Journal Article PT - Research Support, Non-U.S. Gov't PT - Research Support, U.S. Gov't, P.H.S. PL - England TA - Biochem Pharmacol JT - Biochemical pharmacology JID - 0101032 RN - 0 (Piperidines) RN - 0 (Serotonin Antagonists) RN - 10028-17-8 (Tritium) RN - 333DO1RDJY (Serotonin) RN - 41VRH5220H (Paroxetine) RN - 4764-17-4 (3,4-Methylenedioxyamphetamine) RN - 54-16-0 (Hydroxyindoleacetic Acid) RN - 97F9DE4CT4 (Ketanserin) RN - KE1SEN21RM (N-Methyl-3,4-methylenedioxyamphetamine) SB - IM MH - 3,4-Methylenedioxyamphetamine/administration & dosage/*analogs & derivatives/antagonists & inhibitors/pharmacology MH - Animals MH - Blood Platelets/*drug effects/metabolism MH - Frontal Lobe/*drug effects/metabolism MH - Hydroxyindoleacetic Acid/metabolism MH - Ketanserin/administration & dosage MH - Kinetics MH - Male MH - N-Methyl-3,4-methylenedioxyamphetamine MH - Paroxetine MH - Piperidines/*metabolism MH - Rats MH - Rats, Inbred Strains MH - Serotonin/metabolism MH - Serotonin Antagonists/*metabolism MH - Time Factors MH - Tritium EDAT- 1991/01/01 00:00 MHDA- 1991/01/01 00:01 CRDT- 1991/01/01 00:00 PHST- 1991/01/01 00:00 [pubmed] PHST- 1991/01/01 00:01 [medline] PHST- 1991/01/01 00:00 [entrez] AID - 0006-2952(91)90013-U [pii] AID - 10.1016/0006-2952(91)90013-u [doi] PST - ppublish SO - Biochem Pharmacol. 1991 Jan 1;41(1):79-84. doi: 10.1016/0006-2952(91)90013-u.