PMID- 1710592
OWN - NLM
STAT- MEDLINE
DCOM- 19910715
LR  - 20191021
IS  - 0767-3981 (Print)
IS  - 0767-3981 (Linking)
VI  - 4
IP  - 6
DP  - 1990
TI  - Reduction of [3H]6-nitroquipazine-labelled 5-hydroxytryptamine uptake sites in 
      rat brain by 3,4-methylenedioxymethamphetamine.
PG  - 635-41
AB  - 3,4-Methylenedioxymethamphetamine (MDMA; Ecstasy) is a known neurotoxin to 
      5-hydroxytryptamine (5-HT; serotonin) nerve terminals. It has recently been 
      demonstrated that [3H]6-nitroquipazine is a new radioligand for studying the 5-HT 
      transport system in brain. Therefore, we examined the effects of repeated 
      systemic administration (10 mg/kg ip, twice daily for 3 d) of MDMA on 
      [3H]6-nitroquipazine-labelled 5-HT uptake sites in rat brain. Marked reductions 
      in the concentrations of 5-HT and its major metabolite 5-hydroxyindoleacetic acid 
      (5-HIAA) were observed in the cerebral cortex 1 week after the last injection of 
      MDMA. In addition, the density of [3H]6-nitroquipazine-labelled 5-HT uptake sites 
      was significantly decreased by MDMA. Furthermore, the reduction of 5-HT and 
      5-HIAA content and the density of [3H]6-nitroquipazine-labelled 5-HT uptake sites 
      by MDMA were significantly prevented by co-administration of 6-nitroquipazine (5 
      mg/kg), a very potent and selective 5-HT uptake inhibitor. The present results 
      indicate that the 5-HT uptake carrier plays an important role in the neurotoxic 
      action of MDMA.
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  - Fundam Clin Pharmacol
JT  - Fundamental & clinical pharmacology
JID - 8710411
RN  - 0 (Serotonin Antagonists)
RN  - 10028-17-8 (Tritium)
RN  - 333DO1RDJY (Serotonin)
RN  - 4764-17-4 (3,4-Methylenedioxyamphetamine)
RN  - 4WCY05C0SJ (Quipazine)
RN  - 54-16-0 (Hydroxyindoleacetic Acid)
RN  - 77372-73-7 (6-nitroquipazine)
RN  - KE1SEN21RM (N-Methyl-3,4-methylenedioxyamphetamine)
SB  - IM
MH  - 3,4-Methylenedioxyamphetamine/*analogs & derivatives/antagonists & 
      inhibitors/toxicity
MH  - Animals
MH  - Binding Sites
MH  - Brain/*drug effects/metabolism
MH  - Drug Interactions
MH  - Hydroxyindoleacetic Acid/metabolism
MH  - Injections, Intraperitoneal
MH  - Male
MH  - N-Methyl-3,4-methylenedioxyamphetamine
MH  - Quipazine/*analogs & derivatives/metabolism/pharmacology
MH  - Radioligand Assay
MH  - Rats
MH  - Rats, Inbred Strains
MH  - Serotonin/*metabolism
MH  - Serotonin Antagonists/metabolism/*pharmacology
MH  - Tritium
EDAT- 1990/01/01 00:00
MHDA- 1990/01/01 00:01
CRDT- 1990/01/01 00:00
PHST- 1990/01/01 00:00 [pubmed]
PHST- 1990/01/01 00:01 [medline]
PHST- 1990/01/01 00:00 [entrez]
AID - 10.1111/j.1472-8206.1990.tb00043.x [doi]
PST - ppublish
SO  - Fundam Clin Pharmacol. 1990;4(6):635-41. doi: 10.1111/j.1472-8206.1990.tb00043.x.