PMID- 7945733
OWN - NLM
STAT- MEDLINE
DCOM- 19941212
LR  - 20150311
IS  - 0893-133X (Print)
IS  - 0893-133X (Linking)
VI  - 10
IP  - 4
DP  - 1994 Jul
TI  - MDMA (ecstasy) inhibition of MAO type A and type B: comparisons with fenfluramine 
      and fluoxetine (Prozac).
PG  - 231-8
AB  - 3,4-Methylenedioxymethamphetamine (MDMA), a serotonin (5-HT) neurotoxin, has been 
      shown to promote the release of serotonin (5-HT) and block its reuptake. The 
      increased buildup of extracellular 5-HT should normally be degraded by monoamine 
      oxidase (MAO). The effects of both enantiomers of MDMA were examined on MAO-A and 
      monoamine oxidase-B (MAO-B) activity in rat brain homogenates. Both enantiomers 
      competitively inhibited 5-HT catabolism by rat brain MAO-A. The Ki of MDMA for 
      MAO-A was 22 mumol/L. A mixed type of inhibition by MDMA was observed for 
      phenethylamine catabolism by MAO-B for both optical antipodes. Logistical 
      analysis of concentration response curves for MDMA inhibition of MAO-A and MAO-B 
      show an IC50 of 44 mumol/L for inhibition of MAO-A by MDMA. The IC50 value of 
      MDMA inhibition of MAO-B was 370 mumol/L, showing a selective potency for MAO-A 
      inhibition. The MAO inhibitory properties of fenfluramine (FEN) and fluoxetine 
      (FLUOX) were compared to those of MDMA. The rank order potency of these drugs for 
      MAO-A inhibition was MDMA > FLUOX > FEN, whereas for MAO-B inhibition, FLUOX > 
      MDMA > FEN. A combination of FLUOX and MDMA at their respective IC50 did not 
      inhibit MAO activity more than either drug alone at equivalent concentrations. 
      These results indicate that the actions of FEN do not appear to involve MAO 
      inhibition. MDMA (ecstasy) produced a preferential inhibition of MAO-A (IC50 = 44 
      mumol/L), which should increase extracellular 5-HT.(ABSTRACT TRUNCATED AT 250 
      WORDS)
FAU - Leonardi, E T
AU  - Leonardi ET
AD  - Department of Biology, New York University, NY 10003.
FAU - Azmitia, E C
AU  - Azmitia EC
LA  - eng
GR  - NIDA 271-90-7403/DA/NIDA NIH HHS/United States
PT  - Comparative Study
PT  - Journal Article
PT  - Research Support, U.S. Gov't, P.H.S.
PL  - England
TA  - Neuropsychopharmacology
JT  - Neuropsychopharmacology : official publication of the American College of 
      Neuropsychopharmacology
JID - 8904907
RN  - 0 (Monoamine Oxidase Inhibitors)
RN  - 0 (Phenethylamines)
RN  - 01K63SUP8D (Fluoxetine)
RN  - 2DS058H2CF (Fenfluramine)
RN  - 333DO1RDJY (Serotonin)
RN  - KE1SEN21RM (N-Methyl-3,4-methylenedioxyamphetamine)
SB  - IM
MH  - Animals
MH  - Binding, Competitive/drug effects
MH  - Brain/drug effects/enzymology
MH  - Drug Interactions
MH  - Fenfluramine/*pharmacology
MH  - Fluoxetine/*pharmacology
MH  - In Vitro Techniques
MH  - Male
MH  - Monoamine Oxidase Inhibitors/*pharmacology
MH  - N-Methyl-3,4-methylenedioxyamphetamine/*pharmacology
MH  - Phenethylamines/metabolism
MH  - Rats
MH  - Rats, Sprague-Dawley
MH  - Serotonin/metabolism
EDAT- 1994/07/01 00:00
MHDA- 1994/07/01 00:01
CRDT- 1994/07/01 00:00
PHST- 1994/07/01 00:00 [pubmed]
PHST- 1994/07/01 00:01 [medline]
PHST- 1994/07/01 00:00 [entrez]
AID - 10.1038/npp.1994.26 [doi]
PST - ppublish
SO  - Neuropsychopharmacology. 1994 Jul;10(4):231-8. doi: 10.1038/npp.1994.26.