PMID- 1473561
OWN - NLM
STAT- MEDLINE
DCOM- 19930201
LR  - 20221207
IS  - 0014-2999 (Print)
IS  - 0014-2999 (Linking)
VI  - 229
IP  - 1
DP  - 1992 Dec 8
TI  - p-methylthioamphetamine is a potent new non-neurotoxic serotonin-releasing agent.
PG  - 31-8
AB  - p-Methylthioamphetamine (MTA), was compared to p-chloroamphetamine (PCA) in a 
      number of pharmacological assays. MTA was about 2-fold more potent than PCA at 
      inhibiting synaptosomal uptake of [3H]5-hydroxytryptamine ([3H]5-HT), and about 
      7-fold and 10-fold less potent than PCA at inhibiting synaptosomal uptake of 
      [3H]dopamine and [3H]norepinephrine, respectively. In drug discrimination assays, 
      MTA was nearly equipotent to PCA in animals trained to discriminate saline from 
      3,4-methylenedioxymethamphetamine (MDMA), or two related analogues 
      S-(+)-N-methyl-1-(1,3-benzodioxol-5-yl)-2-butanamine (S-MBDB) or 
      5-methoxy-6-methyl-2-aminoindan (MMAI). MTA caused dose-dependent increases of 
      tritium efflux from superfused rat frontal cortex slices preloaded with [3H]5-HT, 
      comparable to that induced by an equal molar concentration of PCA. The potential 
      neurotoxicity of MTA was examined by measuring monoamine and metabolite levels at 
      one week following an acute dose. A 10 mg/kg dose of PCA caused a 70-90% decrease 
      of cortical, hippocampal and striatal 5-HT and 5-hydoxyindoleacetic acid (5-HIAA) 
      levels, while twice the molar dose of MTA (21.3 mg/kg) had no effect. Thus, MTA 
      is a potent, selective, serotonin releaser, apparently devoid of serotonin 
      neurotoxic effects. This work also supports the idea that catecholamine systems 
      may play a critical role in the neurotoxicity of PCA-like compounds.
FAU - Huang, X
AU  - Huang X
AD  - Department of Pharmacology and Toxicology, Purdue University, School of Pharmacy 
      and Pharmacal Sciences, West Lafayette, IN 47907.
FAU - Marona-Lewicka, D
AU  - Marona-Lewicka D
FAU - Nichols, D E
AU  - Nichols DE
LA  - eng
GR  - DA04758/DA/NIDA NIH HHS/United States
PT  - Comparative Study
PT  - Journal Article
PT  - Research Support, U.S. Gov't, P.H.S.
PL  - Netherlands
TA  - Eur J Pharmacol
JT  - European journal of pharmacology
JID - 1254354
RN  - 0 (Amphetamines)
RN  - 0 (Neurotransmitter Uptake Inhibitors)
RN  - 0 (Serotonin Uptake Inhibitors)
RN  - 6JP2T8KXTR (4-methylthioamphetamine)
RN  - VTD58H1Z2X (Dopamine)
RN  - X4W3ENH1CV (Norepinephrine)
SB  - IM
MH  - Amphetamines/*pharmacology/toxicity
MH  - Animals
MH  - Brain/*drug effects/metabolism
MH  - Chromatography, High Pressure Liquid
MH  - Corpus Striatum/drug effects
MH  - Discrimination, Psychological
MH  - Dopamine/metabolism
MH  - Frontal Lobe/drug effects
MH  - Hippocampus/drug effects
MH  - In Vitro Techniques
MH  - Male
MH  - Neurotransmitter Uptake Inhibitors/*pharmacology/toxicity
MH  - Norepinephrine/metabolism
MH  - Rats
MH  - Rats, Sprague-Dawley
MH  - Selective Serotonin Reuptake Inhibitors/*pharmacology/toxicity
MH  - Structure-Activity Relationship
MH  - Synaptosomes/drug effects
EDAT- 1992/12/08 00:00
MHDA- 1992/12/08 00:01
CRDT- 1992/12/08 00:00
PHST- 1992/12/08 00:00 [pubmed]
PHST- 1992/12/08 00:01 [medline]
PHST- 1992/12/08 00:00 [entrez]
AID - 0014-2999(92)90282-9 [pii]
AID - 10.1016/0014-2999(92)90282-9 [doi]
PST - ppublish
SO  - Eur J Pharmacol. 1992 Dec 8;229(1):31-8. doi: 10.1016/0014-2999(92)90282-9.