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p-methylthioamphetamine is a potent new non-neurotoxic serotonin-releasing agent.
Eur J Pharmacol. 1992 Dec 08; 229(1):31-8.EJ

Abstract

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.

Authors+Show Affiliations

Department of Pharmacology and Toxicology, Purdue University, School of Pharmacy and Pharmacal Sciences, West Lafayette, IN 47907.No affiliation info availableNo affiliation info available

Pub Type(s)

Comparative Study
Journal Article
Research Support, U.S. Gov't, P.H.S.

Language

eng

PubMed ID

1473561

Citation

Huang, X, et al. "P-methylthioamphetamine Is a Potent New Non-neurotoxic Serotonin-releasing Agent." European Journal of Pharmacology, vol. 229, no. 1, 1992, pp. 31-8.
Huang X, Marona-Lewicka D, Nichols DE. P-methylthioamphetamine is a potent new non-neurotoxic serotonin-releasing agent. Eur J Pharmacol. 1992;229(1):31-8.
Huang, X., Marona-Lewicka, D., & Nichols, D. E. (1992). P-methylthioamphetamine is a potent new non-neurotoxic serotonin-releasing agent. European Journal of Pharmacology, 229(1), 31-8.
Huang X, Marona-Lewicka D, Nichols DE. P-methylthioamphetamine Is a Potent New Non-neurotoxic Serotonin-releasing Agent. Eur J Pharmacol. 1992 Dec 8;229(1):31-8. PubMed PMID: 1473561.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - p-methylthioamphetamine is a potent new non-neurotoxic serotonin-releasing agent. AU - Huang,X, AU - Marona-Lewicka,D, AU - Nichols,D E, PY - 1992/12/8/pubmed PY - 1992/12/8/medline PY - 1992/12/8/entrez SP - 31 EP - 8 JF - European journal of pharmacology JO - Eur J Pharmacol VL - 229 IS - 1 N2 - 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. SN - 0014-2999 UR - https://www.unboundmedicine.com/medline/citation/1473561/p_methylthioamphetamine_is_a_potent_new_non_neurotoxic_serotonin_releasing_agent_ L2 - https://linkinghub.elsevier.com/retrieve/pii/0014-2999(92)90282-9 DB - PRIME DP - Unbound Medicine ER -