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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
2
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pubmed:dateCreated |
1990-3-9
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pubmed:abstractText |
Four cyclic analogues of the psychoactive phenethylamine derivative 3,4-(methylenedioxy)amphetamine were studied. These congeners, 5,6- and 4,5-(methylenedioxy)-2-aminoindan (3a and 4a, respectively), and 6,7- and 5,6-(methylenedioxy)-2-aminotetralin (3b and 4b, respectively) were tested for stimulus generalization in the two-lever drug-discrimination paradigm. Two groups of rats were trained to discriminate either LSD tartrate (0.08 mg/kg) from saline, or (+/-)-MDMA.HCl (1.75 mg/kg) from saline. In addition, a 2-aminoindan (5a) and 2-aminotetralin (5b) congener of the hallucinogenic amphetamine 1-(2,5-dimethoxy-4- methylphenyl)-2-aminopropane (DOM) were also evaluated. None of the methylenedioxy compounds substituted in LSD-trained rats, while both 3a and 3b fully substituted in MDMA-trained rats. Compounds 4a and 4b did not substitute in MDMA-trained rats. Compounds 5a and 5b did not substitute in MDMA-trained rats, although 5a substituted in LSD-trained rats, but with relatively low potency compared to its open-chain counterpart. In view of the now well-established serotonin neurotoxicity of 3,4-(methylenedioxy)amphetamine and its N-methyl homologue 1, 3a and 3b were evaluated and compared to 1 for similar toxic effects following a single acute dose of 40 mg/kg sc. Sacrifice at 1 week showed that neither 3a nor 3b depressed rat cortical or hippocampal 5-HT or 5-HIAA levels nor were the number of binding sites (Bmax) depressed for [3H]paroxetine. By contrast, and in agreement with other reports, 1 significantly depressed all three indices of neurotoxicity. These results indicate that 3a and 3b have acute behavioral pharmacology similar to 1 but that they lack similar serotonin neurotoxicity.
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pubmed:grant | |
pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/3,4-Methylenedioxyamphetamine,
http://linkedlifedata.com/resource/pubmed/chemical/Amphetamines,
http://linkedlifedata.com/resource/pubmed/chemical/Catecholamines,
http://linkedlifedata.com/resource/pubmed/chemical/Indans,
http://linkedlifedata.com/resource/pubmed/chemical/Lysergic Acid Diethylamide,
http://linkedlifedata.com/resource/pubmed/chemical/N-Methyl-3,4-methylenedioxyamphetami...,
http://linkedlifedata.com/resource/pubmed/chemical/Paroxetine,
http://linkedlifedata.com/resource/pubmed/chemical/Piperidines,
http://linkedlifedata.com/resource/pubmed/chemical/Psychotropic Drugs,
http://linkedlifedata.com/resource/pubmed/chemical/Serotonin,
http://linkedlifedata.com/resource/pubmed/chemical/Tetrahydronaphthalenes
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pubmed:status |
MEDLINE
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pubmed:month |
Feb
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pubmed:issn |
0022-2623
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
33
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
703-10
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pubmed:dateRevised |
2007-11-14
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pubmed:meshHeading |
pubmed-meshheading:1967651-3,4-Methylenedioxyamphetamine,
pubmed-meshheading:1967651-Amphetamines,
pubmed-meshheading:1967651-Animals,
pubmed-meshheading:1967651-Behavior, Animal,
pubmed-meshheading:1967651-Catecholamines,
pubmed-meshheading:1967651-Cerebral Cortex,
pubmed-meshheading:1967651-Hippocampus,
pubmed-meshheading:1967651-Indans,
pubmed-meshheading:1967651-Lysergic Acid Diethylamide,
pubmed-meshheading:1967651-N-Methyl-3,4-methylenedioxyamphetamine,
pubmed-meshheading:1967651-Paroxetine,
pubmed-meshheading:1967651-Piperidines,
pubmed-meshheading:1967651-Psychotropic Drugs,
pubmed-meshheading:1967651-Rats,
pubmed-meshheading:1967651-Serotonin,
pubmed-meshheading:1967651-Structure-Activity Relationship,
pubmed-meshheading:1967651-Tetrahydronaphthalenes
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pubmed:year |
1990
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pubmed:articleTitle |
Nonneurotoxic tetralin and indan analogues of 3,4-(methylenedioxy)amphetamine (MDA).
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pubmed:affiliation |
Department of Medicinal Chemistry, School of Pharmacy and Pharmacal Sciences, Purdue University, West Lafayette, Indiana 47907.
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pubmed:publicationType |
Journal Article,
Research Support, U.S. Gov't, P.H.S.
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