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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
1
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pubmed:dateCreated |
1986-5-9
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pubmed:abstractText |
The (+)- and (-)-enantiomers of the 2-aminotetralin derivatives cis-5-methoxy-1-methyl-2-(di-n-propylamino)tetralin (UH 232) and cis-5-hydroxy-1-methyl-2-(di-n-propylamino)tetralin (UH 242), were pharmacologically evaluated in rats in an extensive series of in vivo biochemical and behavioral experiments. These studies showed that the (+)- and (-)-enantiomers have differential effects on central dopamine (DA) receptors. Thus, (-)-UH 242 is a DA-receptor agonist stimulating both pre- and postsynaptic receptors. (-)-UH 232 is also active as a DA receptor agonist, although with much lower potency than (-)-UH 242. In contrast, (+)-UH 242 and (+)-UH 232 are characterized as DA receptor antagonists. Both (+) forms markedly accelerated DA synthesis and turnover and reversed the biochemical and behavioral effects of apomorphine. Locomotor activity was stimulated by the (+)-enantiomers over a wide dose range; hypomotility was induced only by high doses. The pharmacological profile of the (+)-enantiomers clearly differs from that of classical neuroleptics and suggests a preferential antagonistic action on DA autoreceptors. (+)-UH 232 and (+)-UH 242 may prove useful as experimental tools and as potential therapeutic agents (selectively increasing DA-ergic neurotransmission), e.g. in geriatric practice.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/4-Butyrolactone,
http://linkedlifedata.com/resource/pubmed/chemical/5-Hydroxytryptophan,
http://linkedlifedata.com/resource/pubmed/chemical/5-hydroxy-1-methyl-2-(di-n-propylami...,
http://linkedlifedata.com/resource/pubmed/chemical/8-Hydroxy-2-(di-n-propylamino)tetral...,
http://linkedlifedata.com/resource/pubmed/chemical/Apomorphine,
http://linkedlifedata.com/resource/pubmed/chemical/Dihydroxyphenylalanine,
http://linkedlifedata.com/resource/pubmed/chemical/Naphthalenes,
http://linkedlifedata.com/resource/pubmed/chemical/Norepinephrine,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Dopamine,
http://linkedlifedata.com/resource/pubmed/chemical/Reserpine,
http://linkedlifedata.com/resource/pubmed/chemical/Serotonin,
http://linkedlifedata.com/resource/pubmed/chemical/Tetrahydronaphthalenes,
http://linkedlifedata.com/resource/pubmed/chemical/UH 232
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pubmed:status |
MEDLINE
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pubmed:issn |
0300-9564
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:volume |
65
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pubmed:owner |
NLM
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pubmed:authorsComplete |
N
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pubmed:pagination |
1-27
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:3083041-4-Butyrolactone,
pubmed-meshheading:3083041-5-Hydroxytryptophan,
pubmed-meshheading:3083041-8-Hydroxy-2-(di-n-propylamino)tetralin,
pubmed-meshheading:3083041-Animals,
pubmed-meshheading:3083041-Apomorphine,
pubmed-meshheading:3083041-Behavior, Animal,
pubmed-meshheading:3083041-Dihydroxyphenylalanine,
pubmed-meshheading:3083041-Dopamine,
pubmed-meshheading:3083041-Dose-Response Relationship, Drug,
pubmed-meshheading:3083041-Drug Interactions,
pubmed-meshheading:3083041-Male,
pubmed-meshheading:3083041-Motor Activity,
pubmed-meshheading:3083041-Naphthalenes,
pubmed-meshheading:3083041-Norepinephrine,
pubmed-meshheading:3083041-Rats,
pubmed-meshheading:3083041-Rats, Inbred Strains,
pubmed-meshheading:3083041-Receptors, Dopamine,
pubmed-meshheading:3083041-Reserpine,
pubmed-meshheading:3083041-Serotonin,
pubmed-meshheading:3083041-Stereoisomerism,
pubmed-meshheading:3083041-Tetrahydronaphthalenes
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pubmed:year |
1986
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pubmed:articleTitle |
(+)-UH 232 and (+)-UH 242: novel stereoselective dopamine receptor antagonists with preferential action on autoreceptors.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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