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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
10
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pubmed:dateCreated |
1990-11-20
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pubmed:abstractText |
A series of 2-phenyl-2-(1-hydroxycycloalkyl)ethylamine derivatives was examined for the ability to inhibit both rat brain imipramine receptor binding and the synaptosomal uptake of norepinephrine (NE) and serotonin (5-HT). Neurotransmitter uptake inhibition was highest for a subset of 2-phenyl-2-(1-hydroxycyclohexyl)dimethylethylamines in which the aryl ring has a halogen or methoxy substituent at the 3- and/or 4-positions. Potential antidepressant activity in this subset was assayed in three rodent models--the antagonism of reserpine-induced hypothermia, the antagonism of histamine-induced ACTH release, and the ability to reduce noradrenergic responsiveness in the rat pineal gland. An acute effect seen in the rat pineal gland with several analogues, including 1-[1-(3,4-dichlorophenyl)-2-(dimethylamino)ethyl]cyclohexanol (23) and 1-[2-(dimethylamino)-1)-(4-methoxyphenyl)ethyl]cyclohexanol (4), was taken as a possible correlate of a rapid onset of antidepressant activity. Compound 4 (venlafaxine) is presently undergoing clinical evaluation.
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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/Adrenocorticotropic Hormone,
http://linkedlifedata.com/resource/pubmed/chemical/Antidepressive Agents,
http://linkedlifedata.com/resource/pubmed/chemical/Imipramine,
http://linkedlifedata.com/resource/pubmed/chemical/Neurotransmitter Agents,
http://linkedlifedata.com/resource/pubmed/chemical/Norepinephrine,
http://linkedlifedata.com/resource/pubmed/chemical/Phenethylamines,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Adrenergic, beta,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Serotonin,
http://linkedlifedata.com/resource/pubmed/chemical/Reserpine,
http://linkedlifedata.com/resource/pubmed/chemical/Serotonin
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pubmed:status |
MEDLINE
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pubmed:month |
Oct
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pubmed:issn |
0022-2623
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:volume |
33
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pubmed:owner |
NLM
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pubmed:authorsComplete |
N
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pubmed:pagination |
2899-905
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pubmed:dateRevised |
2008-11-21
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pubmed:meshHeading |
pubmed-meshheading:1976813-Adrenocorticotropic Hormone,
pubmed-meshheading:1976813-Animals,
pubmed-meshheading:1976813-Antidepressive Agents,
pubmed-meshheading:1976813-Binding, Competitive,
pubmed-meshheading:1976813-Biological Assay,
pubmed-meshheading:1976813-Biological Transport,
pubmed-meshheading:1976813-Brain,
pubmed-meshheading:1976813-Chemistry, Physical,
pubmed-meshheading:1976813-Crystallography,
pubmed-meshheading:1976813-Hypothermia,
pubmed-meshheading:1976813-Imipramine,
pubmed-meshheading:1976813-Models, Molecular,
pubmed-meshheading:1976813-Neurotransmitter Agents,
pubmed-meshheading:1976813-Norepinephrine,
pubmed-meshheading:1976813-Phenethylamines,
pubmed-meshheading:1976813-Physicochemical Phenomena,
pubmed-meshheading:1976813-Rats,
pubmed-meshheading:1976813-Receptors, Adrenergic, beta,
pubmed-meshheading:1976813-Receptors, Serotonin,
pubmed-meshheading:1976813-Reserpine,
pubmed-meshheading:1976813-Serotonin,
pubmed-meshheading:1976813-Structure-Activity Relationship,
pubmed-meshheading:1976813-X-Ray Diffraction
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pubmed:year |
1990
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pubmed:articleTitle |
2-Phenyl-2-(1-hydroxycycloalkyl)ethylamine derivatives: synthesis and antidepressant activity.
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pubmed:affiliation |
Wyeth-Ayerst Research, Princeton, New Jersey 08543-8000.
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pubmed:publicationType |
Journal Article,
In Vitro
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