Switch to
Predicate | Object |
---|---|
rdf:type | |
lifeskim:mentions | |
pubmed:issue |
1
|
pubmed:dateCreated |
1980-4-26
|
pubmed:abstractText |
A single treatment with a large dose of methiothepin (20 mg/kg, i.p.) induced, as early as the 2nd day after injection, a significant increase (+20--35%) in the number of specific binding sites for 3H-5-HT in forebrain areas, particularly the hippocampus. Experiments with 3H-methiothepin indicated that the drug remained firmly bound to brain membranes thus maintaining a local concentration high enough to effectively block 5-HT receptors for 10--12 h after its peripheral administration. Accordingly, it can be concluded that the occupancy of central 5-HT receptor sites by methiothepin for several hours was sufficient to induce a supersensitivity phenomenon within the two following days. Although 3H-methiothepin was a useful marker for analyzing the disposition and the kinetics of the 5-HT antagonist in brain tissues, it could not be used as a specific ligand of 5-HT receptors in brain since under in vitro as well as in vivo conditions most of 3H-methiothepin bound to non-specific sites, especially to the lipid component of the membranes.
|
pubmed:language |
eng
|
pubmed:journal | |
pubmed:citationSubset |
IM
|
pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Adenylate Cyclase,
http://linkedlifedata.com/resource/pubmed/chemical/Dibenzothiepins,
http://linkedlifedata.com/resource/pubmed/chemical/Haloperidol,
http://linkedlifedata.com/resource/pubmed/chemical/Methiothepin,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Serotonin,
http://linkedlifedata.com/resource/pubmed/chemical/Serotonin,
http://linkedlifedata.com/resource/pubmed/chemical/Spiperone
|
pubmed:status |
MEDLINE
|
pubmed:month |
Dec
|
pubmed:issn |
0028-1298
|
pubmed:author | |
pubmed:issnType |
Print
|
pubmed:volume |
310
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
|
pubmed:pagination |
25-33
|
pubmed:dateRevised |
2003-11-14
|
pubmed:meshHeading |
pubmed-meshheading:530311-Adenylate Cyclase,
pubmed-meshheading:530311-Animals,
pubmed-meshheading:530311-Brain,
pubmed-meshheading:530311-Dibenzothiepins,
pubmed-meshheading:530311-Haloperidol,
pubmed-meshheading:530311-Male,
pubmed-meshheading:530311-Membranes,
pubmed-meshheading:530311-Methiothepin,
pubmed-meshheading:530311-Rats,
pubmed-meshheading:530311-Receptors, Serotonin,
pubmed-meshheading:530311-Serotonin,
pubmed-meshheading:530311-Spiperone,
pubmed-meshheading:530311-Synaptosomes,
pubmed-meshheading:530311-Time Factors
|
pubmed:year |
1979
|
pubmed:articleTitle |
In vitro and in vivo disposition of 3H-methiothepin in brain tissues. Relationship to the effects of acute treatment with methiothepin on central serotoninergic receptors.
|
pubmed:publicationType |
Journal Article
|