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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
2-3
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pubmed:dateCreated |
1992-12-4
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pubmed:abstractText |
Studies of 1,3-di-(2-[5-3H]tolyl)guanidine ([3H]DTG) binding to rat brain membranes revealed that [3H]DTG binds to a high and a low affinity site with Kd values of 19.8 nM and 1.31 microM (corresponding Bmax values 291 fmol/mg protein and 8.68 pmol/mg protein). The order of potency of competitors for [3H]DTG binding revealed a binding profile typical of sigma site ligands. Several sigma ligands such as the enantiomers of 3-PPP (3-(3-hydroxyphenyl)-N- (n-propyl)piperidine) and (+/-)-pentazocine exhibited biphasic competition profiles for [3H]DTG binding, whereas other sigma ligands such as haloperidol displayed monotonic competition curves. Neither phenytoin nor carbamazepine were observed to enhance [3H]DTG binding. These data support the hypothesis that multiple sigma binding sites exist. The lack of phenytoin and carbamazepine modulation of [3H]DTG binding are in agreement with the proposed greater density of sigma site 2 in the rat, since allosteric modulation has been ascribed to the DM1/sigma 1 site.
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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/1,3-ditolylguanidine,
http://linkedlifedata.com/resource/pubmed/chemical/Carbamazepine,
http://linkedlifedata.com/resource/pubmed/chemical/Guanidines,
http://linkedlifedata.com/resource/pubmed/chemical/Haloperidol,
http://linkedlifedata.com/resource/pubmed/chemical/Pentazocine,
http://linkedlifedata.com/resource/pubmed/chemical/Phenytoin,
http://linkedlifedata.com/resource/pubmed/chemical/Piperidines,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, sigma,
http://linkedlifedata.com/resource/pubmed/chemical/n-N-propyl-3-(3-hydroxyphenyl)piperi...
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pubmed:status |
MEDLINE
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pubmed:month |
Jul
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pubmed:issn |
0014-2999
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:day |
7
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pubmed:volume |
217
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
149-52
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pubmed:dateRevised |
2003-11-14
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pubmed:meshHeading |
pubmed-meshheading:1425936-Animals,
pubmed-meshheading:1425936-Binding, Competitive,
pubmed-meshheading:1425936-Binding Sites,
pubmed-meshheading:1425936-Carbamazepine,
pubmed-meshheading:1425936-Guanidines,
pubmed-meshheading:1425936-Haloperidol,
pubmed-meshheading:1425936-Male,
pubmed-meshheading:1425936-Pentazocine,
pubmed-meshheading:1425936-Phenytoin,
pubmed-meshheading:1425936-Piperidines,
pubmed-meshheading:1425936-Prosencephalon,
pubmed-meshheading:1425936-Rats,
pubmed-meshheading:1425936-Rats, Wistar,
pubmed-meshheading:1425936-Receptors, sigma,
pubmed-meshheading:1425936-Stereoisomerism
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pubmed:year |
1992
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pubmed:articleTitle |
1,3-Di(2-[5-3H]tolyl)guanidine labels more than one site in rat forebrain.
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pubmed:affiliation |
Drug Discovery Research, R.W. Johnson Pharmaceutical Research Institute, Spring House, PA 19477-0776.
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pubmed:publicationType |
Journal Article
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