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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
6
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pubmed:dateCreated |
1990-8-29
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pubmed:abstractText |
In guinea-pig cerebellum, saturation studies reveal that the nonselective opioid [3H]ethylketazocine has a binding capacity (R) of 6.79 pmol/g tissue which is similar to the sum of the individual R values of the mu-, delta- and kappa 1-selective opioids. Conversely, the binding parameters of the nonselective opioid [3H]bremazocine are best-fitted to a two-site model (Kd1 = 0.12 nM, R1 = 11.3 pmol/g tissue; Kd2 = 6.03 nM, R2 = 9.09 pmol/g tissue) with an R TOTAL value of 20.3 pmol/g tissue which is statistically different from the R value of [3H]ethylketazocine or the sum of R mu + R delta + R kappa 1. This suggests that [3H]bremazocine labels additional opioid binding sites. After suppression of the mu-, delta- and kappa 1-receptors, [3H]bremazocine binding is then best-fitted to a one-site model with a Kd value of 1.48 nM and an R value of 11.2 pmol/g tissue. Competition studies done against the binding of [3H]U69593 indicate that the opioid receptors labelled with this ligand are related to the kappa 1-receptor subtype. However, competition studies performed against the binding of [3H]bremazocine (under suppressed conditions) display a pharmacological profile related to another subtype of kappa-receptors previously described in guinea-pig brain as the kappa 2-receptors.
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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/Benzeneacetamides,
http://linkedlifedata.com/resource/pubmed/chemical/Benzomorphans,
http://linkedlifedata.com/resource/pubmed/chemical/Cyclazocine,
http://linkedlifedata.com/resource/pubmed/chemical/Enkephalin, Ala(2)-MePhe(4)-Gly(5)-,
http://linkedlifedata.com/resource/pubmed/chemical/Enkephalin, D-Penicillamine (2,5)-,
http://linkedlifedata.com/resource/pubmed/chemical/Enkephalins,
http://linkedlifedata.com/resource/pubmed/chemical/Ethylketocyclazocine,
http://linkedlifedata.com/resource/pubmed/chemical/Pyrrolidines,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Opioid,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Opioid, delta,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Opioid, kappa,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Opioid, mu,
http://linkedlifedata.com/resource/pubmed/chemical/U 69593,
http://linkedlifedata.com/resource/pubmed/chemical/bremazocine
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pubmed:status |
MEDLINE
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pubmed:month |
Jun
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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 |
12
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pubmed:volume |
188
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
379-89
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:2164939-Animals,
pubmed-meshheading:2164939-Benzeneacetamides,
pubmed-meshheading:2164939-Benzomorphans,
pubmed-meshheading:2164939-Binding, Competitive,
pubmed-meshheading:2164939-Cerebellum,
pubmed-meshheading:2164939-Computers,
pubmed-meshheading:2164939-Cyclazocine,
pubmed-meshheading:2164939-Enkephalin, Ala(2)-MePhe(4)-Gly(5)-,
pubmed-meshheading:2164939-Enkephalin, D-Penicillamine (2,5)-,
pubmed-meshheading:2164939-Enkephalins,
pubmed-meshheading:2164939-Ethylketocyclazocine,
pubmed-meshheading:2164939-Guinea Pigs,
pubmed-meshheading:2164939-Kinetics,
pubmed-meshheading:2164939-Male,
pubmed-meshheading:2164939-Membranes,
pubmed-meshheading:2164939-Pyrrolidines,
pubmed-meshheading:2164939-Receptors, Opioid,
pubmed-meshheading:2164939-Receptors, Opioid, delta,
pubmed-meshheading:2164939-Receptors, Opioid, kappa,
pubmed-meshheading:2164939-Receptors, Opioid, mu
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pubmed:year |
1990
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pubmed:articleTitle |
Demonstration of the heterogeneity of the kappa-opioid receptors in guinea-pig cerebellum using selective and nonselective drugs.
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pubmed:affiliation |
Département de pharmacologie, Université de Montréal, Quebec, Canada.
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pubmed:publicationType |
Journal Article,
In Vitro,
Research Support, Non-U.S. Gov't
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