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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
3
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pubmed:dateCreated |
1986-4-2
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pubmed:abstractText |
The effects of preincubating cerebral cortical membranes with phospholipase A2 (PLA2) were examined on radioligand binding to benzodiazepine receptors of the "central" and "peripheral" types. PLA2 (0.005-0.1 U/ml) increased [3H]flunitrazepam and [3H]3-carboethoxy-beta-carboline binding by increasing the apparent affinities of these ligands with no concomitant change in the maximum number of binding sites. In contrast, neither gamma-aminobutyric acid (GABA)-enhanced [3H]flunitrazepam binding nor [3H]Ro 15-1788 binding was altered by preincubation with PLA2 at concentrations as high as 2 U/ml. Both pyrazolopyridine (SQ 65,396)- and barbiturate (pentobarbital)-enhanced [3H]flunitrazepam binding and [35S]t-butylbicyclophosphorothionate (TBPS) binding were markedly reduced by as little as 0.0025-0.005 U/ml of PLA2. These findings suggest that PLA2 inactivates the TBPS binding site on the benzodiazepine-GABA receptor chloride ionophore complex, which results in a selective loss of allosteric "regulation" between the components of this complex. PLA2 also reduced the apparent affinity of [3H]Ro 5-4864 to peripheral-type benzodiazepine receptors in cerebral cortical, heart, and kidney membranes, but increased the number of [3H]PK 11195 binding sites with no change in apparent affinity. These data demonstrate that PLA2 can differentially affect the lipid microenvironment of "central" and "peripheral" types of benzodiazepine 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/Benzodiazepinones,
http://linkedlifedata.com/resource/pubmed/chemical/Bicyclo Compounds,
http://linkedlifedata.com/resource/pubmed/chemical/Bicyclo Compounds, Heterocyclic,
http://linkedlifedata.com/resource/pubmed/chemical/Carbolines,
http://linkedlifedata.com/resource/pubmed/chemical/Flumazenil,
http://linkedlifedata.com/resource/pubmed/chemical/Flunitrazepam,
http://linkedlifedata.com/resource/pubmed/chemical/Pentobarbital,
http://linkedlifedata.com/resource/pubmed/chemical/Phospholipases,
http://linkedlifedata.com/resource/pubmed/chemical/Phospholipases A,
http://linkedlifedata.com/resource/pubmed/chemical/Phospholipases A2,
http://linkedlifedata.com/resource/pubmed/chemical/Pyrazoles,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, GABA-A,
http://linkedlifedata.com/resource/pubmed/chemical/beta-carboline-3-carboxylic acid...,
http://linkedlifedata.com/resource/pubmed/chemical/cartazolate,
http://linkedlifedata.com/resource/pubmed/chemical/gamma-Aminobutyric Acid,
http://linkedlifedata.com/resource/pubmed/chemical/tert-butylbicyclophosphorothionate
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pubmed:status |
MEDLINE
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pubmed:month |
Mar
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pubmed:issn |
0022-3042
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:volume |
46
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
804-11
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pubmed:dateRevised |
2007-11-15
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pubmed:meshHeading |
pubmed-meshheading:3005493-Animals,
pubmed-meshheading:3005493-Benzodiazepinones,
pubmed-meshheading:3005493-Bicyclo Compounds,
pubmed-meshheading:3005493-Bicyclo Compounds, Heterocyclic,
pubmed-meshheading:3005493-Carbolines,
pubmed-meshheading:3005493-Cerebral Cortex,
pubmed-meshheading:3005493-Flumazenil,
pubmed-meshheading:3005493-Flunitrazepam,
pubmed-meshheading:3005493-Kidney,
pubmed-meshheading:3005493-Male,
pubmed-meshheading:3005493-Myocardium,
pubmed-meshheading:3005493-Pentobarbital,
pubmed-meshheading:3005493-Phospholipases,
pubmed-meshheading:3005493-Phospholipases A,
pubmed-meshheading:3005493-Phospholipases A2,
pubmed-meshheading:3005493-Pyrazoles,
pubmed-meshheading:3005493-Rats,
pubmed-meshheading:3005493-Rats, Inbred Strains,
pubmed-meshheading:3005493-Receptors, GABA-A,
pubmed-meshheading:3005493-gamma-Aminobutyric Acid
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pubmed:year |
1986
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pubmed:articleTitle |
Differential sensitivity of "central" and "peripheral" type benzodiazepine receptors to phospholipase A2.
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pubmed:publicationType |
Journal Article,
Comparative Study,
Research Support, Non-U.S. Gov't
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