rdf:type |
|
lifeskim:mentions |
|
pubmed:issue |
2
|
pubmed:dateCreated |
1999-12-23
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pubmed:abstractText |
The novel GABA(B) receptor antagonist [3H]CGP 62349 binds rat cerebellar synaptosomal membranes with high affinity at a single population of sites (K(d) = 0.9 nM, B(max) = 760 fmol/mg protein). Solubilisation with 1% Triton X-100/0.5 M NaCl/10% glycerol resulted in a marked increase in [3H]CGP 62349 binding (K(d) = 0.5 nM, B(max) = 1285 fmol/mg protein). Competition of [3HCGP 35348 = CGP 36742. The GABA(A) ligand isoguvacine did not displace [3H]CGP 62349 binding. Partial purification of [3H]CGP 62349 binding sites was obtained by sucrose density centrifugation and a predominant protein in the peak binding fraction was recognised by an anti-GABA(B) receptor antibody and had a molecular weight similar to the recombinant expressed GABA(B)R1a. These results demonstrate that [3H]CGP 62349 provides a useful additional tool for further characterisation of the pharmacology and biochemistry of the native GABA(B) receptor.
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pubmed:language |
eng
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pubmed:journal |
|
pubmed:citationSubset |
IM
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pubmed:chemical |
|
pubmed:status |
MEDLINE
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pubmed:month |
Aug
|
pubmed:issn |
0169-328X
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pubmed:author |
|
pubmed:issnType |
Print
|
pubmed:day |
25
|
pubmed:volume |
71
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
|
pubmed:pagination |
279-89
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pubmed:dateRevised |
2010-11-18
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pubmed:meshHeading |
pubmed-meshheading:10521582-Animals,
pubmed-meshheading:10521582-Benzoates,
pubmed-meshheading:10521582-Binding Sites,
pubmed-meshheading:10521582-Biotinylation,
pubmed-meshheading:10521582-COS Cells,
pubmed-meshheading:10521582-Cells, Cultured,
pubmed-meshheading:10521582-Centrifugation, Density Gradient,
pubmed-meshheading:10521582-Cerebellum,
pubmed-meshheading:10521582-Detergents,
pubmed-meshheading:10521582-Electrophoresis, Polyacrylamide Gel,
pubmed-meshheading:10521582-GABA-B Receptor Antagonists,
pubmed-meshheading:10521582-Isonicotinic Acids,
pubmed-meshheading:10521582-Kinetics,
pubmed-meshheading:10521582-Organophosphorus Compounds,
pubmed-meshheading:10521582-Rats,
pubmed-meshheading:10521582-Receptors, GABA-B,
pubmed-meshheading:10521582-Transfection
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pubmed:year |
1999
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pubmed:articleTitle |
Characterisation and partial purification of the GABA(B) receptor from the rat cerebellum using the novel antagonist [3H]CGP 62349.
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pubmed:affiliation |
Department of Anatomy, Medical School, University Walk, Bristol University, Bristol, UK.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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