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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
1-3
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pubmed:dateCreated |
1997-2-12
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pubmed:abstractText |
This is the first study characterising the binding of the new imidazoline I2 receptor selective radioligand [3H]2-(2-benzofuranyl)-2-imidazoline (2-BFI) to rabbit brain membranes. [3H]2-BFI binding was found to be saturable and of high affinity identifying two binding sites with KD1 = 0.27 nM, Bmax = 111.2 fmol mg-1 protein and KD2 = 8.97 nM, Bmax = 268 fmol mg-1 protein. Specific binding represented greater than 90% of total binding. Kinetic studies revealed that the binding was rapid and reversible and also showed [3H]2-BFI interacted with these two sites or two affinity states. In competition binding studies against [3H]2-BFI (0.3-InM) idazoxan, 2-BFI, cirazoline, guanabenz, naphazoline, amiloride and BU224 (2-(4,5-dihydroimidaz-2-yl-quinoline) displaced with high affinity. In contrast the alpha 2-adrenoceptor antagonists efaroxan and rauwolscine, the I1 site selective drug moxonidine, the monoamine oxidase-A inhibitor clorgyline and the proposed endogenous imidazoline receptor ligand, agmatine, were weak at displacing [3H]2-BFI binding. These findings are consistent with [3H]2-BFI recognising imidazoline receptors of the I2 subtype in rabbit brain.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Affinity Labels,
http://linkedlifedata.com/resource/pubmed/chemical/Benzofurans,
http://linkedlifedata.com/resource/pubmed/chemical/Imidazoles,
http://linkedlifedata.com/resource/pubmed/chemical/Imidazoline Receptors,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Drug
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pubmed:status |
MEDLINE
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pubmed:month |
May
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pubmed:issn |
0014-2999
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:day |
23
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pubmed:volume |
304
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pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
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pubmed:pagination |
221-9
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pubmed:dateRevised |
2007-11-15
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pubmed:meshHeading |
pubmed-meshheading:8813605-Affinity Labels,
pubmed-meshheading:8813605-Animals,
pubmed-meshheading:8813605-Benzofurans,
pubmed-meshheading:8813605-Binding, Competitive,
pubmed-meshheading:8813605-Brain,
pubmed-meshheading:8813605-Cell Membrane,
pubmed-meshheading:8813605-Female,
pubmed-meshheading:8813605-Imidazoles,
pubmed-meshheading:8813605-Imidazoline Receptors,
pubmed-meshheading:8813605-Kinetics,
pubmed-meshheading:8813605-Male,
pubmed-meshheading:8813605-Protein Binding,
pubmed-meshheading:8813605-Rabbits,
pubmed-meshheading:8813605-Radioligand Assay,
pubmed-meshheading:8813605-Receptors, Drug
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pubmed:year |
1996
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pubmed:articleTitle |
[3H]2-(2-benzofuranyl)-2-imidazoline: a new selective high affinity radioligand for the study of rabbit brain imidazoline I2 receptors.
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pubmed:affiliation |
Department of Pharmacology, School of Medical Sciences, University of Bristol, UK.
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pubmed:publicationType |
Journal Article,
In Vitro,
Research Support, Non-U.S. Gov't
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