Abstract
The synthesis and in vitro affinity of the alpha5beta3gamma2 (alpha5) subtype selective BzR/GABA(A) antagonist 7 is described. This ligand is selective for alpha5 subtypes in vitro and is a potent antagonist of the effects of diazepam only at alpha5beta3gamma2 subtypes (oocytes). Ligands such as 7 will be important in the determination of which physiological function(s) are subserved by this GABA(A) alpha5 subtype.
Publication types
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Animals
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Benzodiazepinones / chemical synthesis*
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Benzodiazepinones / chemistry
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Benzodiazepinones / pharmacology
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Cell Line
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Chloride Channels / drug effects
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Chloride Channels / physiology
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Crystallography, X-Ray
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GABA Antagonists / chemical synthesis*
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GABA Antagonists / chemistry
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GABA Antagonists / pharmacology
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GABA-A Receptor Antagonists*
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Humans
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Imidazoles / chemical synthesis*
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Imidazoles / chemistry
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Imidazoles / pharmacology
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In Vitro Techniques
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Ligands
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Models, Molecular
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Oocytes / drug effects
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Oocytes / physiology
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Patch-Clamp Techniques
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Radioligand Assay
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Receptors, GABA-A / physiology
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Structure-Activity Relationship
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Xenopus
Substances
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1,3-bis(8-ethynyl-5,6-dihydro-5-methyl-6-oxo-4H-imidazo(1,5-a)(1,4)benzodiazepine-3-carboxy)propyl diester
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Benzodiazepinones
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Chloride Channels
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GABA Antagonists
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GABA-A Receptor Antagonists
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Imidazoles
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Ligands
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Receptors, GABA-A