Antagonists benzodiazepine receptor ligands

Li L, Chen T, Stanton JD, Sueyoshi T, Negishi M, Wang H (2008) The peripheral benzodiazepine receptor ligand l-(2-chlorophenyl-methylpropyl)-3-isoquinoline-carboxamide is a novel antagonist of human constitutive androstane receptor. Mol Pharmacol 74 443-453... 

Figure 11.6 Schematic representation of the GABAa receptor complex. Examples of the many structurally diverse compounds that act at different sites on the receptor (see text for details). Picrotoxinin, the active component of picrotoxin, and TBPS act as non-competitive antagonists. The barbiturates, steroids and anaesthetics are positive allosteric modulators, as are the benzodiazepine site ligands shown, with the exception of DMCM (negative allosteric modulator) and flumazenil (benzodiazepine site antagonist)...

Inadequate activity of an endogenous ligand which is a benzodiazepine receptor agonist and suppresses anxiety. In this case, the administration of the antagonist, fiumazenil, should induce anxiety in normal subjects and exacerbate anxiety in anxious patients. 

The antagonist [methyl- C]Ro 15-1788, an imidazodiazepine 272, high-aliinity and high-specificity ligand for the central benzodiazepine receptor used in PET , has been synthesized by reaction of [ C]methyl iodide with the desmethyl precursor and... 

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