GABAa receptor ligands

GABA, heterocyclic analogues, 22 (1985) 67 GABAa receptor ligands, 36 (1999) 169 Gas-liquid chromatography and mass spectrometry, 12 (1975) 1 Gastric H /K -ATPase inhibitors, 31 (1994) 233... 

Functional Characterization of GABAa Receptor Ligands In Vitro... 

Kristiansen, U., Lambert, J. D., Falch, E and Krogsgaard-Larsen, P. (1991) Electrophysio-logical studies of the GABAA receptor ligand, 4-PIOL, on cultured hippocampal neurones. Br. J. Pharmacol. 104, 85-90. 

DEVELOPMENT OF A NEW PHARMACOPHORE MODEL FOR GABAa RECEPTOR LIGANDS... 

Frplund, B., Ebert, B., Kristiansen, U., Liljefors, T., and Krogsgaard-Larsen, P. (2002) GABAa receptor ligands and their therapeutic potentials. Curr. Med. Chem. 2, 817-832. 

Ito Y, Segawa K, Fukuda H. (1995). Functional diversity of GABAA receptor ligand-gated chloride channels in rat synaptoneurosomes. Synapse. 19(3) 188-96. 

HT3 receptors belong to the ligand-gated ion channel receptor superfamily, similar to the nicotinic acetylcholine or GABAa receptors and share elec-trophysiological and structural patterns. The receptors... 

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)...

Table 19.4 Putative endogenous ligands for the benzodiazepine binding domain on the GABAa receptor...

Dysfunction of the GABAa receptor complex such that the effects of all benzodiazepine receptor ligands are shifted in the direction of inverse agonism. In this case, fiumazenil (which normally has zero efficacy) should induce anxiety in anxious patients but have no effects in healthy subjects because they have normal receptors. 

Wasowski C, Marder M, Viola H, Medina JH, Paladini AC. Isolation and identification of 6-methylapigenin, a competitive ligand for the brain GABAa receptors, from Valeriana wallichii. Planta Med 2002 68 934-936. 

GABAa receptors are chloride channels and members of a superfamily of ligand-gated ion channel receptors 293 A family of pentameric GABAA-receptor protein subtypes exists 294 The GABAa receptor is the major molecular target for the action of many drugs in the brain 296... 

Neuro steroids, which may be physiological modulators of brain activity, enhance GABAa receptor function 297 The three-dimensional structures of ligand-gated ion channel receptors are being modeled successfully 297 Mouse genetics reveal important functions for GABAa receptor subtypes 297... 

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