GABA receptor ligand

Imidazopyridothiazines (and imidazopyridopyrazines) can be prepared from the corresponding aminochloropyr-idines in a one-pot reaction, as shown in Scheme 69. Products in which R= l,2,4-oxadiazol-3-yl are of interest as possible 7-aminobutyric acid (GABA) receptor ligands <2002M653, 2002M1205>. 

A series of imidazopyridopyrimidines of the type 315 have been prepared as in Equation (108) for evaluation as GABA receptor ligands <2002JME5043>. 

Mousah H, Jacqmin P, Lesne M. (1986). Interaction of carbolines and some GABA receptor ligands with the GABA and the benzodiazepine receptors. J Pharmacol. 17(4) 686-91. 

Nonbenzodiazepine Benzodiazepine Receptor Ligands. The simultaneous discovery of the molecular target for the BZs, the GABA /BZ receptor complex, by two teams of workers (34,35) resulted ia the identification of a number of atypical or anxioselective anxiolytics that, whereas not having the BZ pharmacophore, interacted direcdy with the central BZ receptor. The anxioselective nature of such agents was considered to be... 

The undisputed efficacy of benzodiazepines in relief of anxiety led to the question of whether this disorder could arise from abnormal concentrations in the brain of an endogenous ligand or a malfunction of the benzodiazepine/GABA receptor system. An important study, aimed at distinguishing between these possibilities, has been carried out in humans (Nutt et al. 1990) and was based on the premise that anxiety could be caused by either ... 

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... 

Erker and Trinkl synthesized the tricycles 177 as novel GABA-A/benzodiazepine receptor ligands via synthesis of enol phosphates such as 175 and reaction with isocyanides 176 (Scheme 13) <2001H1963>. 

Ebert, B., Storustovu, S., Mortensen, M., and Frplund, B. (2002) Characterization of GABA(A) receptor ligands in the rat cortical wedge preparation evidence for action at extrasynaptic receptors Br. J. Pharmacol. 137,1-8. 

GABA-A receptor ligands GABA uptake inhibitors... 

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