GABA-A ligands

Binds to benzodiazepine receptors at the GABA-A ligand-gated chloride channel complex... 

Schofield, PR, Darlison, MG, Fujita, N, Burt, DR, Stephenson, FA, Rodriguez, H, Rhee, LM, Ramachandran, J, Reale, V, Glencorse, TA et al. (1987) Sequence and functional expression of the GABA A receptor shows a ligand-gated receptor super-family. Nature 328 221-227. 

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>. 

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>. 

Basile AS, Gammal SH, Jones EA, Skolnick P GABA-A receptor complex in an experimental model of hepatic encephalopathy Evidence for elevated levels of an endogenous benzodiazepine receptor complex ligand. J Neurochem 1989 53 1057-1063. 

Ebert, B., Mortensen, M., Thompson, S. A., Kehler, J., Wafford, K. A., and Krogsgaard-Larsen, P. (2001) Bioisosteric determinants for subtype selectivity of ligands for het-eromeric GABA(A) receptors. Bioorg. Med. Chem. Lett. 11, 1573-1577. 

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. 

Chebib, M. and Johnston, G. A. R. (2000) GABA-activated ligand gated ion channels medicinal chemistry and molecular biology../. Med. Chem. 43,1427-1447. 

GABA-A receptor ligands GABA uptake inhibitors... 

Ion channels (center). These receptors contain ligand-gated ion channels. Binding of the signaling substance opens the channels for ions such as Na, Ca, and Cl . This mechanism is mainly used by neurotransmitters such as acetylcholine (nicotinic receptor see p.224) and GABA (A receptor see p.354). 

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