GABA A

Neurosteroids are neuroactive steroids, which are synthesized in the brain. Neurosteroids can bind to and modulate the activity of y-aminobuty tie acidA(GABA A) receptors. 

Chester JA, Cunningham CL GABA(A) receptor modulation of the rewarding and aversive effects of ethanol. Alcohol 26 131—143, 2002 Chick J Safety issues concerning the use of disulfiram in treating alcohol dependence. Drug Saf 20 427 35, 1999... 

Edenberg HJ, Dick DM, Xuei X, et al Variations in GABRA2, encoding the alpha 2 subunit of the GABA(A) receptor, are associated with alcohol dependence and with brain oscillations. Am J Hum Genet 74 705-714, 2004... 

Atack JR Anxioselective compounds acting at the GABA(A) receptor benzodiazepine binding site. Curr Drug Target CNS Neurol Disord 2 213—232, 2003... 

Gamma aminobutyric acid (GABA) receptors are located on the postsynaptic membranes of inhibitory synapses of both vertebrates and insects and contain within their membrane-spanning structure a chloride ion channel. They are found in both vertebrate brains and invertebrate cerebral ganglia (sometimes referred to as brains) as well as in insect muscles. Particular attention has been given to one form of this receptor—the GABA-A receptor—as a target for novel insecticides (Eldefrawi and Eldefrawi 1990). It is found both in insect muscle and vertebrate brain. The remainder of this description will be restricted to this form. 

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. 

Malizia, AL, Cunningham, VJ, Bell, CJ, Liddle, PF, Jones, T and Nutt, DJ (1998) Decreased brain GABA(A)-benzodiazepine receptor binding in panic disorder preliminary results from a quantitative PET study. Arch. Gen. Psychiatry 55 715-720. 

Reddy, DS and Kulkarni, SK (1998) The role of GABA-A and mitochondrial diazepam-binding inhibitor receptors on the effects of neurosteroids on food intake in mice. Psychopharmacology 137 391-100. 

Consider propofol pharmacotherapy, as it agonizes GABA-A receptors and antagonizes NMDA receptors. Phenobarbital can be used as an alternative... 

Serretti, A., Lilli, R., Lorenzi, C. etal. (1999). Dopamine receptor D2 and D4 genes, GABA(A) alpha-1 subunit genes and response to lithium prophylaxis in mood disorders. Psychiatry Res., 87, 7-19. 

Kaur, S., Panchal, M., Faisal, M. et al. (2004). Long term blocking of GABA-A receptor in locus coeruleus by bilateral microinfusion of picrotoxin reduced rapid eye movement sleep and increased brain Na-K ATPase activity in freely moving normally behaving rats. Behav. Brain Res. 151, 185-90. 

Pollock, M. S. Mistlberger, R. E. (2003). Rapid eye movement sleep induction by microinjection of the GABA-A antagonist bicuculline into the dorsal subcoeruleus area of the rat. Brain Res. 962, 68-77. 

Baumann, S. W., Baur, R. 8r Sigel, E. (2003). Individual properties of the two functional agonist sites in GABA(A) receptors./. Neurosci. 23, 11158-66. 

Monti, J. M., Jantos, H. Monti, D. (2001). Increase of waking and reduction of NREM and REM sleep after nitric oxide synthase inhibition prevention with GABA(A) or adenosine A(l) receptor agonists. Behav. Brain Res. 123 (1), 23-35. 

GABA, and molecules that act at GABA-A receptors, have been classically recognized as hypnotics (i.e. benzodiazepines) and anesthetics (i.e. barbiturates). Benzodiazepine (BZD) receptors, a modulatory site on the GABA-A receptor, were... 

Johnston G. A. (2005). GABA(A) receptor channel pharmacology. Curr. Pharm. Des. 11, 1867-85. 

Molher H., Malherbe P., Draguhn A. et al. (1990). GABA-A-receptor subunits ... 

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