GABA-B receptor

Kaupmann K, Malitschek B, Schuler V, et al. GABA(B)-receptor subtypes assemble into functional heteromeric complexes. Nature 1998 396(6712) 683—687. 

GABA(B) receptor antagonist on the sleep-waking cycle in the rat. Brain Res. 773, 8-14. 

Varga V., Sik A., Freund T. F Kocsis B. (2002). GABA(B) receptors in the median raphe nucleus distribution and role in the serotonergic control of hippocampal... 

Nakayasu, H., Nishikawa, M., Mizutani, H., Kimura, H., and Kuriyama, K. (1993) Immunoaffinity purification and characterization of gamma-aminobutyric acid (GABA)b receptor from bovine cerebral cortex../. Biol. Chem. 268, 8658-8664. 

Margeta-Mitrovic, M., Jan, Y. N., and Jan, L. Y. (2001) Ligand-induced signal transduction within heterodimeric GABA(B) receptor. Proc. Natl. Acad. Sci. USA 98,14643-14648. 

Eollowing chronic administration to rats, there is evidence that most antidepressants cause adaptive changes in S-HT a/ 5-HT2a alpha-1, alpha-2 and beta adrenoceptors, GABA-B receptors and possibly the NMDA-glutamate receptors. 

GABA-B receptors. There is evidence that GABA-B receptors play a role in enhancing noradrenaline release in the cortex and in this respect differ fundamentally from the inhibitory GABA-A receptors which facilitate central GABAergic transmission. A decrease in the activity of GABA-B receptors may therefore contribute to the reduced central noradrenergic tone reported to occur in depression. 

The mechanism of action of valproate is complex and still the subject of uncertainty. The drug appears to act by enhancing GABAergic function. Thus it increases GABA release, inhibits catabolism and increases the density of GABA-B receptors in the brain. There is also evidence that it increases the sensitivity of GABA receptors to the action of the inhibitory transmitter. Other actions that may contribute to its therapeutic effects include a decrease in dopamine turnover, a decrease in the activity of the NMDA-glutamate receptors and also a decrease in the concentration of... 

Baclofen is a GABA agonist at GABA B receptors and it has a presynaptic inhibitory function by reducing calcium influx. Its indication is increased extensor tone and clonus. Intrathecal administration may control severe spasticity pain. It is used for the treatment of spastic movement, especially in instances of spinal cord injury, spastic diplegia, multiple sclerosis and amyotrophic lateral sclerosis. Its central nervous system effects include drowsiness, somnolence and seizure activity in epileptic patients. 

Cruz HG et al Bi-directional effects of GABA(B) receptor agonists on the mesolimbic dopamine system. Nat Neurosci 2004 7 153. [PMID 14745451]... 

Kaupmann, K., Huggel, K., Heid, J., Flor, P.J., Bischoff, S., Mickel, S.J., McMaster, G., Angst, C., Bittiger, H., Froestl, W., Bettler, B. Expression cloning of GABA(B) receptors uncovers similarity to metabotropic glutamate receptors, Nature 1997, 386, 223-224. 

A second GABA receptor subtype, the GABA-B receptor (Fig. 8—12) is not allo-sterically modulated by benzodiazepines but binds selectively to the muscle relaxant baclofen. Its physiological role is not well known yet, but does not appear to be closely linked to anxiety disorders or to anxiolytics. 

Ciranna L, Licata F, Li Volsi G, Santangelo F. Role of GABA A and GABA B receptors in GABA-induced... 

Bettler B, Kaupmann K, Mosbacher J, Gassmann M. Molecular structure and physiological functions of GABA (B) receptors. Physiol Rev. 2004 84 835-867. 

Colombo G, Addolorato G, Agabio R, et al. Role of GABA(B) receptor in alcohol dependence reducing effect of baclofen on alcohol intake and alcohol motivational properties in rats and amelioration of alcohol withdrawal syndrome and alcohol craving in human alcoholics. Neurotox Res. 2004 6 403-414. 

Shimizu S, Honda M, Tanabe M, Ono H. GABA B receptors do not mediate the inhibitory actions of gabapentin on the spinal reflex in rats. J Pharmacol Sci. 2004 96 444-449. 

Vacher CM, Bettler B. GABA(B) receptors as potential therapeutic targets. Curr Drug Targets CNS Neurol Disord. 2003 2 248-259. 

Hilakivi LA, Taira T, Hilakivi I, Loikas P. Neonatal treatment with monoamine uptake inhibitors alters later response in behavioural despair test to beta and GABA-B receptor agonists. Pharm Toxicol 1988 63 57-61. 

Junge HJ, Rhee JS, Jahn O et al (2004) Calmodulin and Muncl3 form a Ca2+ sensor/effector complex that controls short-term synaptic plasticity. Cell. 118 389 401 Kajikawa Y, Saitoh N, Takahashi T (2001) GTP-binding protein beta gamma subunits mediate presynaptic calcium current inhibition by GABA(B) receptor. Proc Natl Acad Sci USA... 

Moldavan MG, Irwin RP, Allen CN (2006) Presynaptic GABA(B) receptors regulate retinohy-pothalamic tract synaptic transmission by inhibiting voltage-gated Ca2+ channels. J Neurophysiol 95 3727 41... 

Bettler B, Kaupmann K, Bowery N (1998) GABA-B receptors drugs meet clones. Curr Opin Neurobiol 8 345-50... 

Calver AR, Davies CH, Pangalos M (2002) GABA(B) receptors from monogamy to promiscuity. Neurosignals 11 299-314... 

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