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GABAb modulators

GABA is the most prominent inhibitory neurotransmitter in the mammalian nervous system and acts via GABA receptors. Activation of GABAb receptors by GABA released from local spinal interneurons (Fig. 1) negatively modulates nociceptive transmission in the spinal cord. Agonists at GABAb receptors... [Pg.931]

In the spinal cord GABA can also activate the G-protein-linked GABAb receptor, also found pre- and postsynaptically. Baclofen modulation of nociceptive transmission is seen under inflammatory conditions in animals but in humans the drug appears to lack any analgesic effect. [Pg.466]

Fig. 1. Chemical structures of ligands used to characterize, clone, and purify the GABAb receptor. The recently identified positive allosteric modulators CGP7930 and CGP 13501 are expected to broaden the spectrum of therapeutic applications for GABAb drugs. Fig. 1. Chemical structures of ligands used to characterize, clone, and purify the GABAb receptor. The recently identified positive allosteric modulators CGP7930 and CGP 13501 are expected to broaden the spectrum of therapeutic applications for GABAb drugs.
Hill, D. R. (1985) GABAb receptor modulation of adenylate cyclase activity in rat brain... [Pg.140]

Jarolimek W, Misgeld U (1997) GABAB receptor-mediated inhibition of tetrodotoxin-resistant GABA release in rodent hippocampal CA1 pyramidal cells. J Neurosci 17 1025-32 Jeong SW, Ikeda SR (2000a) Effect of G protein heterotrimer composition on coupling of neurotransmitter receptors to N-type Ca(2+) channel modulation in sympathetic neurons. Proc Natl Acad Sci USA 97 907-12... [Pg.251]

Krueger BK, Font J, Greengard P (1977) Depolarization-induced phosphorylation of specific proteins, mediated by calcium ion influx, in rat brain synaptosomes. J Biol Chem 252 2764-73 Kubista H, Boehm S (2006) Molecular mechanisms underlying the modulation of exocytotic noradrenaline release via presynaptic receptors. Pharmacol Ther 112 213 12 Kulik A, Vida I, Fukazawa Y et al (2006) Compartment-dependent colocalization of Kir3.2-containing K+ channels and GABAB receptors in hippocampal pyramidal cells. J Neurosci 26 4289-97... [Pg.252]

Bischoff S, Leonhard S, Reymann N et al (1999) Spatial distribution of GABAb R1 receptor mRNA and binding sites in the rat brain. J Comp Neurol 412 1-16 Blein S, Ginham R, Uhrin D et al (2004) Structural analysis of the complement control protein (CCP) modules of GABAb receptor la. J Biol Chem 279 48292-306 Bockaert J, Pin J-P (1999) Molecular tinkering of G-protein-coupled receptors an evolutionary success. EMBO J 18 1723-9... [Pg.401]

Bonanno G, Raiteri M, Emson PC (1988) In vitro release of somatostatin from cerebral cortical slices Characterization of electrically-evoked release. Brain Res 447 92-7 Bonanno G, Gemignani A, Schmid G et al (1996) Human brain somatostatin release from isolated cortical nerve endings and its modulation through GABAb receptors. Br J Pharmacol 118 ... [Pg.401]

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GABAb

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