Epigenetic Targets in GABAergic Neurons to Treat Schizophrenia

B. Ruzicka, M. V. Simonini, M. Veldic, and A. Guidotti III. Regulation of Histone Acetylation 98 IV. Chromatin Remodeling at Neuromuscular Junction 98 V. Chromatin Remodeling During Memory Formation 99 VI. Role of Reelin and Apolipoprotein E Receptors in Hippocampal Plasticity and Learning 101 VII. Is Reelin Expressed Only in a Selective Subpopulation of GABAergic Neurons 103 VIII. RELN and GAD67 CpG Island Promoter Hypermethylation and Reelin and GAD67...

Modulation of lonotropic GABA Receptors by Natural Products of Plant Origin

Hanrahan, Mary Chebib, Rujee K. Duke, and Kenneth N. Mewett III. Ionotropic GABA Receptors 287 VI. Other Phenolic Compounds 300 VII. Polyacetylenic Alcohols 303 VIII. Alcoholic Beverages Containing GABA Receptor Modulators 305 IX. GABA Receptor Modulators in Tea and Coffee 307 X. Plant Sources of GABA Receptor Modulating Substances Implications for Herbal Medicines 307

B GABAb Receptor Agents

The effects of GABAB receptor agonists and antagonists on nociception are similar to those reported for agents that act at the GABAA site. Direct-acting GABAb receptor agonists employed for these studies include baclofen and CGP 44532. Baclofen is particularly popular since it is the prototypical GABAB receptor agonist and is used clinically as a treatment for spasticity and as an adjuvant therapy for managing certain types of pain (Fromm, 1994 Lind et al., 2004 Loubser and Akman, 1996 Sindrup...

Info

FIGURE 2 Schematic representation of the GABAb receptor. Listed in the insert are the predominant GABAb receptor subunits. Adapted from cover figure of Biochemical Pharmacology 68(8), 2004 (with permission). antagonists, such as CGP 27492, interact with all GABAB sites, although allosteric modulators may able to discriminate among this receptor population (Binet et al., 2004 Urwyler et al., 2003). Nevertheless, the weight of evidence suggests that agents acting directly on the GABAB receptor...

References

N. (2001). Physiology of the GABA and glycine systems. In Pharmacology of GABA and Glycine Neurotransmission (H. Mohler, Ed.), pp. 3-76. Springer-Verlag, Berlin. Alves, N. D., de Castro-Costa, C. M., de Carvalho, A. M., Santos, F. J., and Silveira, D. G. (1999). Possible analgesic effect of vigabatrin in animal experimental chronic neuropathic pain. Arq. Neuropsiquiatr. 57, 916-920. Andree, T., Kendall, D. A., and Enna, S. J. (1983). THIP analgesia Cross...

Sensory Pathways and GABA

Gaba Pathway

The transmission and perception of pain are complex processes involving both the central and peripheral nervous systems. In general, pain impulses are generated, propagated, and sustained by the liberation of various autocoids, ions, and neurotransmitters at various points between the site of tissue damage, along the afferent sensory fibers, and within the spinal cord and brain. Some endogenous agents, including adenosine and a variety of neuro-peptides, are responsible for initiating,...

N H

FIGURE 1 Structures of the GABAA agonist partial agonist THIP, the GABAA partial agonist antagonist Thio-THIP, and the GABAc antagonist Aza-THIP. as an agonist by a distinct subpopulation of GABA receptors, which was named GABAb receptors (Bowery et al., 1980). Cloning of the GABAbR1 and GABABR2 receptors and the identification of functional heterodimeric GABAB receptors have greatly stimulated GABAB receptor research (Martin et al., 1999 Mohler and Fritschy, 1999). The classical BMC-sensitive...

A GABAa Receptor Agents

The most definitive data supporting a role for GABA in the transmission and perception of pain are derived from pharmacological studies. In general, both clinical and preclinical experiments indicate that agents known to enhance GABAergic transmission display antinociceptive activity (Bowery and Enna, 2000 Dirig and Yaksh, 1995 Hill et al., 1981 Johnston, 1992 Kaneko and Hammond, 1997 Kendall et al., 1982 Kjaer and Nielsen, 1983 Malan et al., 2002 Rode et al., 2005 Vaught et al., 1985 Zorn and...