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GABAB Receptor Antagonists
GABAB receptors (GABABR) are G-protein coupled receptors for gamma-aminobutyric acid (GABA), therefore making them metabotropic receptors, that are linked via G-proteins to potassium channels. The changing potassium concentrations hyperpolarize the cell at the end of an action potential. The reversal potential of the GABAB-mediated IPSP (inhibitory postsynaptic potential) is –100 mV, which is much more hyperpolarized than the GABAA IPSP. GABAB receptors are found in the central nervous system and the autonomic division of the peripheral nervous system. The receptors were first named in 1981 when their distribution in the CNS was determined, which was determined by Norman Bowery and his team using radioactively labelled baclofen. Functions GABABRs stimulate the opening of K+ channels, specifically GIRKs, which brings the neuron closer to the equilibrium potential of K+. This reduces the frequency of action potentials which reduces neurotransmitter release. Thus GABAB r ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
GABBR1
Gamma-aminobutyric acid B receptor, 1 (GABAB1), is a G-protein coupled receptor subunit encoded by the ''GABBR1'' gene. Function GABAB1 is a receptor for Gamma-aminobutyric acid. Upon binding, GABAB1 will produce a slow and prolonged inhibitory effect. GABAB1 is one part of a heterodimer, which is the GABAB receptor, consisting of it and the related GABAB2 protein. The GABA(B) receptor 1 gene is mapped to chromosome 6p21.3 within the HLA class I region close to the HLA-F gene. Susceptibility loci for multiple sclerosis, epilepsy, and schizophrenia have also been mapped in this region. Alternative splicing of this gene generates 4 transcript variants. Interactions GABBR1 has been shown to interact with ATF4 and GABBR2 Gamma-aminobutyric acid (GABA) B receptor, 2 (GABAB2) is a G-protein coupled receptor subunit encoded by the GABBR2 gene in humans. Function B-type receptors for the neurotransmitter GABA (gamma-aminobutyric acid) inhibit neuronal activity thr .... See ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
