GABAA receptor structures solved

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GABAA receptor pharmacology.

gamma-Aminobutyric acid (GABA)A receptors for the inhibitory neurotransmitter GABA are likely to be found on most, if not all, neurons in the brain and spinal cord. They appear to be the most complicated of the superfamily of ligand-gated ion channels in terms of the large number of receptor subtypes and also the variety of ligands that interact with specific sites on the receptors. There appea...

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We studied the effects of phosphorylation by protein kinase A (PKA) on GABAA receptors ( 1 1 2L and 1 3 2L) transiently expressed in HEK 293T cells. Under conditions favorable for PKA activation, currents obtained using whole-cell patch clamp of lifted cells displayed increased rate and extent of the fast phases of desensitization, decreased rate of current deactivation after GABA removal, and ...

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POSSIBLE INVOLVEMENT OF GABAA RECEPTOR SITES IN CATALEPSY

The present work was performed to show the possible interaction of GAB A, and GABAB receptors in catalepsy. The following results were obtained: 1- Muscimol (MUS), a GABAA agonist, induced catalepsy. This effect was dose-dependent. Baclofen (BAC), a GABAB agonist, had no effect in this respect. 2- Catalepsy induced by muscimol was potentiated by pretreatment of animals with bicuculline (BI...

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GABAA Receptor Subunits in Rat Testis and Sperm

Background γ-Aminobutyric acid (GABA) is considered to be the predominant inhibitory neurotransmitter in mammalian central nervous systems (CNS). There are two major classes of GABA receptors: GABAARs and GABABRs. The GABAA receptor is derived from various subunits such as alpha1-alpha 6, beta1-beta 3, gamma1-gamma 4, delta, epsilon, pi, and rho1-3. Intensive research has been performed to und...

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GABARAP and GABAA Receptor Clustering

Coyle et al. (2002), in this issue of Neuron, reveal the crystal structure for the GABA(A) receptor binding protein, GABARAP. They show GABARAP can switch from a monomer to an extended linear polymer form that may function to assemble microtubules during the intracellular trafficking or postsynaptic clustering of GABA(A) receptors.

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ژورنال

عنوان ژورنال: Nature Reviews Drug Discovery

سال: 2019

ISSN: 1474-1776,1474-1784

DOI: 10.1038/d41573-019-00002-1