Pharmacological Properties of GABAA Receptors Containing γ1 Subunits

2005 ◽  
Vol 69 (2) ◽  
pp. 640-649 ◽  
Author(s):  
S. Khom ◽  
I. Baburin ◽  
E. N. Timin ◽  
A. Hohaus ◽  
W. Sieghart ◽  
...  
Keyword(s):  
Gabaa Receptors ◽  
Pharmacological Properties

GABAA receptors: Various stoichiometrics of subunit arrangement in α1β3 and α1β3ε receptors

2018 ◽  
Vol 24 (17) ◽  
pp. 1839-1844 ◽  
Author(s):  
Ahmad Tarmizi Che Has ◽  
Mary Chebib
Keyword(s):  
Central Nervous System ◽  
Gabaa Receptors ◽  
Binding Sites ◽  
New Drugs ◽  
Pharmacological Properties ◽  
Receptor Complex ◽  
The Third ◽  
Γ Subunit ◽  
Subunit Stoichiometry ◽  
The Central Nervous System

GABAA receptors are members of the Cys-loop family of ligand-gated ion channels which mediate most inhibitory neurotransmission in the central nervous system. These receptors are pentameric assemblies of individual subunits, including α1-6, β1-3, γ1-3, δ, ε, π, θ and ρ1-3. The majority of receptors are comprised of α, β and γ or δ subunits. Depending on the subunit composition, the receptors are located in either the synapses or extrasynaptic regions. The most abundant receptors are α1βγ2 receptors, which are activated and modulated by a variety of pharmacologically and clinically unrelated agents such as benzodiazepines, barbiturates, anaesthetics and neurosteroids, all of which bind at distinct binding sites located within the receptor complex. However, compared to αβγ, the binary αβ receptors lack a benzodiazepine α-γ2 interface. In pentameric αβ receptors, the third subunit is replaced with either an α1 or a β3 subunit leading to two distinct receptors that differ in subunit stoichiometry, 2α:3β or 3α:2β. The consequence of this is that 3α:2β receptors contain an α-α interface whereas 2α:3β receptors contain a β-β interface. Apart from the replacement of γ by α1 or β3 in binary receptors, the incorporation of ε subunit into GABAA receptors might be more complicated. As the ε subunit is not only capable of substituting the γ subunit, but also replacing the α/β subunits, receptors with altered stoichiometry and different pharmacological properties are produced. The different subunit arrangement of the receptors potentially constructs novel binding sites which may become new targets of the current or new drugs.

Pharmacological properties of fetal rat hippocampal GABAA receptors

1995 ◽  
Vol 85 (2) ◽  
pp. 280-282 ◽  
Author(s):  
Alexander Y. Valeyev ◽  
Veronica S. Dunlap ◽  
Jeffery L. Barker
Keyword(s):  
Gabaa Receptors ◽  
Pharmacological Properties ◽  
Fetal Rat

The physiological properties and therapeutic potential of α5-GABAA receptors

2009 ◽  
Vol 37 (6) ◽  
pp. 1334-1337 ◽  
Author(s):  
Loren J. Martin ◽  
Robert P. Bonin ◽  
Beverley A. Orser
Keyword(s):  
Science Fiction ◽  
Gabaa Receptors ◽  
Therapeutic Potential ◽  
Memory Performance ◽  
Aminobutyric Acid ◽  
Pharmacological Properties ◽  
Physiological Properties ◽  
Drug Treatments ◽  
Subtype A ◽  
Memory Enhancing

The notion that drug treatments can improve memory performance has moved from the realm of science fiction to that of serious investigation. A popular working hypothesis is that cognition can be improved by altering the balance between excitatory and inhibitory neurotransmission. This review focuses on the unique physiological and pharmacological properties of GABAARs [GABA (γ-aminobutyric acid) subtype A receptors] that contain the α5 subunit (α5-GABAAR), as these receptors serve as candidate targets for memory-enhancing drugs.

scholarly journals Maturation and Pharmacological Properties of Postsynaptic GABAA Receptors

2008 ◽  
Vol 22 (S1) ◽  
Author(s):  
Haiying Wang ◽  
William H. Griffith ◽  
Angelika N. McDermott ◽  
David Murchison ◽  
Gerald D. Frye
Keyword(s):  
Gabaa Receptors ◽  
Pharmacological Properties

scholarly journals GABAA Receptors Expressed in Oligodendrocytes Cultured From the Neonatal Rat Contain α3 and γ1 Subunits and Present Differential Functional and Pharmacological Properties.

2020 ◽  
pp. MOLPHARM-AR-2020-000091
Author(s):  
Rainald Pablo Ordaz ◽  
Edith Garay ◽  
Agenor Limon ◽  
Alberto Pérez-Samartín ◽  
María Victoria Sánchez-Gómez ◽  
...  
Keyword(s):  
Gabaa Receptors ◽  
Neonatal Rat ◽  
Pharmacological Properties

Pharmacologically potentials of different substituted coumarin derivatives

2019 ◽  
Author(s):  
Chem Int
Keyword(s):  
Benzene Ring ◽  
Bioactive Compounds ◽  
Biological Activities ◽  
Pharmacological Properties ◽  
Coumarin Derivatives ◽  
Wide Range ◽  
Anti Oxidant ◽  
Anti Inflammatory ◽  
Coumarin Compounds

Coumarin and its derivatives are widely spread in nature. Coumarin goes to agroup as benzopyrones, which consists of a benzene ring connected to a pyronemoiety. Coumarins displayed a broad range of pharmacologically useful profile.Coumarins are considered as a promising group of bioactive compounds thatexhibited a wide range of biological activities like anti-microbial, anti-viral,antiparasitic, anti-helmintic, analgesic, anti-inflammatory, anti-diabetic, anticancer,anti-oxidant, anti-proliferative, anti-convulsant, and antihypertensiveactivities etc. The coumarin compounds have immense interest due to theirdiverse pharmacological properties. In particular, these biological activities makecoumarin compounds more attractive and testing as novel therapeuticcompounds.

Sign in / Sign up

Export Citation Format

Share Document