International Union of Pharmacology. LXX. Subtypes of γ-Aminobutyric AcidA Receptors: Classification on the Basis of Subunit Composition, Pharmacology, and Function. Update

@article{Olsen2008InternationalUO,
  title={International Union of Pharmacology. LXX. Subtypes of $\gamma$-Aminobutyric AcidA Receptors: Classification on the Basis of Subunit Composition, Pharmacology, and Function. Update},
  author={Richard W. Olsen and Werner Sieghart},
  journal={Pharmacological Reviews},
  year={2008},
  volume={60},
  pages={243 - 260}
}
In this review we attempt to summarize experimental evidence on the existence of defined native GABAA receptor subtypes and to produce a list of receptors that actually seem to exist according to current knowledge. This will serve to update the most recent classification of GABAA receptors (Pharmacol Rev 50:291–313, 1998) approved by the Nomenclature Committee of the International Union of Pharmacology. GABAA receptors are chloride channels that mediate the major form of fast inhibitory… 

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References

SHOWING 1-10 OF 375 REFERENCES
International union of pharmacology. XXIV. Current status of the nomenclature and properties of P2X receptors and their subunits.
TLDR
The structure, distribution, function, and ligand recognition characteristics of P2X receptors, which comprise seven distinct subunits that can function as both homo- and hetero- polymers, are described.
The diversity of GABAA receptors
TLDR
The pharmacology of putative receptor isoforms is summarized and the characteristics of functional channels are emphasized to further the understanding of GABA-related disorders and of the complex interaction of excitatory and inhibitory mechanisms in neuronal processing.
The diversity of GABAA receptors. Pharmacological and electrophysiological properties of GABAA channel subtypes.
TLDR
The pharmacology of putative receptor isoforms is summarized and the characteristics of functional channels are emphasized to further the understanding of GABA-related disorders and of the complex interaction of excitatory and inhibitory mechanisms in neuronal processing.
Importance of a novel GABAA receptor subunit for benzodiazepine pharmacology
TLDR
The isolation of a cloned cDNA encoding a new GABAA receptor subunit, termed γ2, which shares approximately 40% sequence identity with α-and β-subunits and whose messenger RNA is prominently localized in neuronal subpopulations throughout the CNS.
Drug interactions at GABAA receptors
International Union of Pharmacology. XXXIII. Mammalian γ-Aminobutyric AcidB Receptors: Structure and Function
TLDR
The emergence of high-affinity antagonists for GABAB receptors has enabled a synaptic role to be established, however, the antagonists have generally failed to establish the existence of pharmacologically distinct receptor types within the GABAB receptor class.
International Union of Basic and Clinical Pharmacology. LXVII. Recommendations for the Recognition and Nomenclature of G Protein-Coupled Receptor Heteromultimers
TLDR
The present article illustrates well-documented examples of such native multimeric GPCR complexes, lists a number of recommendations for recognition and acceptance of suchMultimeric receptors, and gives recommendations for their nomenclature.
International Union of Pharmacology. XV. Subtypes of gamma-aminobutyric acidA receptors: classification on the basis of subunit structure and receptor function.
TLDR
This article does not aim to review in detail the properties of γ-aminobutyric acidA(GABAA)breceptors, but in this same journal, a review of the binding properties and pharmacology of these receptors has been published.
Subunit composition, distribution and function of GABA(A) receptor subtypes.
TLDR
Together, these results should cause a revival of GABA(A) receptor research and strongly stimulate the development of drugs with a higher selectivity for alpha2-, alpha3-, or alpha5-subunit-containing receptor subtypes.
GABA(A) receptor channel pharmacology.
TLDR
The emphasis of this review is on the rich chemical diversity of ligands that influence GABA(A) receptor function, which provides many avenues for the design and development of new chemical entities acting on GABA (A) receptors.
...
...