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Distinct activities of GABA agonists at synaptic‐ and extrasynaptic‐type GABAA receptors
Compared whole‐cell and single channel currents induced by the agonists, a molecular explanation for their different activation profiles is provided and the ability to specifically increase the efficacy of receptor activation, by selected exogenous agonists over that obtained with the natural transmitter may prove to be of therapeutic benefit under circumstances when synaptic inhibition is compromised or dysfunctional.
Pharmacological Characterization of Agonists at δ-Containing GABAA Receptors: Functional Selectivity for Extrasynaptic Receptors Is Dependent on the Absence of γ2
These data clearly confirm that the presence of the δ subunit in heterotrimeric receptors is a strong determinant of the increased pharmacological activity of compounds with agonist activity and may explain why systemically active compounds such as gaboxadol and muscimol in vivo appear to act as selective extrasynaptic GABAA agonists.
Escitalopram versus citalopram: the surprising role of the R-enantiomer
- C. Sánchez, K. Bogeso, B. Ebert, E. Reines, C. Braestrup
- Psychology, MedicinePsychopharmacology
- 25 May 2004
The R- enantiomer present in citalopram counteracts the activity of the S-enantiomer, thereby providing a possible basis for the pharmacological and clinical differences observed between citalobram and escitaloprams.
Norketamine, the main metabolite of ketamine, is a non-competitive NMDA receptor antagonist in the rat cortex and spinal cord.
The δ Subunit of γ-Aminobutyric Acid Type A Receptors Does Not Confer Sensitivity to Low Concentrations of Ethanol
- C. Borghese, Signe í Stórustovu, R. Harris
- BiologyJournal of Pharmacology and Experimental…
- 1 March 2006
Ethanol at 30 mM did not affect tonic GABA-mediated currents in dentate gyrus reported to be mediated by GABAARs incorporating α4 and δ subunits, suggesting that as yet unidentified factors may play a critical role in the ethanol effects on δ-containing GABA ARs.
Molecular pharmacology of gamma-aminobutyric acid type A receptor agonists and partial agonists in oocytes injected with different alpha, beta, and gamma receptor subunit combinations.
- B. Ebert, K. Wafford, P. Whiting, P. Krogsgaard‐Larsen, J. Kemp
- BiologyMolecular pharmacology
- 1 November 1994
The results of the present study demonstrate that the pharmacology of GABAA agonists is dependent on the subunit composition of the GabAA receptor complex, indicating that two different alpha subunits can be coexpressed in one functional GAB AA receptor complex.
Pharmacological characterization of agonists at delta-containing GABAA receptors: Functional selectivity for extrasynaptic receptors is dependent on the absence of gamma2.
The very similar agonist pharmacology of alphabeta- and alphabetadelta-containing receptors shows that whereas the presence of a gamma subunit impairs the response to an agonist stimulation of the alphabeta receptor complex, the delta subunit does not affect this in any way.
Treating insomnia: Current and investigational pharmacological approaches.
Gaboxadol--a new awakening in sleep.
Emerging anti-insomnia drugs: tackling sleeplessness and the quality of wake time
Current understanding of how hypnotic drugs act is reviewed, and how new, more effective drugs and treatment strategies for insomnia might be achieved by taking into consideration the daytime consequences of disrupted sleep is discussed.