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GABAa Receptor Modulators

Innovation on formulations to improve pharmacokinetics (see Table 1) is a common strategy to address the generic introduction of zolpidem (2007 in the US). [Pg.65]

Zolpidem MR Sanofi-Aventis Launched-Phase IV studies [Pg.65]

Zolpidem Flash Dose (fast Biovail FDA approved [Pg.65]

Zolpidem BEMA film BioDelivery Sciences IND filling in 2007 [Pg.65]

Zolpidem intranasal Fabre-Kramer No data available [Pg.65]


Lancel M., Faulhaber J., Holsboer F., Ruppert R. (1996). Progesterone induces changes in sleep comparable to those of agonists GABAA receptor modulations. Am. J. Physiol. 34, E763-72. [Pg.455]

Currently the safety and efficacy of 20 is being evaluated in a Phase II study. The program is focused on the evaluation of the sleep induction and maintenance in insomnia patients but also will attempt to demonstrate orexin antagonists effects on improved sleep and side effect profiles compared to current GABAa receptor modulators. [Pg.72]

Steiger A, Trachsel AL, Guldner J, et al Neurosteroid pregenolone induces sleep EEG changes in man compatible with inverse agonistic GABAa receptor modulation. Brain Res 615 267-274, 1993... [Pg.751]

Visser, S.A. et al. Mechanism-based phar-macokinetic/pharmacodynamic modeling of the electroencephalogram effects of GABAA receptor modulators in vitro-in vivo correlations. J Pharmacol Exp Ther 2003, 304 88-101. [Pg.445]

In the last few years new anxiolytic agents have emerged which act by a variety of mechanisms, including GABAa receptor modulation [60], More recently, anxiolytics with non-benzodiazepine structures have been reported which are described below. [Pg.179]

Lippa A, Czobor P, Stark J, et al. Selective anxiclysis prcduced by ccinapicn, a GABAa receptor modulator. Proc Natl Acad Sci U S A 2005 102 7380-7385. [Pg.937]

Ramharter J, Mulzer J. Total synthesis of valerenic acid, a potent GABAA receptor modulator. Org. Lett. 2009 11 (5) 1151 1153. [Pg.908]

Figure 11.6 Schematic representation of the GABAa receptor complex. Examples of the many structurally diverse compounds that act at different sites on the receptor (see text for details). Picrotoxinin, the active component of picrotoxin, and TBPS act as non-competitive antagonists. The barbiturates, steroids and anaesthetics are positive allosteric modulators, as are the benzodiazepine site ligands shown, with the exception of DMCM (negative allosteric modulator) and flumazenil (benzodiazepine site antagonist)... Figure 11.6 Schematic representation of the GABAa receptor complex. Examples of the many structurally diverse compounds that act at different sites on the receptor (see text for details). Picrotoxinin, the active component of picrotoxin, and TBPS act as non-competitive antagonists. The barbiturates, steroids and anaesthetics are positive allosteric modulators, as are the benzodiazepine site ligands shown, with the exception of DMCM (negative allosteric modulator) and flumazenil (benzodiazepine site antagonist)...
Lancel, M. (1999). Role of GABAA receptors in the regulation of sleep initial sleep responses to peripherally administered modulators and agonists. Sleep 22,... [Pg.77]

Churn, S. B., Rana, A., Lee, K. el al. (2002). Calcium/calmodulin-dependent kinase II phosphorylation of the GABAa receptor alphal subunit modulates benzodiazepine binding. J. Neurochem. 82, 1065-76. [Pg.304]


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GABAa receptors

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