Ro 16-6028: A Novel Anxiolytic Acting as a Partial Agonist at the Benzodiazepine Receptor

Martin, James R.; Pieri, L.; Bonetti, E. P.; Schaffner, R.; Burkard, W. P.; Cumin, R.; Haefely, W.

doi:10.1055/s-2007-1021947

Cited by 87 publications

(20 citation statements)

References 5 publications

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“…This degree of selectivity is also observed in the rat where respective ID 50 values for cerebellum and spinal cord were 6 and 19 mg/kg for CL 218,872 and 7 and Ͼ100 mg/kg for zolpidem (Benavides et al 1992), although direct comparisons between effective doses in mice and rats is complicated by the possible species differences in pharmacokinetics (e.g., bretazenil, Martin et al 1988).…”

Section: Discussionmentioning

confidence: 89%

Regional Differences in the Inhibition of Mouse In Vivo [3H]Ro 15-1788 Binding Reflect Selectivity for α1 versus α2 and α3 Subunit-Containing GABAA Receptors

Atack

Smith

Emms

et al. 1999

Neuropsychopharmacology

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Section: Discussionmentioning

confidence: 89%

Regional Differences in the Inhibition of Mouse In Vivo [3H]Ro 15-1788 Binding Reflect Selectivity for α1 versus α2 and α3 Subunit-Containing GABAA Receptors

Atack

Smith

Emms

et al. 1999

Neuropsychopharmacology

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“…Repeated administration of bretazenil resulted in low levels of PTZ-lever responding at all time points. Given that bretazenil is anxiolytic, but shows little or no sedation, cognitive impairment, or muscle relaxant properties, a low addiction liability, and less tolerance to its effects Haigh and Feely, 1988;Martin et al, 1988;Moreau et al, 1990], it may be a better alternative to diazepam and chlordiazepoxide for the treatment of EW.…”

Section: Major Sites Of Ethanol Action Gaba a Receptorsmentioning

confidence: 98%

Animal models of the anxiogenic effects of ethanol withdrawal

Gatch¹,

Lal²

2001

Drug Development Research

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Although anxiety is a major feature of ethanol withdrawal (EW) and much of treatment related to EW is focused on amelioration of the anxiety experienced during EW, less attention has been given to the anxiogenic effects of EW than to the convulsant effects. In this article, we review the animal literature on the anxiogenic effects of EW. Both GABA A and serotonin (5-HT) receptors are important targets in the treatment of anxiety. The roles of each of these two receptors on the anxiogenic effects of EW as well as their potential interrelation are discussed. The contribution of other receptor systems to the modulation of these effects is reviewed. Additionally, males and females show very different levels of anxiety during EW and studies on the role of the HPA axis in mediating these effects are examined. Finally, potential directions for better treatments for EW are discussed. Drug Dev. Res. 54:95-115, 2001.

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“…the hypnoselective agent zolpidem, which recognizes preferentially the a 1 -containing GABA A receptor) (Depoortere et al, 1986) and/or show different efficacies at GABA A receptors (e.g. bretazenil, imidazenil, SL651498) (Giusti et al, 1993;Griebel et al, 2001b;Martin et al, 1988). The heterogeneity of GABA A receptors has prompted speculation that a particular behavioral response might be associated with an action at a defined receptor subtype.…”

Section: Gaba a -Benzodiazepine Receptor Ligandsmentioning

confidence: 99%

The Mouse Defense Test Battery: pharmacological and behavioral assays for anxiety and panic

Blanchard

Griebel

Blanchard

2003

European Journal of Pharmacology

256

159

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The Mouse Defense Test Battery was developed from tests of defensive behaviors in rats, reflecting earlier studies of both acute and chronic responses of laboratory and wild rodents to threatening stimuli and situations. It measures flight, freezing, defensive threat and attack, and risk assessment in response to an unconditioned predator stimulus, as well as pretest activity and postthreat (conditioned) defensiveness to the test context. Factor analyses of these indicate four factors relating to cognitive and emotional aspects of defense, flight, and defensiveness to the test context. In the Mouse Defense Test Battery, GABA A -benzodiazepine anxiolytics produce consistent reductions in defensive threat/attack and risk assessment, while panicolytic and panicogenic drugs selectively reduce and enhance, respectively, flight. Effects of GABA A -benzodiazepine, serotonin, and neuropeptide ligands in the Mouse Defense Test Battery are reviewed. This review suggests that the Mouse Defense Test Battery is a sensitive and appropriate tool for preclinical evaluation of drugs potentially effective against defense-related disorders such as anxiety and panic. D

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Ro 16-6028: A Novel Anxiolytic Acting as a Partial Agonist at the Benzodiazepine Receptor

Cited by 87 publications

References 5 publications

Regional Differences in the Inhibition of Mouse In Vivo [3H]Ro 15-1788 Binding Reflect Selectivity for α1 versus α2 and α3 Subunit-Containing GABAA Receptors

Regional Differences in the Inhibition of Mouse In Vivo [3H]Ro 15-1788 Binding Reflect Selectivity for α1 versus α2 and α3 Subunit-Containing GABAA Receptors

Animal models of the anxiogenic effects of ethanol withdrawal

The Mouse Defense Test Battery: pharmacological and behavioral assays for anxiety and panic

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