L-655,708 is a potent and selective inverse agonist for the benzodiazepine site of GABAA R alpha5 (μ5-containing GABAA receptors). Displays high selectivity over GABAA receptors containing α1, α2, α3 or α6 subunits in combination with β3 and γ2.
1. Quirk, K. et al. 1996. Neuropharmacology. 35(9-10): 1331-1335. PMID: 9014149 2. Sur, C. et al. 1998. Mol. Pharmacol. 54(5): 928-933. PMID: 9804628 3. Atack, J.R. et al. 2006. Neuropharmacology. 51(6): 1023-1029. PMID: 17046030
Soluble in DMSO (5 mM), and 1eq. HCl (10 mM). Insoluble in water.
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What concentration should be used for in vivo rat studies?
Asked by: SCM4
This chemical, L-655,708 (CAS 130477-52-0), L-655,708 was prepared at a concentration of 5 mM in 75% saline/25% DMSO. The dose used in this study (0.7 mg/kg i.p.) was taken from the study of Martin et al (2009), in which L-655,708 was shown to reverse the amnestic properties of the anesthetic etomidate; a positive sign of its efficacy in the brain. This dose is sufficient to occupy ~70% of forebrain binding sites (Atack et al, 2005).
From PMID: 25900119 Fischell, et. al. 2015. Rapid Antidepressant Action and Restoration of Excitatory Synaptic Strength After Chronic Stress by Negative Modulators of Alpha5-Containing GABAA Receptors.
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