L-655,708A potent and selective inverse agonist for the benzodiazepine

L-655,708 (CAS 130477-52-0)

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Synonym: Ethyl (S)-11,12,13,13a-Tetrahydro-7-methoxy-9-oxo-9H-imidazo[1,5-a]pyrrolo[2,1-c][1,4]benzodiazepine-1-carboxylate; L-655708
Application: A potent and selective inverse agonist for the benzodiazepine
CAS Number: 130477-52-0
Purity: ≥98%
Molecular Weight: 341.37
Molecular Formula: C18H19N3O4
* Refer to Certificate of Analysis for lot specific data (including water content).
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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

Physical State :
Solubility :
Soluble in DMSO (5 mM), and 1eq. HCl (10 mM). Insoluble in water.
Storage :
Desiccate at 4° C
Melting Point :
193-195° C
Boiling Point :
~584.4° C at 760 mmHg (Predicted)
Density :
~1.4 g/cm3 (Predicted)
Refractive Index :
n20D 1.68 (Predicted)
Ki Data :
GABA receptor beta-3 subunit: Ki= 0.4 nM (human); GABA receptor gamma-2 subunit: Ki= 0.4 nM (human); GABA receptor alpha-5 subunit: Ki= 0.4 nM (human)
pK Values :
pKb: 1.50
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
PubChem CID :
MDL Number :

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Certificate of Analysis

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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.
Answered by: Chemical Support 1
Date published: 2017-03-24
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