L-655,708
L-655,708 structure
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Common Name | L-655,708 | ||
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| CAS Number | 130477-52-0 | Molecular Weight | 341.36100 | |
| Density | 1.42g/cm3 | Boiling Point | 584.4ºC at 760mmHg | |
| Molecular Formula | C18H19N3O4 | Melting Point | N/A | |
| MSDS | Chinese USA | Flash Point | 307.2ºC | |
Use of L-655,708L-655708 is a potent α5 subunit-selective GABAA receptor inverse agonist (Ki = 0.45 nM).IC50: 0.45 nM (Ki)Target: GABAin vitro: L-655708 is a potent, selective inverse agonist for the benzodiazepine site of GABAA receptors containing the α5 subunit (Ki = 0.45 nM). Displays 50-100-fold selectivity over GABAA receptors containing α1, α2, α3 orα6 subunits in combination with β3 and γ2. Enhances LTP in a mouse hippocampal slice model and increases spatial learning, without displaying proconvulsant activity.in vivo: L-655708 at 0.7 mg/kg, administered intraperitoneally, would result in 60-70% occupancy of α5 GABAA receptors with limited binding to α1, α2, and α3 subunit-containing GABAA receptors and no significant off-target behavioral effects, such as sedation and motor impairment.[1] |
| Name | L-655,708,11,12,13,13a-Tetrahydro-7-methoxy-9-oxo-9H-imidazo[1,5-a]pyrrolo[2,1-c][1,4]benzodiazepine-1-carboxylicacid,ethylester |
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| Synonym | More Synonyms |
| Description | L-655708 is a potent α5 subunit-selective GABAA receptor inverse agonist (Ki = 0.45 nM).IC50: 0.45 nM (Ki)Target: GABAin vitro: L-655708 is a potent, selective inverse agonist for the benzodiazepine site of GABAA receptors containing the α5 subunit (Ki = 0.45 nM). Displays 50-100-fold selectivity over GABAA receptors containing α1, α2, α3 orα6 subunits in combination with β3 and γ2. Enhances LTP in a mouse hippocampal slice model and increases spatial learning, without displaying proconvulsant activity.in vivo: L-655708 at 0.7 mg/kg, administered intraperitoneally, would result in 60-70% occupancy of α5 GABAA receptors with limited binding to α1, α2, and α3 subunit-containing GABAA receptors and no significant off-target behavioral effects, such as sedation and motor impairment.[1] |
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| Related Catalog | |
| References |
| Density | 1.42g/cm3 |
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| Boiling Point | 584.4ºC at 760mmHg |
| Molecular Formula | C18H19N3O4 |
| Molecular Weight | 341.36100 |
| Flash Point | 307.2ºC |
| Exact Mass | 341.13800 |
| PSA | 73.66000 |
| LogP | 2.28620 |
| Vapour Pressure | 1.21E-13mmHg at 25°C |
| Index of Refraction | 1.675 |
| InChIKey | YKYOQIXTECBVBB-AWEZNQCLSA-N |
| SMILES | CCOC(=O)c1ncn2c1C1CCCN1C(=O)c1cc(OC)ccc1-2 |
| Storage condition | 2-8℃ |
| Personal Protective Equipment | Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter |
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| RIDADR | NONH for all modes of transport |
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Rat and human hippocampal alpha5 subunit-containing gamma-aminobutyric AcidA receptors have alpha5 beta3 gamma2 pharmacological characteristics.
Mol. Pharmacol. 54 , 928-933, (1998) The gamma-aminobutyric acid (GABA)A receptor is a hetero-oligomer consisting of five subunits, the combination of which confers unique pharmacological properties to the receptor. To understand the phy... |
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Autoradiographic localization of alpha5 subunit-containing GABAA receptors in rat brain.
Brain Res. 822 , 265-270 Multiple subtypes of GABAA receptors are expressed in the rat central nervous system (CNS). To determine the distribution and proportion of alpha5 subunit containing receptors, quantitative autoradiog... |
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Rapid Antidepressant Action and Restoration of Excitatory Synaptic Strength After Chronic Stress by Negative Modulators of Alpha5-Containing GABAA Receptors.
Neuropsychopharmacology 40 , 2499-509, (2015) Selective serotonin reuptake inhibitors (SSRIs) are the primary pharmacological treatment for depression, but SSRIs are effective in only half of the patients and typically take several weeks to relie... |
| l-655,708 |
| L-655708 |