Structure of L-655708
CAS No.: 130477-52-0
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The BI-3802 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.
L-655708 is an effective, selective GABAA receptor inverse agonist with a Ki of 0.45 nM.
Synonyms: L-655708
4.5
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Batch number can be found on the product's label following the word 'Batch'.
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Batch number can be found on the product's label following the word 'Batch'.
Search for reports by entering the product batch number.
Batch number can be found on the product's label following the word 'Batch'.
Search for reports by entering the product batch number.
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CAS No. : | 130477-52-0 |
Formula : | C18H19N3O4 |
M.W : | 341.36 |
SMILES Code : | COC1=CC=C(C2=C1)N3C=NC(C(OCC)=O)=C3[C@@]4([H])N(CCC4)C2=O |
Synonyms : |
L-655708
|
MDL No. : | MFCD02684528 |
GHS Pictogram: |
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Signal Word: | Warning |
Hazard Statements: | H302-H315-H319 |
Precautionary Statements: | P501-P270-P264-P280-P302+P352-P337+P313-P305+P351+P338-P362+P364-P332+P313-P301+P312+P330 |
In Vivo:
Species
|
Animal Model
|
Administration | Dosage | Frequency | Description | References |
18-month-old C57BL/6J mice | Laparotomy-induced perioperative neurocognitive disorder model | Intraperitoneal injection | 0.5 mg/kg | Once daily for 3 consecutive days | To determine whether inhibition of α5GABA ARs prevents cognitive deficits. Results showed that L-655708 improved spatial reference learning and memory ability in mice subjected to anesthesia and surgery. | J Neuroinflammation. 2021 Sep 16;18(1):204 |
Sprague-Dawley rats | Forced Swim Test (FST) and Open Field Test | Intraperitoneal injection (i.p.) | 3 mg/kg | Single administration, tests conducted 24 hours or 7 days after administration | To investigate the antidepressant-like effects of L-655708 and its mechanisms. Results showed that L-655708 significantly reduced immobility time and increased swimming behavior in the forced swim test, with effects lasting up to 7 days post-administration. Additionally, L-655708 increased GluA1 levels in the medial prefrontal cortex (mPFC) and enhanced neuronal excitability by reducing inhibitory postsynaptic current (IPSC) half-width and increasing action potential frequency in ventral hippocampal CA1 neurons. | Neuropsychopharmacology. 2020 Dec;45(13):2289-2298 |
Mice | Repeated mild traumatic brain injury model | Subcutaneous administration | 200 μg/kg/day | Continued for 12 days | Prevention of neurovascular impairments induced by mTBI, including reduced neuronal reactivity and increased venular blood flow speed | Theranostics. 2021 Jun 16;11(16):7685-7699 |
Wistar rats | Isoflurane-induced memory impairment model | Subcutaneous injection | 0.7 mg/kg | Single dose, 30 minutes before anesthesia or 23.5 hours after anesthesia | To investigate the preventive and therapeutic effects of L-655708 on isoflurane-induced memory impairment in aged rats. Results showed that L-655708 administered before anesthesia could prevent memory impairment, but administration after anesthesia could not reverse the impairment. | Neural Regen Res. 2019 Jun;14(6):1029-1036 |
Female Wistar rats | Formalin-induced long-lasting secondary allodynia and hyperalgesia | Peripheral and intrathecal administration | 0.15–15 nmol | Single administration, effects assessed 1 hour post-injection | L-655708 prevented and reversed formalin-induced long-lasting secondary allodynia and hyperalgesia | Pain. 2016 Mar;157(3):613-626 |
Rats | Chronic Restraint Stress (CRS) and Chronic Unpredictable Stress (CUS) | Intraperitoneal injection | 0.7 mg/kg | Single injection, tested after 24 hours | L-655708 reversed the alterations in hedonic behavior in the sucrose preference and social interaction tests produced by two different chronic stress paradigms in rats within 24 h of systemic administration, restored the strength of excitatory synaptic transmission, and increased levels of the GluA1 subunit of the AMPA receptor. | Neuropsychopharmacology. 2015 Oct;40(11):2499-509 |
Rats | ET-1-induced focal ischemia model | Subcutaneous implantation | 1.5 mg/L | Every 24 hours for 2 weeks | To evaluate the effects of L-655708 on brain anatomy and forelimb skilled reaching, results showed a progressive decrease in total stroke volume (13±4 mm3 per week) and improvement in skilled reaching (9%±1% per week) | J Cereb Blood Flow Metab. 2015 Oct;35(10):1601-9 |
Female C57BL/6J mice | Laparotomy model | Intraperitoneal injection | 0.5 mg/kg | L655,708 reversed laparotomy-induced hippocampus-dependent memory deficits and long-term potentiation (LTP) impairment. | CNS Neurosci Ther. 2020 Sep;26(9):913-924 | |
Sprague-Dawley rats | Alcohol Deprivation Effect (ADE) model | Intraperitoneal injection | 0.3, 1, 3 and 5.6 mg/kg | Twice daily for three days | To evaluate the effect of L-655708 on the alcohol deprivation effect, results showed that L-655708 dose-dependently inhibited expression of the ADE. | Neuropharmacology. 2021 Nov 1;199:108785 |
Tags: L-655708 | L655708 | L 655708 | GABA Receptor | Gamma-aminobutyric acid Receptor | γ-Aminobutyric acid Receptor | inhibitor | 130477-52-0 |
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