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GABAA (α1β2γ2) Receptor Current using Patch-Clamp Technique from US Patent US20240132445: "PHENOL DERIVATIVE AND APPLICATION THEREOF IN MEDICAMENTS"
Assay data:1 Active, 2 Tested
SummaryCompounds, ActiveRelated BioAssays by Target
Oral bioavailability in Beagle dog at 10 mg/kg by LC-MS/MS analysis
Assay data:2 Tested
SummaryPubMed Citation
AUC (0 to t) in Beagle dog at 10 mg/kg, po by LC-MS/MS analysis
AUC (0 to t) in Beagle dog at 2 mg/kg, iv administered as single bolus dose by LC-MS/MS analysis
Cmax in Beagle dog at 10 mg/kg, po by LC-MS/MS analysis
Assay data:2 Active, 1 Activity ≤ 1 µM, 2 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed Citation
Cmax in Beagle dog at 2 mg/kg, iv administered as single bolus dose by LC-MS/MS analysis
Assay data:2 Active, 2 Tested
SummaryCompounds, ActivePubMed Citation
Half life in Beagle dog at 10 mg/kg, po by LC-MS/MS analysis
Half life in Beagle dog at 2 mg/kg, iv administered as single bolus dose by LC-MS/MS analysis
Anesthetic activity in iv dosed ICR mouse assessed as dose required to produce 10 min of anesthesia administered 7 to 8 doses at 10 secs for each dose
Assay data:20 Tested
Toxicity in iv dosed ICR mouse administered 7 to 8 doses at 10 secs for each dose
Assay data:28 Tested
Anesthetic activity in iv dosed ICR mouse assessed as loss of righting reflex administered 7 to 8 doses at 10 secs for each dose
Anesthetic activity in iv dosed ICR mouse assessed as recovery time of righting reflex by measuring the ability to grip and climb a steel frame and ambulated normally administered 7 to 8 doses at 10 secs for each dose
Anesthetic activity in iv dosed ICR mouse assessed as anesthetic duration time administered 7 to 8 doses at 10 secs for each dose
Anesthetic activity in iv dosed ICR mouse assessed as onset time for loss of righting reflex administered 7 to 8 doses at 10 secs for each dose
Cmax in Sprague-Dawley rat at 1 mg/kg, iv by LC-MS/MS analysis
Assay data:4 Tested
Clearance in Sprague-Dawley rat at 1 mg/kg, iv by LC-MS/MS analysis
Volume of distribution at steady state in Sprague-Dawley rat at 1 mg/kg, iv by LC-MS/MS analysis
Half life in Sprague-Dawley rat at 1 mg/kg, iv by LC-MS/MS analysis
AUC (0 to t) in Sprague-Dawley rat at 1 mg/kg, iv by LC-MS/MS analysis
Displacement of [35S]TBPS from GABAA receptor in Wistar rat cerebral cortex membranes at 1 uM after 3 hrs by scintillation counting method
Assay data:13 Tested
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