MK0343 readily penetrates the brain in rats and occupies the benzodiazepine site of GABAA receptors, measured using an in vivo [H]flumazenil binding assay, with an Occ50 of 2.2 mg/kg p.o. and a corresponding plasma EC50 of 115 ng/mL.
Animal Model: |
Male Sprague-Dawley rats (approximately 250–300g) (pharmacokinetics) |
Dosage: |
1, 2 or 3 mg/kg |
Administration: |
Oral administration |
Result: |
Readily penetrated the brain in rats and occupies the benzodiazepine site of GABAA receptors, with an Occ50 of 2.2 mg/kg p.o. and a corresponding plasma EC50 of 115 ng/mL. |