| Bioactivity | MRK-623 (Compound 14k) is an orally active, high-affinity GABAA receptor agonist, with the Ki values of 0.85 nM, 3.7 nM, 4.0 nM, and 0.53 nM for α1, α2, α3, and α5, respectively. MRK-623 shows anxiolytic effect[1]. |
| Invitro | MRK-623 shows efficacy at human GABAA receptor subtypes expressed in L(tk-) cells measured by whole cell patch-clamp electrophysiology[1]. |
| In Vivo | MRK-623 (oral gavage; 0.3, 1, and 3 mg/kg; once) shows anxiolytic effects in the rat elevated plus maze assay[1]. Animal Model: |
| Name | MRK-623 |
| CAS | 461449-78-5 |
| Formula | C20H17FN4O |
| Molar Mass | 348.37 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Simon C Goodacre, et al. Imidazo[1,2-a]pyrimidines as functionally selective and orally bioavailable GABA(A)alpha2/alpha3 binding site agonists for the treatment of anxiety disorders. J Med Chem. 2006 Jan 12;49(1):35-8. |