| Bioactivity | FR194921 is a potent, selective and orally active and cross the blood-brain barrier Adenosine A1 antagonist with Ki value of 6.6, 5400 nM for A1, A2A, respectively. FR194921 shows cognitive-enhancing and anxiolytic activity[1][2]. |
| In Vivo | FR194921 (32 mg/kg; p.o.) 在大鼠中具有良好的口服生物利用度，AUC 为 6.91 µg·h/mL，Cmax 为 2.13 µg/mL，Tmax 为 0.63 h，BA 为 60.6%[1].FR194921 (0.032、0.1、0.32 mg/kg；口服) 剂量依赖性地减弱 CPA (HY-103181) 诱导的低运动[2]。FR194921 (0.1-10 mg/kg；腹腔注射) 显着改善东莨菪碱 (HY-N0296) 诱导的记忆缺陷[2]。 Animal Model: |
| Name | FR194921 |
| CAS | 202646-80-8 |
| Formula | C23H23N5O |
| Molar Mass | 385.46 |
| 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]. Kuroda S, et al. Design, synthesis and biological evaluation of a novel series of potent, orally active adenosine A1 receptor antagonists with high blood-brain barrier permeability. Chem Pharm Bull (Tokyo). 2001 Aug;49(8):988-98. [2]. Maemoto T, et al. Pharmacological characterization of FR194921, a new potent, selective, and orally active antagonist for central adenosine A1 receptors. J Pharmacol Sci. 2004 Sep;96(1):42-52. |