FR194921

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].

Research Areas >> Neurological Disease

Signaling Pathways >> GPCR/G Protein >> Adenosine Receptor

A1R:6.6 nM (Ki)

A2AR:5400 nM (Ki)

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: SD rats[2] Dosage: 0.032, 0.1, 0.32 mg/kg Administration: P.o.; administered orally 25 min prior to intraperitoneal administration of CPA (0.056 mg/kg; i.p.) Result: Dose-dependently attenuated the hypolocomotion induced by CPA with an ED50 value of 0.08 mg/kg and statistical significance at 0.32 mg/kg. Animal Model: SD rats[2] Dosage: 0.1, 0.32, 1, 3.2, 10 mg/kg Administration: I.p.; Scopolamine (HY-N0296)(1 mg/kg, i.p.) Result: Significant cognitive enhanced following scopolamine-induced memory deficits in rats.

[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.