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.
FR194921 (32 mg/kg; p.o.) shows good oral bioavailability with AUC of 6.91 µg·h/mL, Cmax of 2.13 µg/mL and Tmax OF 0.63 h, BA of 60.6% in rats[1].FR194921 (0.032, 0.1, 0.32 mg/kg; p.o.) dose-dependently attenuates the polocomotion induced by CPA [2].FR194921 (0.1-10 mg/kg; i.p.) significantly ameliorates scopolamine -induced memory deficits[2].
References:
[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.