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FR194921

Cat. No. M8788

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FR194921 Structure

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Quality Control & Documentation
Biological Activity

FR194921 is a blood-brain barrier-permeable A1R adenosine receptor antagonist. The measured Ki values of FR194921 for the human adenosine A1 receptors have been in the low nM range with no binding affinity for A2A and A3 receptors up to 1μM. It is orally active and has good bioavailability. FR194921 was used in a recent study to restore auditory cortex plasticity. Paired with sound exposure, FR194921 resulted in cortical map plasticity and improved auditory perception in adult mice.

Chemical Information
Molecular Weight 385.46
Formula C23H23N5O
CAS Number 202646-80-8
Solubility (25°C) DMSO: 2 mg/mL (warmed)
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
References

[1] Jay A Blundon, et al. Restoring auditory cortex plasticity in adult mice by restricting thalamic adenosine signaling

[2] Takahiro Matsuya, et al. Synthesis and evaluation of [11C]FR194921 as a nonxanthine-type PET tracer for adenosine A1 receptors in the brain

[3] Takuya Maemoto, et al. Pharmacological characterization of FR194921, a new potent, selective, and orally active antagonist for central adenosine A1 receptors

[4] S Kuroda, 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

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Keywords: FR194921 supplier, Adenosine Receptor, inhibitors, activators

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