2. GPCR/G Protein
  3. Adenosine Receptor
  4. 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.

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FR194921 Chemical Structure

FR194921 Chemical Structure

CAS No. : 202646-80-8

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Description

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].

IC50 & Target[1]

A1R

6.6 nM (Ki)

A2AR

5400 nM (Ki)

In Vivo

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 hypolocomotion induced by CPA (HY-103181)[2].
FR194921 (0.1-10 mg/kg; i.p.) significantly ameliorates scopolamine (HY-N0296)-induced memory deficits[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Molecular Weight

385.46

Formula

C23H23N5O
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C1C=CC(C2=C3C=CC=CN3N=C2C4=CC=CC=C4)=NN1C5CCN(CC5)C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility

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In Vivo:

The following protocol is derived from the literature and is for reference only. It is recommended to first try a small sample.

  • Protocol 1

    FR194921 is suspended in 0.5% methylcellulose[2].

In Vivo Dissolution Calculator
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Purity & Documentation

Purity: 98.10%

COA (256 KB)

Handling Instructions (2659 KB)
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FR194921 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

FR194921202646-80-8FR 194921FR-194921Adenosine ReceptorP1 receptororally activecross the blood-brain barrierhypolocomotionmemory deficitsInhibitorinhibitorinhibit

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