202646-80-8
202646-80-8 structure
- Name: FR194921
- Chemical Name: 2-(1-methylpiperidin-4-yl)-6-(2-phenylpyrazolo[1,5-a]pyridin-3-yl)pyridazin-3-one
- CAS Number: 202646-80-8
- Molecular Formula: C23H23N5O
- Molecular Weight: 385.46
- Create Date: 2018-06-11 11:00:27
- Modify Date: 2024-04-12 03:29:43
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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].
| Name | 2-(1-methylpiperidin-4-yl)-6-(2-phenylpyrazolo[1,5-a]pyridin-3-yl)pyridazin-3-one |
|---|---|
| Synonyms | unii-9765j8qb7q |
| 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]. |
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| Related Catalog | |
| Target |
A1R:6.6 nM (Ki) A2AR:5400 nM (Ki) |
| 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: 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. |
| References |
| Molecular Formula | C23H23N5O |
|---|---|
| Molecular Weight | 385.46 |
| Exact Mass | 385.19000 |
| PSA | 55.43000 |
| LogP | 3.42960 |