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CAS No. : 1971937-18-4
MCE 国际站：ARN19702
产品活性：ARN19702 是一种选择性，具有口服活性的，可逆的，可透过血脑屏障的 N-乙酰乙醇胺酸酰胺酶 (NAAA) 抑制剂，对人 NAAA 的 IC50 为 230 nM。ARN19702 具有缓解疼痛的作用。
研究领域：Others
作用靶点：Others
In Vivo: ARN19702 (3-10 mg/kg; po; daily; for 7 consecutive days) reduces nociception associated with Paclitaxel-induced neuropathy without development of subacute antinociceptive tolerance in male rats.
In male mice, ARN19702 (0.1-30 mg/kg; po) attenuates in a dose-dependent manner the spontaneous nocifensive response elicited by intraplantar formalin injection and the hypersensitivity caused by intraplantar carrageenan injection, paw incision, or sciatic nerve ligation.
. ARN19702 (3-10 mg/kg; po) produces remarkable protective effects against multiple sclerosis in mice.
Pharmacokinetic properties of ARN19702 in mice
| 3 mg/kg,i.v | 3 mg/kg, p.o. |
| Cmax (ng/mL) | 1660±166 | 613±68 |
| Tmax (min) | (5.0) | 30 |
| CL (mL/min/Kg) | 33.2±1.6 | 49±8 |
| t1/2 (min) | 73.9±3.7 | 104±16 |
| AUCplasma (h×ng/mL) | 1366.8±68.3 | 988±157 |
| AUCbrain (h×ng/mL) | 404.3±109.1 | 181±28 |
| F (%) | - | 72±11 |
