产品
编 号:F741328
分子式:C21H22FN3O3S2
分子量:447.55
产品类型
结构图
CAS No: 1971937-18-4
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产品详情
生物活性:
ARN19702 is a selective, orally active, reversible, and brain-penetrant N-acylethanolamine acid amidase (NAAA) inhibitor with an IC50 of 230 nM for human NAAA. ARN19702 has pain relief effects.
体内研究:
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 mice3 mg/kg,i.v3 mg/kg, p.o.
Cmax (ng/mL)1660±166613±68
Tmax (min)(5.0)30
CL (mL/min/Kg)33.2±1.649±8
t1/2 (min)73.9±3.7104±16
AUCplasma (h×ng/mL)1366.8±68.3988±157
AUCbrain (h×ng/mL)404.3±109.1181±28
F (%)-72±11
Animal Model:Sprague-Dawley rats (200-220 g) injected with Paclitaxel
Dosage:3 mg/kg and 10 mg/kg
Administration:Oral administration; daily; for 7 consecutive days (sub-chronic)
Result:Reduced nociception associated with Paclitaxel-induced neuropathy.