Nefopam (Fenazoxine) 是一种具有口服活性的非阿片类和非甾体类中枢作用止痛剂。Nefopam 能阻断电压敏感性钠通道 (IC50=27 μM) 并调节啮齿动物的谷氨酸能传递。Nefopam 可用于研究抗神经性疼痛、抗惊厥以及预防术后寒战和打嗝。

Nefopam (Fenazoxine) is an orally active, non-opioid and non-steroidal centrally acting analgesic agent. Nefopam blocks voltage-sensitive sodium channels (IC 50 =27 μM) and modulates glutamatergic transmission in rodents. Nefopam can be used in studies of neuropathic pain, anticonvulsant, and prevention of postoperative shivering and hiccups [1] [2] [3].

Nefopam (0.1-100 μM; 15 min) inhibits 22 Na uptake in SK-N-SH cells in a concentration-dependent manner [1]. Cell Viability Assay [1] Cell Line: SK-N-SH cells Concentration: 0.1-100 μM Incubation Time: 15 min (preincubate) Result: Inhibited the uptake of 22 Na with an IC 50 value of 27 μM.

Nefopam (0-10 mg/kg; i.v.; single) protects mice from electroshock induced seizures [1]. Nefopam (10, 30, 60 mg/kg; i.p.; single) shows a dose-dependent attenuation of mechanical allodynia and decreased neurokinin-1 receptor concentration in vincristine-induced peripheral neuropathy model [2]. Animal Model: Adult male NMRI mice (25-30 g; 6 to7-week-old; electroshock-induced seizures model) [1] Dosage: 0-10 mg/kg Administration: Intravenous injection; single Result: Produced dose-dependent protection against maximal electroshock seizures in mice with an ED 50 of 3.8 (2.9-5.1) mg/kg. Animal Model: Adult male mice (10-week-old; 25-30 g; vincristine-induced peripheral neuropathy model) [2]. Dosage: 10, 30, 60 mg/kg Administration: Intraperitoneal injection; single Result: Significantly decreased the percentage of NK1 receptors in the spinal cord at dosage of 60 mg/kg. Showed a sustained increase in paw withdrawal threshold against mechanical stimuli.

13669-70-0

C17H19NO

253.345

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years