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编 号：F139479
分子式：C17H19NO
分子量：253.34
分子式：C17H19NO
分子量：253.34
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CAS No: 13669-70-0
产品详情
生物活性：
Nefopam (Fenazoxine) is an orally active, non-opioid and non-steroidal centrally acting analgesic agent. Nefopam blocks voltage-sensitive sodium channels (IC50=27 μM) and modulates glutamatergic transmission in rodents. Nefopam can be used in studies of neuropathic pain, anticonvulsant, as well as the prevention of postoperative shivering and hiccups.
体内研究：
Nefopam (0-10 mg/kg; i.v.; single) protects mice against electroshock induced seizures.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.Animal Model:Adult male NMRI mice (25-30 g; 6 to7-week-old; electroshock-induced seizures model)
Dosage:0-10 mg/kg
Administration:Intravenous injection; single
Result:Produced dose-dependent protection against maximal electroshock seizures in mice with an ED50 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).
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.
体外研究：
Nefopam (0.1-100 μM; 15 min) inhibits the uptake of 22Na in a concentration-dependent manner in SK-N-SH cells.
Nefopam (Fenazoxine) is an orally active, non-opioid and non-steroidal centrally acting analgesic agent. Nefopam blocks voltage-sensitive sodium channels (IC50=27 μM) and modulates glutamatergic transmission in rodents. Nefopam can be used in studies of neuropathic pain, anticonvulsant, as well as the prevention of postoperative shivering and hiccups.
体内研究：
Nefopam (0-10 mg/kg; i.v.; single) protects mice against electroshock induced seizures.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.Animal Model:Adult male NMRI mice (25-30 g; 6 to7-week-old; electroshock-induced seizures model)
Dosage:0-10 mg/kg
Administration:Intravenous injection; single
Result:Produced dose-dependent protection against maximal electroshock seizures in mice with an ED50 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).
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.
体外研究：
Nefopam (0.1-100 μM; 15 min) inhibits the uptake of 22Na in a concentration-dependent manner in SK-N-SH cells.
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