Nefopam

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[1][2][3].

Signaling Pathways >> Others >> Others

Research Areas >> Neurological Disease

Nefopam (0.1-100 µM; 15 min) inhibits the uptake of 22Na in a concentration-dependent manner in SK-N-SH cells[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 22Na with an IC50 value of 27 µM.

Nefopam (0-10 mg/kg; i.v.; single) protects mice against 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 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)[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.

MOLECULAR FORMULA :

C17-H19-N-O

MOLECULAR WEIGHT :

253.37

WISWESSER LINE NOTATION :

T68 HN KO&TJ H1 LR

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :

TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :

Oral

SPECIES OBSERVED :

Human - woman

DOSE/DURATION :

15 mg/kg

TOXIC EFFECTS :

Behavioral - changes in motor activity (specific assay) Cardiac - change in rate

REFERENCE :

BMJOAE British Medical Journal. (British Medical Assoc., BMA House, Tavistock Sq., London WC1H 9JR, UK) V.1- 1857- Volume(issue)/page/year: 283,1508,1981

TYPE OF TEST :

TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :

Oral

SPECIES OBSERVED :

Human - man

DOSE/DURATION :

17 mg/kg

TOXIC EFFECTS :

Behavioral - hallucinations, distorted perceptions Behavioral - excitement Cardiac - pulse rate increase, without fall in BP

REFERENCE :

BMJOAE British Medical Journal. (British Medical Assoc., BMA House, Tavistock Sq., London WC1H 9JR, UK) V.1- 1857- Volume(issue)/page/year: 283,1508,1981

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Oral

SPECIES OBSERVED :

Rodent - mouse

DOSE/DURATION :

180 mg/kg

TOXIC EFFECTS :

Details of toxic effects not reported other than lethal dose value

REFERENCE :

USXXAM United States Patent Document. (U.S. Patent Office, Box 9, Washington, DC 20231) Volume(issue)/page/year: #4198424

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Intraperitoneal

SPECIES OBSERVED :

Rodent - mouse

DOSE/DURATION :

50 mg/kg

TOXIC EFFECTS :

Sense Organs and Special Senses (Eye) - mydriasis (pupillary dilation)

REFERENCE :

DDEVD6 Drug Development and Evaluation. (Gustav Fischer Verlag, Postfach 720143, D-7000 Stuttgart 70, Fed. Rep. Ger.) V.1- 1977- Volume(issue)/page/year: 3,10,1979