In SK-N-SH cells, nevopam (0.1-100 µM; 15 min) inhibits 22Na absorption in a concentration-dependent manner[1].

Nefopam (0-10 mg/kg; iv; single) shields mice from seizures brought on by electroshock[1]. In a vincristine-induced peripheral neuropathy model, neviropam (10, 30, 60 mg/kg; ip; single) exhibits a dose-dependent reduction in mechanical allodynia and a drop in neurokinin -1 receptor concentration[2].

Cell Viability Assay[1]
Cell Types: SK-N-SH cells
Tested Concentrations: 0.1 -100 µM
Incubation Duration: 15 min (preincubate)
Experimental Results: Inhibited the uptake of 22Na with an IC50 value of 27 µM.

Animal/Disease Models: Adult male NMRI mice (25-30 g; 6 to7weeks old; electroshock-induced seizures model)[1]
Doses: 0-10 mg /kg
Route of Administration: intravenous (iv) injection; single
Experimental Results: Produced dose-dependent protection against maximal electroshock seizures in mice with an ED50 of 3.8 (2.9-5.1) mg/kg.

---

Animal/Disease Models: Adult male mice (10weeks old; 25- 30 g; vincristine-induced peripheral neuropathy model)[2].
Doses: 10, 30, 60 mg/kg
Route of Administration: intraperitoneal (ip) injection; single
Experimental Results: Dramatically diminished the percentage of NK1 receptors in the spinal cord at dosage of 60 mg/kg. demonstrated a sustained increase in paw withdrawal threshold against mechanical stimuli.

Effects During Pregnancy and Lactation
◉ Overview of Use During Lactation
Nefopam has not been approved by the U.S. Food and Drug Administration (FDA). Nefopam levels in breast milk are very low when the mother is taking the usual dose. Nefopam does not appear to have adverse effects on breast milk production or the neurobehavioral scores of breastfed newborns. Breastfeeding is possible while the mother is taking nefopam, but some experts recommend discontinuing use 48 hours postpartum.
◉ Effects on Breastfed Infants
66 women who underwent cesarean section were randomly assigned to two groups postpartum: one group received 20 mg of nefopam intravenously every 6 hours, and the other group received 1 g of acetaminophen intravenously every 6 hours. Both groups also received 50 mg of ketoprofen intravenously. Neonatal neurobehavioral scores were recorded by a pediatrician unaware of the group assignments at 12, 24, 48, and 72 hours postpartum. There were no differences in behavioral scores between the groups.
◉ Effects on Lactation and Breast Milk
Sixty-six women who underwent cesarean section were divided into two groups: one group received 20 mg of nefopam intravenously every 6 hours, and the other group received 1 g of acetaminophen intravenously every 6 hours. All women received the same preoperative analgesia regimen, including spinal bupivacaine, sufentanil, and morphine, as well as intravenous ephedrine and phenylephrine to prevent hypotension. Postoperatively, all women received intravenous oxytocin and 50 mg of ketoprofen intravenously every 6 hours. Milk production was assessed by weighing the newborns before and after each feeding on days 2 and 3 postnatally. There were no statistically significant differences between the two groups in terms of weight change before and after each feeding, daily weight curve changes in newborns, or weight loss from day 0 to day 2. Mothers also scored breast fullness to assess the initiation of lactation stage II; there was no difference in the time required for the animals to reach lactation stage II between the two groups. Serum prolactin levels were also similar between the two groups.

[1]. Nefopam blocks voltage-sensitive sodium channels and modulates glutamatergic transmission in rodents. Brain Res. 2004 Jul 9;1013(2):249-55.

[2]. The Antiallodynic Effect of Nefopam on Vincristine-Induced Neuropathy in Mice. J Pain Res. 2020 Feb 7;13:323-329.

[3]. Rediscovery of nefopam for the treatment of neuropathic pain. Korean J Pain. 2014 Apr;27(2):103-11.

5-Methyl-1-phenyl-3,4,5,6-tetrahydro-1H-2,5-benzoxazole octane belongs to the benzoxazole octane class of compounds. Its structure is 3,4,5,6-tetrahydro-1H-2,5-benzoxazole octane with phenyl and methyl groups substituted at positions 1 and 5, respectively. It is a benzoxazole octane compound and also a tertiary amine. Nefopa is being investigated for the prevention of cholecystitis and post-anesthesia chills. Nefopa has also been investigated for the prevention of kidney transplantation. Nefopa is a non-narcotic analgesic with a chemical structure similar to ophenadin. Its mechanism of action is not yet clear. It is used to relieve acute and chronic pain. (Excerpt from Martindale Pharmacopoeia, 30th edition, p. 26) See also: Nefopa hydrochloride (note moved here).

C17H19NO

253.34

253.146

13669-70-0

Nefopam hydrochloride;23327-57-3

4450

Typically exists as solid at room temperature

1.1±0.1 g/cm3

369.5±37.0 °C at 760 mmHg

109.0±28.8 °C

0.0±0.8 mmHg at 25°C

1.564

3.44

0

2

1

19

274

0

CN1CCOC(C2=CC=CC=C2)C3=CC=CC=C3C1

RGPDEAGGEXEMMM-UHFFFAOYSA-N

InChI=1S/C17H19NO/c1-18-11-12-19-17(14-7-3-2-4-8-14)16-10-6-5-9-15(16)13-18/h2-10,17H,11-13H2,1H3

5-methyl-1-phenyl-1,3,4,6-tetrahydro-2,5-benzoxazocine

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples

Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.

---

Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)
*Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution.
Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)
Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil)
Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals).

View More

Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)]
*Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)

---

Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium)
Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose
Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals).

View More

Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders

---

Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

---

 (Please use freshly prepared in vivo formulations for optimal results.)