Nefopam HCl
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MedKoo CAT#: 329820

CAS#: 23327-57-3 (HCl)

Description: Nefopam is a centrally-acting non-opioid analgesic drug. It is widely used, mainly in European countries, for the relief of moderate to severe pain as an alternative to opioid analgesic drugs. Animal studies have shown that nefopam has a potentiating (analgesic-sparing) effect on morphine and other opioids by broadening the antinociceptive action of the opioid and possibly other mechanisms, generally lowering the dose requirements of both when they are used concomitantly.

Chemical Structure

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Nefopam HCl
CAS# 23327-57-3 (HCl)
Product data Instruction

Theoretical Analysis

MedKoo Cat#: 329820
Name: Nefopam HCl
CAS#: 23327-57-3 (HCl)
Chemical Formula: C17H20ClNO
Exact Mass: 0.00
Molecular Weight: 289.803
Elemental Analysis: C, 70.46; H, 6.96; Cl, 12.23; N, 4.83; O, 5.52

Price and Availability

Size Price Availability Quantity
1g USD 350 2 Weeks
2g USD 550 2 Weeks
5g USD 1050 2 Weeks
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Related CAS #: 13669-70-0 (free base)   23327-57-3 (HCl)    

Synonym: Fenazoxine hydrochloride; Lenipan; Leoplexamin; Nefopam HCl; Nefopam hydrochloride; Oxadol; Pallopikeron, Brand name Acupan.

IUPAC/Chemical Name: 5-Methyl-1-phenyl-3,4,5,6-tetrahydro-1H-2,5-benzoxazocine hydrochloride

InChi Key: CNNVSINJDJNHQK-UHFFFAOYSA-N

InChi Code: InChI=1S/C17H19NO.ClH/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;1H

SMILES Code: CN1CCOC(C2=CC=CC=C2)C3=CC=CC=C3C1.[H]Cl

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info: Nefopam has additional action in the prevention of shivering, which may be a side effect of other drugs used in surgery. Nefopam was significantly more effective than aspirin as an analgesic in one clinical trial, although with a greater incidence of side effects such as sweating, dizziness and nausea, especially at higher doses. Nefopam is around a third to half the potency and slightly less effective as an analgesic compared to morphine, or oxycodone, but tends to produce fewer side effects, does not produce respiratory depression, and has much less abuse potential, and so is useful either as an alternative to opioids, or as an adjunctive treatment for use alongside opioid(s) or other analgesics. Nefopam is also used to treat severe hiccups.

Product Data:
Product Data
Instruction:
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Biological target: Nefopam is a centrally-acting non-opioid analgesic drug.
In vitro activity: The screen identified Neofopam, as an agent that inhibited cell numbers to 42% of baseline in cell cultures from β-catenin driven fibroproliferative disorders. Nefopam decreased cell proliferation and β-catenin protein level to 50% of baseline in these same cell cultures. The half maximal effective concentration in-vitro was 0.5 uM and there was a plateau in the effect after 48 hours of treatment. Reference: PLoS One. 2012;7(5):e37940. https://pubmed.ncbi.nlm.nih.gov/22666417/
In vivo activity: Mechanical and heat antinociception induced by oral doses of paracetamol, nefopam or their combination was studied by isobolographic analysis in a murine model of postsurgical pain. Oral nefopam induced dose-dependent antinociception with similar efficacy for mechanical and heat hypersensitivity (ED50 s 5.42 ± 0.81 vs. 5.83 ± 0.72). Combinations of increasing isoeffective doses revealed that combined ED17.5 s (85.76 mg/kg paracetamol and 1.9 mg/kg nefopam) and ED35 s (132.67 mg/kg and 3.73 mg/kg) showed synergistic effects leading to 75% and 90% mechanical antinociception, respectively. Reference: Eur J Pain. 2021 Sep;25(8):1770-1787. https://pubmed.ncbi.nlm.nih.gov/33909343/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 6.8 23.29
Water 16.8 57.80

Preparing Stock Solutions

The following data is based on the product molecular weight 289.80 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol: 1. Poon R, Hong H, Wei X, Pan J, Alman BA. A high throughput screen identifies Nefopam as targeting cell proliferation in β-catenin driven neoplastic and reactive fibroproliferative disorders. PLoS One. 2012;7(5):e37940. doi: 10.1371/journal.pone.0037940. Epub 2012 May 30. PMID: 22666417; PMCID: PMC3364163. 2. Novelli A, Groppetti A, Rossoni G, Manfredi B, Ferrero-Gutiérrez A, Pérez-Gómez A, Desogus CM, Fernández-Sánchez MT. Nefopam is more potent than carbamazepine for neuroprotection against veratridine in vitro and has anticonvulsant properties against both electrical and chemical stimulation. Amino Acids. 2007;32(3):323-32. doi: 10.1007/s00726-006-0419-6. Epub 2006 Oct 6. PMID: 17021653. 3. Cabañero D, Maldonado R. Synergism between oral paracetamol and nefopam in a murine model of postoperative pain. Eur J Pain. 2021 Sep;25(8):1770-1787. doi: 10.1002/ejp.1787. Epub 2021 May 20. PMID: 33909343. 4. Chae JW, Kang DH, Li Y, Kim SH, Lee HG, Choi JI, Yoon MH, Kim WM. Antinociceptive effects of nefopam modulating serotonergic, adrenergic, and glutamatergic neurotransmission in the spinal cord. Neurosci Lett. 2020 Jul 13;731:135057. doi: 10.1016/j.neulet.2020.135057. Epub 2020 May 23. PMID: 32450186.
In vitro protocol: 1. Poon R, Hong H, Wei X, Pan J, Alman BA. A high throughput screen identifies Nefopam as targeting cell proliferation in β-catenin driven neoplastic and reactive fibroproliferative disorders. PLoS One. 2012;7(5):e37940. doi: 10.1371/journal.pone.0037940. Epub 2012 May 30. PMID: 22666417; PMCID: PMC3364163. 2. Novelli A, Groppetti A, Rossoni G, Manfredi B, Ferrero-Gutiérrez A, Pérez-Gómez A, Desogus CM, Fernández-Sánchez MT. Nefopam is more potent than carbamazepine for neuroprotection against veratridine in vitro and has anticonvulsant properties against both electrical and chemical stimulation. Amino Acids. 2007;32(3):323-32. doi: 10.1007/s00726-006-0419-6. Epub 2006 Oct 6. PMID: 17021653.
In vivo protocol: 1. Cabañero D, Maldonado R. Synergism between oral paracetamol and nefopam in a murine model of postoperative pain. Eur J Pain. 2021 Sep;25(8):1770-1787. doi: 10.1002/ejp.1787. Epub 2021 May 20. PMID: 33909343. 2. Chae JW, Kang DH, Li Y, Kim SH, Lee HG, Choi JI, Yoon MH, Kim WM. Antinociceptive effects of nefopam modulating serotonergic, adrenergic, and glutamatergic neurotransmission in the spinal cord. Neurosci Lett. 2020 Jul 13;731:135057. doi: 10.1016/j.neulet.2020.135057. Epub 2020 May 23. PMID: 32450186.

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1: Girard P, Chauvin M, Verleye M. Nefopam analgesia and its role in multimodal analgesia: A review of preclinical and clinical studies. Clin Exp Pharmacol Physiol. 2016 Jan;43(1):3-12. doi: 10.1111/1440-1681.12506. Review. PubMed PMID: 26475417.

2: Kim KH, Abdi S. Rediscovery of nefopam for the treatment of neuropathic pain. Korean J Pain. 2014 Apr;27(2):103-11. doi: 10.3344/kjp.2014.27.2.103. Epub 2014 Mar 28. Review. PubMed PMID: 24748937; PubMed Central PMCID: PMC3990817.

3: Kakkar M, Derry S, Moore RA, McQuay HJ. Single dose oral nefopam for acute postoperative pain in adults. Cochrane Database Syst Rev. 2009 Jul 8;(3):CD007442. doi: 10.1002/14651858.CD007442.pub2. Review. PubMed PMID: 19588431; PubMed Central PMCID: PMC4170989.

4: Evans MS, Lysakowski C, Tramèr MR. Nefopam for the prevention of postoperative pain: quantitative systematic review. Br J Anaesth. 2008 Nov;101(5):610-7. doi: 10.1093/bja/aen267. Epub 2008 Sep 15. Review. PubMed PMID: 18796441.

5: Tracqui A, Berthelon L, Ludes B. Fatal overdosage with nefopam (Acupan). J Anal Toxicol. 2002 May-Jun;26(4):239-43. Review. PubMed PMID: 12054367.

6: Bilotta F, Pietropaoli P, Rosa G. Nefopam for refractory postoperative hiccups. Anesth Analg. 2001 Nov;93(5):1358-60. Review. PubMed PMID: 11682430.

7: Heel RC, Brogden RN, Pakes GE, Speight TM, Avery GS. Nefopam: a review of its pharmacological properties and therapeutic efficacy. Drugs. 1980 Apr;19(4):249-67. Review. PubMed PMID: 6991238.