Orphenadrine hydrochloride

Disipal®, Mebedrol®, Mephenamin®
An Antagonist of Muscarinic, H1 Histamine, NMDA Receptors and Voltage-Gated Na+ Channels
    Cat #: O-101
    Alternative Name Disipal®, Mebedrol®, Mephenamin®
  • Lyophilized Powder
  • Bioassay Tested
  • Source Synthetic
    MW: 305.8
    Purity: >96%
    Effective concentration 0.3-100 µM.
    • Orphenadrine hydrochloride
    Chemical name β-Dimethylaminoethyl 2-methylbenzhydryl ether hydrochloride.
    Molecular formula C18H24ClNO.
    CAS No.: 341-69-5.
    Activity Orphenadrine was found to act as muscarinic receptor antagonist, H1 histamine receptor antagonist, muscle relaxant, inhibitor of the noradrenergic transporter, NMDA receptor antagonist and NaV channel blocker1-4.
    Shipping and storage Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
    Solubility DMSO. Centrifuge all product preparations before use (10000 x g 5 min).
    Storage of solutions Up to four weeks at 4°C or three months at -20°C.
    Our bioassay
    • Orphenadrine hydrochloride
      Alomone Labs Orphenadrine hydrochloride inhibits charbacol-induced Ca2+ signaling in M1 muscarinic receptor expressing C6 cells.
      Changes in intracellular Ca2+ were detected via changes in Fluo-3 emission following application. A. Normalized fluorescence before and after co-application (at 20 seconds, see arrow) of 10 µM carbachol and 0-100 µM Orphenadrine hydrochloride (#O-101) as indicated. The blank response to PBS perfusion is in gray. B. Inhibition (as percent of control) of 10 µM Carbachol evoked Ca2+ rise, plotted against Orphenadrine concentrations.
    References - Scientific background
    1. Brocks, D.R. et al. (1999) J. Pharm. Pharm. Sci. 2, 39.
    2. Desaphy, J.F. et al. (2009) Pain 142, 225.
    3. Kornhuber, J. et al. (1995) J. Neural. Transm. Gen. Sect. 102, 237.
    4. Pubill, D. et al. (1999) J. Pharm. Pharmacol. 51, 307.
    Scientific background

    The group of anticholinergic drugs includes benztropine, biperiden, diphenhydramine, ethopropazine, orphenadrine, procyclidine and trihexyphenidyl. Orphenadrine as the citrate salt is used for the treatment of Parkinson’s disease and in musculoskeletal disorders. It is also used as an analgesic, although its mechanism of action is still unknown1,2. Orphenadrine binds to and modulates the activity of muscarinic receptors of rat brain, with IC50 of 0.37 µM1.

    Orphenadrine inhibits NaV channels in a concentration-, voltage- and frequency-dependent manner by binding to the same receptor as the local anesthetics2. Orphenadrine was reported as a Muscarinic receptor antagonist, H1 histamine receptor antagonist, muscle relaxant, and inhibits the noradrenergic transporter and blocks the NMDA receptor ion channel3,4.

    Target Muscarinic, H1 histamine, NMDA receptors, NaV Na+ channels
    Last update: 24/01/2020

    Orphenadrine hydrochloride (#O-101) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use
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