Nitrendipine

A Potent and Selective Blocker of L-type CaV Channels
    Cat #: N-155
  • Lyophilized Powder
  • Bioassay Tested
  • Source Synthetic
    MW: 360.4
    Purity: >98%
    Effective concentration 1-200 µM.
    Structure
    • Nitrendipine
    Chemical name Ethyl methyl 1,4-dihydro-2,6-dimethyl-4-(meta-nitrophenyl)-3,5-pyridinedicarboxylate.
    Molecular formula C18H20N2O6.
    CAS No.: 39562-70-4.
    Activity 10 μM inhibited 50% of L-type current expressed in Xenopus oocytes, with no effect on T-type channels.
    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
    • Nitrendipine
      Alomone Labs Nitrendipine inhibits L-type voltage-gated Ca2+ currents expressed in Xenopus oocytes.
      A. Time course of CaV1.2/α2-δ1/β2a (L-type) current inhibition by 200 µM of Nitrendipine (#N-155). Currents were elicited by application of voltage steps from a holding potential of -100 mV to 0 mV (100 msec). B. Superimposed example traces of current responses before and during perfusion of 200 µM Nitrendipine as indicated.
    References - Scientific background
    1. Furukawa, T. et al. (2005) J. Cardiovasc. Pharmacol45, 241.
    2. Furukawa, T. et al. (1999) J. Pharmacol. Exp. Ther. 291, 464.
    3. Hering, S. et al. (1998) Trends Pharmacol. Sci. 19, 439.
    4. Hockerman, G.H. et al. (1997) Ann. Rev. Pharmacol. Toxicol. 37, 361.
    5. Haller, H. (2008) Int. J. Clin. Practice 62, 781.
    6. Peterson, B.Z. et al. (1996) J. Biol. Chem. 271, 5293.
    7. Furukawa, T. et al. (2005) .J. Cardiovasc. Pharmacol. 45, 241.
    Scientific background

    Native voltage-gated Ca2+ channels (VGCC, CaV) are pharmacologically classified into at least five different subclasses (L-, N-, P-, Q-, and R-type), the characteristics of which are determined by the pore- forming α1 subunit. The subunits CaV1.1-1.4 (α1S, α1C, α1D and α1F) form L-type Ca2+ channels and bind dihydropyridines (DHPs) with high affinity1,2.

    L-type (CaV1), voltage-gated Ca2+ channels are plasma membrane protein complexes which allow the passage of Ca2+ ions into cells following depolarization of the membrane potential.

    They are widely expressed in cardiac and smooth muscle in which they control contraction and therefore were recognized as a therapeutic target for cardiovascular diseases3,4.

    Nitrendipine is a dihydropyridine Ca2+ channel blocker. Once Nitrendipine is metabolized, it reaches the cells of the smooth muscles and cardiac muscle. It binds more effectively with L-type calcium channels in smooth muscle cells as a result of its lower resting membrane potential5.

    10 μM of Nitrendipine inhibited 50% of L-type current expressed in Xenopus oocytes, with no effect on T-type channels6.

    Target L-type Ca2+ channels
    Last update: 24/01/2020

    Nitrendipine (#N-155) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use
    Shipping and Ordering information