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Lomerizine dihydrochloride

A Blocker of L-Type Voltage-Gated Ca2+ Channels
    Cat #: L-125
  • Lyophilized Powder
  • Bioassay Tested
    • Source Synthetic
    MW: 541.5
    Purity: >99%
    Effective concentration 0.5-100 µM.
    Structure
    • Lomerizine dihydrochloride
    Chemical name 1-[Bis(4-fluorophenyl)methyl]-4-[(2,3,4-trimethoxyphenyl)methyl]piperazine dihydrochloride.
    Molecular formula C27H32N2F2O3Cl2.
    CAS No.: 101477-54-7.
    Activity Lomerizine dihydrochloride inhibited CaV currents in PC12 cells with IC50 of 1.9 µM1. It inhibits L-type Ca2+ channels2.
    References-Activity
    1. Watano, T. et al. (1997) Jpn. J. Pharmacol. 75, 209.
    2. Iwamoto, T. et al. (1988) Jpn J Pharmacol 48, 241.
    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
    • Lomerizine dihydrochloride
      Alomone Labs Lomerizine dihydrochloride inhibits L-type voltage-gated CaV1.2 currents heterologously expressed in Xenopus oocytes.
      A. Time course of CaV1.2/α2-δ1/β2a (L-type) current inhibition by 10 and 100 µM Lomerizine dihydrochloride (#L-125). 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 10 and 100 µM Lomerizine dihydrochloride as indicated.
    References - Scientific background
    1. Catterall, W.A. et al. (2003) Pharmacol. Rev. 55, 579.
    2. Streissnig, J. et al. (1998) Trends. Pharmacol Sci. 19, 108.
    3. Hara, T. et al. (1995) CNS Drug Rev. 1, 204.
    4. Ito, Y. et al. (2010) CNS Neurosci. Ther. 16, 103.
    5. Watano, T. et al. (1997) Jpn. J. Pharmacol. 75, 209.
    6. Iwamoto, T. et al. (1988) Jpn J Pharmacol 48, 241.
    Scientific background

    Voltage-dependent L-type Ca2+ channels play an important role Ca2+ influx. L-type calcium currents typically require a strong depolarization for activation and are long-lasting1.

    The common pharmacological profile of L-type channels is determined by the α1 subunit, which forms the Ca2+ selective pore, and is encoded by one of the CaV1 (α 1S) channel genes2. Cav1.2 (CACNA1C) in humans is widely expressed in cardiac myocytes, smooth muscle myocytes, endocrine cells, neuronal cell bodies and proximal dendrites1.

    Lomerizine dihydrochloride is a Ca2+ channel blocker with relatively selective CNS effects. Lomerizine was developed as a potential agent for the selective improvement of the ocular or cerebrovascular circulation with minimal adverse cardiovascular effects3, and it is used as an anti migraine drug4. Lomerizine selectively relaxes smooth muscle cells by inhibiting L-type Ca2+ influx, thereby reducing tone and increasing blood flow in cerebral vessels4.

    Lomerizine blocked Ba2+ current through the voltage-gated Ca2+ channel in rat pheochromocytoma (PC12) cells5, and it is suggested to bind to the 1,4-dihydropyridine binding site, as obtained by a [3H]nitrendipine binding study6.

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

    Lomerizine dihydrochloride (#L-125) is a highly pure, synthetic, and biologically active compound.

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

    Resources

    L-Type (CaV1) Channels

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