Benidipine hydrochloride

A Dihydropyridine Blocker of Voltage-Gated Ca2+ Channels
    Cat #: B-120
  • Lyophilized Powder
  • Bioassay Tested
  • Source Synthetic
    MW: 542
    Purity: >99% (HPLC)
    Effective concentration 1-100 µM.
    Structure
    • Benidipine hydrochloride
    Chemical name (4R)-rel-1,4-Dihydro-2,6-dimethyl-4-(3-nitrophenyl)-3,5-pyridinedicarboxylic acid 3-methyl 5-[(3R)-1-(phenylmethyl)-3-piperidinyl] ester hydrochloride.
    Molecular formula C28H32N3O6Cl.
    CAS No.: 91599-74-5.
    Activity Benidipine hydrochloride is a state-dependent Ca2+ channel blocker. It inhibits N-type and P/Q-type channels with IC50 of ~30 µM and is an order of magnitude more potent towards L-type channels, exhibiting the following IC50: 14 µM at -80mV and 5 µM at -60 mV holding potentials1.
    References-Activity
    1. Furukawa, T. et al. (1999) J. Pharmacol. Exp. Ther. 291, 464.
    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
    • Benidipine hydrochloride
      Alomone Labs Benidipine hydrochloride inhibits T- and L-type voltage-gated Ca2+ currents expressed in Xenopus oocytes.
      A. Time course of CaV3.1 (T-type) current reversible inhibition by increasing concentrations of Benidipine hydrochloride (#B-120). Currents were elicited by application of voltage ramps from a holding potential of -100 mV to +60 mV (40 msec). B. Superimposed example traces of current response to voltage ramps before and during perfusion of 10 and 50 µM Benidipine hydrochloride as indicated. C. Time course of CaV1.2/α2-δ1/β2a (L-type) current inhibition 10 µM of Benidipine hydrochloride. Currents were elicited by application of voltage steps from a holding potential of -100 mV to 0 mV (100 msec). D. Superimposed example traces of current responses before and during perfusion of 10 µM Benidipine hydrochloride as indicated.
    References - Scientific background
    1. Furukawa, T. et al. (1999) J. Pharmacol. Exp. Ther. 291, 464.
    2. Minor, D.L. and Findeisen, F. et al. (2010) Channels (Austin) 4, 459.
    3. Godfraind, T. (2005) Philos. Trans. R. Soc. Lond. B. Biol. Sci. 360, 2259.
    4. Clunn, G.F. et al. (2010) Int. J. Cardiol. 139, 2.
    5. Yao, K. et al. (2006) J. Pharmacol. Sci. 100, 243.
    6. Kitakaze, M. et al. (1999) Cardiovasc. Drug Rev. 17, 1.
    Scientific background

    Both L-type (CaV1) and T-type (CaV3) voltage-gated Ca2+ channels are large (~0.5 MDa), transmembrane proteins which control the cellular influx of Ca2+ in response to electrical stimuli. While CaV1s require a strong depolarization (~+40 mV) to perform, a much weaker pulse (~-40 mV) is sufficient to activate CaV3s1.

    Ca2+ channel blockers (CCBs) are a diverse class of pharmaceutical agents, usually targeted at CaV1s, of which dihydropyridines (DHPs) constitute a major subgroup2,3. Inhibitors of Ca2+-mediated smooth muscle contractions, CCBs produce vasodilation, thus therapeutically managing hypertension and coronary heart disease2. Additionally, benidipine is known to be an endothelium protectant as well as an antioxidant4,5.

    A DHP derivative, benidipine hydrochloride acts as a triple-channel (CaV1, CaV2 and CaV3) blocker and is characterized by slow onset of action and high affinity for the binding sites of its target channels4; with a Ki value of 0.08-0.13 nmol/L benidipine's cell-membrane association is considerably greater than other DHPs, and a dissociation rate which is 9 times slower than that of nifedipine makes it distinguishably long-lasting4,5.

    Target CaV1, CaV3 Ca2+ channels
    Last update: 24/01/2020

    Benidipine hydrochloride (#B-120) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use
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