Diltiazem hydrochloride

Cardizem®, Dilacorxr®
A Potent and Selective Blocker of L-Type CaV Channels
    Cat #: D-135
    Alternative Name Cardizem®, Dilacorxr®
  • Lyophilized Powder
  • Bioassay Tested
  • Source Synthetic
    MW: 451
    Purity: >98%
    Effective concentration 10 µM - 1 mM.
    Structure
    • Diltiazem hydrochloride
    Chemical name [(2S,3S)-5-[2-(dimethylamino)ethyl]-2-(4-methoxyphenyl)-4-oxo-2,3-dihydro-1,5-benzothiazepin-3-yl] acetate;hydrochloride.
    Molecular formula C22H27ClN2O4S.
    CAS No.: 33286-22-5, 42399-41-7 (as free base).
    Activity IC50 was 33 µM on CaV1.2 channels in expression systems1.
    References-Activity
    1. Hockerman, G.H. et al. (2000) Mol. Pharmacol. 58, 1264.
    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 Water. 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
    • Diltiazem hydrochloride
      Alomone Labs Diltiazem hydrochloride inhibits L-type voltage-gated Ca2+ currents expressed in Xenopus oocytes.
      A. Time course of CaV1.2/α2-δ1/β1 (L-type) current inhibition by 100 µM and 1 mM Diltiazem hydrochloride (#D-135). Currents were elicited by application of voltage ramp from a holding potential of -80 mV to 0 mV (100 msec). B. Superimposed example traces of current responses before and during perfusion of 100 µM and 1 mM Diltiazem hydrochloride as indicated.
    References - Scientific background
    1. Bers, D.M. and Perez-Reyes, E. (1999) Cardiovasc. Res. 42, 339.
    2. Hockerman, G.H. et al. (1997) Annu. Rev. Pharmacol. Toxicol. 37, 361.
    3. Hockerman, G.H. et al. (2000) Mol. Pharmacol. 58, 1264.
    4. Balino, P. et al. (2010) Behav. Brain Res. 209, 196.
    5. Verma, V. et al. (2001) Indian J. Exp. Biol. 39, 636.
    Scientific background

    Ca2+ influx via voltage-dependent L-type Ca2+ channels (CaV1.2) found in cardiac and vascular smooth muscle initiates contraction and contributes to timing of the cardiac action potential1. CaV1.2 is sensitive to blockade by three distinct chemical classes of small-molecule drugs: dihydropyridines (DHPs), phenylalkylamines (PAAs), and benzothiazepines (BZPs).

    Diltiazem hydrochloride is structurally related to benzothiazepine (BZP) Ca2+ channel blockers2. Diltiazem hydrochloride blocks CaV1.2 channels at low micromolar concentrations in both primary cardiac myocytes and heterologous expression systems. Diltiazem hydrochloride causes a modest decrease in heart muscle contractility and reduces myocardium oxygen consumption3. Research has demonstrated that diltiazem hydrochloride is able to reduce cocaine cravings in drug-addicted rats due to the effects of Ca2+ blockers on dopaminergic and glutamatergic signaling in the brain4. Diltiazem hydrochloride also enhances the analgesic effect of morphine in animal tests and reduces the development of tolerance5.

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

    Diltiazem hydrochloride (#D-135) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use
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