Nifedipine

Nifediac®, Nifedical®
A Blocker of L-Type CaV Channels
    Cat #: N-120
    Alternative Name Nifediac®, Nifedical®
  • Lyophilized Powder
  • Bioassay Tested
  • Source Synthetic
    MW: 346.3
    Purity: >99.8%
    Effective concentration 0.1 -10 μM.
    Structure
    • Nifedipine
    Chemical name 1, 4-Dihydro-2,6-dimethyl-4-(2-nitrophenyl)-3,5 pyridinedicarboxylic acid dimethyl ester.
    Molecular formula C17H18N2O6.
    CAS No.: 21829-25-4.
    Activity Nifedipine, the prototype of dihydropyridines (DHPs), is an L-type voltage-gated Ca2+ channel selective blocker1. Nifedipine scarcely blocks the two N- and P/Q-type channels in Xenopus oocytes, whereas the effect of 10 μM Nifedipine on the L- type channel, at a holding potential of −80 mV, is approximately 65% block1. In the clinic Nifedipine is used for the prophylaxis of angina pectoris symptoms and as an anti-hypertensive agent2-3.
    References-Activity
    1. Furukawa, T. et al. (1999) J. Pharmacol. Exp.Ther. 291, 464.
    2. Sorkin, E.M. et al. (1985) Drugs 30, 182.
    3. Lundy, A. et al. (2009) Vasc. Health  Risk Mang. 5, 429.
    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
    • Nifedipine
      Alomone Labs Nifedipine blocks L-type Ca2+ currents in Xenopus oocytes.
      A. Time course of L-type channel (CaV1.2+α2δ1+β1a) activity before and during applications of 0.1, 0.5, 1, 2, and 10 μM Nifedipine (#N-120) as indicated, and upon wash.  Holding potential was -80 mV and currents were elicited every 10 seconds by 100 ms ramp to +50 mV. B. Superimposed current traces of L-type channels (CaV1.2+α2δ1+β1a), before and during applications of 0.1, 1 and 10 μM Nifedipine as indicated.  Holding potential was -100 mV and currents were elicited every 10 seconds by 100 ms steps to +10 mV.
    References - Scientific background
    1. Hockerman, G.H. et al. (1997) Annu. Rev. Pharmacol. Toxicol 37, 361.
    2. Hering, S. et al. (1998) Trends. Pharmacol. Sci. 19, 439.
    3. Furukawa, T. et al. (1999) J. Pharmacol. Exp.Ther. 291, 464.
    4. Sorkin, E.M. et al (1985) Drugs 30, 182.
    5. Croom, K.F. et al. (2006) Drugs 66, 497.
    6. Pope, J.E. (2011) Clin. Evid. 2011, pii. 1119.
    7. Conde Agudelo, A. et al (2011) Am. J. Obstet. Gynecol. 204, e1.
    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 a1 subunit. The subunits CaV1.1-1.4 (α1S, α1C, α1D and α1F) form L-type Ca2+ channels and bind dihydropyridines (DHPs) with high affinity.1-3 Nifedipine, a DHP, is a selective L-type Ca2+ channel blocker3. 10 µM Nifedipine inhibits ~65% of the L-type channel current at a holding potential of -80 mV, in Xenopus oocytes3.

    Nifedipine was initially developed for the prophylaxis of angina symptoms, and then later used as an anti-hypertensive agent4. Nifedipine acts by inhibiting the transmembrane influx of calcium into cardiac and vascular smooth muscle cells, thus reducing muscle contraction and has predominantly vasodilatory effects on arteries with minimal effects on the myocardium and cardiac conduction5. For the same reason Nifedipine is also useful in the reduction of the frequency and severity of the attacks in Raynaud’s phenomenon, an episodic vasospasm of the peripheral arteries6.

    Uterine contractions are the most frequently recognized symptom and sign of preterm labor and hence, inhibition of uterine contractility with tocolytic agents to prolong pregnancy and reduce neonatal complications continues to be the focus of treatment of preterm labor. The efficacy and safety of Nifedipine as a tocolytic agent in women with preterm labor were determined and provide another indication for Nifedipine7.

    Target L-type CaV channels
    Image & Title Nifedipine
    Alomone Labs Nifedipine and SNX-482 block L-type and R-type CaV channels respectively in rat pancreatic INS-1 832/13 β-cells.Representative CaV currents from INS-1 832/13 cells before and after treatment with Nifedipine (#N-120), a general L-type CaV channel blocker and SNX-482 (#RTS-500), a CaV2.3 channel blocker. 52% of the currents were blocked by Nifedipine (n = 8; p < 0.05) while 31% (n = 10; p < 0.001) of currents were blocked by SNX-482. Cells were held at −70 mV for 2 min after formation of whole-cell mode, and currents elicited by stepped 300 or 500 milliseconds depolarizations in 10 mV increments.Adapted from Xie, L. et al. (2016) PLoS ONE 11, e0147862. with permission of PLoS.
    Last update: 24/01/2020

    Nifedipine (#N-120) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use

    Applications

    Specifications

    Scientific Background

    Citations

    Citations
    Electrophysiology
    1. Rat DRGs (patch clamp).
      Moutal, A. et al. (2018) Neuroscience 381, 79.
    Product citations
    1. Garcia-Delgado, N. et al. (2018) Front. Endocrinol. 9, 40.
    2. Hou, J.W. et al. (2018) Br. J. Pharmacol. 175, 4325.
    3. Dahan, T. et al. (2017) Diabetes 66, 426.
    4. Huang, C.Y. et al. (2017) J. Neurosci. 37, 4433.
    5. Moutal, A. et al. (2016) Pain 157, 1448.
    6. Xie, J.Y. et al. (2016) Pain 157, 2124.
    7. Xie, L. et al. (2016) PLoS ONE 11, e0147862.
    8. Kim, S.H. et al. (2013) Cell Calcium 54, 295.
    9. Munoz, E. et al. (2013) Cell Calcium 54, 375.
    10. Tian, N. et al. (2012) J. Biol. Chem. 287, 44447.
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