1,1-Dimethyl-4-phenylpiperazinium iodide

An Agonist of nAChR
Cat #: D-125
  • Lyophilized Powder
  • Bioassay Tested
  • Source Synthetic
    MW: 318.2
    Purity: >98%
    Effective concentration 0.5-200 µM.
    Chemical name 1,1-Dimethyl-4-phenylpiperazinium iodide.
    Molecular formula C12H19IN2.
    CAS No.: 54-77-3.
    Activity DMPP activates α4 nicotinic channels expressed in Xenopus oocytes with an IC50 of 0.77 μM1.
      • Bertrand, D. et al. (1990) Proc. Natl. Acad.Sci. U.S.A. 87, 1993.

    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.
      • Alomone Labs 1,1-Dimethyl-4-phenylpiperazinium iodide activates muscle fetal α1/β1/γ/δ nAChR heterologously expressed in Xenopus oocytes.
        A. Time course of current repetitive and reversible activation by 100 µM 1,1-Dimethyl-4-phenylpiperazinium iodide (#D-125). Holding potential was -60 mV and currents were elicited by application of 100 µM acetylcholine. B. Example traces of current responses to 10 mM or 100 mM acetylcholine as indicated.
      • Blanchet, M.R. et al. (2007) J. Leuk. Biol. 81, 1245.
      • Dorion, G. et al. (2005) Am. J. Physiol. 288, L1139.
      • Guandalini, L. et al. (2005) Il Farmaco 60, 99.
      • Bertrand, D. et al. (1990) Proc. Natl. Acad.Sci. U.S.A. 87, 1993.
      • Kalra, R. et al. (2004) Clin. Diagn. Lab. Immunol. 11, 563.
      • Matsunaga K. et al. (2001) J. Immunol. 167, 6518.
      • Nicotinic acetylcholine receptors (nAChRs) are ligand-gated ion channels comprising five subunits. The muscle-type receptor is made of two α1 β, γ and δ subunits, while the neuronal nicotinic receptors are formed by different combination of 2 α and 3 β subunits. These receptors are expressed on neuronal and different types of non-neuronal cells like: lymphocytes, alveolar macrophages, airway smooth muscle cells, epithelial cells, and fibroblasts1.

        nAChRs mediate numerous specific physiological functions depending on the type of cell involved. For example, nicotine induces the release of dopamine in the central nervous system and stimulates nitric oxide (NO) synthase gene expression in endothelial cells2.

        1,1-Dimethyl-4-phenylpiperazinium iodide (DMPP) is a selective nAChR agonist. For a long time, DMPP was considered to be the prototype of ganglionic stimulating agents, since it was able to activate the nicotinic receptor in sympathetic ganglia with higher potency than the muscle-type. However, it has since been shown that DMPP binds with higher affinity to the nicotinic receptor in the brain3. 1,1-Dimethyl-4-phenylpiperazinium iodide activates had IC50 of 0.77 uM on α4 nicotinic channel expressed in Xenopus oocytes4.

        Nicotinic agonists, such as DMPP, have anti-inflammatory effects in mouse models of hypersensitivity pneumonitis, asthma, airway inflammation, and Type I diabetes5. DMPP reduces the release of IL-1 and TNF from isolated spleen cells, and the release of TNF and IL-6 from macrophages6.

    Target nAChR
    Last update: 02/07/2019

    1,1-Dimethyl-4-phenylpiperazinium iodide (#D-125) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use