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(-)-Cytisine

Baphitoxine, Sophorine

A nAChR Agonist and a Partial Agonist of β2 Subunit

Cat #: C-130
Alternative Name Baphitoxine, Sophorine
Lyophilized Powder yes
  • Bioassay Tested
  • Source Synthetic
    MW: 190.2
    Purity: >95%
    Effective concentration 40 nM - 1 μM.
    Structure
    Chemical name (1R,5S)-1,2,3,4,5,6-hexahydro-1,5-methano-8H-pyrido[1,2-a][1,5]diazocin-8-one.
    Molecular formula C11H14N2O.
    CAS No.: 485-35-8
    Activity (-)-Cytisine is a potent and selective agonist of neuronal nAChR. It acts as a partial agonist at β2-containing nAChR1,2.
    References-Activity
    1. Albuquerque, E.X. et al. (2009) Physiol. Rev. 89, 73.
    2. Luetje, C.W. and Patrick, J. (1991) J. Neurosci. 11, 837.
    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 Any aqueous buffer (up to 100mM stock). Centrifuge all product preparations before use (10000 x g 5 min).
    Storage of solutions Up to one week at 4°C or six months at -20°C.
    Our bioassay
    • Alomone Labs (-)-Cytisine activates α2/β4 nicotinic acetylcholine receptor channels heterologously expressed in Xenopus oocytes.
      Alomone Labs (-)-Cytisine activates α2/β4 nicotinic acetylcholine receptor channels heterologously expressed in Xenopus oocytes.
      Current traces of α2/β4 nicotinic acetylcholine receptor channels activity at -60 mV holding potential. The bars above the trace represent periods where (-)-Cytisine (#C-130) or acetylcholine were applied at the indicated concentration.
    References - Scientific background
    1. Banko, P.C. et al. (2002) J. Chem. Ecol. 28, 1393.
    2. Albuquerque, E.X. et al. (2009) Physiol. Rev. 89, 73.
    3. Luetje, C.W. and Patrick, J. (1991) J. Neurosci. 11, 837.
    4. Chavez-Noriega, L.E. et al. (1997) J. Pharmacol. Exp. Ther. 280, 346.
    5. Papke, R.L. and Heinemann, S.F. (1994) Mol. Pharmacol. 45, 142.
    6. Mineur, Y.S. et al. (2007) Neuropharmacology 52, 1256.
    7. Reavill, C. et al. (1990) Neuropharmacology 29, 619.
    Scientific background

    (-)-Cytisine is an alkaloid, which occurs naturally in several types of plants as well as in animals feeding on them (see example in reference 1). (-)-Cytisine is a potent and selective agonist of neuronal nAChR2. It acts as a partial agonist of β2-containing nAChR3.

    EC50s differ for different subunit-composed channels; for recombinant human channels expressed in Xenopus oocytes the following EC50 values were reported: 25 µM, 39 µM, 67 µM, 72 µM, 2.6 µM 0.9 µM and 71 µM for α2/β2, α2/β4, α3/β2, α3/β4, α4/β2, α4/β4 and α7 respectively4.

    However, in β2-containing channels, the response to acetylcholine (ACh) is largely reduced when applied in combination with (-)-Cytisine5. Therefore, when applied in vivo it exerts a compound effect of both activating certain nAchRs and inhibiting the effect of ACh on others. For example, (-)-Cytisine was found to have antidepressant-like effects in several animal models of antidepressant efficacy. This was probably achieved by inhibiting the effect of ACh on α2/β4 channel in the basolateral amygdala6.

    In another study, the effects of (-)-Cytisine were compared to nicotine. Rats were trained to discriminate nicotine from saline and it was confirmed that (-)-Cytisine had a nicotine-like discriminative effect, but it was much less potent than nicotine itself7.

    Target nAChR
    Last update: 12/08/2021

    (-)-Cytisine (#C-130) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use
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