(-)-Cytisine

Baphitoxine, Sophorine
A nAChR Agonist and a Partial Agonist of β2 Subunit
Cat #: C-130
Alternative Name Baphitoxine, Sophorine
  • Lyophilized Powder
  • Bioassay Tested
  • Source Synthetic
    MW: 190.2
    Purity: >95%
    Effective concentration 40 nM - 1 μM.
    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.
    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.
      • 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.
      • (-)-Cytisine is an alkaloid, which occurs naturally in several types of plants as well as in animals feeding on them (see an 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 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: 03/03/2019

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

    For research purposes only, not for human use