Catalog Number: 5236
Chemical Name: (1R,5S)-1,2,3,4,5,6-Hexahydro-3-[2-[(1R,5S)-1,5,6,8-tetrahydro-8-oxo-1,5-methano-2H-pyrido[1,2-a][1,5]diazocin-3(4H)-yl]ethyl]-1,5-methano-8H-pyrido[1,2-a][1,5]diazocin-8-one
Biological Activity
High affinity and subtype selective α6β2 and α4β2 partial agonist (Ki values are 12 and 26nM for rat α6β2 and α4β2 receptors respectively). Has low affinity for α3β4 and α7 receptors (Ki values are 4.8 and 13 μM for human α3β4 and rat α7 receptors respectively). Stimulates dopamine release from striatal slices in vitro. Attenuates nicotine-induced self-administration and conditional place preference in rats.
Technical Data
  • M.Wt:
    406.52
  • Formula:
    C24H30N4O2
  • Solubility:
    Soluble to 20 mM in water and to 100 mM in DMSO
  • Purity:
    >98%
  • Storage:
    Store at +4°C
  • CAS No:
    492-02-4
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. CC4, a dimer of cytisine, is a selective partial agonist at α4β2/α6β2 nAChR with improved selectivity for tobacco smoking c
    Sala et al.
    Br.J.Pharmacol., 2013;168:835
  2. Long-term exposure to the new nicotinic antagonist 1,2-bisN-cytisinylethane upregulates nicotinic receptor subtypes of SH-SY5Y human neuroblastoma cells.
    Riganti et al.
    Br.J.Pharmacol., 2005;146:1096
  3. Nitrogen substitution modifies the activity of cytisine on neuronal nicotinic receptor subtypes.
    Carbonnelle et al.
    Eur.J.Pharmacol., 2003;471:85

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