DOI: 10.1055/s-00000084

Synthesis

References

Sala M. Braida D. Pucci L. Manfredi I. Marks MJ. Wageman CR. Grady SR. Loi B. Fucile S. Fasoli F. Zoli M. Tasso B. Sparatore F. Clementi F. Gotti C.
Br. J. Pharmacol. 2013;
168: 835 ; CC4 7 was reported to bind to the α4β2 and α7 nicotinic acetylcholine receptors with Ki values of 26 nM and 13000 nM, respectively. This compares to Ki values for cytisine 6a of 2.1 nM (at α4β2) and 228 nM (at α7). Correspondingly, whereas CC4 is less potent at α4β2, this dimeric ligand is more selective for this receptor than for α7 when compared to cytisine (and indeed varenicline, see Figure 1)

Sala M. Braida D. Pucci L. Manfredi I. Marks MJ. Wageman CR. Grady SR. Loi B. Fucile S. Fasoli F. Zoli M. Tasso B. Sparatore F. Clementi F. Gotti C.
Br. J. Pharmacol. 2013;
168: 835 ; CC4 7 was reported to bind to the α4β2 and α7 nicotinic acetylcholine receptors with Ki values of 26 nM and 13000 nM, respectively. This compares to Ki values for cytisine 6a of 2.1 nM (at α4β2) and 228 nM (at α7). Correspondingly, whereas CC4 is less potent at α4β2, this dimeric ligand is more selective for this receptor than for α7 when compared to cytisine (and indeed varenicline, see Figure 1)

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