Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)

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Chemical Compound Review:

AC1L2WWH cyclohexyl-[(4,4-dimethyl- 2,3,5,6...

Synonyms: L001247, 124393-85-7, Silahexocyclium, Sila-hexocyclium

Waelbroeck, M. et al., Wess, J. et al., Kopp, R. et al.

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High impact information on Silahexocyclium

AQ-RA 741, himbacine, and sila-hexocyclium bound to the various chimeric receptors, expressed in COS-7 cells, with affinity profiles indicative of multiple receptor domains contributing to the subtype selectivities of these antagonists [1].
4. In binding studies, o-methoxy-sila-hexocyclium (M1 = M4 > or = M3 > or = M2) had a much lower affinity than sila-hexocyclium for the four receptor subtypes, and discriminated the receptor subtypes more poorly than sila-hexocyclium (M1 = M3 > M4 > M2) [2].
The M3 subtype-selective antagonists sila-hexocyclium and hexahydro-sila-difenidol had high affinity to the muscarinic receptors in HT-29 cells (KD = 3.1 nM and 27 nM, respectively) and inhibited IP release at nanomolar concentrations [3].

References

Structural basis of the subtype selectivity of muscarinic antagonists: a study with chimeric m2/m5 muscarinic receptors. Wess, J., Gdula, D., Brann, M.R. Mol. Pharmacol. (1992) [Pubmed]
Binding and functional properties of hexocyclium and sila-hexocyclium derivatives to muscarinic receptor subtypes. Waelbroeck, M., Camus, J., Tastenoy, M., Feifel, R., Mutschler, E., Tacke, R., Strohmann, C., Rafeiner, K., Rodrigues de Miranda, J.F., Lambrecht, G. Br. J. Pharmacol. (1994) [Pubmed]
Human HT-29 colon carcinoma cells contain muscarinic M3 receptors coupled to phosphoinositide metabolism. Kopp, R., Lambrecht, G., Mutschler, E., Moser, U., Tacke, R., Pfeiffer, A. Eur. J. Pharmacol. (1989) [Pubmed]

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