SB 202026: a novel muscarinic partial agonist with functional selectivity for M1 receptors.

@article{Loudon1997SB2A,
  title={SB 202026: a novel muscarinic partial agonist with functional selectivity for M1 receptors.},
  author={J. M. Loudon and Steven M Bromidge and Fraser Brown and Michael S. G. Clark and Jonathan P. Hatcher and Jeff Hawkins and Graham J. P. Riley and G. A. Noy and Barry S Orlek},
  journal={The Journal of pharmacology and experimental therapeutics},
  year={1997},
  volume={283 3},
  pages={1059-68}
}
The finding that ascending cholinergic systems are severely degenerated in Alzheimer's disease has driven the search for a cholinomimetic therapy. Adverse effects observed with cholinesterase inhibitors and high-efficacy muscarinic agonists led us to design compounds with an improved profile. SB 202026 (R-(Z)-(+)-alpha-(methoxyimino)-1-azabicyclo[2.2.2] octane-3-acetonitrile) displaced [3H]-oxotremorine-M from muscarinic receptors in the rat brain with high affinity (IC50 = 14 nM), a potency… CONTINUE READING
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