Sabcomeline Explained

Sabcomeline (Memric; SB-202,026) is a selective M1 receptor partial agonist that was under development for the treatment of Alzheimer's disease.[1] It made it to phase III clinical trials before being discontinued due to poor results.

It is a non-selective agonist of all five muscarinic acetylcholine receptors with similar affinities.[2] However, functional selectivity for the M1 receptor has been claimed in vitro and in vivo.

See also

Notes and References

  1. Loudon JM, Bromidge SM, Brown F, etal . SB 202026: a novel muscarinic partial agonist with functional selectivity for M1 receptors . The Journal of Pharmacology and Experimental Therapeutics . 283 . 3 . 1059–68 . December 1997 . 9399977 .
  2. Wood MD, Murkitt KL, Ho M, Watson JM, Brown F, Hunter AJ, Middlemiss DN . Functional comparison of muscarinic partial agonists at muscarinic receptor subtypes hM1, hM2, hM3, hM4 and hM5 using microphysiometry . Br J Pharmacol . 126 . 7 . 1620–1624 . April 1999 . 10323594 . 1565933 . 10.1038/sj.bjp.0702463 .

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