Sabcomeline

Last updated
Sabcomeline
Sabcomeline skeletal.svg
Clinical data
ATC code
  • None
Legal status
Legal status
  • Never marketed
Identifiers
  • (3Z,3R)-N-methoxy-1-azabicyclo[2.2.2]octane-3-carboximidoyl cyanide
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
UNII
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
Formula C10H15N3O
Molar mass 193.250 g·mol−1
3D model (JSmol)
  • C2CC1CCN2CC1\C(\C#N)=N\OC

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 . [2]

See also

References

  1. ↑ Loudon JM, Bromidge SM, Brown F, et al. (December 1997). "SB 202026: a novel muscarinic partial agonist with functional selectivity for M1 receptors" . The Journal of Pharmacology and Experimental Therapeutics. 283 (3): 1059–68. doi:10.1016/S0022-3565(24)37135-6. PMID   9399977.
  2. 1 2 Wood MD, Murkitt KL, Ho M, Watson JM, Brown F, Hunter AJ, Middlemiss DN (April 1999). "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. doi:10.1038/sj.bjp.0702463. PMC   1565933 . PMID   10323594.
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