sabcomeline
{{Short description|Chemical compound}}
{{Drugbox
| IUPAC_name = (3Z,3R)-N-methoxy-1-azabicyclo[2.2.2]octane-3-carboximidoyl cyanide
| image = Sabcomeline skeletal.svg
| tradename =
| pregnancy_category =
| legal_status = Never marketed
| routes_of_administration =
| bioavailability =
| metabolism =
| elimination_half-life =
| excretion =
| CAS_number_Ref = {{cascite|correct|CAS}}
| index2_label = HCl
| CAS_number2_Ref = {{cascite|correct|CAS}}
| CAS_number2 = 159912-58-0
| UNII2_Ref = {{fdacite|correct|FDA}}
| UNII2 = A24BK93DRR
| CAS_number = 159912-53-5
| ATC_prefix = None
| PubChem = 9577995
| IUPHAR_ligand = 306
| ChemSpiderID = 7852359
| UNII_Ref = {{fdacite|correct|FDA}}
| UNII = P8P92V596C
| ChEMBL = 134641
| C=10 | H=15 | N=3 | O=1
| smiles = 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.{{cite journal |vauthors=Loudon JM, Bromidge SM, Brown F, etal | title = SB 202026: a novel muscarinic partial agonist with functional selectivity for M1 receptors | journal = The Journal of Pharmacology and Experimental Therapeutics | volume = 283 | issue = 3 | pages = 1059–68 |date=December 1997 | doi = 10.1016/S0022-3565(24)37135-6 | pmid = 9399977 | url = http://jpet.aspetjournals.org/cgi/pmidlookup?view=long&pmid=9399977| url-access = subscription }} 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.{{cite journal | vauthors = Wood MD, Murkitt KL, Ho M, Watson JM, Brown F, Hunter AJ, Middlemiss DN | title = Functional comparison of muscarinic partial agonists at muscarinic receptor subtypes hM1, hM2, hM3, hM4 and hM5 using microphysiometry | journal = Br J Pharmacol | volume = 126 | issue = 7 | pages = 1620–1624 | date = April 1999 | pmid = 10323594 | pmc = 1565933 | doi = 10.1038/sj.bjp.0702463 | url = }} However, functional selectivity for the M1 receptor has been claimed in vitro and in vivo.
See also
References
{{Reflist}}
{{Anti-dementia drugs}}
{{Muscarinic acetylcholine receptor modulators}}