219581-36-9

Alvameline (Lu 25-109) maleate is a partial agonist of M1 and an antagonist of M2/M3. Alvameline maleate competitively antagonizes contractions induced by ammonium chloride (HY-Y1269) and electrical field stimulation in human detrusor muscle, indicating its potential application in regulating bladder function. Additionally, alvameline maleate can improve cognitive function following traumatic brain injury in rats[1].

[1] Jensen KG, et al. In vitro metabolism of the M1-muscarinic agonist 5-(2-ethyl-2H-tetrazol-5-yl)-1-methyl-1,2,3,6-tetrahydropyridine by human hepatic cytochromes P-450 determined at pH 7.4 and 8.5. Drug Metab Dispos. 1999 Jan;27(1):125-32. PMID:9884321
[2] Waldeck K, et al. Actions of the new antimuscarinic compound Lu 25-109 on isolated human and pig detrusor. Neurourol Urodyn. 2002;21(1):92-8. DOI:10.1002/nau.2124
[3] Pike BR, et al. Chronic administration of a partial muscarinic M1 receptor agonist attenuates decreases in forebrain choline acetyltransferase immunoreactivity following experimental brain trauma. Exp Neurol. 1997 Sep;147(1):55-65 DOI:10.1006/exnr.1997.6582