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Chemical Compound Review

Alvameline     3-(2-ethyltetrazol-5-yl)-1- methyl-5,6...

Synonyms: CHEMBL131428, SureCN6024870, CHEBI:317676, AKOS006328125, AC1L434B, ...
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Disease relevance of Alvameline


Psychiatry related information on Alvameline


High impact information on Alvameline

  • Lu 25-109 [5-(2-ethyl-2H-tetrazol-5-yl)-1,2,3,6-tetrahydro-1-methylpyridine] , has M agonistic and M2/M3 antagonistic effects at muscarinic receptors in vitro; a pharmacological profile that may be beneficial in treatment of Alzheimer's disease [1].
  • In vivo muscarinic cholinergic mediated effects of Lu 25-109, a M1 agonist and M2/M3 antagonist in vitro [1].
  • Lu 25-109 had no effect on mean blood pressure in anaesthetized rats [1].
  • Lu 25-109 and O-Me-THPO produced a significant increase in heart rate [1].
  • Radioligand binding experiments demonstrated a small difference in affinity for Lu 25-109 in the parotid gland compared with the bladder, the pKi values being 6.2+/-0.1 versus 6.5+/-0.1 (n=4) [3].

Biological context of Alvameline

  • Biotransformation of the M1-muscarinic agonist Lu 25-109 (5-(2-ethyl-2H-tetrazol-5-yl)-1-methyl-1,2,3,6-tetrahydropyridine) , in development for the treatment of Alzheimer's disease, was investigated to obtain information on the identity of human hepatic cytochrome P-450 enzymes involved in its metabolism [4].
  • This double-blind, placebo-controlled, two-part, inpatient bridging study was designed to evaluate the safety and tolerability of multiple oral doses of Lu 25-109 in patients with Alzheimer's Disease(AD), and to determine the maximum tolerated dose (MTD) in this population [5].

Anatomical context of Alvameline


Associations of Alvameline with other chemical compounds

  • The aim of this study was to evaluate the effects of a novel antimuscarinic agent, Lu 25-109, a partial M1 receptor agonist, and M2/M3 receptor antagonist in human and pig detrusor to establish its affinity for muscarinic receptors in human detrusor and parotid gland and to compare the results with those obtained with oxybutynin [3].
  • To examine the effects of the combined muscarinic ml-agonist/m2-antagonist Lu 25-109 on regulated processing of the amyloid protein precursor (APP), we used both transfected cells expressing human muscarinic m1 or m2 acetylcholine receptors, and fresh rat hippocampal slices [7].

Gene context of Alvameline

  • Both responses appeared to reflect post-translational mechanisms because levels of APP message were unchanged after 60 minutes of stimulation with Lu 25-109 [7].
  • In as much as stimulation of APPs secretion is associated with reduced formation of A beta peptides, Lu 25-109 may be useful to reduce A beta generation, and thus, slow amyloid plaque formation [7].
  • One metabolite, Lu 32-181 (N-oxide), could be reduced back to Lu 25-109, a reaction not inhibited by the applied cytochrome P-450 inhibitors [4].

Analytical, diagnostic and therapeutic context of Alvameline

  • In the present study, we compare functional in vivo effects of Lu 25-109 and reference compounds in animal models of muscarinic cholinergic function [1].
  • Thus, the titration regimen employed did not improve the overall tolerability of Lu 25-109 [5].


  1. In vivo muscarinic cholinergic mediated effects of Lu 25-109, a M1 agonist and M2/M3 antagonist in vitro. Sánchez, C., Arnt, J., Didriksen, M., Dragsted, N., Moltzen Lenz, S., Matz, J. Psychopharmacology (Berl.) (1998) [Pubmed]
  2. Lu 25-109, a muscarinic agonist, fails to improve cognition in Alzheimer's disease. Lu25-109 Study Group. Thal, L.J., Forrest, M., Loft, H., Mengel, H. Neurology (2000) [Pubmed]
  3. Actions of the new antimuscarinic compound Lu 25-109 on isolated human and pig detrusor. Waldeck, K., Larsson, B., Sandberg, B., Andersson, K.E. Neurourology and urodynamics. (2002) [Pubmed]
  4. 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. Jensen, K.G., Dalgaard, L. Drug Metab. Dispos. (1999) [Pubmed]
  5. A bridging study of LU 25-109 in patients with probable Alzheimer's disease. Sramek, J.J., Forrest, M., Mengel, H., Jhee, S.S., Hourani, J., Cutler, N.R. Life Sci. (1998) [Pubmed]
  6. Evaluation of blood-brain barrier passage of a muscarine M1 agonist and a series of analogous tetrahydropyridines measured by in vivo microdialysis. Sveigaard, H.H., Dalgaard, L. Pharm. Res. (2000) [Pubmed]
  7. Lu 25-109, a combined m1 agonist and m2 antagonist, modulates regulated processing of the amyloid precursor protein of Alzheimer's disease. Müller, D., Wiegmann, H., Langer, U., Moltzen-Lenz, S., Nitsch, R.M. Journal of neural transmission (Vienna, Austria : 1996) (1998) [Pubmed]
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