Talsaclidine

Talsaclidine

Talsaclidine
Systematic (IUPAC) name
(3R)-3-(prop-2-yn-1-yloxy)-1-azabicyclo[2.2.2]octane
Clinical data
Legal status
?
Pharmacokinetic data
Bioavailability 70%
Protein binding 7%
Excretion Renal (86%)
Identifiers
CAS number
ATC code None
PubChem
ChemSpider
UNII  YesY
Chemical data
Formula C10H15NO 
Mol. mass 165.23 g/mol

Talsaclidine (WAL-2014) is a non-selective muscarinic acetylcholine receptor agonist which acts as a full agonist at the M1 subtype, and as a partial agonist at the M2 and M3 subtypes.[1][2][3] It was under development for the treatment of Alzheimer's disease but showed only modest or poor efficacy in rhesus monkeys and humans, respectively,[4][3] perhaps due to an array of dose-limiting side effects including increased heart rate and blood pressure, increased salivation, urinary frequency and burning upon urination, increased lacrimation and nasal secretion, abnormal accommodation, heartburn, upset stomach as well as cramps, nausea, vomiting and diarrhea, excessive sweating and palpitations.[5]

See also

References

  1. ^ Ensinger HA, Doods HN, Immel-Sehr AR, et al. (1993). "WAL 2014--a muscarinic agonist with preferential neuron-stimulating properties". Life Sciences 52 (5-6): 473–80.  
  2. ^ Walland A, Burkard S, Hammer R, Tröger W (1997). "In vivo consequences of M1-receptor activation by talsaclidine". Life Sciences 60 (13-14): 977–84.  
  3. ^ a b Wienrich M, Meier D, Ensinger HA, et al. (April 2001). "Pharmacodynamic profile of the M1 agonist talsaclidine in animals and man". Life Sciences 68 (22-23): 2593–600.  
  4. ^ Terry AV, Buccafusco JJ, Borsini F, Leusch A (July 2002). "Memory-related task performance by aged rhesus monkeys administered the muscarinic M(1)-preferring agonist, talsaclidine". Psychopharmacology 162 (3): 292–300.  
  5. ^ Adamus WS, Leonard JP, Tröger W (1995). "Phase I clinical trials with WAL 2014, a new muscarinic agonist for the treatment of Alzheimer's disease". Life Sciences 56 (11-12): 883–90.