Talsaclidine

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Talsaclidine
Skeletal formula of talsaclidine
Ball-and-stick model of the talsaclidine molecule
Systematic (IUPAC) name
(3R)-3-(prop-2-yn-1-yloxy)-1-azabicyclo[2.2.2]octane
Clinical data
Pharmacokinetic data
Bioavailability 70%
Protein binding 7%
Excretion Renal (86%)
Identifiers
147025-53-4
None
PubChem CID 71792
ChemSpider 64819
UNII 1O8VSL798T YesY
Chemical data
Formula C10H15NO
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[edit]

References[edit]

  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. doi:10.1016/0024-3205(93)90304-L. PMID 8441328. 
  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. doi:10.1016/S0024-3205(97)00037-4. PMID 9121364. 
  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. doi:10.1016/S0024-3205(01)01057-8. PMID 11392631. 
  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. doi:10.1007/s00213-002-1105-3. PMID 12122487. 
  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. doi:10.1016/0024-3205(95)00024-Z. PMID 10188789.