fbpx
Wikipedia

Talsaclidine

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,[3][4] 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]

Talsaclidine
Clinical data
ATC code
  • None
Pharmacokinetic data
Bioavailability70%
Protein binding7%
ExcretionRenal (86%)
Identifiers
  • (3R)-3-(Prop-2-yn-1-yloxy)-1-azabicyclo[2.2.2]octane
CAS Number
  • 147025-53-4
PubChem CID
  • 71792
ChemSpider
  • 64819
UNII
  • 1O8VSL798T
CompTox Dashboard (EPA)
  • DTXSID20163565
ECHA InfoCard100.161.949
Chemical and physical data
FormulaC10H15NO
Molar mass165.236 g·mol−1
3D model (JSmol)
  • Interactive image
  • O([C@@H]2C1CCN(CC1)C2)CC#C

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. S2CID 23323985.
  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.

talsaclidine, 2014, selective, muscarinic, acetylcholine, receptor, agonist, which, acts, full, agonist, subtype, partial, agonist, subtypes, under, development, treatment, alzheimer, disease, showed, only, modest, poor, efficacy, rhesus, monkeys, humans, resp. 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 3 4 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 TalsaclidineClinical dataATC codeNonePharmacokinetic dataBioavailability70 Protein binding7 ExcretionRenal 86 IdentifiersIUPAC name 3R 3 Prop 2 yn 1 yloxy 1 azabicyclo 2 2 2 octaneCAS Number147025 53 4PubChem CID71792ChemSpider64819UNII1O8VSL798TCompTox Dashboard EPA DTXSID20163565ECHA InfoCard100 161 949Chemical and physical dataFormulaC 10H 15N OMolar mass165 236 g mol 13D model JSmol Interactive imageSMILES O C H 2C1CCN CC1 C2 CC CSee also editAceclidine VedaclidineReferences edit 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 Walland A Burkard S Hammer R Troger 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 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 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 S2CID 23323985 Adamus WS Leonard JP Troger 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 Retrieved from https en wikipedia org w index php title Talsaclidine amp oldid 1217259853, wikipedia, wiki, book, books, library,

article

, read, download, free, free download, mp3, video, mp4, 3gp, jpg, jpeg, gif, png, picture, music, song, movie, book, game, games.