Talsaclidine Explained

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]

See also

• Aceclidine
• Vedaclidine

Notes and References

1. Ensinger HA, Doods HN, Immel-Sehr AR, etal . WAL 2014--a muscarinic agonist with preferential neuron-stimulating properties . Life Sciences . 52 . 5–6 . 473–80 . 1993 . 8441328 . 10.1016/0024-3205(93)90304-L.
2. Walland A, Burkard S, Hammer R, Tröger W . In vivo consequences of M1-receptor activation by talsaclidine . Life Sciences . 60 . 13–14 . 977–84 . 1997 . 9121364 . 10.1016/S0024-3205(97)00037-4.
3. Wienrich M, Meier D, Ensinger HA, etal . Pharmacodynamic profile of the M1 agonist talsaclidine in animals and man . Life Sciences . 68 . 22–23 . 2593–600 . April 2001 . 11392631 . 10.1016/S0024-3205(01)01057-8.
4. Terry AV, Buccafusco JJ, Borsini F, Leusch A . Memory-related task performance by aged rhesus monkeys administered the muscarinic M(1)-preferring agonist, talsaclidine . Psychopharmacology . 162 . 3 . 292–300 . July 2002 . 12122487 . 10.1007/s00213-002-1105-3 . 23323985 .
5. Adamus WS, Leonard JP, Tröger W . 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 . 1995 . 10188789 . 10.1016/0024-3205(95)00024-Z.