Talsaclidine information

Talsaclidine
Clinical data
ATC code	None;
Pharmacokinetic data
Bioavailability	70%
Protein binding	7%
Excretion	Renal (86%)
Identifiers
	IUPAC name (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 InfoCard	100.161.949
Chemical and physical data
Formula	C10H15NO
Molar mass	165.236 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES O([C@@H]2C1CCN(CC1)C2)CC#C;

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]

^ 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, 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.
^ ^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, 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.

[pmid8441328-1] 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.

[pmid9121364-2] 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.

[pmid11392631-3] 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.

[pmid12122487-4] 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.

[pmid10188789-5] 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.

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Clinical data


ATC code	None
Pharmacokinetic data
Bioavailability	70%
Protein binding	7%
Excretion	Renal (86%)
Identifiers
IUPAC name (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 InfoCard	100.161.949
Chemical and physical data
Formula	C₁₀H₁₅NO
Molar mass	165.236 g·mol⁻¹
3D model (JSmol)	Interactive image
SMILES O([C@@H]2C1CCN(CC1)C2)CC#C