Talsaclidine

{{Short description|Chemical compound}}

{{Drugbox

| IUPAC_name = (3R)-3-(Prop-2-yn-1-yloxy)-1-azabicyclo[2.2.2]octane

| image = Talsaclidine.svg

| alt = Skeletal formula of talsaclidine

| width = 175

| image2 = Talsaclidine 3D ball.png

| alt2 = Ball-and-stick model of the talsaclidine molecule

| tradename =

| pregnancy_category =

| legal_status =

| routes_of_administration =

| bioavailability = 70%

| protein_bound = 7%

| metabolism =

| elimination_half-life =

| excretion = Renal (86%)

| CAS_number = 147025-53-4

| ATC_prefix = None

| ATC_suffix =

| PubChem = 71792

| ChemSpiderID = 64819

| UNII_Ref = {{fdacite|correct|FDA}}

| UNII = 1O8VSL798T

| C=10 | H=15 | N=1 | O=1

| 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.{{cite journal |vauthors=Ensinger HA, Doods HN, Immel-Sehr AR, etal | title = WAL 2014--a muscarinic agonist with preferential neuron-stimulating properties | journal = Life Sciences | volume = 52 | issue = 5–6 | pages = 473–80 | year = 1993 | pmid = 8441328 | doi = 10.1016/0024-3205(93)90304-L}}{{cite journal |vauthors=Walland A, Burkard S, Hammer R, Tröger W | title = In vivo consequences of M1-receptor activation by talsaclidine | journal = Life Sciences | volume = 60 | issue = 13–14 | pages = 977–84 | year = 1997 | pmid = 9121364 | doi = 10.1016/S0024-3205(97)00037-4}}{{cite journal |vauthors=Wienrich M, Meier D, Ensinger HA, etal | title = Pharmacodynamic profile of the M1 agonist talsaclidine in animals and man | journal = Life Sciences | volume = 68 | issue = 22–23 | pages = 2593–600 |date=April 2001 | pmid = 11392631 | doi = 10.1016/S0024-3205(01)01057-8}} It was under development for the treatment of Alzheimer's disease but showed only modest or poor efficacy in rhesus monkeys and humans, respectively,{{cite journal |vauthors=Terry AV, Buccafusco JJ, Borsini F, Leusch A | title = Memory-related task performance by aged rhesus monkeys administered the muscarinic M(1)-preferring agonist, talsaclidine | journal = Psychopharmacology | volume = 162 | issue = 3 | pages = 292–300 |date=July 2002 | pmid = 12122487 | doi = 10.1007/s00213-002-1105-3 | s2cid = 23323985 }} 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.{{cite journal |vauthors=Adamus WS, Leonard JP, Tröger W | title = Phase I clinical trials with WAL 2014, a new muscarinic agonist for the treatment of Alzheimer's disease | journal = Life Sciences | volume = 56 | issue = 11–12 | pages = 883–90 | year = 1995 | pmid = 10188789 | doi = 10.1016/0024-3205(95)00024-Z}}