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. It was under development for the treatment of Alzheimer's disease but showed only modest or poor efficacy in rhesus monkeys and humans, respectively, 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. — Wikipedia
Clinical trial activity
7 trials · 1 clinical orgs · 0 marketing orgs
Earliest trial started Jul 1, 1998 (NCT02264067)
Timeline
Indications
Mechanism of action
Muscarinic acetylcholine receptor M1 agonist
- Alpha-1a adrenergic receptorANTAGONIST
ADRA1A antagonist
- Muscarinic acetylcholine receptor M2PARTIAL AGONIST
Muscarinic acetylcholine receptor M2 partial agonist
- Muscarinic acetylcholine receptor M3PARTIAL AGONIST
Muscarinic acetylcholine receptor M3 partial agonist
Chemistry & pharmacology
SMILES
C#CCO[C@H]1CN2CCC1CC2- Mol. weight
- 165.24 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- Yes
- Chirality
- Single Stereoisomer
- Inorganic
- No
- Polymer
- No
Oral
No
Parenteral
No
Topical
No
Sources
- WikipediaTalsaclidine ↗
- ChEMBLCHEMBL2111051 ↗
Also known as
- talsaclidine
- talsaclidine
- talsaclidine
- wal2014
- wal2014
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT02249351 | Phase 2 | Dec 1, 1999 | Boehringer Ingelheim |
| NCT02264093 | Phase 1 | Nov 1, 1999 | Boehringer Ingelheim |
| NCT02248116 | Phase 2/Phase 3 (Phase 3) | May 1, 1999 | Boehringer Ingelheim |
| NCT02264080 | Phase 1 | Mar 1, 1999 | Boehringer Ingelheim |
| NCT02264054 | Phase 1 | Feb 1, 1999 | Boehringer Ingelheim |
| NCT02249403 | Phase 2 | Jan 1, 1999 | Boehringer Ingelheim |
| NCT02264067 | Phase 1 | Jul 1, 1998 | Boehringer Ingelheim |
Organizations
Research & Development (1)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Boehringer Ingelheim | For profit | 7 | 7 | 3 | 1998 |