TABLE 2.
Selective M1R/M3R agents used for research and under clinical investigation.
| Agent | Activity/MR selectivity | Source | Potential clinical applications |
|---|---|---|---|
| 2′ biaryl amides Budzik et al. (2010) | M1R Agonist | GlaxoSmithKline | |
| 77-LH-28-1 Langmead et al. (2008) | M1R Agonist | Alzheimer’s disease, schizophrenia | |
| AC-42 Heinrich et al. (2009) | M1R Agonist | ||
| HTL0018318 Bakker et al. (2021) | M1R Agonist | Sosei Heptares Therapeutics | Dementia |
| PPBI Wood et al. (2017) | M1R Agonist | AstraZeneca | Analgesia |
| Nitrocaramiphen Hudkins et al. (1993) | M1R Ant | ||
| PIPE-307 | M1R Ant | Pipeline Therapeutics | Multiple sclerosis; clinical trials (NCT04941781, NCT04725175) |
| PIPE-359 Schrader et al. (2021) | M1R Ant | Pipeline Therapeutics | |
| Telenzepine Eveleigh et al. (1989) | M1R Ant | Theracos | Peptic ulcer disease; obesity (Clinical trial NCT01155531) |
| VU 0255035 Tsentsevitsky et al. (2017) | M1R Ant | Vanderbilt University | Seizure disorder |
| L-689,660 Hargreaves et al., (1992) | M1R, M3R Agonist | ||
| Oxotremorine Veena et al., (2011) | M1R, M3R Agonist | ||
| R2HBJJ Hua et al. (2012) | M1R, M3R Ant | Non-small cell lung cancer | |
| McN-A-343 Mitchelson (2012b) | M1R, M4R Agonist | ||
| Xanomeline Heinrich et al. (2009) | M1R, M4R Agonist | Alzheimer’s disease | |
| 4-DAMP Honda et al. (2007) | M3R Ant | ||
| AZD8871 Aparici et al. (2019) | M3R Ant | Almirall | Chronic obstructive lung disease |
| DA-8010 Lee et al. (2019) | M3R Ant | Overactive bladder | |
| DAU 5884 Gosens et al. (2004) | M3R Ant | ||
| J-104129 Mitsuya et al. (1999) | M3R Ant | Merck | Obstructive airway disease |
| Temiverine Kikukawa et al. (1998) | M3R Ant | Urinary incontinence | |
| YM905 Kobayashi et al. (2001) | M3R Ant | Astellas (Yamanouchi) | Irritable bowel syndrome |
| Arecoline Heinrich et al. (2009) | NS Agonist | Alzheimer’s disease, schizophrenia |
Ant, antagonist; NS, nonselective.