Any drug that binds to and activates a muscarinic cholinergic receptor.
ChEBI ID: 38325
| Member | Definition | Class |
|---|---|---|
| arecoline | A tetrahydropyridine that is 1,2,5,6-tetrahydropyridine with a methyl group at position 1, and a methoxycarbonyl group at position 3. An alkaloid found in the areca nut, it acts as an agonist of muscarinic acetylcholine. | arecoline |
| bethanechol | The carbamic acid ester of 2-methylcholine. A slowly hydrolysed muscarinic agonist with no nicotinic effects, it is used as its chloride salt to increase smooth muscle tone, as in the gastrointestinal tract following abdominal surgery, treatment of gastro-oesophageal reflux disease, and as an alternative to catheterisation in the treatment of non-obstructive urinary retention. | bethanechol |
| bethanechol chloride | The chloride salt of bethanechol. A slowly hydrolysed muscarinic agonist with no nicotinic effects, it is used to increase smooth muscle tone, as in the gastrointestinal tract following abdominal surgery, treatment of gastro-oesophageal reflux disease, and as an alternative to catheterisation in the treatment of non-obstructive urinary retention. | bethanechol chloride |
| carbachol | carbachol | |
| distigmine | A carbamate ester resulting from the formal condensation of both carboxy groups of hexane-1,6-diylbis(methylcarbamic acid) with the hydroxy group of 3-hydroxy-1-methylpyridinium. | distigmine |
| guvacoline | The methyl ester of guvacine. | guvacoline |
| methacholine | A quaternary ammonium ion in which the nitrogen is substituted with three methyl groups and a 2-acetoxypropyl group. Parasympathomimetic bronchoconstrictor drug used in clinical diagnosis. | methacholine |
| oxotremorine m | oxotremorine M | |
| xanomeline | xanomeline |
| Timeframe | Studies, Drugs with This Role(%) | All Drugs % |
|---|---|---|
| pre-1990 | 6,113 (39.43) | 18.7374 |
| 1990's | 5,043 (32.53) | 18.2507 |
| 2000's | 2,757 (17.78) | 29.6817 |
| 2010's | 1,341 (8.65) | 24.3611 |
| 2020's | 250 (1.61) | 2.80 |
| Publication Type | Studies, Drugs with this Role (%) | All Drugs (%) |
|---|---|---|
| Trials | 174 (1.06%) | 5.53% |
| Reviews | 259 (1.58%) | 6.00% |
| Case Studies | 99 (0.60%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 15,895 (96.76%) | 84.16% |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| acetylcholinesterase | Homo sapiens (human) | Potency | 28.2737 | 2 | 2 |
| AR protein | Homo sapiens (human) | Potency | 26.6516 | 3 | 3 |
| ATP-dependent phosphofructokinase | Trypanosoma brucei brucei TREU927 | Potency | 42.5615 | 1 | 1 |
| Bloom syndrome protein isoform 1 | Homo sapiens (human) | Potency | 0.0008 | 2 | 2 |
| Chain A, Beta-lactamase | Escherichia coli K-12 | Potency | 5.0119 | 1 | 1 |
| Chain A, Ferritin light chain | Equus caballus (horse) | Potency | 0.3162 | 1 | 1 |
| Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASE | Homo sapiens (human) | Potency | 6.3096 | 1 | 1 |
| chromobox protein homolog 1 | Homo sapiens (human) | Potency | 33.3531 | 2 | 3 |
| cytochrome P450 2D6 isoform 1 | Homo sapiens (human) | Potency | 3.9811 | 1 | 1 |
| D(1A) dopamine receptor | Homo sapiens (human) | Potency | 0.7943 | 1 | 1 |
| estrogen nuclear receptor alpha | Homo sapiens (human) | Potency | 33.4915 | 1 | 1 |
| euchromatic histone-lysine N-methyltransferase 2 | Homo sapiens (human) | Potency | 10.2330 | 1 | 4 |
| EWS/FLI fusion protein | Homo sapiens (human) | Potency | 17.5434 | 3 | 3 |
| flap endonuclease 1 | Homo sapiens (human) | Potency | 8.4368 | 1 | 1 |
| GALC protein | Homo sapiens (human) | Potency | 0.7079 | 1 | 1 |
| geminin | Homo sapiens (human) | Potency | 6.3590 | 2 | 3 |
| GLI family zinc finger 3 | Homo sapiens (human) | Potency | 24.5818 | 2 | 4 |
| GLS protein | Homo sapiens (human) | Potency | 10.3006 | 1 | 2 |
| glucocorticoid receptor [Homo sapiens] | Homo sapiens (human) | Potency | 6.0070 | 1 | 1 |
| histone acetyltransferase KAT2A isoform 1 | Homo sapiens (human) | Potency | 11.2202 | 1 | 1 |
| IDH1 | Homo sapiens (human) | Potency | 29.0929 | 1 | 1 |
| Inositol monophosphatase 1 | Rattus norvegicus (Norway rat) | Potency | 3.5481 | 1 | 1 |
| lamin isoform A-delta10 | Homo sapiens (human) | Potency | 3.3117 | 1 | 2 |
| lethal factor (plasmid) | Bacillus anthracis str. A2012 | Potency | 12.5893 | 1 | 1 |
| M-phase phosphoprotein 8 | Homo sapiens (human) | Potency | 4.2684 | 1 | 2 |
| Microtubule-associated protein tau | Homo sapiens (human) | Potency | 1.5849 | 1 | 1 |
| mitogen-activated protein kinase 1 | Homo sapiens (human) | Potency | 3.9811 | 1 | 1 |
| muscarinic acetylcholine receptor M1 | Rattus norvegicus (Norway rat) | Potency | 0.0100 | 1 | 1 |
| NFKB1 protein, partial | Homo sapiens (human) | Potency | 28.1838 | 2 | 2 |
| nuclear receptor subfamily 1, group I, member 3 | Homo sapiens (human) | Potency | 31.6180 | 1 | 1 |
| peripheral myelin protein 22 | Rattus norvegicus (Norway rat) | Potency | 40.5334 | 1 | 2 |
| peroxisome proliferator activated receptor gamma | Homo sapiens (human) | Potency | 33.4889 | 1 | 1 |
| polyunsaturated fatty acid lipoxygenase ALOX12 | Homo sapiens (human) | Potency | 4.4668 | 1 | 1 |
| regulator of G-protein signaling 4 | Homo sapiens (human) | Potency | 7.7580 | 1 | 4 |
| TDP1 protein | Homo sapiens (human) | Potency | 29.9520 | 2 | 3 |
| thioredoxin reductase | Rattus norvegicus (Norway rat) | Potency | 0.6774 | 1 | 2 |
| thyroid hormone receptor beta isoform a | Homo sapiens (human) | Potency | 0.0355 | 1 | 1 |
| thyroid stimulating hormone receptor | Homo sapiens (human) | Potency | 4.9299 | 4 | 5 |
| thyrotropin-releasing hormone receptor | Homo sapiens (human) | Potency | 3.1949 | 1 | 2 |
| transcriptional regulator ERG isoform 3 | Homo sapiens (human) | Potency | 8.9125 | 1 | 1 |
| USP1 protein, partial | Homo sapiens (human) | Potency | 112.2020 | 1 | 1 |
| v-jun sarcoma virus 17 oncogene homolog (avian) | Homo sapiens (human) | Potency | 11.9632 | 2 | 4 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Bile salt export pump | Homo sapiens (human) | IC50 | 1,000.0000 | 1 | 2 |
| Muscarinic acetylcholine receptor | Cavia porcellus (domestic guinea pig) | IC50 | 107.5000 | 1 | 2 |
| Muscarinic acetylcholine receptor | Cavia porcellus (domestic guinea pig) | Ki | 54.1046 | 4 | 5 |
| Muscarinic acetylcholine receptor M1 | Homo sapiens (human) | IC50 | 35.6101 | 13 | 14 |
| Muscarinic acetylcholine receptor M1 | Rattus norvegicus (Norway rat) | IC50 | 49.2630 | 15 | 38 |
| Muscarinic acetylcholine receptor M1 | Homo sapiens (human) | Ki | 78.2382 | 21 | 32 |
| Muscarinic acetylcholine receptor M1 | Mus musculus (house mouse) | Ki | 3.0098 | 6 | 8 |
| Muscarinic acetylcholine receptor M1 | Rattus norvegicus (Norway rat) | Ki | 17.0904 | 16 | 26 |
| Muscarinic acetylcholine receptor M2 | Homo sapiens (human) | IC50 | 10.0299 | 9 | 14 |
| Muscarinic acetylcholine receptor M2 | Rattus norvegicus (Norway rat) | IC50 | 13.7079 | 13 | 28 |
| Muscarinic acetylcholine receptor M2 | Homo sapiens (human) | Ki | 0.9054 | 27 | 35 |
| Muscarinic acetylcholine receptor M2 | Rattus norvegicus (Norway rat) | Ki | 17.0812 | 11 | 20 |
| Muscarinic acetylcholine receptor M3 | Homo sapiens (human) | IC50 | 19.7450 | 3 | 4 |
| Muscarinic acetylcholine receptor M3 | Rattus norvegicus (Norway rat) | IC50 | 75.9183 | 12 | 23 |
| Muscarinic acetylcholine receptor M3 | Homo sapiens (human) | Ki | 20.6390 | 14 | 17 |
| Muscarinic acetylcholine receptor M3 | Rattus norvegicus (Norway rat) | Ki | 12.0258 | 30 | 37 |
| Muscarinic acetylcholine receptor M4 | Homo sapiens (human) | IC50 | 8.6626 | 5 | 8 |
| Muscarinic acetylcholine receptor M4 | Rattus norvegicus (Norway rat) | IC50 | 15.9587 | 11 | 23 |
| Muscarinic acetylcholine receptor M4 | Homo sapiens (human) | Ki | 6.7615 | 16 | 23 |
| Muscarinic acetylcholine receptor M4 | Rattus norvegicus (Norway rat) | Ki | 10.3225 | 9 | 18 |
| Muscarinic acetylcholine receptor M5 | Homo sapiens (human) | IC50 | 43.8500 | 2 | 2 |
| Muscarinic acetylcholine receptor M5 | Rattus norvegicus (Norway rat) | IC50 | 17.4343 | 10 | 21 |
| Muscarinic acetylcholine receptor M5 | Homo sapiens (human) | Ki | 25.3346 | 17 | 24 |
| Muscarinic acetylcholine receptor M5 | Rattus norvegicus (Norway rat) | Ki | 11.9470 | 8 | 15 |
| Neuronal acetylcholine receptor subunit alpha-10 | Rattus norvegicus (Norway rat) | Ki | 0.4500 | 1 | 2 |
| Neuronal acetylcholine receptor subunit alpha-2 | Rattus norvegicus (Norway rat) | Ki | 0.3700 | 2 | 3 |
| Neuronal acetylcholine receptor subunit alpha-3 | Rattus norvegicus (Norway rat) | Ki | 1.7000 | 3 | 4 |
| Neuronal acetylcholine receptor subunit alpha-4 | Rattus norvegicus (Norway rat) | Ki | 0.5550 | 5 | 6 |
| Neuronal acetylcholine receptor subunit alpha-5 | Rattus norvegicus (Norway rat) | Ki | 0.4500 | 1 | 2 |
| Neuronal acetylcholine receptor subunit alpha-6 | Rattus norvegicus (Norway rat) | Ki | 0.4500 | 1 | 2 |
| Neuronal acetylcholine receptor subunit alpha-7 | Rattus norvegicus (Norway rat) | Ki | 0.4500 | 1 | 2 |
| Neuronal acetylcholine receptor subunit alpha-9 | Rattus norvegicus (Norway rat) | Ki | 0.4500 | 1 | 2 |
| Neuronal acetylcholine receptor subunit beta-2 | Rattus norvegicus (Norway rat) | Ki | 0.4771 | 6 | 7 |
| Neuronal acetylcholine receptor subunit beta-3 | Rattus norvegicus (Norway rat) | Ki | 0.4500 | 1 | 2 |
| Neuronal acetylcholine receptor subunit beta-4 | Rattus norvegicus (Norway rat) | Ki | 1.7500 | 3 | 4 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Muscarinic acetylcholine receptor M1 | Homo sapiens (human) | EC50 | 554,238,899.1213 | 24 | 36 |
| Muscarinic acetylcholine receptor M1 | Mus musculus (house mouse) | EC50 | 24.2333 | 1 | 3 |
| Muscarinic acetylcholine receptor M1 | Rattus norvegicus (Norway rat) | EC50 | 0.5250 | 1 | 2 |
| Muscarinic acetylcholine receptor M1 | Homo sapiens (human) | Kd | 17.0000 | 1 | 2 |
| Muscarinic acetylcholine receptor M2 | Homo sapiens (human) | EC50 | 1,290,683,339.5529 | 9 | 12 |
| Muscarinic acetylcholine receptor M2 | Homo sapiens (human) | Kd | 17.0000 | 1 | 2 |
| Muscarinic acetylcholine receptor M3 | Homo sapiens (human) | EC50 | 6,917,646,157.8290 | 10 | 13 |
| Muscarinic acetylcholine receptor M3 | Mus musculus (house mouse) | EC50 | 10.9667 | 1 | 3 |
| Muscarinic acetylcholine receptor M3 | Rattus norvegicus (Norway rat) | EC50 | 0.6762 | 21 | 22 |
| Muscarinic acetylcholine receptor M3 | Homo sapiens (human) | Kd | 17.0000 | 1 | 2 |
| Muscarinic acetylcholine receptor M4 | Homo sapiens (human) | EC50 | 4.9434 | 14 | 15 |
| Muscarinic acetylcholine receptor M4 | Homo sapiens (human) | Kd | 17.0000 | 1 | 2 |
| Muscarinic acetylcholine receptor M5 | Homo sapiens (human) | EC50 | 5,066,727,785.2035 | 13 | 18 |
| Muscarinic acetylcholine receptor M5 | Homo sapiens (human) | Kd | 17.0000 | 1 | 2 |
| NPYLR7B | Aedes aegypti (yellow fever mosquito) | EC50 | 20.0000 | 1 | 1 |
| Sigma non-opioid intracellular receptor 1 | Cavia porcellus (domestic guinea pig) | EC50 | 19,952,600,000.0000 | 1 | 1 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Delta-type opioid receptor | Mus musculus (house mouse) | K app | 45.0000 | 1 | 1 |
| Muscarinic acetylcholine receptor M1 | Homo sapiens (human) | ED50 | 5.6000 | 2 | 2 |
| Muscarinic acetylcholine receptor M1 | Rattus norvegicus (Norway rat) | K app | 8.4204 | 13 | 39 |
| Muscarinic acetylcholine receptor M1 | Rattus norvegicus (Norway rat) | Kapp | 11.0024 | 2 | 2 |
| Muscarinic acetylcholine receptor M2 | Homo sapiens (human) | ED50 | 0.2700 | 1 | 1 |
| Muscarinic acetylcholine receptor M2 | Rattus norvegicus (Norway rat) | K app | 6.3236 | 13 | 38 |
| Muscarinic acetylcholine receptor M2 | Mus musculus (house mouse) | KH | 0.0008 | 1 | 1 |
| Muscarinic acetylcholine receptor M2 | Mus musculus (house mouse) | KL | 0.0063 | 1 | 2 |
| Muscarinic acetylcholine receptor M2 | Mus musculus (house mouse) | Km | 0.0242 | 1 | 2 |
| Muscarinic acetylcholine receptor M3 | Homo sapiens (human) | ED50 | 1.3000 | 2 | 2 |
| Muscarinic acetylcholine receptor M3 | Rattus norvegicus (Norway rat) | K app | 6.4431 | 12 | 37 |
| Muscarinic acetylcholine receptor M3 | Mus musculus (house mouse) | KH | 0.0560 | 1 | 1 |
| Muscarinic acetylcholine receptor M3 | Mus musculus (house mouse) | KL | 0.0046 | 1 | 2 |
| Muscarinic acetylcholine receptor M4 | Homo sapiens (human) | ED50 | 0.1000 | 1 | 1 |
| Muscarinic acetylcholine receptor M4 | Rattus norvegicus (Norway rat) | K app | 6.4431 | 12 | 37 |
| Muscarinic acetylcholine receptor M5 | Homo sapiens (human) | ED50 | 2.0500 | 2 | 2 |
| Muscarinic acetylcholine receptor M5 | Rattus norvegicus (Norway rat) | K app | 6.4431 | 12 | 37 |