| S5258 |
Revefenacin |
Revefenacin (TD-4208, GSK-1160724) is a potent, lung-selective, long-acting muscarinic antagonist that may be for the treatment of respiratory disease. |
Selective |
|
| S5873 |
Scopolamine HBr trihydrate |
Scopolamine HBr is a competitive muscarinic acetylcholine receptor antagonist with an IC50 of 55.3 nM. |
Selective |
|
| S4713 |
Atropine |
Atropine (Atropen, Atnaa, Tropine tropate, DL-Hyoscyamine) is a competitive muscarinic acetylcholine receptor (mAChR) antagonist with anti-myopia effect. |
Selective |
|
| S4031 |
Aclidinium Bromide |
Aclidinium Bromide (LAS 34273, LAS-W 330) inhibits human muscarinic AChR M1, M2, M3, M4 and M5 with Ki of 0.1 nM, 0.14 nM, 0.14 nM, 0.21 nM and 0.16 nM, respectively. |
Selective |
M1 mAChR, Ki: 0.1 nM; M2 mAChR, Ki: 0.14 nM; M3 mAChR, Ki: 0.14 nM; M4 mAChR, Ki: 0.21 nM; M5 mAChR, Ki: 0.16 nM |
| S9790 |
JHU37160 |
JHU37160 is a Designer Receptors Exclusively Activated by Designer Drug (DREADD) agonist with Ki of 1.9 nM and 3.6 nM for human muscarinic acetylcholine M3 receptors (hM3Dq) and hM4Di in vitro, respectively. And EC50 values are 18.5 nM and 0.2 nM for hM3Dq and hM4Di in fluorescent and BRET-based assays in HEK-293 cells, respectively. |
Selective |
hM3Dq, Ki: 1.9 nM; hM4Di, Ki: 3.6 nM; hM3Dq, EC50: 18.5 nM; hM4Di, EC50: 0.2 nM |
| S5385 |
Imidafenacin |
Imidafenacin (KRP-197, ONO-8025) is a urinary antispasmodic of the anticholinergic class. It is a novel antimuscarinic agent with safety and efficacy, has been clinically used for the treatment of overactive bladder. Imidafenacin(KRP-197; ONO-8025) is a potent and selective inhibitor of M3 receptors with Kb of 0.317 nM; less potent for M2 receptors(IC50=4.13 nM). IC50 value: 0.3 nM(M3). |
Selective |
M3 receptor, IC50: 0.3 nM; M3 receptor, Kd: 0.317 nM; M2 receptor, IC50: 4.13 nM |
| S3913 |
Pimethixene maleate |
Pimethixene (Pimetixene) maleate, an antihistamine, anntimigraine agent and antiserotonergic compound, is a highly potent antagonist of a broad range of monoamine receptors, including a variety of serotonin receptors. Pimethixene maleate inhibits 5-HT2A, 5-HT2B, 5-HT2C, 5-HT1A, 5-HT1B, 5-HT6, 5-HT7, Adrenergic α-1A, Dopamine D1 Receptor, Dopamine D2 Receptor, Dopamine D4.4 Receptor, Histamine H1 Receptor, Muscarinic M1 and Muscarinic M2 with pKi of 10.22, 10.44, 8.42, 7.63, < 5, 7. |
Selective |
Muscarinic M1, pKi: 8.61; Muscarinic M2, pKi: 9.38 |
| S9789 |
JHU37152 |
JHU37152 is a Designer Receptors Exclusively Activated by Designer Drug (DREADD) agonist with Ki of 1.8 nM and 8.7 nM for human muscarinic acetylcholine M3 receptors (hM3Dq) and hM4Di in vitro, respectively. And EC50 values are 5 nM and 0.5 nM for hM3Dq and hM4Di in fluorescent and BRET-based assays in HEK-293 cells, respectively. |
Selective |
hM3Dq, Ki: 1.8 nM; hM4Di, Ki: 8.7 nM; hM3Dq, EC50: 5 nM; hM4Di, EC50: 0.5 nM |
| S3144 |
Darifenacin HBr |
Darifenacin HBr (UK-88525) is a selective M3 muscarinic receptor antagonist with pKi of 8.9. |
Selective |
M3 mAChR, pKi: 8.9 |
| S0032 |
Batefenterol |
Batefenterol (GSK961081, TD-5959) is both a muscarinic receptor antagonist and a β2-adrenoceptor agonist with Ki of 1.4 nM, 1.3 nM and 3.7 nM for hM2, hM3 muscarinic receptors and hβ2-adrenoceptor, respectively. |
Selective |
hM2 muscarinic receptor, Ki: 1.4 nM; hM3 muscarinic receptor, Ki: 1.3 nM |
| S5921 |
Cyclopentolate Hydrochloride |
Cyclopentolate is an antagonist of muscarinic acetylcholine receptors with Ki values of 1.62, 27.5, and 2.63 nM for M1, M2, and M3 receptors, respectively. |
Selective |
M1 receptor, Ki: 1.62 nM; M2 receptor, Ki: 27.5 nM; M3 receptor, Ki: 2.63 nM |
| S0457 |
DREADD agonist 21 |
DREADD agonist 21 is a potent agonist of human muscarinic acetylcholine M3 receptors (hM3Dq) with EC50 of 1.7 nM. |
Selective |
hM3Dq, EC50: 1.7 nM |
| S5777 |
Ipratropium bromide monohydrate |
Ipratropium bromide (Atrovent, Sch 1000) monohydrate is an antagonist of muscarinic acetylcholine receptors (mAChR) with IC50 of 2.9 nM, 2.0 nM, and 1.7 nM for M1, M2, and M3 receptors, respectively. |
Selective |
M1 receptor, IC50: 2.9 nM; M2 receptor, IC50: 2.0 nM; M3 receptor, IC50: 1.7 nM |
| S2130 |
Atropine sulfate monohydrate |
Atropine sulfate monohydrate is a competitive antagonist for the muscarinic acetylcholine receptor, used to decrease the production of saliva and secretions of the airway prior to surgery. |
Selective |
mAChR, IC50: 2.5 nM |
| S1913 |
Tropicamide |
Tropicamide(Ro 1-7683) is an anticholinergic and a muscarinic receptor subtype M4-preferring antagonist with IC50 of 8.0 nM. |
Selective |
M4 mAChR, IC50: 8 nM |
| S2508 |
Scopolamine (LSM-4015) HBr |
Scopolamine HBr (LSM-4015,NSC 61806,(-)-Scopolamine hydrobromide, Hyoscine hydrobromide, Scopine hydrobromide) is a competitive muscarinic acetylcholine receptor antagonist with an IC50 of 55.3 nM. |
Selective |
mAChR, IC50: 55.3 nM |
| S4025 |
Homatropine Bromide |
Homatropine Bromide is an muscarinic AChR antagonist, inhibits endothelial and smooth muscle muscarinic receptors of WKY-E and SHR-E with IC50 of 162.5 nM and 170.3 nM, respectively. |
Selective |
mAChR (WKY-E), IC50: 162.5 nM; mAChR (SHR-E), IC50: 170.3 nM |
| S4024 |
Homatropine Methylbromide |
Homatropine Methylbromide is muscarinic AChR antagonist, inhibits endothelial and smooth muscle muscarinic receptors of WKY-E and SHR-E with IC50 of 162.5 nM and 170.3 nM, respectively. |
Selective |
mAChR (WKY-E), IC50: 162.5 nM; mAChR (SHR-E), IC50: 170.3 nM |
| S6795 |
VU0357017 Hydrochloride |
VU0357017 hydrochloride (CID-25010775) is a potent, highly selective and CNS-penetrant agonist of M1 which is a subtype of muscarinic acetylcholine receptors (mAChRs). VU0357017 hydrochloride appears to act at an allosteric site to activate the receptor with EC50 of 477 nM and Ki of 9.91 μM. |
Selective |
M1 mAChR, EC50: 477 nM; M1 mAChR, Ki: 9.91 μM |
| S2646 |
VU0238429 |
VU0238429 (M5 PAM) is the first positive allosteric modulator of muscarinic acetylcholine receptor subtype 5 (mAChR5/M5) with EC50 of 1.16 μM at M5 and both > 30 μM at M1 and M3. VU0238429 shows no potentiator activity at M2 or M4. |
Selective |
M5 mAChR, IC50: 1.16 μM; M1 mAChR, : ; M3 mAChR, : |
| S0782 |
VU0238441 |
VU0238441 is a pan muscarinic acetylcholine receptor (mAChR) positive allosteric modulator (PAM) with EC50 of 2.1 μM, 2.2 μM, 2.8 μM, 3.2 μM and >10 μM for M5, M3, M2, M1 and M4, respectively. |
Selective |
mAChR M5, IC50: 2.1 μM; mAChR M3, IC50: 2.2 μM; mAChR M2, IC50: 2.8 μM; mAChR M1, IC50: 3.2 μM; mAChR M4, IC50: >10 μM |
| S0783 |
VU0119498 |
VU0119498 is a pan Gq muscarinic acetylcholine receptor (mAChR) M1, M3, M5 positive allosteric modulator (PAM) with EC50 of 6.1 μM, 6.4 μM, 4.1 μM, respectively. |
Selective |
mAChR M1, IC50: 6.1 μM; mAChR M3, IC50: 6.4 μM; mAChR M5, IC50: 4.1 μM |
| S4027 |
Flavoxate HCl |
Flavoxate (NSC-114649) is a muscarinic AChR antagonist with IC50 of 12.2 μM. |
Selective |
mAChR, IC50: 12.2 μM |
| S3047 |
Otilonium Bromide |
Otilonium bromide is an antimuscarinic. |
Selective |
|
| S1929 |
Irsogladine |
Irsogladine(Dicloguamine) is an anti-gastric ulcer agent that facilitates gap-junctional intercellular communication through M1 muscarininc acetylcholine receptor binding. |
Selective |
|
| S3735 |
Umeclidinium bromide |
Umeclidinium bromide(GSK573719A) is a long-acting muscarinic antagonist approved for the maintenance treatment of chronic obstructive pulmonary disease (COPD). |
Selective |
|
| S3048 |
Solifenacin succinate |
Solifenacin succinate (YM905) is a urinary antispasmodic of the antimuscarinic class. |
Selective |
|
| S2455 |
Bethanechol chloride |
Bethanechol chloride(Myocholine,Urecholine) is a selective muscarinic receptor agonist without any effect on nicotinic receptors. |
Selective |
|
| S4292 |
Diphenidol HCl |
Diphenidol HCl(Diphenidol hydrochloride) is a potent antagonist of muscarinic M2 and M3 receptor with pKb of 6.72 and 7.02, respectively, used in the treatment of vomiting and vertigo.
|
Selective |
|
| S4034 |
Diphemanil Methylsulfate |
Diphemanil Methylsulfate is a quaternary ammonium anticholinergic, it binds muscarinic acetycholine receptors (mAchR). |
Selective |
|
| S2614 |
Arecoline HBr |
Arecoline(NSC-31750) is a muscarinic acetylcholine receptor agonist. |
Selective |
|
| S4231 |
Pilocarpine HCl |
Pilocarpine HCl (NSC 5746) is a nonselective muscarinic acetylcholine receptor agonist used to produce an experimental model of epilepsy. |
Selective |
|
| S1683 |
Ipratropium Bromide |
Ipratropium Bromide is an antagonist of M3 type muscarinic acetylcholine receptors, used for the treatment of chronic obstructive pulmonary disease (COPD). |
Selective |
|
| S1978 |
Methscopolamine |
Methscopolamine is a muscarinic acetylcholine receptor blocker. |
Selective |
|
| S4143 |
Pentoxyverine Citrate |
Pentoxyverine Citrate (Carbetapentane) is an antitussive (cough suppressant) commonly used for cough associated with illnesses like common cold. |
Selective |
|
| S3117 |
Oxybutynin hydrochloride |
Oxybutynin(MJ4309-1) is an anticholinergic medication used to relieve urinary and bladder difficulties. |
Selective |
|
