m2 machr

SCH 57790 is a novel and selective muscarinic M(2) receptor antagonist that releases acetylcholine and enhances cognition in experimental animals for the treatment of Alzheimer's disease.

Pimethixene (Calmixen) is a highly potent 5-HT1A, 5-HT2A, 5-HT2B, 5-HT2C, histamine H1, dopamine D2 and D4.4 as well as muscarinic M1 and M2 receptors antagonist(pKis of 7.63, 10.22, 10.44, 8.42, 10.14, 8.19, 7.54, 8.61 and 9.38, respectively).

Pimethixene maleate (Pimetixene maleate) is a potent 5-HT2B receptor antagonist with sedative and antitussive activity.Pimethixene maleate inhibits 5-HT1A, 5-HT2A, 5-HT2B, 5-HT2C, histamine H1, dopamine D2 and D4.4 as well as muscarinic M1 and M2, and can be used in studies of dry and irritant cough in children. irritant cough in children.

Otenzepad (AF-DX 116) is a selective M2 mAChR antagonist with IC50 values of 386 nM in rat heart and 640 nM in rabbit peripheral lung.

(S)-(+)-Dimethindene maleate is an orally available, selective muscarinic M2 receptor and histamine H1 receptor antagonist that also inhibits muscarinic M1, M3, and M4 receptors.

Aclidinium bromide (LAS-W 330) is a synthetic anticholinergic agent that is used as an inhalant for treatment of acute bronchospasm due to chronic bronchitis or emphysema. Aclidinium has not been implicated in causing liver enzyme elevations or clinically apparent acute liver injury.

Umeclidinium bromide (GSK573719A) is a novel mAChR antagonist.

LY2119620 is a specific, and allosteric agonist of human M2 and M4 muscarinic acetylcholine receptors.

Fesoterodine ((R) Fesoterodine) is an orally active, competitive mAChR antagonist with pKi values of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively. It is used for the overactive bladder (OAB).

YM-58790 free base is a potent mAChR antagonist that inhibits M1 mAChR, M2 mAChR, and M3 mAChR with Ki values of 28 nM, 260 nM, and 15 nM, respectively. It inhibits reflex rhythmic bladder contractions in rats by inhibiting bladder pressurization.

Ipratropium bromide monohydrate (Ipratropium bromide hydrate) is a muscarinic antagonist structurally related to ATROPINE but often considered safer and more effective for inhalation use. It is used for various bronchial disorders, in rhinitis, and as an antiarrhythmic.

Solifenacin (YM905 free base) (YM905 free base) is a novel muscarinic receptor antagonist, its pKis for M1, M2 and M3 receptors is of 7.6, 6.9 and 8.0, respectively.

YM-58790 is a potent M3 muscarinic receptor antagonist(Ki of 15 nM).

Bryonolic acid (20-epi-Bryonolic acid), a triterpenoid extracted from Sandoricum indicum, possesses immunomodulatory, anti-inflammatory, antioxidant and anticancer activities and protects PC12 cells from NMDA-induced apoptosis by inhibiting Ca2+ in-flux and modulating gene expression in the Ca2+-CaMKII-CREB signalling pathway.

TAAR1 agonist 2 (compound 30), a full agonist at trace amine-associated receptor 1 (TAAR1) (pEC50=7.5), also displays agonistic properties at H1 receptors and activates various muscarinic acetylcholine receptors, including the M2 receptor (pEC50=5). This compound is utilized in researching neuropsychiatric diseases.

AF-DX 384 free base is a selective and efficient M2 muscarinic acetylcholine receptor (M2 mAChR) and M4 muscarinic acetylcholine receptor (M4 mAChR) antagonist. It can be used for research on neurodegenerative diseases like Parkinson's.

muscarinic receptor ligand

Telenzepine dihydrochloride is a highly selective M1 muscarinic receptor antagonist. It inhibits gastric acid secretion and is used for ulcer and cholinergic neuropharmacology research.

Hexocyclium metilsulfate has anti-gastric secretory effects in humans.

Lu AE51090 is a highly selective agonist of the muscarinic M1 receptor, displaying minimal off-target activity across other muscarinic subtypes and a broad panel of G-protein-coupled receptors, ion channels, transporters, and enzymes, making Lu AE51090 a valuable pharmacological tool for studying muscarinic receptor function and selective receptor modulation.

J-104129 fumarate is a potent M3 muscarinic receptor antagonist.

Lu 26-046 is a muscarinic receptor agonist.

LAS190792 (AZD8999) is a dual-action chemical compound that simultaneously acts as a strong muscarinic antagonist and β2-adrenoceptor agonist. It exhibits significant potency across a range of receptors, with pIC50 values of 8.9 for M1, 8.8 for M2, 8.8 for M3, 9.2 for M4, 8.2 for M5, 7.5 for β1, 9.1 for β2, and 5.6 for β3. Its effectiveness across these receptors makes LAS190792 a viable candidate for bronchodilator applications [1].

Compound 42, also known as M1/M2/M4 muscarinic agonist 1, is a muscarinic M4/M1/M2 agonist exhibiting EC50 values of 6.5, 26, and 210 nM for M4, M1, and M2 respectively. This compound is utilized in research focused on mental disorders, including schizophrenia and delusion [1].