muscarinic

Flavoxate hydrochloride (DW61) , a muscarinic AChR antagonist, is used in the therapy of various urinary syndromes and as an antispasmodic.

Mepenzolate Bromide (Colibantil) is a muscarinic antagonist used to treat gastrointestinal conditions.

Arecoline hydrobromide (Arecoline HBr) is a muscarinic acetylcholine receptor agonist.

Desfesoterodine (5-HMT) is a new muscarinic receptor antagonist with Kb of 0.84 nM.

DREADD agonist 21 is a potent agonist of human muscarinic acetylcholine M3 receptors (EC50=1.7 nM).

VU0357017 hydrochloride (ML071 hydrochloride) is highly selective M1 agonists act at an allosteric site to activate the receptor (EC50: 477 ± 172 nM; Pec50: 6.37 ± 0.15).

L-Hyoscyamine (Daturine) functions as a non-selective, competitive antagonist of muscarinic receptors, thereby inhibiting the parasympathetic activities of acetylcholine on the salivary, bronchial, and sweat glands, as well as the eye, heart, bladder, and gastrointestinal tract. Hyoscyamine is a belladonna alkaloid derivative and the levorotatory form of racemic atropine isolated from the plants Hyoscyamus niger or Atropa belladonna, which exhibits anticholinergic activity. These inhibitory effects cause a decrease in saliva, bronchial mucus, gastric juices, and sweat. Furthermore, its inhibitory action on smooth muscle prevents bladder contraction and decreases gastrointestinal motility.

Cevimeline hydrochloride hemihydrate is a novel muscarinic receptor agonist, used as a candidate therapeutic drug for xerostomia in Sjogren's syndrome.

Anisotropine Methylbromide is an anticholinergic agent and has been used for relief of gastrointestinal spasm and for the suppression of gastric acid secretion.

L-Hyoscyamine sulfate (Levsin Sulfate) is the sulfate salt of a belladonna alkaloid derivative and the levorotatory form of racemic atropine isolated from the plants Hyoscyamus niger or Atropa belladonna, which exhibits anticholinergic activity. Hyoscyamine functions as a non-selective, competitive antagonist of muscarinic receptors, thereby inhibiting the parasympathetic activities of acetylcholine on the salivary, bronchial, and sweat glands, as well as the eye, heart, bladder, and gastrointestinal tract. These inhibitory effects cause a decrease in saliva, bronchial mucus, gastric juices, and sweat. Furthermore, its inhibitory action on smooth muscle prevents bladder contraction and decreases gastrointestinal motility.

Anisodamine Hydrobromide (6-Hydroxyhyoscyamine) is an anticholinergic and α1-adrenergic receptor antagonist used in the treatment of acute circulatory shock.

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).

Muscarinic toxin 7 (MT7) is a peptide exhibiting selective, noncompetitive antagonistic activity at the muscarinic M1 receptor [1].

Muscarinic toxin 3 (MT3), a potent non-competitive antagonist of mAChR and adrenoceptors, exhibits pIC50 values of 6.71 for M1, 8.79 for M4, 8.86 for α1A, 7.57 for α1B, 8.13 for α1D, 8.49 for α2A, <6.5 for α2B, and 7.29 for α2C receptors. MT3 notably demonstrates significant adrenoceptor activity [1].

Compound 40 is a selective M1 M4 muscarinic antagonist with an IC50 of 19 nM for M1 receptors and 42 nM for M4 receptors [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].

Muscarinic agonist 3 (compound 45) is a muscarinic mAChR M1 M2 M4 agonist with EC50 values of 3.2 nM, 32 nM, and 1.7 nM, respectively [1].

Compound 44, identified as an M1 M4 muscarinic agonist, exhibits potent activity with EC50 values of 31 nM at M1 and 9.3 nM at M4 mAChRs, respectively [1].

Clozapine N-oxide is the major metabolite of Clozapine and is blood-brain barrier permeable. Clozapine N-oxide is an agonist of DREADDs and activates the DREADD receptors hM3Dq and hM4Di. Clozapine N-oxide is also a dopamine antagonist and selective muscarinic M4 receptor agonist.

(±)-Tazifylline is a selective and long-acting antagonist of histamine H1 receptor. Tazifylline shows much lower affinity for H2 receptors, α- and β-adrenoceptors, 5-hydroxytryptamine and muscarinic receptor subtypes.

BTM-1086 is a potent gastric secretory inhibitor and an anti-ulcer agent.

Cyclodrine hydrochloride is a dual cholinergic muscarinic receptor (mAChR) and nicotinic receptor (nAChR) antagonist that can be used in the study of neurologically related diseases.

Cyclodrine (Cyclopent) is a cholinergic (muscarinic, nicotinic) (mAChR and nAChR) receptor antagonist.

Darenzepine is a muscarinic receptor inhibitor.