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.

Tropicamide (Ro 1-7683) is a synthetic muscarinic antagonist with anticholinergic properties similar to atropine. Upon ocular administration, it binds to and blocks muscarinic receptors in the sphincter and ciliary muscles, inhibiting cholinergic responses and causing pupil dilation and ciliary muscle paralysis. Tropicamide is used as a diagnostic agent to induce short-duration mydriasis and cycloplegia.

Fesoterodine fumarate (Toviaz) is the fumarate salt form of fesoterodine, a competitive muscarinic receptor antagonist with muscle relaxant and urinary antispasmodic properties. Fesoterodine is rapidly hydrolyzed in vivo into its active metabolite 5-hydroxymethyl tolterodine, which binds and inhibits muscarinic receptors on the bladder detrusor muscle, thereby preventing bladder contractions or spasms caused by acetylcholine.

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).

Zamifenacin fumarate (UK-76654 fumarate) is a potent, gut-selective antagonist of the muscarinic M3 receptor.

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.

Sofpironium bromide (BBI4000) belongs to a class of drugs called anticholinergics, which exert their effect by blocking the action of acetylcholine.

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).

Emraclidine (CVL-231) is a novel, highly selective allosteric modulator of the muscarinic M4 receptor positive receptor for the study of neurological diseases.

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.

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

Darenzepine is a muscarinic receptor inhibitor.

CHF5407(SVT-47060) is a potent and selective muscarinic M3 receptor antagonist with prolonged action at muscarinic receptors.CHF5407 has an effect on bronchospasm and may be used in the study of respiratory disorders.CHF5407 is a potent and selective muscarinic M3 receptor antagonist with prolonged action at muscarinic receptors.

Anisodamine (6-beta-Hydroxyhyoscyamine) is an antagonist of muscarinic and nicotinic cholinoceptor with similar affinities at the muscarinic receptor as scopolamine and atropine. Anisodamine improve the microcirculation in states of shock and can be used in studies about organophosphate poisoning.

GSK233705 (Darotropium bromide) is a muscarinic receptor antagonist used in conjunction with the prevention and treatment of chronic obstructive pulmonary disease (COPD) and asthma in humans.

Sabcomeline HCl is an M1 receptor agonist that can be used to study Alzheimer's disease.

Tazomeline is a muscarinic M1 receptor agonist with neuroprotective activity.

Orphenadrine is a noncompetitive N-methyl-D-aspartate (NMDA) receptor antagonist that inhibits clonal HERG channels in a concentration-dependent manner, producing an IC of 0.85 μM in HEK cells.Orphenadrine is an antagonist of central and peripheral muscarinic receptors. Attenuation is blocked by mutations in pore residues Y652 or F656. Orphenadrine has antispasmodic, analgesic, and anticholinergic activity and protects against glutamatergic neurotoxicity in vitro and in vivo.Orphenadrine has inhibitory effects on sodium channels and can be used in the treatment of Parkinson's disease.