muscarinic

Tolterodine tartrate (PNU-200583E) is a potent antagonist for muscarinic receptor. It show selectivity for the urinary bladder and salivary glands in vivo.

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.

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).

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

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.

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.

M1/M4 muscarinic agonist 1 (Compound 41) is a selective muscarinic M4/M1 agonist with EC50 values of 14 nM for M4 receptors and 55 nM for M1 receptors. This compound is utilized in research related to psychiatric disorders, including schizophrenia and delusional disorders.

Compound 43, known as M1/M2/M4 muscarinic agonist 2, functions as an mAChR M1/M2/M4 agonist with respective EC50 values of 30 nM, 200 nM, and 6.2 nM.

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].