mAChR Inhibitor

Methscopolamine bromide ((-)-Scopolamine methyl bromide; Hyoscine methyl bromide) is a peripherally acting muscarinic receptor (mAChR) antagonist that cannot cross the blood-brain barrier. Methscopolamine bromide blocks the muscarinic negative feedback regulation of acetylcholine release from striatal cholinergic terminals, thereby increasing acetylcholine release in the striatum of freely moving rats. Methscopolamine bromide does not induce motor excitation in freely moving rats, nor does it alter the duration of ethanol-induced loss of righting reflex in mice. Methscopolamine bromide fails to antagonize the arecoline-mediated reduction in the duration of ethanol-induced loss of righting reflex in mice.

Otilonium bromide (OB) is an orally active mAChR inhibitor and smooth muscle relaxant which can interfere with the mobilization of calcium in intestinal smooth muscle, OB can be used for research of irritable bowel syndrome.

(-)-Vesamicol (AH5183) is a vesicular acetylcholine transporter inhibitor. (-)-Vesamicol reversibly and non-competitively inhibits the transport of acetylcholine into circulating synaptic vesicles and blocks the activity of vesicular acetylcholine transporters in medial amygdala neurons. (-)-Vesamicol is applicable to research related to central precocious puberty.

Biperiden (KL 373) is a non-selective muscarinic receptor antagonist that competitively binds to M1 muscarinic receptors, thereby inhibiting acetylcholine and enhancing dopamine signaling in the central nervous system. Biperiden has the potential for the research of Parkinson's disease and other related psychiatric disorders.

BQCA a highly selective allosteric modulator of the M1 mAChR.

RHC 80267 (U-57908) is a potent and selective inhibitor of diacylglycerol lipase (DAGL) (with IC₅₀ of 4 μM in canine platelets). RHC-80267 inhibits cholinesterase activity with an IC₅₀ of 4 μM, thereby enhancing the relaxation evoked by acetylcholine. RHC 80267 also inhibits COX and the hydrolysis of phosphatidylcholine (PC).

Arborine inhibits the peripheral action of acetylcholine and induces a fall in blood pressure.

Propiverine hydrochloride is a bladder spasmolytic with calcium antagonistic and anticholinergic properties. Propiverine hydrochloride can be used for the research of overactive blaqdder and urinary incontinence.

Methylbenactyzium Bromide is a muscarinic acetylcholine receptor (mAChR) inhibitor.

Propantheline-d₃ (bromide) is the deuterium labeled Propantheline bromide. Propantheline bromide is an antimuscarinic agent, used for the treatment of hyperhidrosis, cramps or spasms of the stomach, intestines or bladder, and enuresis.

Pirmenol ((±)-Pirmenol) hydrochloride is an orally active antiarrhythmic agent. Pirmenol hydrochloride inhibits I_K.ACh (IC₅₀: 0.1 μM) by blocking mAchR. Pirmenol hydrochloride can be used in the research of cardiovascular disease, such as atrial fibrillation.

Piperidolate hydrochloride is a cholinergic antagonist. Piperidolate hydrochloride prevents ventricular fibrillation during hypothermic cardiac manipulations to support cardiac procedures post-preoperative defibrillation. Piperidolate hydrochloride causes dose-dependent cardiac depression. Piperidolate hydrochloride can be used for the research of ventricular fibrillation.

Isopropamide iodide is a long-acting quaternary anticholinergic agent. Isopropamide iodide is used in peptic ulcer and other gastrointestinal disorders marked by hyperacidity and hypermotility.

Camylofin is an antimuscarinic, is a smooth muscle relaxant .

Valethamate bromide is an ester, serving as an effective rapidly acting anticholinergic antispasmodic and muscle relaxant. Valethamate bromide accelerates labor by improving cervical dilation. Valethamate bromide can significantly shorten the labor process and have fewer side effects.

Amitriptyline-d3 hydrochloride is the deuterium labeled Amitriptyline (hydrochloride). Amitriptyline hydrochloride is an inhibitor of serotonin reuptake transporter (SERT) and noradrenaline reuptake transporter (NET), with K_is of 3.45 nM and 13.3 nM for human SERT and NET, respectively. Amitriptyline hydrochloride also weakly binds to dopamine reuptake transporter (DAT) with a K_i of 2.58 μM. Amitriptyline hydrochloride also inhibits adrenergic, muscarinic, histamine and 5-HT receptors. Amitriptyline hydrochloride is a TrkA and TrkB receptors agonist with potent neurotrophic activity. Amitriptyline hydrochloride has antidepressant activity.

Levetimide is a potent and stereoselective inhibitor of [³H](+)pentazocine binding, with a K_i of 2.2 nM.

G-Protein antagonist peptide TFA is a truncated substance P-related peptide, competes with receptor for G protein binding. G-Protein antagonist peptide TFA inhibits the activation of G_i or G_o by M2 muscarinic cholinergic receptor (M2 mAChR) or of G_s by beta-adrenergic receptor in the reconstituted phospholipid vesicles, assayed by receptor-promoted GTP hydrolysis.

Fentonium bromide is an anti-ulcerogenic, anticholinergic and antispasmodic agent. Fentonium bromide can be used in the research of neurological conditions, such as unstable bladder.

VU6016235 is a highly selective, orally available, positive allosteric modulator of the M4 mAChR with in vivo inhibitory potency in animal models of psychosis..