mAChR Inhibitor

VU 6008667 is a selective negative allosteric modulator of M5 NAM with IC₅₀s of 1.2 μM and 1.6 μM for human M5 and rat M5, respectively. High CNS penetration.

Brompheniramine ((±)-Brompheniramine) is a potent and orally active antihistamine of the alkylamine class. Brompheniramine is a selective histamine H1 receptor antagonist with a K_d of 6.06 nM. Brompheniramine can block the hERG channels, calcium channels, and sodium channels with IC₅₀s of 0.90 μM, 16.12 μM and 21.26 μM, respectively. Brompheniramine has anticholinergic, antidepressant and anesthetic properties and can be used for allergic rhinitis research.

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.

Camylofine is an antispasmodic agent with myogenic and neurogenic effects. Camylofine exhibits mild anticholinergic activity and blocks the M3 receptors on colonic smooth muscle. Camylofine dihydrochloride inhibits phosphodiesterase, elevates intracellular cAMP levels and reduces intracellular Ca²⁺ levels, thereby promoting smooth muscle relaxation. Camylofine can be used in studies related to antispasmodia, gastrointestinal smooth muscle and ulcerative colitis.

Ebelin lactone is an acetylcholinesterase (AChE) inhibitor, with a K_i of 0.45 μM against human M1 muscarinic acetylcholine receptor (mAChR) and a K_i of 4.21 μM against human 5-HT2A serotonin receptor. Ebelin lactone binds to the allosteric cavity above the orthosteric site of M1 via nonpolar interactions with subtype-selective residues. Ebelin lactone binds to the cavity between transmembrane helices 4 and 5 of 5-HT2A through nonpolar interactions with orthosteric site residues. Ebelin lactone exhibits free radical scavenging activity, inhibits cancer cell proliferation, and regulates memory and cognitive processes by interacting with M1 and 5-HT2A receptors. Ebelin lactone can be used in studies related to Alzheimer's disease, breast cancer and colorectal cancer.

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.

(Rac)-VU 6008667 is a selective negative allosteric modulator of muscarinic acetylcholine receptor subtype 5 (M5 NAM) (IC₅₀=1.8 μM, pIC₅₀= 5.75), has high CNS penetration.

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.

Trihexyphenidyl-d₅ hydrochloride is deuterium labeled Trihexyphenidyl hydrochloride (HY-B1277). Trihexyphenidyl hydrochloride is a selective and orally active M₁ muscarinic receptor antagonist with an IC₅₀ of 3.7 nM for rat cerebral cortex M1 muscarinic receptors. Trihexyphenidyl hydrochloride modulates cholinergic activity, countering acetylcholine supersensitivity in neural pathways. Trihexyphenidyl hydrochloride improves movement disorder, inhibits McN-A-343 (HY-107648)-induced pressor responses, vagally-induced bradycardia and vasodilatation. Trihexyphenidyl hydrochloride can be used for the research of Parkinson's disease..

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

[D-Trp7,9,10]-Substance P TFA is a substance P analogue. Substance P stimulates substance P receptors but also inhibits ion conductance through nicotinic acetylcholine receptors.

rel-Biperiden EP impurity A-d₅ is deuterium labeled Biperiden (hydrochloride).

Darenzepine is a muscarinic receptor inhibitor extracted from patent US 20170095465 A1.

Ethybenztropine (Ponalid) is a muscarinic receptor blocker. Ethybenztropine is an anticholinergic and antihistaminergic agent.

Ethybenztropine hydrobromide (Ponalid hydrobromide) is an anticholinergic drug with antiparkinsonian activity. Ethybenztropine hydrobromide may also act as a dopamine reuptake inhibitor. Ethybenztropine hydrobromide is commonly used to suppress Parkinson's disease.