mAChR Muscarinic acetylcholine receptor mAChRs (muscarinic acetylcholine receptors) are acetylcholine receptors that form G protein-receptor complexes in the cell membranes of certainneurons and other cells. They play several roles, including acting as the main end-receptor stimulated by acetylcholine released from postganglionic fibersin the parasympathetic nervous system. mAChRs are named as such because they are more sensitive to muscarine than to nicotine. Their counterparts are nicotinic acetylcholine receptors (nAChRs), receptor ion channels that are also important in the autonomic nervous system. Many drugs and other substances (for example pilocarpineand scopolamine) manipulate these two distinct receptors by acting as selective agonists or antagonists. Acetylcholine (ACh) is a neurotransmitter found extensively in the brain and the autonomic ganglia. www.MedChemExpress.com 1 mAChR Inhibitors & Modulators (+)-Cevimeline hydrochloride hemihydrate (-)-Cevimeline hydrochloride hemihydrate Cat. No.: HY-76772A Cat. No.: HY-76772B Bioactivity: Cevimeline hydrochloride hemihydrate, a novel muscarinic Bioactivity: Cevimeline hydrochloride hemihydrate, a novel muscarinic receptor agonist, is a candidate therapeutic drug for receptor agonist, is a candidate therapeutic drug for xerostomia in Sjogren's syndrome. IC50 value: Target: mAChR xerostomia in Sjogren's syndrome. IC50 value: Target: mAChR The general pharmacol. properties of this drug on the The general pharmacol. properties of this drug on the gastrointestinal, urinary, and reproductive systems and other… gastrointestinal, urinary, and reproductive systems and other… Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 1 mg, 5 mg 1 mg, 5 mg AC260584 Aclidinium Bromide Cat. No.: HY-100336 (LAS 34273; LAS-W 330) Cat. No.: HY-14144 Bioactivity: AC260584 is an M1 muscarinic receptor allosteric agonist Bioactivity: Aclidinium Bromide(LAS 34273; LAS-W 330) is a long-acting, inhaled muscarinic antagonist as a maintenance treatment for with a pEC50 of 7.6. chronic obstructive pulmonary disease (COPD). Purity: 98.02% Purity: 99.54% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 1 mg, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg Alvameline Ambutonium bromide (Lu 25-109) Cat. No.: HY-101586 (BL700) Cat. No.: HY-U00067 Bioactivity: Alvameline (Lu25-109) is a partial M1 agonist and M2/M3 Bioactivity: Ambutonium bromide is an acetylcholine antagonist. antagonist. Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg Size: 1 mg, 5 mg, 10 mg, 20 mg Anisodamine Arecoline hydrobromide (6-Hydroxyhyoscyamine) Cat. No.: HY-N0584 (Arecoline bromide) Cat. No.: HY-B0489 Bioactivity: Anisodamine is an anticholinergic and α1-adrenergic receptor Bioactivity: Arecoline Hydrobromide is a muscarinic acetylcholine receptor antagonist used in the treatment of acute circulatory shock, agonist. is also a naturally occurring tropane alkaloid found in some plants of the Solanaceae family. Purity: 98.0% Purity: 99.0% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 100 mg 500 mg, 1 g Atropine Atropine methyl bromide (Tropine tropate; DL-Hyoscyamine) Cat. No.: HY-B1205 (Methylatropine bromide) Cat. No.: HY-112076 Bioactivity: Atropine is a medication used to treat certain types of nerve Bioactivity: Atropine methyl bromide, a muscarinic receptor (mAChR) agent and pesticide poisonings, some types of slow heart rate, antagonist, is a quaternary ammonium salt of atropine and a and to decrease saliva production during surgery. mydriatic for dilation of the pupil during ophthalmic examination. It is introduced for relieving pyloric spasm in infants for its highly polar nature. It penetrates less… Purity: 99.55% Purity: 95.0% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 100 mg 10 mg, 50 mg, 100 mg 2 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] Atropine sulfate Atropine sulfate monohydrate (Sulfatropinol) Cat. No.: HY-B1205A (Atropine sulfate hydrate) Cat. No.: HY-B0394 Bioactivity: Atropine sulfate is a competitive muscarinic acetylcholine Bioactivity: Atropine sulfate monohydrate is a competitive muscarinic receptor antagonist. acetylcholine receptor antagonist. Target: mAChR Atropine is a naturally occurring tropane alkaloid extracted from deadly nightshade (Atropa belladonna), Jimson weed (Datura stramonium), mandrake (Mandragora officinarum) and other… Purity: >98% Purity: 99.62% Clinical Data: Launched Clinical Data: Launched Size: 100 mg Size: 10mM x 1mL in DMSO, 100 mg Batefenterol Benzamide Derivative 1 (GSK961081; TD-5959) Cat. No.: HY-12980 Cat. No.: HY-U00415 Bioactivity: Batefenterol (GSK961081;TD-5959) is a novel muscarinic Bioactivity: Benzamide Derivative 1 is a benzamide derivative from patent EP0213775A1, compound 18. Benzamide Derivative 1 may be useful receptor antagonist and β2-adrenoceptor agonist; displays in treatment of gastrointestinal disorders. high affinity for hM2, hM3 muscarinic and hβ 2-adrenoceptor with Ki values of 1.4, 1.3 and 3.7 nM, respectively. Purity: 98.30% Purity: >98% Clinical Data: Phase 2 Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg, 10 mg 5 mg, 10 mg, 50 mg, 100 mg Benzetimide hydrochloride Benztropine mesylate (Benzatropine mesylate; Benzotropine (R4929) Cat. No.: HY-B1547A mesylate; Benztropine methanesulfonate) Cat. No.: HY-B0520A Bioactivity: Benzetimide hydrochloride is a muscarinic acetylcholine Bioactivity: Benzotropine is a centrally-acting, antimuscarinic agent used receptor antagonist. as an adjunct in the treatment of Parkinson's disease. Target: mAChR Benzotropine is a centrally-acting, antimuscarinic agent used as an adjunct in the treatment of Parkinson's disease. It may also be used to treat extrapyramidal reactions, such as… Purity: 99.44% Purity: 99.86% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in Water, 10 mg, 50 mg 1 g Beperidium iodide Bethanechol (SX 810) Cat. No.: HY-100152 (Carbamyl-β-methylcholine) Cat. No.: HY-B0406 Bioactivity: Beperidium iodide shows a competitive antagonistic effect Bioactivity: Bethanechol is a parasympathomimetic choline carbamate that against acetylcholine receptor with a pA2 of 7.93. selectively stimulates muscarinic receptors without any effect on nicotinic receptors. Target: muscarinic receptor Hyoscine butylbromide concentration dependently reduced muscle contractions, calcium mobilization, and epithelial secretion… Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: Launched Size: 1 mg, 5 mg, 10 mg Size: 1 g Bethanechol chloride Biperiden (Carbamyl-β-methylcholine chloride) Cat. No.: HY-B0406A (KL 373) Cat. No.: HY-13204A Bioactivity: Bethanechol Chloride is a selective muscarinic receptor Bioactivity: Biperiden(KL 373) is an antiparkinsonian agent, which is the agonist without any effect on nicotinic receptors. selective central M1 cholinoreceptors blocker. Target: M1 receptors Biperiden is an antiparkinsonian agent of the anticholinergic type. It is used for the adjunctive treatment of all forms of Parkinson's disease (postencephalitic,… Purity: 95.00% Purity: >98% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in Water, Size: 100 mg, 500 mg 200 mg, 5 g www.MedChemExpress.com 3 Biperiden Hydrochloride BQCA (KL 373 (Hydrochloride)) Cat. No.: HY-13204 Cat. No.: HY-101858 Bioactivity: Biperiden Hydrochloride (KL 373 Hydrochloride) is an Bioactivity: BQCA a highly selective allosteric modulator of the M1 antiparkinsonian agent, which is the selective central M1 mAChR. cholinoreceptors blocker. Target: M1 receptors Biperiden is an antiparkinsonian agent of the anticholinergic type. It is used for the adjunctive treatment of all forms of Parkinson's… Purity: 98.0% Purity: 98.0% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in Water, Size: 10mM x 1mL in DMSO, 100 mg, 500 mg 5 mg, 10 mg, 25 mg, 50 mg, 100 mg BTM-1086 Camylofine Cat. No.: HY-U00406 Cat. No.: HY-B1230 Bioactivity: BTM-1086 is a potent anti-ulcer and gastric secretory Bioactivity: Camylofin is an antimuscarinic, is a smooth muscle relaxant. inhibiting agent. Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: Launched Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 1 g Carbamoylcholine chloride CDD0102 (Carbachol; Carbamylcholine chloride) Cat. No.: HY-B1208 (CDD0102A) Cat. No.: HY-U00230 Bioactivity: Carbamoylcholine chloride is used to study responses mediated Bioactivity: CDD0102 is a potent M1 Muscarinic receptor agonist. by nAChR and mAChR, including smooth muscle contraction, gut motility, and neuronal signaling. IC50 value: 10 to 10,000 nM (Ki) Target: nAChR, mAChR Carbamoylcholine is an analog of acetylcholine that activates acetylcholine receptors (AChR).… Purity: 98.0% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg, 10 mg, 20 mg 100 mg Cevimeline Cevimeline hydrochloride (AF-102B) Cat. No.: HY-70020 (AF-102B hydrochloride; SNI-2011 hydrochloride) Cat. No.: HY-70020B Bioactivity: Cevimeline (AF-102B) is a parasympathomimetic and muscarinic Bioactivity: Cevimeline (Evoxac) Hcl is a parasympathomimetic