mAChR-Antagonists-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/mAChR.html mAChRMuscarinic acetylcholine receptormAChRs (muscarinic acetylcholine receptors) are acetylcholine receptors that form G protein-receptor complexes in the cellmembranes of certainneurons and other cells. They play several roles, including acting as

2、the main end-receptor stimulated byacetylcholine released from postganglionic fibersin the parasympathetic nervous system. mAChRs are named as such because theyare more sensitive to muscarine than to nicotine. Their counterparts are nicotinic acetylcholine receptors (nAChRs), receptor ionchannels th

3、at are also important in the autonomic nervous system. Many drugs and other substances (for example pilocarpineandscopolamine) manipulate these two distinct receptors by acting as selective agonists or antagonists. Acetylcholine (ACh) is aneurotransmitter found extensively in the brain and the auton

4、omic ganglia.www.MedChemE 1 HYPERLINK https:/www.MedChemE/Targets/mAChR.html mAChR HYPERLINK https:/www.MedChemE/Targets/mAChR.html HYPERLINK https:/www.MedChemE/Targets/mAChR.html Inhibitors, HYPERLINK https:/www.MedChemE/Targets/mAChR.html HYPERLINK https:/www.MedChemE/Targets/mAChR.html Agonists,

5、 HYPERLINK https:/www.MedChemE/Targets/mAChR.html HYPERLINK https:/www.MedChemE/Targets/mAChR.html Antagonists, HYPERLINK https:/www.MedChemE/Targets/mAChR.html HYPERLINK https:/www.MedChemE/Targets/mAChR.html Activators HYPERLINK https:/www.MedChemE/Targets/mAChR.html HYPERLINK https:/www.MedChemE/

6、Targets/mAChR.html & HYPERLINK https:/www.MedChemE/Targets/mAChR.html HYPERLINK https:/www.MedChemE/Targets/mAChR.html Modulators HYPERLINK https:/www.MedChemE/_addition_-Cevimeline-hydrochloride-hemihydrate.html (+)-Cevimeline HYPERLINK https:/www.MedChemE/_addition_-Cevimeline-hydrochloride-hemihy

7、drate.html HYPERLINK https:/www.MedChemE/_addition_-Cevimeline-hydrochloride-hemihydrate.html hydrochloride HYPERLINK https:/www.MedChemE/_addition_-Cevimeline-hydrochloride-hemihydrate.html HYPERLINK https:/www.MedChemE/_addition_-Cevimeline-hydrochloride-hemihydrate.html hemihydrate(+)-SNI-2011; (

8、+)-AF102B hydrochloride hemihydrate) Cat. No.: HY-76772A HYPERLINK https:/www.MedChemE/_-_-Cevimeline-hydrochloride-hemihydrate.html (-)-Cevimeline HYPERLINK https:/www.MedChemE/_-_-Cevimeline-hydrochloride-hemihydrate.html HYPERLINK https:/www.MedChemE/_-_-Cevimeline-hydrochloride-hemihydrate.html

9、hydrochloride HYPERLINK https:/www.MedChemE/_-_-Cevimeline-hydrochloride-hemihydrate.html HYPERLINK https:/www.MedChemE/_-_-Cevimeline-hydrochloride-hemihydrate.html hemihydrate(-)-SNI-2011; (-)-AF102B hydrochloride hemihydrate) Cat. No.: HY-76772B(+)-Cevimeline hydrochloride hemihydrate(+)-SNI-2011

10、), a potent muscarinic receptoragonist, is a candidate therapeutic drug forxerostomia in Sjogrens syndrome. IC50 value:Target: mAChR The general pharmacol.(-)-Cevimeline hydrochloride hemihydrate(-)-SNI-2011), a novel muscarinic receptoragonist, is a candidate therapeutic drug forxerostomia in Sjogr

11、ens syndrome. IC50 value:Target: mAChR The general pharmacol.Purity: 98%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 1 mg, 5 mgPurity: 98%Clinical Data: LaunchedSize: 10 mM 1 mL, 1 mg, 5 mg HYPERLINK https:/www.MedChemE/1r-3s-solifenacin-d5-hydrochloride.html (1R,3S-)Solifenacin-d5 HYPERL

12、INK https:/www.MedChemE/1r-3s-solifenacin-d5-hydrochloride.html HYPERLINK https:/www.MedChemE/1r-3s-solifenacin-d5-hydrochloride.html hydrochlorideCat. No.: HY-135329S HYPERLINK https:/www.MedChemE/r-r-glycopyrrolate.html (R,R)-Glycopyrrolate HYPERLINK https:/www.MedChemE/r-r-glycopyrrolate.html (R,

13、R)-Glycopyrronium bromide;(R,R)-Glycopyrrolate bromide) Cat. No.: HY-B0761(1R,3S-)Solifenacin-d5 hydrochloride is thedeuterium labeled Solifenacin D5 hydrochloride.Solifenacin D5 hydrochloride is a deuteriumlabeled Solifenacin hydrochloride.(R,R)-Glycopyrrolate (R,R)-Glycopyrronium(bromide); (R,R)-G

14、lycopyrrolate (bromide) is ananticholinergic agent.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/rac-5-hydroxymethyl-tolterodine.html (Rac)-5-Hydroxymethyl HYPERLINK https:/www.MedChemE

15、/rac-5-hydroxymethyl-tolterodine.html HYPERLINK https:/www.MedChemE/rac-5-hydroxymethyl-tolterodine.html Tolterodine(Rac)-Desfesoterodine; (Rac)-PNU-200577) Cat. No.: HY-76570 HYPERLINK https:/www.MedChemE/rac-5-hydroxymethyl-tolterodine-hydrochloride.html (Rac)-5-Hydroxymethyl HYPERLINK https:/www.

16、MedChemE/rac-5-hydroxymethyl-tolterodine-hydrochloride.html HYPERLINK https:/www.MedChemE/rac-5-hydroxymethyl-tolterodine-hydrochloride.html Tolterodine HYPERLINK https:/www.MedChemE/rac-5-hydroxymethyl-tolterodine-hydrochloride.html HYPERLINK https:/www.MedChemE/rac-5-hydroxymethyl-tolterodine-hydr

17、ochloride.html hydrochloride(Rac)-Desfesoterodine hydrochloride; ) Cat. No.: HY-76570A(Rac)-5-Hydroxymethyl Tolterodine(Rac)-Desfesoterodine), an active metabolite ofTolterodine, is a mAChR antagonist (K valuesiof 2.3 nM, 2 nM, 2.5 nM, 2.8 nM, and 2.9 nM forM1, M2, M3, M4, and M5 receptors,respectiv

18、ely).(Rac)-5-Hydroxymethyl Tolterodine(Rac)-Desfesoterodine) hydrochloride, an activemetabolite of Tolterodine, is a mAChRantagonist (K values of 2.3 nM, 2 nM, 2.5 nM, 2.8inM, and 2.9 nM for M1, M2, M3, M4, andM5 receptors,Purity: 98%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 m

19、g, 25 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/rac-desfesoterodine.html (Rac)-5-Hydroxymethyl HYPERLINK https:/www.MedChemE/rac-desfesoterodine.html HYPERLINK https:/www.MedChemE/rac-desfesoterodine.html Tolterodine-d14 HYPERLIN

20、K https:/www.MedChemE/rac-desfesoterodine.html HYPERLINK https:/www.MedChemE/rac-vu-6008667.html (Rac)-VU HYPERLINK https:/www.MedChemE/rac-vu-6008667.html HYPERLINK https:/www.MedChemE/rac-vu-6008667.html 6008667(Rac)-Desfesoterodine-d14; (Rac)-PNU-200577-d14) Cat. No.: HY-76570SCat. No.: HY-101281

21、A(Rac)-5-Hydroxymethyl Tolterodine-d14(Rac)-Desfesoterodine-d14) is the deuteriumlabeled (Rac)-5-Hydroxymethyl Tolterodine.(Rac)-VU 6008667 is a selective negativeallosteric modulator of muscarinic acetylcholinereceptor subtype 5 (M5 NAM) (IC =1.8 M,50pIC = 5.75), has high CNS penetration.50Purity:

22、98%Clinical Data: No Development ReportedSize: 1 mg, 10 mgPurity: 98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg HYPERLINK https:/www.MedChemE/s-plus-dimethindene-maleate.html (S)-(+)-Dimethindene HYPERLINK https:/www.MedChemE/s-plus-dimethindene-maleate.html HYPERLINK http

23、s:/www.MedChemE/s-plus-dimethindene-maleate.html maleate HYPERLINK https:/www.MedChemE/s-plus-dimethindene-maleate.html HYPERLINK https:/www.MedChemE/racemic-darifenacin.html ()-DarifenacinCat. No.: HY-107647()-UK-88525) Cat. No.: HY-22437(S)-(+)-Dimethindene maleate, an enantiomer, is apotent M -se

24、lective muscarinic receptor2antagonist (pA2 = 7.86/7.74; pKi = 7.78).()-Darifenacin is the racemate of Darifenacin.Darifenacin is a selective M3 muscarinic receptorantagonist.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98.10%Clinical Data: LaunchedSize: 10 mM 1 mL, 50 mg

25、, 100 mg2 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/racemic-darifenacin-d4.html ()-Darifenacin-d4()-UK-88525-d4) Cat. No.: HY-22437S HYPERLINK https:/www.MedChemE/racemic-darifenacin-d4-hydrobromide.html ()-Darifenacin-d4 HYPERLINK https:/www.MedChemE/rac

26、emic-darifenacin-d4-hydrobromide.html HYPERLINK https:/www.MedChemE/racemic-darifenacin-d4-hydrobromide.html hydrobromide()-UK-88525-d4 hydrobromide) Cat. No.: HY-22437S1()-Darifenacin-d4 is deuterium labeled()-Darifenacin. ()-Darifenacin is the racemateof Darifenacin. Darifenacin is a selective M3m

27、uscarinic receptor antagonist.()-Darifenacin-d4 (hydrobromide) is deuteriumlabeled ()-Darifenacin. ()-Darifenacin is theracemate of Darifenacin. Darifenacin is aselective M3 muscarinic receptor antagonist.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No D

28、evelopment ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/racemic-muscarine-chloride.html ()-Muscarine HYPERLINK https:/www.MedChemE/racemic-muscarine-chloride.html HYPERLINK https:/www.MedChemE/racemic-muscarine-chloride.html chloride(DL-Muscarin chloride) Cat. No.: HY-139126 HYPERLINK http

29、s:/www.MedChemE/4-damp.html 4-DAMP(4-DAMP methiodide) Cat. No.: HY-100958()-Muscarine chloride is the racemate ofMuscarine chloride. Muscarine is a prototypemuscarinic acetylcholine receptor agonist.4-DAMP is a potent antagonist of M3 receptorand also has a high affinity for theclosely-related M5 re

30、ceptor.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/5-hydroxymethyl-tolterodine-d14-formate.html 5-Hydroxymethyl HYPERLINK https:/www.MedChemE/5-hydroxymethyl-tolterodine-d14-formate.h

31、tml HYPERLINK https:/www.MedChemE/5-hydroxymethyl-tolterodine-d14-formate.html Tolterodine-d14 HYPERLINK https:/www.MedChemE/5-hydroxymethyl-tolterodine-d14-formate.html HYPERLINK https:/www.MedChemE/5-hydroxymethyl-tolterodine-d14-formate.html (formate) HYPERLINK https:/www.MedChemE/5-hydroxymethyl

32、-tolterodine-d14-formate.html HYPERLINK https:/www.MedChemE/AC260584.html AC260584Cat. No.: HY-76570S1 Cat. No.: HY-1003365-Hydroxymethyl Tolterodine-d14 (formate) isdeuterium labeled (Rac)-5-HydroxymethylTolterodine.AC260584 is an M1 muscarinic receptorallosteric agonist with a pEC of 7.6.50Purity:

33、 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.25%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 1 mg, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/aceclidine.html Aceclidine HYPERLINK https:/www.MedChemE/aceclidine.html HYPERLINK https:/www.MedChemE/Aclidi

34、nium-Bromide.html Aclidinium HYPERLINK https:/www.MedChemE/Aclidinium-Bromide.html HYPERLINK https:/www.MedChemE/Aclidinium-Bromide.html Bromide(Quinuclidin-3-yl acetate) Cat. No.: HY-32067 (LAS 34273; LAS-W 330) Cat. No.: HY-14144Aceclidine is a modulator of M3 muscarinicacetylcholine receptor. Ace

35、clidine is acycloplegic agent, a surfactant, a tonicityadjustor and optionally a viscosity enhancer andan antioxidant.Aclidinium Bromide (LAS 34273; LAS-W 330) is along-acting, inhaled muscarinic antagonist.Aclidinium Bromide has the potential for chronicobstructive pulmonary disease (COPD) research

36、.Purity: 98%Clinical Data: No Development ReportedSize: 100 mg, 500 mgPurity: 98.08%Clinical Data: LaunchedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/af-dx-384.html AF-DX HYPERLINK https:/www.MedChemE/af-dx-384.html HYPERLINK https:/www.MedChemE/af-dx-384.html 384 HYP

37、ERLINK https:/www.MedChemE/af-dx-384.html HYPERLINK https:/www.MedChemE/Alvameline.html AlvamelineCat. No.: HY-107652(Lu 25-109) Cat. No.: HY-101586AF-DX 384 is a selective antagonist of M2 and M4muscarinic acetylcholine receptors (Ks=6.03 andi10 nM, respectively). AF-DX 384 reverses deficitsin nove

38、l object recognition and passive avoidancein aged rats, as well as in young rats withimpairments induced by scopolamine.Alvameline (Lu25-109) is a partial M1 agonistand M2/M3 antagonist.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development Reported

39、Size: 1 mg, 5 mgwww.MedChemE 3 HYPERLINK https:/www.MedChemE/Ambutonium_(bromide).html Ambutonium HYPERLINK https:/www.MedChemE/Ambutonium_(bromide).html HYPERLINK https:/www.MedChemE/Ambutonium_(bromide).html bromide(BL700) Cat. No.: HY-U00067 HYPERLINK https:/www.MedChemE/ambutonium-d5-bromide.htm

40、l Ambutonium-d5 HYPERLINK https:/www.MedChemE/ambutonium-d5-bromide.html HYPERLINK https:/www.MedChemE/ambutonium-d5-bromide.html bromide(BL700-d5) Cat. No.: HY-U00067SAmbutonium bromide is an acetylcholine antagonist.Ambutonium-d5 bromide (BL700-d5) is the deuteriumlabeled Ambutonium bromide. Ambut

41、onium bromide isan acetylcholine antagonist.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/amitriptyline-hydrochloride.html Amitriptyline HYPERLINK https:/www.MedChemE/amitriptyline-hydr

42、ochloride.html HYPERLINK https:/www.MedChemE/amitriptyline-hydrochloride.html hydrochloride HYPERLINK https:/www.MedChemE/amitriptyline-hydrochloride.html HYPERLINK https:/www.MedChemE/amitriptyline-d3-hydrochloride.html Amitriptyline-d3 HYPERLINK https:/www.MedChemE/amitriptyline-d3-hydrochloride.h

43、tml HYPERLINK https:/www.MedChemE/amitriptyline-d3-hydrochloride.html hydrochlorideCat. No.: HY-B0527A Cat. No.: HY-135096Amitriptyline hydrochloride is an inhibitor ofserotonin reuptake transporter (SERT) andnoradrenaline reuptake transporter (NET), with Ksiof 3.45 nM and 13.3 nM for human SERT and

44、 NET,respectively.Amitriptyline-d3 hydrochloride is the deuteriumlabeled Amitriptyline (hydrochloride).Purity: 99.56%Clinical Data: LaunchedSize: 10 mM 1 mL, 500 mg, 1 g, 5 gPurity: 98%Clinical Data: No Development ReportedSize: 2.5 mg, 1 mg, 5 mg, 10 mg HYPERLINK https:/www.MedChemE/amitriptyline-d

45、6-hydrochloride.html Amitriptyline-d6 HYPERLINK https:/www.MedChemE/amitriptyline-d6-hydrochloride.html HYPERLINK https:/www.MedChemE/amitriptyline-d6-hydrochloride.html hydrochlorideCat. No.: HY-B0527AS HYPERLINK https:/www.MedChemE/anagyrine.html Anagyrine(-)-Anagyrine; Monolupine; Rhombinine) Cat

46、. No.: HY-121027Amitriptyline-d6 hydrochloride is the deuteriumlabeled Amitriptyline hydrochloride.Anagyrine is an alkaloid that has been found in L.albus and has nematocidal and anticanceractivities.It binds to muscarinic and nicotinicacetylcholine receptors (AChRs) with IC values50of 132 and 2096

47、M respectively.Purity: 98%Clinical Data: No Development ReportedSize: 2.5 mg, 1 mg, 5 mg, 25 mgPurity: 98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg HYPERLINK https:/www.MedChemE/Anethole-trithione.html Anethole HYPERLINK https:/www.MedChemE/Anethole-trithione.html HYPERLINK http

48、s:/www.MedChemE/Anethole-trithione.html trithione HYPERLINK https:/www.MedChemE/Anethole-trithione.html HYPERLINK https:/www.MedChemE/Anisodamine.html AnisodamineCat. No.: HY-B1223(6-Hydroxyhyoscyamine) Cat. No.: HY-N0584Anethole trithione, a sulfur heterocycliccholeretic, is a bile secretion-stimul

49、ating agent.Anethole trithione enhances salivary secretion andincreases mAChRs, and can be used for dry mouthresearch.Anisodamine (6-Hydroxyhyoscyamine), a belladonnaalkaloid, is a non-subtype-selectivemuscarinic, and also a nicotinic cholinoceptorantagonist.Purity: 99.67%Clinical Data: LaunchedSize

50、: 10 mM 1 mL, 100 mg, 500 mgPurity: 98.01%Clinical Data: LaunchedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/anisodamine-hydrobromide.html Anisodamine HYPERLINK https:/www.MedChemE/anisodamine-hydrobromide.html HYPERLINK https:/www.MedChemE/anisodamine-hydrobromide.html hydrobromide HYPERLINK htt

51、ps:/www.MedChemE/anisodamine-hydrobromide.html HYPERLINK https:/www.MedChemE/arborine.html Arborine(6-Hydroxyhyoscyamine hydrobromide) Cat. No.: HY-N0584ACat. No.: HY-N7004Anisodamine hydrobromide (6-Hydroxyhyoscyaminehydrobromide), a belladonna alkaloid, is anon-subtype-selective muscarinic and a n

52、icotiniccholinoceptor antagonist. Anisodamine hydrobromideshows antioxidant, anti-inflammatory properties.Arborine inhibits the peripheral action ofacetylcholine and induces a fall in bloodpressure.Purity: 98.35%Clinical Data: LaunchedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development Reported

53、Size: 1 mg, 5 mg, 10 mg4 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/Atropine.html Atropine(Tropine tropate; DL-Hyoscyamine) Cat. No.: HY-B1205 HYPERLINK https:/www.MedChemE/Atropine_methyl_bromide.html Atropine HYPERLINK https:/www.MedChemE/Atropine_methyl

54、_bromide.html HYPERLINK https:/www.MedChemE/Atropine_methyl_bromide.html methyl HYPERLINK https:/www.MedChemE/Atropine_methyl_bromide.html HYPERLINK https:/www.MedChemE/Atropine_methyl_bromide.html bromide(Methylatropine bromide) Cat. No.: HY-112076Atropine (Tropine tropate) is a competitivemuscarin

55、ic acetylcholine receptor (mAChR)antagonist, with anti-myopia effect. Atropineblocks the inhibitory effect of ACh on heart rateand contractility, potentially also leading totachyarrhythmias.Atropine methyl bromide, a muscarinic receptor(mAChR) antagonist, is a quaternary ammoniumsalt of atropine and

56、 a mydriatic for dilation ofthe pupil during ophthalmic examination. It isintroduced for relieving pyloric spasm in infantsfor its highly polar nature.Purity: 99.55%Clinical Data: LaunchedSize: 10 mM 1 mL, 100 mgPurity: 95.0%Clinical Data: LaunchedSize: 10 mM 1 mL, 10 mg, 50 mg, 100 mg HYPERLINK htt

57、ps:/www.MedChemE/Atropine-sulfate.html Atropine HYPERLINK https:/www.MedChemE/Atropine-sulfate.html HYPERLINK https:/www.MedChemE/Atropine-sulfate.html sulfate HYPERLINK https:/www.MedChemE/Atropine-sulfate.html (Tropine tropate sulfate; DL-Hyoscyaminesulfate; Sulfatropinol) Cat. No.: HY-B1205A HYPE

58、RLINK https:/www.MedChemE/Atropine-sulfate-monohydrate.html Atropine HYPERLINK https:/www.MedChemE/Atropine-sulfate-monohydrate.html HYPERLINK https:/www.MedChemE/Atropine-sulfate-monohydrate.html sulfate HYPERLINK https:/www.MedChemE/Atropine-sulfate-monohydrate.html HYPERLINK https:/www.MedChemE/A

59、tropine-sulfate-monohydrate.html monohydrate HYPERLINK https:/www.MedChemE/Atropine-sulfate-monohydrate.html (Tropine tropate sulfatemonohydrate; DL-Hyoscyamine sulfate monohydrate) Cat. No.: HY-B0394Atropine (Tropine tropate) sulfate is abroad-spectrum and competitive muscarinicacetylcholine recept

60、or (mAChR) antagonist.Atropine (Tropine tropate) sulfate monohydrate isa broad-spectrum and competitive muscarinicacetylcholine receptor (mAChR) antagonist withanti-myopia effect.Purity: 98.07%Clinical Data: LaunchedSize: 100 mgPurity: 99.62%Clinical Data: LaunchedSize: 10 mM 1 mL, 100 mg HYPERLINK