Cat. No. | Product name | CAS No. |
DC11748 |
LY2033298
Featured
LY2033298 is a robust allosteric potentiator that is highly selective for the human M4 muscarinic acetylcholine receptor subtype. LY2033298 enhances inhibition by oxotremorine of light-induced phase shifts in hamster circadian activity rhythms. |
886047-13-8 |
DC10293 |
AC260584
AC260584 is an M1 muscarinic receptor allosteric agonist with a pEC50 of 7.6. |
560083-42-3 |
DC11747 |
Iperoxo
Iperoxo is a superagonist of the muscarinic acetylcholine receptors and an OxotremorineM analog. |
247079-84-1 |
DC10731 |
Arecaidine but-2-ynyl ester tosylate
Arecaidine but-2-ynyl ester tosylate is a potent muscarinic agonist that shows 4.6-fold that is selectivity for mAChR M2 in the atrium versus those in the ileum. |
119630-77-2 |
DC10021 |
Batefenterol
Featured
Batefenterol(GSK961081,TD-5959)is a Muscarinic Antagonist and β2-Agonist possessing both muscarinic antagonist (MA) and β2-adrenoceptor agonist (BA) properties (MABA). |
743461-65-6 |
DCAPI1702 |
Diphemanil methylsulfate
Featured
Diphemanil Methylsulfate is a quaternary ammonium anticholinergic, it binds muscarinic acetycholine receptors (mAchR). |
62-97-5 |
DC10039 |
DREADD Agonist 21
Featured
DREADD agonist 21 is a potent muscarinic hM3Dq DREADD agonist (EC50 = 1.7 nM). Highly selective for hM3Dq DREADDs over endogenous hM3 receptors. |
56296-18-5 |
DC8912 |
Fesoterodine fumarate
Featured
Fesoterodine Fumarate is an antimuscarinic agent and is rapidly de-esterified to its active metabolite 5-hydroxymethyl tolterodine that is a muscarinic receptor antagonist. |
286930-03-8 |
DC8779 |
Glycopyrrolate
Featured
Glycopyrrolate(Glycopyrronium Br) is a muscarinic competitive antagonist used as an antispasmodic. |
596-51-0 |
DC8435 |
LY2119620
Featured
LY2119620 is a specific, and allosteric agonist of human M2 and M4 muscarinic acetylcholine receptors. |
886047-22-9 |
DC11111 |
PF-06764427
PF-06764427 (PF06764427) is a potent, selective M1 muscarinic acetylcholine receptor (mAChR) positive allosteric modulator with EC50 of 55 nM, has no measurable agonist or PAM activity at the M2-M5 receptors at 10 uM. |
1842371-08-7 |
DC11116 |
PF-06827443
PF-06827443 (PF06827443) is a potent, orally bioavailable, and CNS-penetrant M1-selective positive allosteric modulator (PAM) with EC50 of 47 nM, shows no activity against M2-M5 at 10 uM. |
2115022-67-6 |
DC10012 |
Pirmenol hydrochloride
Featured
Pirmenol hydrochloride inhibits IK.ACh by blocking muscarinic receptors. The IC50 of Pirmenol for inhibition of Carbachol-induced IK.ACh is 0.1 μM. |
61477-94-9 |
DC11208 |
TAK-071
Featured
TAK-071 is a novel, potent and highly selective muscarinic acetylcholine receptor 1 (M1R) positive allosteric modulator. EC50 of TAK-071 M1R agonist activities is 520 nM. |
1820812-16-5 |
DC7932 |
TBPB
Featured
TBPB is an allosteric M1 mAChR agonist(EC50=289 nM) that regulates amyloid processing and produces antipsychotic-like activity in rats. |
634616-95-8 |
DC8813 |
TD-4208
Featured
TD-4208 is a potent and selective inhaled muscarinic antagonist with functional lung selectivity and long duration of action in preclinical models of bronchoconstriction. |
864750-70-9 |
DCAPI1449 |
Tiotropium Bromide
Featured
Tiotropium Bromide is a muscarinic acetylcholine receptor (mAChR M) antagonist that blocks the binding of the acetylcholine ligand and subsequent opening of the ligand-gated ion channel. This stops signaling between neurons and leads to muscle relaxation. |
136310-93-5 |
DCAPI1429 |
Tolterodine tartrate
Tolterodine L-Tartrate is a muscarinic receptor antagonist that is active at all mAChR M subtypes. This compound blocks the opening of ion channels by acetylcholine, which in turn leads to muscle relaxation by blocking neuronal signaling. |
124937-52-6 |
DC8153 |
Umeclidinium bromide
Featured
Umeclidinium bromide(GSK573719A) is a muscarinic receptor antagonist which is useful in treatment of chronic obstructive pulmonary disease (COPD). |
869113-09-7 |
DC12159 |
VU 0238429
Featured
VU 0238429 is positive allosteric modulator of muscarinic acetylcholine receptor subtype 5 (mAChR5 or M5), with an EC50 of 1.16 μM. |
1160247-92-6 |
DC12165 |
VU 0365114
Featured
VU 0365114 is a mAChR M5 positive allosteric modulator, with an EC50 of 2.7 μM. |
1208222-39-2 |
DC9497 |
VU0152100
Featured
VU0152100 is a potent and selective allosteric potentiator of M4 mAChR with an EC50 of 380 ± 93 nM. |
409351-28-6 |
DC9255 |
VU0357017
Featured
VU0357017 hydrochloride is a highly selective M1 agonists that appear to act at an allosteric site to activate the receptor (EC50 = 477 ± 172 nM; pEC50 = 6.37 ± 0.15). |
1135242-13-5 |
DC11112 |
VU0453595
VU0453595 (VU453595) is a potent, selective M1 positive allosteric modulator (PAM) with EC50 of 3.2 uM (rM1). |
1432436-13-9 |
DC11123 |
VU0467154
VU0467154 (VU 0467154) is a potent, selective M4 mAChR positive allosteric modulator with EC50 of 17.7 nM. |
1451993-15-9 |
DC11120 |
VU6004256
VU6004256 (VU 6004256) is a highly potent, selective M1 muscarinic acetylcholine receptor (mAChR) positive allosteric modulator with EC50 of 155 nM (mouse M1), significant selectivity over M2-M5 (EC50>30 uM). |
2011034-33-4 |
DC9498 |
Xanomeline (oxalate)
Xanomeline(LY246708) is a selective M1 muscarinic receptor agonist. |
141064-23-5 |
DC28123 |
Otenzepad
Otenzepad (AF-DX 116) is a selective and competitive M2 muscarinic acetylcholine receptor antagonist, with IC50 values of 640 nM and 386 nM for rabbit peripheral lung and rat heart, respectively. |
102394-31-0 |
DC28321 |
Nebracetam hydrochloride
Nebracetam hydrochloride, a nootropic M1-muscarinic agonist, induces a rise of intracellular Ca2+ concentration. Nebracetam hydrochloride exhibits an EC50 of 1.59 mM for elevating [Ca2+]i. |
1177279-49-0 |
DC28388 |
PQCA
PQCA is a highly selective and potent muscarinic M1 receptor positive allosteric modulator. PQCA has an EC50 value of 49 nM and 135 nM on rhesus and human M1 receptor, respectively, and is inactive for other muscarinic receptors. PQCA improves cognitive performance and cerebral blood flow in rat, cynomolgus macaque, and rhesus macaque. PQCA has potential to reduce the cognitive deficits associated with Alzheimer's disease. |
1144504-35-7 |
DC28434 |
PCS1055 dihydrochloride
PCS1055 dihydrochloride is a potent, selective and competitive muscarinic M4 receptor antagonist with an IC50 of 18.1 nM and a Kd of 5.72 nM. PCS1055 dihydrochloride inhibits radioligand [3H]-NMS binding to the M4 receptor with a Ki of 6.5 nM. PCS1055 dihydrochloride exhibits >100-fold selectivity over M1-, M3-, and M5-receptors and 30-fold selectivity at the M2 receptor. PCS1055 dihydrochloride is also a potent AChE inhibitor with IC50 s of 22 nM and 120 nM for electric eel and human AChE, respectively. |
361979-40-0 |
DC28809 |
Solifenacin D5 hydrochloride
Solifenacin D5 hydrochloride is a deuterium labeled Solifenacin hydrochloride. Solifenacin hydrochloride is a muscarinic receptor antagonist with pKis of 7.6, 6.9 and 8.0 for M1, M2 and M3 receptors, respectively. |
1426174-05-1 |
DC28989 |
Terodiline hydrochloride
Terodiline hydrochloride is an M1-selective muscarinic receptor (mAChR) antagonist with Kbs of 15, 160, 280, and 198 nM in rabbit vas deferens (M1), atria (M2), bladder (M3) and ileal muscle (M3), respectively. Terodiline hydrochloride also is a Ca2+ blocker. Terodiline hydrochloride acts as a treatment for urinary frequency and urge incontinence. |
7082-21-5 |
DC29053 |
(R,R)-Glycopyrrolate
(R,R)-Glycopyrrolate ((R,R)-Glycopyrronium (bromide); (R,R)-Glycopyrrolate (bromide)) is an anticholinergic agent. (R,R)-Glycopyrrolate ((R,R)-Glycopyrronium (bromide); (R,R)-Glycopyrrolate (bromide)) has the ability to reduce the frequency of drooling in vivo with developmental disabilities. |
475468-09-8 |
DC40216 |
VU0119498
Featured
VU0119498 is a pan Gq mAChR M1, M3, M5 positive allosteric modulator (PAM), with EC50s of 6.04, 6.38, and 4.08 μM, respectively. VU0119498 has antidiabetic activity. |
79183-37-2 |
DC40289 |
VU0238441
Featured
VU0238441 is a pan muscarinic acetylcholine receptor (mAChR) positive allosteric modulator (PAM) with EC50s of 3.2 μM, 2.8 μM, 2.2 μM, 2.1 μM, >10 μM for M1, M2, M3, M5 and M4, respectively. |
85511-68-8 |
DC41142 |
Nor-benzetimide
Featured
Nor-benzetimide is a major metabolite of Benzetimide. Benzetimide is a mAChR antagonist with anticholinergic activity. |
19315-71-0 |
DC41213 |
Clidinium-D5 bromide
Clidinium-D5 bromide (Ro 2-3773-D5) is the deuterium labeled Clidinium bromide. Clidinium bromide is a quaternary amine antimuscarinic agent. |
|
DC41236 |
Telenzepine dihydrochloride
Telenzepine dihydrochloride is a selective and orally active muscarinic M1 receptor antagonist with a Ki of 0.94 nM. Telenzepine dihydrochloride inhibits gastric acid secretion and has antiulcer effects. |
147416-96-4 |
DC41296 |
Anisodamine hydrobromide
Anisodamine hydrobromide (6-Hydroxyhyoscyamine hydrobromide), a belladonna alkaloid, is a non-subtype-selective muscarinic and a nicotinic cholinoceptor antagonist. Anisodamine hydrobromide shows antioxidant, anti-inflammatory properties. |
55449-49-5 |
DC41809 |
[D-Trp7,9,10]-Substance P
[D-Trp7,9,10]-Substance P is the substance P analog that inhibits activation of Gq/11 by M1 muscarinic ACh receptors. [D-Trp7,9,10]-Substance P does not inhibit Gi/o activation by M2 ACh receptors. |
89430-38-6 |
DC41810 |
[D-Trp7,9,10]-Substance P TFA
[D-Trp7,9,10]-Substance P TFA is the substance P analog that inhibits activation of Gq/11 by M1 muscarinic ACh receptors. [D-Trp7,9,10]-Substance P TFA does not inhibit Gi/o activation by M2 ACh receptors. |
|
DC41811 |
G-Protein antagonist peptide
G-Protein antagonist peptide is the substance P-related peptide that inhibits binding of G proteins to their receptors. G-Protein antagonist peptide competitively and reversibly inhibits M2 muscarinic receptor activation of Gi or Go and inhibits Gs activation by β-adrenoceptors. |
143675-79-0 |
DC41812 |
G-Protein antagonist peptide TFA
G-Protein antagonist peptide TFA is the substance P-related peptide that inhibits binding of G proteins to their receptors. G-Protein antagonist peptide TFA competitively and reversibly inhibits M2 muscarinic receptor activation of Gi or Go and inhibits Gs activation by β-adrenoceptors. |
|
DC44703 |
Ipratropium bromide monohydrate
Ipratropium bromide (Atrovent, Sch 1000) monohydrate is an antagonist of muscarinic acetylcholine receptors (mAChR) with IC50 of 2.9 nM, 2.0 nM, and 1.7 nM for M1, M2, and M3 receptors, respectively. |
66985-17-9 |
DC44944 |
JHU37160
Featured
JHU37160 is a potent and brain-penetrant DREADD agonist, with EC50s of 18.5 nM and 0.2 nM for hM3Dq and hM4Di DREADDs in HEK-293 cells, respectively. JHU37160 exhibits selective [3H]Clozapine displacement from DREADDs and not from other Clozapine-binding sites in mice brain tissue. |
2369979-68-8 |
DC44945 |
JHU37152
Featured
JHU37152 is a Designer Receptors Exclusively Activated by Designer Drug (DREADD) agonist with Ki of 1.8 nM and 8.7 nM for human muscarinic acetylcholine M3 receptors (hM3Dq) and hM4Di in vitro, respectively. And EC50 values are 5 nM and 0.5 nM for hM3Dq and hM4Di in fluorescent and BRET-based assays in HEK-293 cells, respectively.,hM4Di [1](Cell-free assay) hM3Dq [1](Cell-free assay) hM3Dq [1](Cell-free assay) hM4Di [1](Cell-free assay) 0.5 nM(EC50) 1.8 nM(Ki) 5 nM(EC50) 8.7 nM(Ki),JHU37152 is a potent DREADD agonist with high potency and efficacy in fluorescent and BRET-based assays in HEK-293 cells, whereas no responses are observed in untransfected HEK-293 cells.[1],JHU37152 exhibits high in vivo DREADD potency. JHU37152 exhibits selective [3H]clozapine displacement from DREADDs in brain tissue from WT and D1-DREADD mice.[1] |
2369979-67-7 |
DC45324 |
Sofpironium bromide
Featured
Sofpironium bromide (BBI 4000) is an anticholinergic agent used in the study of primary axillary hyperhidrosis (PAH). Sofpironium bromide reduces sweating by inhibiting M3 muscarinic receptors in eccrine glands at the application site. Sofpironium bromide also has a high afnity for the M1, M2, M4 and M5 subtypes. |
1628106-94-4 |
DC45404 |
Guvacoline hydrochloride
Guvacoline hydrochloride, a pyridine alkaloid found in Areca triandra, can act as a weak full agonist of atrial and ileal muscarinic receptors. |
6197-39-3 |
DC45571 |
VU6000918
VU6000918 is a muscarinic acetylcholine (M4) positive allosteric modulator, with an EC50 of 19 nM for hM4. |
2101737-32-8 |
DC45777 |
Xanomeline
Xanomeline, as an effective and selective muscarinic type 1 and type 4 (M1/M4) receptor agonist, increases neuronal excitability. Xanomeline can be used for the research of neurological disorders, such as schizophrenia. |
131986-45-3 |
DC46288 |
Dronedarone D6 hydrochloride
Dronedarone D6 hydrochloride is the deuterium labeled Dronedarone. Dronedarone hydrochloride, a derivative of Amiodarone, is a class III antiarrhythmic agent for the study of atrial fibrillation (AF) and atrial flutter. Dronedarone hydrochloride is a potent blocker of multiple ion currents, including potassium current, sodium current, and L-type calcium current, and exhibits antiadrenergic effects by noncompetitive binding to β-adrenergic receptors. Dronedarone hydrochloride is a substrate for and a moderate inhibitor of CYP3A4. |
1329809-23-5 |
DC46290 |
Muscarine iodide
Muscarine ((+)-Muscarine) iodide is a toxin that can stimulate the parasympathetic nervous system. Muscarine iodide is a prototype muscarinic acetylcholine receptor agonist. |
24570-49-8 |
DC46423 |
W-84 dibromide
W-84 (dibromide) is a potent allosteric modulator of M2-cholinoceptors, which retards [3H]N-methylscopolamine dissociation. W-84 dibromide can stabilize cholinergic antagonist-receptor complexes. W-84 (dibromide) is a non-competitive muscarinic acetylcholine receptors antagonist with allosteric effects. W-84 (dibromide) protects over additively against an organophosphate-intoxication when applied in combination with atropine. |
21093-51-6 |
DC46843 |
(S)-(+)-Dimethindene maleate
(S)-(+)-Dimethindene maleate, an enantiomer, is a potent M2-selective muscarinic receptor antagonist (pA2 = 7.86/7.74; pKi = 7.78). (S)-(+)-Dimethindene maleate shows lower affinities for the muscarinic M1 (pA2 = 6.83/6.36; pKi = 7.08), the M3 (pA2 = 6.92/6.96; pKi = 6.70) and the M4 receptors (pKi = 7.00), respectively. (S)-(+)-Dimethindene maleate also is a histamine H1 receptor antagonist (pA2 = 7.8). |
136152-65-3 |
DC46844 |
Emraclidine
Featured
Emraclidine is a muscarinic M4 receptor positive allosteric modulator (WO2018002760, compound 11). Emraclidine can be used for the research of neurological diseases. |
2170722-84-4 |
DC47080 |
Velufenacin
Velufenacin is a muscarinic receptor antagonist. |
1648737-78-3 |
DC47097 |
Navafenterol saccharinate
Navafenterol (AZD-8871) saccharinate is an inhaled, long-acting bronchodilator, which is a muscarinic antagonist and β2 agonist. |
1648550-37-1 |
DC47237 |
PD 102807
Featured
PD 102807 is a M4 muscarinic receptor antagonist with an IC50 of 90.7 nM. PD 102807 inhibits M1, M2, M3, M5 muscarinic receptor with IC50s of 6558.7, 3440.7, 950.0, and 7411.7 nM, respectively. Antidyskinetic effect. |
23062-91-1 |
DC47578 |
(Rac)-5-Hydroxymethyl Tolterodine
(Rac)-5-Hydroxymethyl Tolterodine ((Rac)-Desfesoterodine), an active metabolite of Tolterodine, is a mAChR antagonist (Ki values of 2.3 nM, 2 nM, 2.5 nM, 2.8 nM, and 2.9 nM for M1, M2, M3, M4, and M5 receptors, respectively). (Rac)-5-Hydroxymethyl Tolterodine can be used for overactive bladder research. |
200801-70-3 |
DC47579 |
(Rac)-5-Hydroxymethyl Tolterodine hydrochloride
(Rac)-5-Hydroxymethyl Tolterodine ((Rac)-Desfesoterodine) hydrochloride, an active metabolite of Tolterodine, is a mAChR antagonist (Ki values of 2.3 nM, 2 nM, 2.5 nM, 2.8 nM, and 2.9 nM for M1, M2, M3, M4, and M5 receptors, respectively). (Rac)-5-Hydroxymethyl Tolterodine hydrochloride can be used for overactive bladder research. |
250214-40-5 |
DC47580 |
Navafenterol
Navafenterol (AZD-8871) is an inhaled dual-acting, potent, selective, and long-lasting M3-antagonist/β2-agonist (MABA) with long-lasting effects and favorable safety profile. The pIC50 is 9.5 for human M3 receptor, and the pEC50 is 9.5 for β2-adrenoceptor. Navafenterol can be used for the research of chronic obstructive pulmonary disease (COPD). Bronchoprotective and antisialagogue effects. Favorable cardiovascular profile. |
1435519-06-4 |
DC48161 |
MK-6884-11C
MK-6884-11C is a positron emission tomography (PET) imaging agent for the study of M4 muscarinic receptor positive allosteric modulators (PAMs) in neurodegenerative diseases. |
|
DC48162 |
Milameline
Milameline is a muscarinic receptor agonist that improves cognition. |
139886-32-1 |
DC48163 |
Sabcomeline hydrochloride
Sabcomeline (hydrochloride) is a potent and functionally selective muscarinic M1 receptor partial agonist that improve cognition. |
159912-58-0 |
DC48164 |
Aceclidine
Featured
Aceclidine is a modulator of M3 muscarinic acetylcholine receptor. Aceclidine is a cycloplegic agent, a surfactant, a tonicity adjustor and optionally a viscosity enhancer and an antioxidant. Aceclidine has the potential for the research of disorders such as refractive errors of the eye, xerostomia, Sjogren's syndrome, glaucoma, conjunctivitis, lacrimal gland disease, and esotropia (extracted from patent US20150290125A1/US20110091459A1). |
827-61-2 |
DC48165 |
Xanomeline tartrate
Xanomeline (LY 246708) is the potent agonist of muscarinic M1/M4 receptor with antipsychotic-like activity. Xanomeline (LY 246708) increases neuronal excitability. Xanomeline (LY 246708) can be used for the research of schizophrenia. |
152854-19-8 |
DC48166 |
Methoctramine tetrahydrochloride
Methoctramine tetrahydrochloride is a potent and cardioselectivity antagonist of M2 muscarinic receptor. Methoctramine tetrahydrochloride can inhibit Muscarine-induced bradycardia in vivo. |
104807-46-7 |
DC48591 |
Octamylamine
Octamylamine is an anticholinergic and antispasmodic agent. |
502-59-0 |
DC48870 |
Prifinium bromide
Prifinium bromide is antimuscarinic agent with antispasmodic, antiemetic effect. |
4630-95-9 |
DC49039 |
AF-DX 384
AF-DX 384 is a selective antagonist of M2 and M4 muscarinic acetylcholine receptors (Kis=6.03 and 10 nM, respectively). AF-DX 384 reverses deficits in novel object recognition and passive avoidance in aged rats, as well as in young rats with impairments induced by scopolamine. |
118290-26-9 |
DC49392 |
(±)-Muscarine chloride
(±)-Muscarine chloride is the racemate of Muscarine chloride. Muscarine is a prototype muscarinic acetylcholine receptor agonist. |
2936-25-6 |
DC49642 |
VU0455691
VU0455691 is a potent, selective orthosteric M1 mAChR antagonist (pIC50=6.64; IC50=0.23 µM for hM1). |
1392443-41-2 |
DC49643 |
Heliosupine N-oxide
Heliosupine N-oxide, Heliosupin metabolite, inhibits muscarinic acetylcholine receptor (mAChR) with the IC50 of 350 μM. Heliosupine N-oxide is a pyrrolizidine alkaloid (PA). |
31701-88-9 |
DC49644 |
McN-A-343
McN-A-343 is a selective M1 muscarinic agonist that stimulates muscarinic transmission in sympathetic ganglia. McN-A-343 reduces inflammation and oxidative stress in an experimental model of ulcerative colitis. |
55-45-8 |
DC70216 |
ASP8302
Featured
ASP8302 (ASP 8302) is a potent, selective, positive allosteric modulator (PAM) of muscarinic M3 receptor.Threonine 230 (Thr 230) is the amino acid essential for the PAM effect of ASP8302. |
1839583-42-4 |
DC70446 |
GSK1034702
GSK1034702 (GSK-1034702) is a potent, allosteric M1 receptor agonist, inhibits binding of [3H]-NMS (0.5 nM) to M1 mAChR with pKi of 6.5; improves memory encoding potentially by modulating hippocampal function. |
932373-87-0 |
DC70573 |
LSN3172176
LSN3172176 is a novel potent, selectiive M1 mAChR partial agonist (EC50 2.4-7.0nM, Emax 43%-73%), shows binding selectivity for M1 mAChRs (Kd=1.5 nM); LSN3172176 is a potential PET tracer for assessment of M1 mAChR target engagement in the clinic and to further elucidate the function of M1 mAChRs in health and disease. |
|
DC70606 |
ML381 fumarate
ML381 (VU0488130) is a highly mAChR subtype selective M5 orthosteric antagonist with IC50/Ki of 450/340 nM for hM5, has no inhibitory activity on hM1-4 (IC50>30 uM); exhibits good DMPK properties and CNS penetration (B:P ratio of 0.58) to support both in vitro and in vivo studies. |
|
DC70893 |
VU6007215
VU6007215 is a potent, selective M4 positive allosteric modulator (PAM) with EC50 of 144 nM (hM4) and 295 nM (rM4). |
2170552-89-1 |
DC70894 |
VU6009048
VU6009048 is a potent, selective M4 positive allosteric modulator (PAM) with EC50 of 85 nM (hM4) and 379 nM (rM4). |
2226116-93-2 |
DC70895 |
VU6015241
VU6015241 (VU 6015241) is a highly potent and selective antagonist of M4 muscarinic acetylcholine receptor (mAChR4) with IC50 of 71 nM.VU6015241 demonstrates selectivity across multiple species, excellent aqueous solubility, and moderate brain exposure in rodents after intraperitoneal administration. |
2264025-00-3 |
DC70896 |
VU6019650
VU6019650 is a potent, highly selective M5 mAChR orthosteric antagonist with IC50 of 36 nM, >100-fold selectivity against human M1-4.VU6019650 blocked the nonselective muscarinic agonist oxotremorine-M-induced increases in neuronal firing rates of midbrain dopamine neurons in the ventral tegmental area.VU6019650 also inhibited oxycodone self-administration in male Sprague-Dawley rats without impair general motor output. |
|
DC70897 |
VU6028418
VU6028418 (VU 6028418) is a potent, highly selective, orally bioavailable M4 mAChR antagonist for the treatment of dystonia and other movement disorders. |
2649803-05-2 |
DC71204 |
Sabcomeline
Sabcomeline (SB-202026) is a potent and functionally selective muscarinic M1 receptor partial agonist that improve cognition. Sabcomeline can be used for Alzheimer's disease research. |
159912-53-5 |
DC71228 |
Penehyclidine hydrochloride
Penehyclidine (Penequinine) hydrochloride, a anticholinergic drug, is a selective antagonist of M1 and M3 receptors. Penehyclidine hydrochloride activates NF-kβ in lung tissue and inhibits the release of inflammatory factors. Penehyclidine hydrochloride can alleviate the pulmonary inflammatory response in rats with chronic obstructive pulmonary disease (COPD) undergoing mechanical ventilation. |
151937-76-7 |
DC71337 |
Terodiline
Terodiline is an M1-selective muscarinic receptor (mAChR) antagonist with Kbs of 15, 160, 280, and 198 nM in rabbit vas deferens (M1), atria (M2), bladder (M3) and ileal muscle (M3), respectively. Terodiline also is a Ca2+ blocker. Terodiline acts as a treatment for urinary frequency and urge incontinence. |
15793-40-5 |
DC71338 |
M1 ligand 1
M1 ligand 1 (compound 3b-b) is a muscarinic acetylcholine receptor M1 ligand. M1 ligand 1 is a N-desmethyl congener of arecoline derivative. M1 ligand 1 can be used as PET (positron emission tomography) radiotracer. |
2479356-53-9 |
DC71339 |
Propiverine
Propiverine is a potent antimuscarinic agent. Propiverine inhibits cellular calcium influx, thereby diminishing muscle spasm. Propiverine has neurotropic and musculotropic effects on the urinary bladder smooth muscle. Propiverine can used for overactive bladder (OAB) research. |
60569-19-9 |
DC71524 |
Penehyclidine
Penehyclidine, a anticholinergic agent, is a selective antagonist of M1 and M3 receptors. Penehyclidine activates NF-kβ in lung tissue and inhibits the release of inflammatory factors. Penehyclidine can alleviate the pulmonary inflammatory response in rats with chronic obstructive pulmonary disease (COPD) undergoing mechanical ventilation. |
87827-02-9 |
DC71525 |
Biperiden lactate
Biperiden (KL 373) lactate is an orally active non-selective muscarinic receptor antagonist that competitively binds to M1 muscarinic receptors. Biperiden (KL 373) lactate inhibits acetylcholine and enhances dopamine signaling in the central nervous system. Biperiden (KL 373) lactate has the potential for the research of Parkinson's disease and other related psychiatric disorders. |
7085-45-2 |
DC71637 |
Deschloroclozapine
Deschloroclozapine, a metabolite of Clozapine, is a highly potent muscarinic DREADDs (muscarinic Designer Receptors Exclusively Activated by Designer Drugs) agonist, and binds to DREADD receptor subtypes hM3Dq and hM4Di with Ki of 6.3 and 4.2 nM, respectively. |
1977-07-7 |
DC71638 |
Nitrocaramiphen hydrochloride
Nitrocaramiphen hydrochloride is an antagonist of muscarinic acetylcholine receptor M1 (mAChR M1), which can completely remove the hyperpolarizing effect of muscarine. |
98636-73-8 |
DC71778 |
Cycrimine
Cycrimine is an orally active muscarinic cholinergic receptor (mAChR) M1 antagonist, reduces the acetylcholine levels in parkinson model. Cycrimine shows antispasmodic activity, can be used in studies of behavioral and mental disorder. |
77-39-4 |
DC72037 |
CHF-6366
Featured
CHF-6366 is a potent M3 muscarinic antagonist and β2-adrenergic receptors agonist with pKi values of 10.4 and 11.4, respectively. CHF-6366 is also a weak calcium channel inhibitor (IC50~50 μM). CHF-6366 inhibits bronchoconstriction in guinea pigs. |
1615208-41-7 |
DC72200 |
Parapenzolate bromide
Parapenzolate bromide, an antispasmodic, is an orally active mAChR antagonist. Parapenzolate bromide is an anticholinergic agent. |
5634-41-3 |
DC72201 |
Oxyphencyclimine
Oxyphencyclimine is an orally active muscarinic receptor (mAChR) antagonist. Oxyphencyclimine is effective in reducing ulceration index and increasing pepsin activity in rat gastric ulcer model. Oxyphencyclimine can be used in studies of peptic ulcer disease and gastrointestinal spasm. |
125-53-1 |
DC72202 |
Pirenzepine
Pirenzepine (LS 519 free base) is a selective M1 mAChR (muscarinic acetylcholine receptor) antagonist. Pirenzepine reduces gastric acid secretion and reduces muscle spasm, can be used in peptic ulcers research. Pirenzepine shows anti-proliferative activity to cancer cells. |
28797-61-7 |
DC72203 |
Homatropine
Homatropine is an orally active muscarinic acetylcholine receptor antagonist and can be used as an anticholinergic agent. |
87-00-3 |
DC72337 |
YM-58790 free base
YM-58790 free base is a potent antagonist of mAChR. YM-58790 free base binds M1, M2, M3 with Ki values of 28 nM, 260 nM, and 15 nM. YM-58790 free base exhibits potent inhibitory activity on bladder pressuer in reflexly-evoked rhythmic contraction in rats. |
168830-70-4 |
DC72338 |
DIBA-Cy5
DIBA-Cy5 is a fluorescent DIBA antagonist made up be DIBA-alkyne binding Cyanine5 fluorophores (Cy5) and polyethylene glycol (PEG) biomolecules. DIBA-Cy5 can serve as a fluorescent ligand, suitable for probe attachment through click chemistry. DIBA-Cy5 exerts a high binding affinity to type-2 mAChR (M2R) with the Kd value of 1.80 nM, can directly stain M2R receptors in the sinoatrial node of a mouse heart. |
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DC72627 |
PTAC oxalate
PTAC oxalate is a selective muscarinic receptor ligand. PTAC oxalate is an partial agonist of M2 and M4 but antagonist of M1, M3, and M5 (Ki values of 0.2-2.8 nM for hM1-5 in CHO cells). PTAC oxalate alleviates the mechanical allodynia on the neuropathic pain and has antidepression effects. |
201939-40-4 |
DC72628 |
Afacifenacin
Afacifenacin (SMP-986) is a potent and orally active muscarinic receptor antagonist. Afacifenacin inhibits the bladder afferent pathway through the sodium-channel blockade, increasing volume, and reducing the frequency of urination and incontinence. Afacifenacin has the potential for the research of overactive bladder (OAB). |
877606-63-8 |
DC72629 |
Eucatropine
Eucatropine is a potent muscarinic acetylcholine receptor (mAChR) inhibitor with an IC50 value of 0.583 μM. Eucatropine is an anticholinergic agent. |
100-91-4 |
DC72833 |
Muscarine
Featured
Muscarine ((+)-Muscarine) is a toxin that can stimulate the parasympathetic nervous system. Muscarine is an agonist of muscarinic acetylcholine receptor (mAChR). |
300-54-9 |
DC73462 |
VU0405645
VU0405645 is a potent, biased M1 receptor-positive allosteric modulator, potentiates Ca2+ mobilization in CHO cells stably expressing the M1 receptor with EC50 of 340 nM. |
1222886-16-9 |