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mAChR

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Cat. No. Product Name Field of Application Chemical Structure
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.
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DC71638 Nitrocaramiphen hydrochloride
Nitrocaramiphen hydrochloride is an antagonist of muscarinic acetylcholine receptor M1 (mAChR M1), which can completely remove the hyperpolarizing effect of muscarine.
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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.
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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.
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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.
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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.
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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.
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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.
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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.
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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.
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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.
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DC7932 TBPB Featured
TBPB is an allosteric M1 mAChR agonist(EC50=289 nM) that regulates amyloid processing and produces antipsychotic-like activity in rats.
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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.
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DC8153 Umeclidinium bromide Featured
Umeclidinium bromide(GSK573719A) is a muscarinic receptor antagonist which is useful in treatment of chronic obstructive pulmonary disease (COPD).
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DC70897 VU6028418
VU6028418 (VU 6028418) is a potent, highly selective, orally bioavailable M4 mAChR antagonist for the treatment of dystonia and other movement disorders.
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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.
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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.
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DC70894 VU6009048
VU6009048 is a potent, selective M4 positive allosteric modulator (PAM) with EC50 of 85 nM (hM4) and 379 nM (rM4).
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DC70893 VU6007215
VU6007215 is a potent, selective M4 positive allosteric modulator (PAM) with EC50 of 144 nM (hM4) and 295 nM (rM4).
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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.
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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.
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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.
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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.
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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).
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DC49642 VU0455691
VU0455691 is a potent, selective orthosteric M1 mAChR antagonist (pIC50=6.64; IC50=0.23 µM for hM1).
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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.
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DC49392 (±)-Muscarine chloride
(±)-Muscarine chloride is the racemate of Muscarine chloride. Muscarine is a prototype muscarinic acetylcholine receptor agonist.
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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.
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DC48870 Prifinium bromide
Prifinium bromide is antimuscarinic agent with antispasmodic, antiemetic effect.
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DC48591 Octamylamine
Octamylamine is an anticholinergic and antispasmodic agent.
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