Catalog No.
Product Name
Application
Product Information
Citations
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Muscarinic antagonist
Procyclidine hydrochloride is a muscarinic antagonist that crosses the blood-brain barrier and is used in the treatment of drug-induced extrapyramidal disorders and in Parkinsonism. -
Muscarinic antagonist
Mepenzolate Bromide is a muscarinic antagonist used to treat gastrointestinal disorders. It decreases the severity of elastase-induced airspace enlargement and respiratory dysfunction. -
M1 muscarinic receptor antagonist
Pirenzepine dihydrochloride (LS519) is a selective M1 muscarinic receptor antagonist. - Pirmenol hydrochloride inhibits IK.ACh by blocking muscarinic receptors. The IC50 of Pirmenol for inhibition of Carbachol-induced IK.ACh is 0.1 μM.
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mAChR antagonist
Atropine methyl bromide, a muscarinic receptor (mAChR) antagonist, is a quaternary ammonium salt of atropine and a 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 readily into the central nervous system than atropine. -
mAChR agonist
Cevimeline (Evoxac) Hcl is a parasympathomimetic and muscarinic agonist, with particular effect on M3 receptors; used in the treatment of dry mouth associated with sjogren's syndrome. - Piperidolate hydrochloride is an antimuscarinic, Also a potential inhibitor of human glutathione transferase P1-1.
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alpha-1 adrenergic receptors / mAChRs inhibitor
Anisodamine is an inhibitor of alpha-1 adrenergic receptors and mAChRs isolated from Chinese solanacea plant. -
mAChR inhibitor
Piperidolate is a tertiary amine antimuscarinic. It is similar to atropine. It is mainly used in the smooth muscle spasm of the gastrointestinal tract and inhibits intestinal cramp induced by acetylcholine in rats and dogs. -
mAChR antagonist
Cimetropium Bromide (DA-3177) is a mAChR antagonist for long-term treatment of irritable bowel syndrome. -
muscarinic agonist
Talsaclidine is a muscarinic agonist with preferential neuron-stimulating properties. Talsaclidine is a full agonist at the M1 subtype, and as a partial agonist at the M2 and M3 subtypes. - Dexetimide ((+)-Benzetimide) is a high-affinity muscarinic receptor antagonist and a potent and persistent anticholinergic agent used to treat neuroleptic-induced parkinsonism.
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partial M1 agonist and M2/M3 antagonist
Alvameline (Lu25-109) is a partial M1 agonist and M2/M3 antagonist. -
mAChR M5 positive allosteric modulator
VU 0365114 is a mAChR M5 positive allosteric modulator, with an EC50 of 2.7 μM. -
M5 NAM
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. -
hM3Dq agonist.
DREADD agonist 21 is a potent human muscarinic acetylcholine M3 receptors (hM3Dq) agonist(EC50=1.7 nM). -
Sigma-1 receptor agonist/muscarinic M1 agonist
Blarcamesine, also known as AVex-73 and AE-37, is a muscarinic M1 agonist potentially for the treatment of Alzheimer's disease. It is an ς receptor ligand. -
mAChR modulator
Rapacuronium bromide is an allosteric modulator of muscarinic acetylcholine receptor (mAChR). -
mAChR antagonist
mAChR-IN-1 hydrochloride is a potent muscarinic cholinergic receptor (mAChR) antagonist, with an IC50 of 17 nM. -
M3 muscarinic receptor antagonist
Tarafenacin D-tartrate (SVT-40776 D-tartrate) is a highly selective M3 muscarinic receptor antagonist (Ki= 0.19 nM), ~200 fold selectivity over M2 receptor. -
mAChR antagonist
mAChR-IN-1 is a potent muscarinic cholinergic receptor(mAChR) antagonist with IC50 of 17 nM. -
mAChR5 modulator
VU 0238429 is positive allosteric modulator of muscarinic acetylcholine receptor subtype 5 (mAChR5 or M5), with an EC50 of 1.16 μM. -
[3H](+)pentazocine binding inhibitor
Levetimide is a potent and stereoselective inhibitor of [3H](+)pentazocine binding, with a Ki of 2.2 nM. -
muscarinic antagonist
Aclidinium Bromide(LAS 34273; LAS-W 330) is a long-acting, inhaled muscarinic antagonist as a maintenance treatment for chronic obstructive pulmonary disease (COPD). -
mAChR M5 negative allosteric modulator
(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. -
mAChR agonist
Oxotremorine M iodide is a potent and non-selective muscarinic acetylcholine receptor (mAChR) agonist. -
muscarinic acetylcholine receptor antagonist
Benzetimide hydrochloride is a muscarinic acetylcholine receptor antagonist. -
mAChR antagonist
Nor-benzetimide is a major metabolite of Benzetimide. Benzetimide is a mAChR antagonist with anticholinergic activity. -
Anticholinergic agent
Penehyclidine hydrochloride (also known as Penequinine hydrochloride) is a selective anticholinergic agent that acts as an antagonist of muscarinic M1 and M3 receptors. It exerts anti-inflammatory effects by modulating immune signaling in lung tissue, notably through activation of the NF-κB pathway and inhibition of pro-inflammatory cytokine release. In preclinical studies, Penehyclidine hydrochloride has been shown to alleviate pulmonary inflammation in rat models of chronic obstructive pulmonary disease (COPD), particularly under conditions of mechanical ventilation. These properties suggest its potential utility in managing respiratory inflammatory conditions and improving outcomes in mechanically ventilated patients with COPD. -
mAChR Agonist
Pilocarpine Hydrochloride is a selective agonist for the M3 muscarinic acetylcholine receptor (mAChR). It plays a significant role in stimulating glandular secretion, particularly in the treatment of dry mouth and glaucoma. This compound is valuable in research focused on neuropharmacology, as well as studies investigating cholinergic signaling and its implications in various physiological processes. -
PDE Inhibitor
Flavoxate hydrochloride is a competitive inhibitor of phosphodiesterase (PDE), providing significant antispasmodic effects through its action as a muscarinic acetylcholine receptor (mAChR) antagonist. In addition to its PDE inhibition, it exhibits moderate calcium antagonistic properties and local anesthetic effects. Flavoxate hydrochloride is utilized in research focused on overactive bladder (OAB) and related lower urinary tract infections, contributing to a better understanding of these conditions and potential therapeutic approaches. -
mAChR Antagonist
GS 283 is a muscarinic acetylcholine receptor (mAChR) antagonist that exhibits calcium antagonist properties. This compound effectively modulates smooth muscle contraction by inhibiting contractions induced by carbachol and histamine in guinea pig tracheal smooth muscle, as well as high H+ levels in both guinea pig and rat tracheal smooth muscle. Additionally, GS 283 has been shown to inhibit Ca2+-induced contractions, and at elevated concentrations, it can completely abolish carbachol-induced contractions in a Ca2+-free environment. This makes GS 283 a valuable tool for research related to respiratory physiology and the pharmacological modulation of smooth muscle activity. -
mAChR Ligand
Azacyclonol hydrochloride is a selective ligand for the M3 muscarinic acetylcholine receptor, demonstrating significant inhibition of proliferation in androgen-refractory cancer cell lines, including DU145 and PC-3. This compound exhibits notable anticancer activity, particularly in A549 human lung cancer cells, by inhibiting NOX-derived reactive oxygen species. Additionally, Azacyclonol hydrochloride has shown antitumor effects in xenografted chorioallantoic membrane models. Beyond its anticancer applications, it is also explored for its potential in the treatment of chronic schizophrenia. -
mAChR Agonist
Isopteropodine is a positive modulator that selectively targets muscarinic acetylcholine receptors (mAChRs), exhibiting notable agonistic activity. It demonstrates an EC50 of 9.92 μM for acetylcholine and 14.5 μM for 5-hydroxytryptamine (5-HT), highlighting its potential in neuroscience research related to cognitive function. Additionally, Isopteropodine displays antibacterial efficacy against Gram-positive bacteria, with minimum inhibitory concentrations (MICs) of 150 μg/mL for Staphylococcus aureus and 250 μg/mL for Bacillus subtilis, making it suitable for studies in antimicrobial activity and cognitive impairment. -
M3 mAChR Antagonist
p-F-HHSiD hydrochloride is a potent and selective antagonist of the M3 muscarinic acetylcholine receptor (mAChR). This compound also demonstrates antagonistic properties towards other mAChR subtypes and the alpha1-adrenoceptor. p-F-HHSiD hydrochloride is useful for research applications involving cancer, metabolic disorders, neurological conditions, and cardiovascular diseases, including colon cancer, Alzheimer’s disease, and diabetes. -
mAChR Antagonist
Batefenterol Succinate is an inhaled bifunctional bronchodilator that acts as a muscarinic acetylcholine receptor (mAChR) antagonist and a beta2-adrenoceptor agonist. This dual mechanism results in effective smooth muscle relaxation, enhancing respiratory function. Batefenterol Succinate is primarily utilized in research focused on chronic obstructive pulmonary disease (COPD) and other respiratory conditions, providing insights into therapeutic strategies for airway obstruction. -
mAChR/Adrenergic Receptor Antagonist
Muscarinic toxin 3 (MT3) is a selective and non-competitive antagonist of muscarinic acetylcholine receptors (mAChRs) and adrenergic receptors. It exhibits high potency with pIC50 values of 6.71, 8.79, 8.86, 7.57, 8.13, and 8.49 against M1, M4, α1A, α1B, α1D, α2A, α2B, and α2C receptors, respectively, highlighting its prominent adrenoceptor activity. This compound is valuable in studying receptor signaling pathways and has potential applications in pharmacological research focused on nervous system disorders and cardiovascular diseases. -
M3 mAChR Antagonist
p-F-HHSiD (p-Fluorohexahydrosiladifenidol) functions as a selective antagonist of the M3 muscarinic acetylcholine receptor (mAChR). This compound exhibits antagonistic activity against various muscarinic receptor subtypes as well as the alpha-1 adrenergic receptor. p-F-HHSiD is valuable for research in cancer, metabolic disorders, neurological pathologies, and cardiovascular diseases, including colon cancer, Alzheimer's disease, and diabetes. -
mAChR Antagonist
DAU 5884 is a selective antagonist of muscarinic acetylcholine receptors (mAChRs), with particular potency towards the M1 receptor subtype while exhibiting discrimination between M4 and M2 subtypes. This compound demonstrates significant biological activity in modulating signaling pathways associated with mAChR, making it a valuable tool for research in neuropharmacology and potential therapeutic applications in disorders related to cholinergic signaling. Functional assays and radioligand binding studies characterize its subtype specificity and efficacy. -
mAChR Agonist
KTX-005 is a selective agonist of the muscarinic acetylcholine receptor (mAChR), which modulates the signaling pathways associated with acetylcholine neurotransmission. This compound is primarily utilized in research focused on neuropsychiatric disorders, specifically schizophrenia. KTX-005's effects on mAChR activity make it a valuable tool for studying synaptic transmission and receptor dynamics in neurological contexts. -
mAChR Regulator
Dimethyl-W84 dibromide is a modulator of M2 muscarinic acetylcholine receptors. This compound exhibits significant regulatory activity on mAChRs, making it a valuable tool in the study of nervous system functions and disorders. Its application in research can help elucidate the role of acetylcholine signaling in various neurological conditions.
