Catalog No.
Product Name
Application
Product Information
Citations
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M1 mAChR Agonist
GSK1034702 is an allosteric agonist of the M1 muscarinic acetylcholine receptor (mAChR) with a pEC50 of 8.1 and the capability to cross the blood-brain barrier. It activates the Gq/11 protein-mediated signaling pathway, promoting neuronal firing and enhancing long-term potentiation (LTP) in the hippocampal CA1 region. This compound is valuable for investigating cognitive impairment mechanisms, including those related to Alzheimer's disease, and has demonstrated pro-cognitive effects in models of nicotine withdrawal cognitive dysfunction. Additionally, GSK1034702 may elicit certain side effects associated with peripheral M receptor activation, including gastrointestinal reactions. -
Diacylglycerol Lipase Inhibitor
RHC 80267 is a potent and selective inhibitor of diacylglycerol lipase (DAGL), exhibiting an IC50 of 4 μM in canine platelets. This compound is valuable for research applications focusing on the modulation of lipid signaling pathways, particularly in the context of acetylcholine-induced relaxation. Additionally, RHC 80267 demonstrates inhibitory effects on cholinesterase with an IC50 of 4 μM and also inhibits cyclooxygenase (COX) and the hydrolysis of phosphatidylcholine (PC), making it a versatile tool for exploring lipid metabolism and neuronal signaling. -
Muscarinic M1 Receptor Antagonist
Telenzepine dihydrochloride is a selective antagonist of the muscarinic M1 receptor, exhibiting a Ki value of 0.94 nM. This compound effectively inhibits gastric acid secretion and demonstrates significant antiulcer properties, making it a valuable tool for research into gastrointestinal disorders and therapeutic interventions in related conditions. -
mAChR Antagonist
Fesoterodine L-mandelate is a competitive antagonist of muscarinic acetylcholine receptors (mAChR), demonstrating non-subtype selectivity with pKi values of 8.0, 7.7, 7.4, 7.3, and 7.5 for M1, M2, M3, M4, and M5 receptors, respectively. This orally active compound is primarily utilized in the treatment of overactive bladder (OAB). Its inhibition of mAChRs contributes to a reduction in bladder contractions, providing therapeutic benefits for managing urinary incontinence. -
mAChR Antagonist
Dipeptide diaminobutyroyl benzylamide diacetate functions as a muscarinic acetylcholine receptor (mAChR) antagonist. It induces muscle relaxation, making it relevant in studies related to skin aging and facial wrinkles, including crow's feet and periorbital creases. This compound can be utilized in research focused on dermatological applications and the physiological mechanisms underlying muscle tone regulation in the skin. -
Muscarinic Receptor Full Activator
Guvacoline hydrochloride is a muscarinic receptor full activator, primarily targeting atrial and ileal muscarinic receptors. As a pyridine alkaloid derived from Areca triandra, it demonstrates the ability to act as a weak full agonist at these receptors. Guvacoline hydrochloride is utilized in research applications focusing on muscarinic receptor activation and its physiological implications. -
M1 Agonist
VU0357017 hydrochloride is a selective allosteric agonist of the M1 muscarinic acetylcholine receptor, demonstrating a potent efficacy with an EC50 of 477 nM. This compound exhibits high selectivity for the M1 receptor, showing no activity at M2-M5 subtypes even at concentrations up to 30 μM. VU0357017 hydrochloride is valuable for research applications related to Alzheimer's disease and schizophrenia. -
M5 mAChR NAM
ML375 is a potent negative allosteric modulator (NAM) of the M5 muscarinic acetylcholine receptor. With IC50 values of 300 nM and 790 nM for human and rat M5 receptors respectively, ML375 exhibits high selectivity and significant brain penetration. Its ability to selectively inhibit M5 mAChR makes ML375 a valuable tool for research applications, particularly in studies exploring cholinergic signaling and neurological functions. -
M4 Receptor Antagonist
PD 102807 is an antagonist of the M4 muscarinic receptor, exhibiting an IC50 of 90.7 nM. This compound also inhibits M1, M2, M3, and M5 muscarinic receptors with IC50 values of 6558.7 nM, 3440.7 nM, 950.0 nM, and 7411.7 nM, respectively. Due to its selective action, PD 102807 is valuable for studying muscarinic receptor signaling and has potential applications in research focused on antidyskinetic effects. -
M3 Receptor PAM
ASP8302 is a positive allosteric modulator of the muscarinic M3 receptor. It has demonstrated efficacy in enhancing voiding efficiency and decreasing residual urine volume in models of voiding dysfunction. ASP8302 is suitable for research applications focused on underactive bladder conditions. -
M1 Receptor Positive Modulator
PQCA is a selective and potent positive allosteric modulator of the muscarinic M1 receptor. With EC50 values of 49 nM and 135 nM for the rhesus and human M1 receptors, respectively, PQCA demonstrates high specificity, showing inactivity towards other muscarinic receptors. This compound has significant potential in addressing cognitive deficits associated with Alzheimer's disease, making it a valuable tool for research into therapeutic strategies for neurodegenerative disorders. -
M1 Positive Allosteric Modulator
VU0467319 is a highly selective, orally active M1 positive allosteric modulator (PAM) with a blood-brain barrier permeability and an EC50 of 492 nM. It demonstrates significant selectivity over M2-5 (EC50 > 30 μM) in both human and rat models. This compound enhances cognitive function through central M1 muscarinic receptors, making it a promising candidate for research into Alzheimer's disease without causing cholinergic adverse reactions. VU0467319 holds potential for advancing understanding and treatment strategies in cognitive impairments associated with neurodegenerative disorders. -
Anticholinergic Agent
Sofpironium bromide is an anticholinergic agent that primarily targets M3 muscarinic receptors in eccrine glands, effectively reducing sweating. This compound is utilized in research focused on primary axillary hyperhidrosis (PAH). Additionally, it demonstrates a high affinity for M1, M2, M4, and M5 muscarinic receptor subtypes, making it a valuable tool for studying various cholinergic pathways and their physiological effects. -
mAChR Antagonist
Fesoterodine is a competitive antagonist of muscarinic acetylcholine receptors (mAChR), exhibiting pKi values of 8.0, 7.7, 7.4, 7.3, and 7.5 for the M1, M2, M3, M4, and M5 subtypes, respectively. This orally active compound is primarily utilized in the treatment of overactive bladder (OAB) conditions. Its broad receptor targeting allows for effective modulation of bladder function, making it a valuable tool in urological research and therapy development. -
Relative Configuration of VU6021625
rel-VU6021625, a derivative of VU6021625, serves as a potent and selective antagonist of the mAChR M4 receptor, exhibiting IC50 values of 0.44 nM for human M4 and 57 nM for rat M4. This compound demonstrates significant potential in neurological research, particularly in the study of disorders related to cholinergic signaling. Its use can aid in understanding mAChR M4 functions and therapeutic applications targeting this receptor. -
nAChR Desensitizer
Anagyrine is a quinolizidine alkaloid that acts as a desensitizer of nicotinic acetylcholine receptors (nAChR). It demonstrates binding affinity with IC50 values of 132 µM for muscarinic receptors and 2096 µM for nicotinic receptors, effectively modulating nAChR activity. This compound is utilized in research to study nAChR desensitization mechanisms and its implications in various neural and pharmacological contexts. -
mAChR Activator
VU0238441 is a positive allosteric modulator targeting pan muscarinic acetylcholine receptors (mAChRs), demonstrating EC50 values of 3.2 μM, 2.8 μM, 2.2 μM, 2.1 μM for M1, M2, M3, and M5, respectively, while maintaining minimal activity against M4 (>10 μM). This compound enhances the receptor activity in a pharmacologically relevant manner and is valuable for exploring the role of mAChRs in neurological and cognitive research. Its applications include drug discovery and the study of receptor signaling pathways associated with cholinergic systems. -
M5 mAChR PAM
ML380 is a selective positive allosteric modulator (PAM) targeting the M5 muscarinic acetylcholine receptor (mAChR) with EC50 values of 190 nM for human and 610 nM for rat receptors. It demonstrates moderate selectivity over the M1 and M3 mAChR subtypes. By enhancing the affinity of acetylcholine for the M5 mAChR, ML380 may play a significant role in research focused on neurological and cognitive functions, offering potential avenues for the study of related disorders. -
M4 Receptor Antagonist
PCS1055 dihydrochloride is a selective and competitive antagonist of the muscarinic M4 receptor, with an IC50 value of 18.1 nM and a Kd of 5.72 nM. This compound effectively inhibits the binding of the radioligand [3H]-NMS to the M4 receptor, displaying a Ki of 6.5 nM. PCS1055 dihydrochloride demonstrates over 100-fold selectivity against M1, M3, and M5 receptors, and 30-fold selectivity at the M2 receptor. Additionally, it serves as a potent acetylcholinesterase inhibitor, with IC50 values of 22 nM and 120 nM for electric eel and human AChE, respectively, highlighting its potential for various neurological research applications. -
mAChR M5 Orthosteric Antagonist
ML381 is a selective orthosteric antagonist of the mAChR M5 receptor, with an IC50 of 450 nM and a Ki value of 340 nM. This compound is known for its ability to penetrate the central nervous system, making it a valuable tool for investigating the role of mAChR M5 in neurological research. Due to its instability in rat plasma, ML381 is primarily utilized as a molecular probe for in vitro studies and electrophysiological applications. -
mAChR Antagonist
Ipratropium bromide hydrate is a muscarinic acetylcholine receptor (mAChR) antagonist, exhibiting IC50 values of 2.9 nM, 2 nM, and 1.7 nM for M1, M2, and M3 receptors, respectively. This compound effectively induces relaxation of smooth muscle, making it valuable for research applications in chronic obstructive pulmonary disease (COPD) and asthma. Its selective inhibition of mAChRs contributes to its therapeutic potential in respiratory disorders. -
mAChR Antagonist
Tiotropium bromide monohydrate is a long-acting antagonist of muscarinic acetylcholine receptors (mAChRs). It exhibits significant bronchodilator activity, making it effective in the management of chronic obstructive pulmonary disease (COPD) and asthma. This compound is widely utilized in research studies investigating respiratory pharmacology and cholinergic signaling pathways. -
M4 mAChR Antagonist
VU6028418 is a potent and highly selective antagonist of the M4 muscarinic acetylcholine receptor (mAChR), exhibiting an IC50 of 4.1 nM against the human M4 receptor. This compound demonstrates promise in the modulation of cholinergic signaling pathways, making it an invaluable tool for research on neuropharmacology and therapeutic interventions in disorders linked to M4 mAChR activity. Its oral bioavailability further supports its use in in vivo studies, aiding in the exploration of its potential effects on cognition and metabolic processes. -
Antiacetylcholine Compound
Oxyphenonium bromide is an antiacetylcholine compound that functions as a muscarinic acetylcholine receptor (mAChR) antagonist. It effectively mitigates bronchial obstruction by blocking acetylcholine's action, thereby reducing airway constriction. This compound is primarily utilized in research investigating respiratory conditions and the modulation of cholinergic signaling pathways. -
mAChR M1/3/5 PAM
VU0119498 is a positive allosteric modulator of muscarinic acetylcholine receptors M1, M3, and M5, showing EC50 values of 6.04 µM, 6.38 µM, and 4.08 µM, respectively. This compound exhibits significant antidiabetic activity, making it a valuable tool for studying metabolic disorders and receptor signaling pathways related to glucose homeostasis. Its modulation of mAChR activity provides insights into therapeutic strategies for diabetes and other related conditions. -
Muscarinic Receptors Antagonist
Cyclopentolate hydrochloride is a muscarinic receptor antagonist, exhibiting a pKB value of 7.8 on the circular ciliary muscle. This anti-muscarinic agent is primarily utilized in ophthalmology for its ability to induce mydriasis and cycloplegia. It serves as a valuable tool in various research applications related to eye physiology and pharmacology. -
mAChR Inhibitor
Arborine is a potent mAChR inhibitor that modulates the peripheral actions of acetylcholine, leading to a significant reduction in blood pressure. This compound is particularly valuable in research applications focused on cardiovascular physiology and the mechanistic study of cholinergic signaling pathways. Its ability to influence blood pressure dynamics makes it an important tool for investigating therapeutic interventions in hypertension and related disorders. -
mAChR Antagonist
(±)-Darifenacin is a selective antagonist of the M3 muscarinic acetylcholine receptor (mAChR), functioning primarily by inhibiting receptor activation. This compound demonstrates potent activity in modulating smooth muscle contraction and glandular secretion, making it particularly useful for research in gastrointestinal disorders and urinary incontinence. Applications include studies on the mechanism of muscarinic receptor signaling and the development of therapeutic strategies targeting mAChR-related conditions. -
M4 mAChR Agonist
M4 mAChR agonist-1 is a selective agonist targeting the M4 muscarinic acetylcholine receptor. This compound exhibits potent activation of the M4 receptor with an EC50 greater than 10 μM in human cell systems. It is valuable for research applications focused on studying cholinergic signaling and neuropharmacology. -
Sigma-1 Receptor Agonist
Pentoxyverine is an orally active sigma-1 receptor agonist, exhibiting affinity with Kis of 41 nM for σ1, 894 nM for σ2, and 75 nM for guinea-pig brain membran σ1. This compound acts as a muscarinic antagonist and demonstrates significant biological activities, including antitussive, anticonvulsant, and spasmolytic effects. Pentoxyverine is utilized in research for its potential to inhibit bronchial interceptors, diminish the cough reflex, induce relaxation of bronchial smooth muscle, and reduce airway resistance in various pulmonary conditions. -
Muscarinic M1 Receptor Agonist
LY593093 is a selective agonist of the muscarinic M1 receptor, demonstrating an EC50 of 22.8 nM. This compound is orally active and effectively penetrates the blood-brain barrier, making it a valuable tool for investigating mechanisms underlying Alzheimer's disease. Its selectivity for the muscarinic M1 receptor positions LY593093 as a promising reagent for research in neurodegenerative disorders. -
M3 Receptor Antagonist
Zamifenacin fumarate is a potent antagonist of the muscarinic M3 receptor, primarily targeting the gastrointestinal system. It demonstrates significant efficacy in reducing colonic motility, making it relevant for research in conditions such as irritable bowel syndrome. This compound is essential for studies exploring gut motility modulation and the pharmacological mechanisms underlying gastrointestinal disorders. -
M4 Positive Allosteric Modulator
VU0467485 is a potent and selective positive allosteric modulator of the muscarinic acetylcholine receptor 4 (M4). It enhances acetylcholine activity at M4 receptors, exhibiting EC50 values of 26.6 nM in rat and 78.8 nM in human systems. VU0467485 shows high selectivity for M4 over the other muscarinic receptor subtypes (M1, M2, M3, and M5) in both human and rat samples. This compound also demonstrates moderate to high central nervous system penetration and possesses antipsychotic-like properties, making it a valuable tool for the study of neurological disorders. -
mAChR M1 Antagonist
Cycrimine is an orally active antagonist of the muscarinic acetylcholine receptor M1, effectively inhibiting acetylcholine levels in models of Parkinson's disease. Its antispasmodic properties make Cycrimine a valuable tool for research in behavioral and mental disorders, providing insights into cholinergic signaling pathways. This compound is suitable for studies aimed at understanding the role of mAChRs in neurodegenerative conditions and related therapeutic interventions. -
mAChR 4 Antagonist
PCS1055 is a selective competitive antagonist of the muscarinic M4 receptor, exhibiting an IC50 of 18.1 nM and a Kd of 5.72 nM. It effectively inhibits radioligand [3H]-NMS binding to the M4 receptor with a Ki of 6.5 nM. Additionally, PCS1055 demonstrates inhibitory activity against acetylcholinesterase (AChE), with IC50 values of 22 nM for electric eel AChE and 120 nM for human AChE. This compound is valuable for research focused on muscarinic receptor signaling and cholinergic modulation. -
mAChR M2 Agonist
Arecaidine but-2-ynyl ester tosylate is a selective agonist of the mAChR M2 receptor, known to induce dose-dependent reductions in mean arterial pressure and heart rate in rodent models. This compound serves as a valuable tool in cardiovascular disease research, elucidating the role of mAChR M2 in cardiac function. Additionally, as a click chemistry reagent, Arecaidine but-2-ynyl ester tosylate contains an alkyne functional group, enabling its application in copper-catalyzed azide-alkyne cycloaddition reactions with azide-containing molecules for further synthetic applications. -
M3 Receptor Antagonist
Zamifenacin is a potent antagonist of the muscarinic M3 receptor, demonstrating gut-selective activity. This compound effectively reduces colonic motility, making it a valuable tool in the study of irritable bowel syndrome and related gastrointestinal disorders. Its mechanism of action provides insights into the modulation of gastrointestinal function and potential therapeutic applications in digestive health. -
mAChR Agonist
Muscarine iodide is a potent agonist of the muscarinic acetylcholine receptors (mAChR). It actively stimulates the parasympathetic nervous system, making it a valuable tool in studying cholinergic signaling pathways. This compound is commonly utilized in research focused on neuropharmacology and the physiological effects of muscarinic receptor activation. -
M1 Positive Allosteric Modulator
VU0486846 is a selective positive allosteric modulator of the M1 muscarinic acetylcholine receptor. This compound enhances receptor activity in a manner dependent on the presence of the endogenous ligand. VU0486846 is utilized in research to explore its potential therapeutic effects in cognitive disorders and neurodegenerative diseases. Its oral bioavailability makes it a valuable tool for in vivo studies of M1 modulation. -
Muscarinic M1 Agonist
PF-06767832 is a selective positive allosteric modulator of the muscarinic M1 receptor, exhibiting an EC50 value of 60 nM. This compound demonstrates favorable penetration into the central nervous system, enhancing M1 receptor signaling. It is primarily used in research focused on neuropharmacology, cognition, and potential treatments for cognitive disorders. -
mAChR Agonist
LASSBio-873 is a potent muscarinic acetylcholine receptor (mAChR) agonist that effectively crosses the blood-brain barrier. It exhibits significant analgesic properties in models of acute and inflammatory pain. Research indicates that the analgesic effects of LASSBio-873 can be antagonized by the M2 receptor inhibitor methoctramine, making it a valuable tool for studying pain mechanisms and mAChR signaling pathways. -
M4 Positive Allosteric Modulator
VU6000918 is a positive allosteric modulator of the muscarinic acetylcholine receptor M4, demonstrating an EC50 of 19 nM for human M4. This compound enhances the receptor's activity in response to acetylcholine, making it a valuable tool for studying M4 receptor function. VU6000918 can be utilized in research related to neurological disorders and cognitive functions, providing insights into the therapeutic potential of modulating M4 receptor signaling. -
Muscarinic M3 Receptor Antagonist
DAU 5884 hydrochloride is a potent antagonist of the muscarinic M3 receptor. It effectively inhibits methacholine-induced cellular proliferation and muscle contractility, making it a valuable tool for research into muscarinic signaling pathways and related physiological effects. This compound is useful for studies investigating respiratory physiology and disorders associated with muscarinic receptor activation. -
mAChR Antagonist
L-Hyoscyamine sulfate is a competitive antagonist of muscarinic acetylcholine receptors (mAChRs). This natural tropane alkaloid demonstrates significant biological activity by inhibiting mAChRs, making it useful in research applications focused on neuropharmacology and the modulation of cholinergic signaling. Its structural similarity to atropine further emphasizes its relevance in studies related to anticholinergic effects and the exploration of receptor interaction mechanisms. -
M4 Positive Allosteric Modulator
LY 2033298 is a selective positive allosteric modulator of the muscarinic M4 receptor, enhancing the receptor's activity. This compound is valuable for investigating psychiatric disorders and related neurobiological pathways, providing insights into the potential therapeutic mechanisms for disorders associated with M4 receptor dysfunction. -
Anticholinergic Agent
Tridihexethyl chloride is an anticholinergic agent that acts as a muscarinic acetylcholine receptor (mAChR) antagonist. It exhibits significant antimuscarinic and antisecretory properties, providing pronounced antispasmodic effects on the gastrointestinal system. This compound is valuable for research related to peptic ulcer disease and acquired nystagmus, facilitating studies on gastrointestinal motility and secretion modulation. -
M4 mAChR Activator
Thiochrome is a selective enhancer of muscarinic acetylcholine receptor subtype M4. As a natural oxidation product and metabolite of thiamine, Thiochrome exhibits neutral cooperativity with acetylcholine at M1 to M3 receptors. This compound is valuable for studying the modulation of cholinergic signaling and its implications in neuropharmacology and therapeutic research. -
Muscarinic M3 Receptor Antagonist
CHF5407 is a selective, competitive antagonist of the muscarinic M3 receptor, exhibiting subnanomolar affinities for human muscarinic receptors M1, M2, and M3. This compound demonstrates prolonged antibronchospastic activity, making it a valuable tool for research into bronchial hyperreactivity and related respiratory conditions. CHF5407 is suitable for studies investigating the role of muscarinic receptors in various biological processes and potential therapeutic applications. -
Stable Isotope
Tiotropium-d6 bromide is a deuterium-labeled analogue of Tiotropium, primarily targeting muscarinic acetylcholine receptors (mAChR). As a potent mAChR antagonist, it effectively inhibits the binding of acetylcholine, preventing the activation of ligand-gated ion channels. This reagent is valuable for studies involving receptor binding assays, pharmacokinetics, and metabolic pathway analysis. -
DREADD Agonist
JHU37152 is a potent agonist for Designer Receptors Exclusively Activated by Designer Drugs (DREADDs), specifically targeting the hM3Dq and hM4Di receptors with EC50 values of 5 nM and 0.5 nM, respectively, in HEK-293 cells. This compound demonstrates selective displacement of [3H]Clozapine from DREADD sites without affecting other Clozapine-binding sites in mouse brain tissue. JHU37152 is valuable for research applications involving neural circuit manipulation and the study of neuropharmacology.
