Catalog No.
Product Name
Application
Product Information
Citations
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mAChR Antagonist
Hexocyclium methylsulfate is a potent antagonist of muscarinic acetylcholine receptors (mAChR), exhibiting pKi values of 8.9, 7.7, 8.4, and 8.8 for the M1, M2, M3, and M4 subtypes, respectively. This compound demonstrates significant biological activity in modulating cholinergic signaling pathways. It is valuable in research applications related to gastrointestinal conditions such as duodenal ulcers and irritable bowel syndrome. -
mAChR M4 PAM
VU0152099 is a selective positive allosteric modulator of the mAChR M4 receptor, exhibiting an EC50 of 0.4 µM for the rat M4 receptor. This compound demonstrates significant brain penetrance and is inactive against other mAChR subtypes and GPCRs. VU0152099 does not possess agonist activity; instead, it enhances the response of M4 to acetylcholine, making it a valuable tool for research into neuropharmacology and the modulation of cholinergic signaling. -
Muscarinic Receptor Full Activator
Guvacoline hydrobromide is a pyridine alkaloid that functions as a full activator of muscarinic receptors. It exhibits biological activity as a weak full agonist of both atrial and ileal muscarinic acetylcholine receptors (mAChR). This compound is valuable for research applications involving cholinergic signaling and receptor pharmacology. -
mAChR M5 NAM
(R)-VU 6008667 acts as a negative allosteric modulator (NAM) of the muscarinic acetylcholine receptor subtype M5. This compound has demonstrated potential in modulating M5 receptor-mediated pathways, which are implicated in various neurological conditions. Its selectivity and pharmacological profile make it a valuable research tool for studying M5 receptor functions and associated signaling mechanisms. -
mAChR Antagonist
(Rac)-5-Hydroxymethyl Tolterodine hydrochloride is an mAChR antagonist, demonstrating Ki values of 2.3 nM, 2.0 nM, 2.5 nM, 2.8 nM, and 2.9 nM for M1, M2, M3, M4, and M5 muscarinic receptors, respectively. This active metabolite of Tolterodine is primarily utilized in research related to overactive bladder conditions. Its selective inhibition of muscarinic acetylcholine receptors provides a valuable tool for investigating bladder dysfunction and potential therapeutic interventions. -
mAChR Antagonist
Terodiline hydrochloride is an M1-selective muscarinic acetylcholine receptor (mAChR) antagonist, exhibiting binding affinities of 15 nM for M1, 160 nM for M2, and 280 nM for M3 receptors, with further action as a calcium channel blocker. This compound is primarily used in the treatment of urinary frequency and urge incontinence. Its ability to selectively inhibit specific mAChR subtypes makes it a valuable reagent for investigating the pharmacological modulation of urinary tract function. -
M4 mAChR Potentiator
VU10010 is a selective allosteric potentiator of the M4 muscarinic acetylcholine receptor (mAChR) with an EC50 of 400 nM. This compound enhances the receptor's affinity for acetylcholine and promotes coupling to G proteins by binding to an allosteric site. VU10010 has been shown to increase carbachol-induced depression of transmission at excitatory synapses in the hippocampus, making it a valuable tool for research into neurological processes and the modulation of synaptic activity. -
mAChR Antagonist
mAChR antagonist 1 is a selective antagonist for muscarinic acetylcholine receptors (mAChRs), exhibiting Ki values of 255 nM, 121 nM, 158 nM, and 255 nM for the M1, M3, M4, and M5 subtypes, respectively. This compound is useful for studies investigating the role of mAChR signaling in various physiological and pathological processes. Its application extends to neuropharmacology and drug development, making it a valuable tool for exploring mAChR-related pathways. -
mAChR Antagonist
Oxyphencyclimine hydrochloride is a tertiary amine that acts as a muscarinic acetylcholine receptor (mAChR) antagonist. It primarily targets the peripheral parasympathetic nervous system, exhibiting key biological activities related to the inhibition of smooth muscle contraction. This compound is utilized in research focused on gastrointestinal motility and the modulation of parasympathetic responses. -
mAChR Antagonist
Tigloidin is an antagonist of muscarinic acetylcholine receptors (mAChRs) with notable anticholinergic activity. This compound has potential implications in research related to neuropharmacology and the modulation of cholinergic signaling pathways. Its ability to inhibit mAChR activity makes it a valuable tool for investigating conditions influenced by acetylcholine activity. -
mAChR Antagonist
4-Piperidyl N-(2-biphenyl)carbamate is a competitive antagonist of muscarinic acetylcholine receptors (mAChR), exhibiting notable selectivity for the M2 and M3 subtypes. With pKi values of 7.33 for M2 and 7.51 for M3, this compound demonstrates a markedly higher affinity compared to β2 adrenergic receptors, which has a pKi of 4.94. This specificity makes it a valuable tool for research into mAChR-related signaling pathways and potential therapeutic applications in various neurological disorders. -
mAChR Agonist
Bethanechol is a selective agonist for muscarinic acetylcholine receptors (mAChRs), specifically targeting subtypes M1, M2, M3, M4, and M5. This parasympathomimetic compound promotes various parasympathetic responses, making it valuable in studies related to gastrointestinal motility, urinary retention, and other conditions influenced by parasympathetic activation. Research applications include evaluating the physiological effects of mAChR stimulation and investigating therapeutic strategies for disorders involving cholinergic transmission. -
mAChR Antagonist
Nuvenzepine is an mAChR antagonist that demonstrates potential therapeutic applications in the treatment of gastrospasm. By selectively inhibiting muscarinic acetylcholine receptors, Nuvenzepine may help alleviate symptoms associated with gastrointestinal motility disorders. This compound is of particular interest in pharmacological research focused on gastrointestinal therapies. -
mAChR Antagonist
Oxitropium Bromide is a muscarinic acetylcholine receptor (mAChR) antagonist that serves as an effective anticholinergic bronchodilator. It is primarily utilized in the management of asthma and chronic obstructive pulmonary disease (COPD), where it helps alleviate bronchoconstriction and improve airflow. This compound is essential for research focused on respiratory health and the development of treatments for airway obstructive disorders. -
M5 mAChR Antagonist
VU6036864 is a selective antagonist of the M5 muscarinic acetylcholine receptor (mAChR) with an IC50 of 20 nM for human M5. This compound exhibits over 500-fold selectivity against human M1-4 receptors, making it a valuable tool for studying M5 receptor functions in both in vitro and in vivo settings. VU6036864 is characterized by its ability to penetrate the blood-brain barrier and demonstrate high oral bioavailability, providing a promising avenue for research in neuropharmacology and related fields. -
nAChR/mAChR Agonist
Arecoline hydrochloride is a partial agonist of nicotinic and muscarinic acetylcholine receptors (nAChR/mAChR). This psychoactive alkaloid demonstrates stimulation, increased alertness, anxiolytic effects, and possesses anti-parasitic properties. Additionally, Arecoline hydrochloride can induce oxidative stress, making it a valuable compound for research in neuropharmacology and parasitology. -
M4 Antagonist
VU6021625 is a selective antagonist of the M4 muscarinic acetylcholine receptor (mAChR), exhibiting an IC50 of 0.44 nM for human M4 and 57 nM for rat M4. This compound is valuable for studies exploring the role of M4 receptors in neurological processes and potential therapeutic targets for neurodegenerative diseases. Its selectivity and potency make it an important tool for researchers investigating cholinergic signaling pathways. -
Stable Isotope
(Rac)-5-Hydroxymethyl Tolterodine-d14 is a deuterium-labeled derivative of (Rac)-5-Hydroxymethyl Tolterodine, a potent muscarinic acetylcholine receptor (mAChR) antagonist. It exhibits high affinity with 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. This stable isotope is instrumental in studies related to overactive bladder syndrome and facilitates pharmacokinetic research by enabling sensitive detection and quantification in biological samples. -
Stable Isotope
Tiotropium-d3 bromide is a deuterium-labeled variant of Tiotropium bromide, a selective antagonist of muscarinic acetylcholine receptors (mAChRs). By inhibiting acetylcholine binding, it prevents the opening of ligand-gated ion channels, leading to bronchial dilation. This compound is primarily used in pharmacological studies related to respiratory disorders and can be utilized in isotopic labeling experiments to investigate drug metabolism and pharmacokinetics. -
M4 mAChR Modulator
VU6016235 is a selective positive allosteric modulator of the M4 muscarinic acetylcholine receptor (mAChR). It demonstrates notable in vivo inhibitory potency in animal models of psychosis, indicating potential therapeutic applications in neuropsychiatric disorders. This compound may be valuable for researchers investigating the modulation of cholinergic signaling and its effects on behavior and cognition. -
Antimuscarinic
Telenzepine is an antimuscarinic agent that selectively targets muscarinic receptors, demonstrating binding affinities with Kis of 0.94 nM for M1 mAChR and 17.8 nM for M2 mAChR. It effectively inhibits synaptic transmission induced by muscarinic or M1 receptor agonists, resulting in a reduction of extracellular slow excitatory postsynaptic potentials with an EC50 of 38 nM and slow inhibitory postsynaptic potentials with an EC50 of 253 nM. This compound is valuable for research in neuropharmacology and the study of cholinergic signaling pathways. -
Precursor of Triazolobenzodiazepines
Desalkylquazepam, a precursor in the synthesis of triazolobenzodiazepines, is recognized for its role as a mAChR modulator with an EC50 value of 0.317 µM. This compound is utilized in research related to the development of therapeutic agents targeting benzodiazepine receptors. Its biological activity makes it a valuable reagent for studies exploring anxiety, sedation, and other central nervous system disorders. -
mAChR Antagonist
L-Hyoscyamine sulfate hydrate is a potent and competitive antagonist of muscarinic acetylcholine receptors (mAChR). As a naturally occurring tropane alkaloid, it exhibits significant biological activity by inhibiting mAChR-mediated signaling pathways. This compound is primarily utilized in pharmacological research and studies related to the modulation of synaptic transmission, making it valuable for investigating various physiological and pathological processes. -
M4 mAChR Positive Allosteric Modulator
VU6002703 is a positive allosteric modulator (PAM) of the M4 muscarinic acetylcholine receptor (mAChR), exhibiting an EC50 of 0.6 μM for human M4. This compound is designed for research into neuropsychiatric disorders and rare genetic conditions affecting the central nervous system (CNS). Its ability to penetrate the blood-brain barrier makes it a valuable tool for studying the modulation of cholinergic signaling in various models of CNS diseases. -
M2 mAChR Ligand
Bibn 140 is a pyridine derivative that acts as a selective antagonist of the M2 muscarinic acetylcholine receptor (mAChR), exhibiting high affinity with a Ki value of 12 nM. This compound is primarily utilized in research exploring cholinergic signaling and its implications in neurological disorders. Its specificity for the M2 subtype over the M1 receptor positions it as a valuable tool for studying M2 receptor-related biological processes. -
mAChR Antagonist
(S)-Vamicamide is a selective antagonist of the muscarinic acetylcholine receptors (mAChRs). This compound exhibits notable anticholinergic activity, making it useful for studies related to neurotransmission and receptor signaling pathways. Its application extends to research in conditions influenced by cholinergic modulation, such as cognitive disorders and movement disorders. -
Stable Isotope
Pirenzepine-d8 dihydrochloride is a deuterium-labeled derivative of Pirenzepine, a selective antagonist of the M1 muscarinic acetylcholine receptor (mAChR). This compound exhibits significant biological activity by inhibiting gastric acid secretion and alleviating muscle spasms, making it valuable for research in peptic ulcers. Additionally, Pirenzepine-d8 demonstrates anti-proliferative effects in cancer cell lines, contributing to its use in cancer research applications. -
M1/M4 Muscarinic Agonist
M1/M4 Muscarinic Agonist 3 is a selective agonist for the M1 and M4 muscarinic acetylcholine receptors (mAChRs), exhibiting EC50 values of 31 nM and 9.3 nM, respectively. This compound is instrumental in the investigation of cholinergic signaling pathways and has potential applications in neurological research, particularly in the study of cognitive function and memory modulation. Its efficacy in activating M1/M4 receptors makes it a valuable tool for studying muscarinic receptor pharmacology. -
mAChR Antagonist
Vamicamide is a competitive antagonist of muscarinic acetylcholine receptors (mAChRs) that functions by inhibiting the binding of mAChR agonists, thereby preventing contractions induced by cholinergic nerve stimulation. It demonstrates significant anti-bladder spasm effects, exhibiting a pA2 value of 6.82 in bladder tissue. Vamicamide is valuable for research in the study of neurological diseases and disorders related to bladder dysfunction. -
M1-mAChR Agonist
HTL-9936 is a selective agonist of the M1 muscarinic acetylcholine receptor (M1-mAChR), which plays a crucial role in cognitive function and memory. This compound demonstrates potential therapeutic effects in the context of neurodegenerative disorders, particularly Alzheimer's disease. HTL-9936 is a valuable tool for researchers investigating cholinergic signaling pathways and developing novel treatments for cognitive decline. -
mAChR Agonist
(Rac)-Sabcomeline is a selective agonist for M1 and M4 muscarinic acetylcholine receptors (mAChRs), providing a valuable resource for investigating neurological disorders, particularly schizophrenia. Its activation of mAChRs can facilitate insights into cholinergic signaling pathways and their implications in neuropsychiatric conditions. This compound supports research into the development of therapeutic strategies targeting muscarinic receptors in the treatment of various cognitive and mood disorders. -
M1 mAChR Positive Allosteric Modulator
M1 mAChR modulator-1 is a positive allosteric modulator of the muscarinic M1 receptor (mAChR1). It enhances gastrointestinal motility and facilitates defecation in mouse models, exhibiting low permeability to the central nervous system. This compound is valuable for research focused on gastrointestinal disorders, particularly constipation. -
nAChR Desensitizer
Anagyrine hydrochloride is a quinolizidine alkaloid that serves as a desensitizer of nicotinic acetylcholine receptors (nAChR). It exhibits potent binding to muscarinic acetylcholine receptors with an IC50 value of 132 µM and a weaker interaction with nAChR at 2096 µM. This compound effectively desensitizes nAChR without requiring metabolic conversion, making it valuable for research involving cholinergic signaling and receptor function studies. -
M3 mAChR Antagonist
YM-58790 free base is a potent antagonist of the muscarinic acetylcholine receptors (mAChR), specifically targeting the M3 subtype with a Ki value of 15 nM, along with M1 and M2 subtypes at 28 nM and 260 nM, respectively. This compound demonstrates significant inhibitory effects on bladder pressure during reflexly-evoked rhythmic contractions in rat studies. YM-58790 free base is used in research focused on neuropharmacology and the modulation of cholinergic signaling pathways, particularly in relation to bladder function and potential therapeutic applications in urological disorders. -
mAChR Agonist
Arecaidine-propargyl ester tosylate acts as a potent agonist of muscarinic acetylcholine receptors (mAChR). Its primary biological activity includes stimulation of mAChR, which is critical for neuropharmacological research and studies related to the central nervous system. This compound is useful for exploring the role of muscarinic signaling in various physiological processes and developing potential therapeutic strategies targeting mAChR pathways. -
mAChR Inhibitor
(Rac)-Sabcomeline hydrochloride is a selective agonist of the M1 muscarinic acetylcholine receptor (mAChR). It exhibits potential neuroprotective effects and is of significant interest in research related to Alzheimer's disease and cognitive disorders. This compound is utilized in studies aimed at understanding the role of muscarinic receptors in synaptic plasticity and memory function. -
mAChR Modulator
(E/Z)-VU0029767 is an allosteric modulator of M1 muscarinic acetylcholine receptors (mAChRs), enhancing receptor activity by increasing agonist affinity. This compound exhibits distinct properties across various experimental conditions, including its interaction with mutant M1 receptors and effects on downstream signaling pathways. (E/Z)-VU0029767 is employed in research to explore mAChR function and develop therapeutic strategies targeting related neurological disorders. -
mAChR Antagonist
Parapenzolate bromide is an orally active antagonist of muscarinic acetylcholine receptors (mAChRs). As an anticholinergic agent, it demonstrates antispasmodic properties, making it useful for studies related to gastrointestinal motility and smooth muscle relaxation. This compound is valuable in research applications focusing on the modulation of cholinergic signaling and its effects on various physiological processes. -
mAChR Antagonist
Sintropium bromide is a muscarinic acetylcholine receptor (mAChR) antagonist that exerts notable anticholinergic effects. Its primary biological activity includes alleviating pain and reducing muscle spasms, making it a valuable tool for research in pain management and neuromuscular studies. -
M4 mAChR PAM
VU6009453 is a positive allosteric modulator (PAM) of the M4 muscarinic acetylcholine receptor (mAChR), exhibiting an EC50 of 383 nM. This compound effectively enhances M4 receptor activity and is valuable for research focused on neurological disorders. Its ability to penetrate the blood-brain barrier makes it a pertinent tool in studies investigating potential therapeutic strategies for conditions related to M4 mAChR function. -
M4 mAChR PAM
M4 mAChR Modulator-2 is a selective positive allosteric modulator (PAM) of the M4 muscarinic acetylcholine receptor (M4 mAChR) with an EC50 of 513 nM. This compound exhibits a high degree of target selectivity, demonstrating minimal affinity for non-target receptors, such as D1R/D2R/D3R, various 5-HT subtypes, opioid receptors, and M1/M2 receptors. M4 mAChR Modulator-2 is effective in reversing hyperlocomotion induced by Dizocilpine (MK-801) in murine models and is utilized in research focused on schizophrenia. -
M1 mAChR PAM
ML169 is a potent and selective positive allosteric modulator (PAM) of the M1 muscarinic acetylcholine receptor (mAChR), demonstrating an EC50 of 1.38 µM. This compound exhibits significant brain penetrance and is a valuable tool for research in Alzheimer's disease. Its modulation of M1 mAChR enhances cholinergic signaling, making it an important probe for studying cognitive function and potential therapeutic strategies in neurodegenerative disorders. -
mAChR Inhibitor
BTM-1042 is a selective muscarinic acetylcholine receptor (mAChR) inhibitor with notable antispasmodic properties. It effectively inhibits electrical stimulation-induced contraction in the guinea pig ileum and demonstrates a dose-dependent reduction in spontaneous movement of the rabbit stomach. BTM-1042 displays similar activity to atropine in blocking muscarinic receptors while having a minimal impact on other receptor types. Additionally, it suppresses ileal responses triggered by nicotine and 5-hydroxytryptamine, highlighting its potential utility in gastrointestinal research applications and studies related to smooth muscle contraction modulation. -
Stable Isotope
Fesoterodine-d7 fumarate is a deuterium-labeled derivative of Fesoterodine fumarate, serving as a stable isotope for research applications. Fesoterodine fumarate acts as a competitive antagonist of muscarinic acetylcholine receptors (mAChRs), 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, respectively. It is primarily utilized in studies related to overactive bladder (OAB) and provides valuable insight into muscarinic receptor function and pharmacology. -
M1 mAChR Agonist
GSK1034702 hydrochloride is a potent allosteric agonist of the M1 muscarinic acetylcholine receptor (mAChR), with a pEC50 value of 8.1, capable of crossing the blood-brain barrier. This compound activates the Gq/11 protein-mediated signaling pathway, leading to enhanced neuronal firing and long-term potentiation (LTP) in the hippocampal CA1 region. GSK1034702 hydrochloride is valuable for investigating cognitive impairments associated with neurological conditions, such as Alzheimer's disease, and demonstrates pro-cognitive effects in animal models, especially relevant in studies of nicotine withdrawal-induced cognitive dysfunction. Potential side effects related to peripheral M receptor activation, such as gastrointestinal reactions, should be considered in research applications. -
mAChR Antagonist
Oxyphencyclimine is an orally active antagonist of muscarinic acetylcholine receptors (mAChR). This compound is demonstrated to reduce ulceration index and enhance pepsin activity in rat models of gastric ulcers. Oxyphencyclimine is suitable for investigation in studies related to peptic ulcer disease and gastrointestinal spasms, providing a valuable tool for understanding these conditions. -
mAChR Antagonist
Atropine hydrobromide is a competitive antagonist of muscarinic acetylcholine receptors (mAChRs), demonstrating IC50 values of 0.39 nM and 0.71 nM for human mAChR M4 and chicken mAChR M4, respectively. It effectively inhibits acetylcholine-induced relaxations in human pulmonary veins. This compound is valuable for research applications related to anti-myopia and the treatment of bradycardia. -
AChE/mAChR Antagonist
CI-1002, a potent antagonist of acetylcholinesterase (AChE) and muscarinic acetylcholine receptors (mAChR), is utilized in neuroscience research. Its ability to inhibit AChE activity makes it particularly valuable for investigating the underlying mechanisms of cognitive dysfunction associated with Alzheimer’s disease. CI-1002 serves as a crucial tool for studying neurodegenerative processes and potential therapeutic strategies. -
mAChR Antagonist
AF-DX 384 methanesulfonate is a selective antagonist of M2 and M4 muscarinic acetylcholine receptors, with inhibitory constants of 6.03 nM and 10 nM, respectively. This compound has demonstrated the ability to reverse cognitive deficits in novel object recognition and passive avoidance assays in both aged rats and young rats subjected to scopolamine-induced impairments. It serves as a valuable tool in neuroscientific research focused on memory and learning processes. -
Antiarrhythmic Agent
Pirmenol is an orally active antiarrhythmic agent that primarily targets the muscarinic acetylcholine receptor (mAChR), leading to the inhibition of the I(K.ACh) current (IC50: 0.1 μM). It demonstrates significant antiarrhythmic properties, making it valuable for investigating cardiovascular disorders, particularly atrial fibrillation. Pirmenol serves as a useful tool for research aimed at understanding and developing treatments for cardiac arrhythmias.
