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. -
M1 Muscarinic Positive Allosteric Modulator
VU6004256 is a potent and selective positive allosteric modulator of the M1 muscarinic receptor, exhibiting an EC50 value of 155 nM. This compound enhances M1 receptor activity and shows promise in addressing cognitive deficits associated with schizophrenia. It is a valuable tool for research into therapeutic strategies targeting muscarinic receptors in neuropsychiatric disorders. -
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. -
M4 Positive Allosteric Modulator
VU0448088 is a potent positive allosteric modulator targeting the M4 muscarinic acetylcholine receptor, demonstrating EC50 values of 56 nM and 176 nM for human and rat receptors, respectively. This tricyclic compound effectively crosses the blood-brain barrier, making it a valuable tool for investigating neuropsychiatric conditions, particularly those related to psychosis. Its ability to enhance M4 receptor activity highlights its potential in research applications focused on neuromodulation and cognitive function. -
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. -
Muscarinic Acetylcholine Receptor M2 Modulator
BAY-2413555 is an orally active modulator of the muscarinic acetylcholine receptor M2, primarily targeting cardiac function. This compound demonstrates protective effects on the heart and enhances cardiac performance, making it a valuable tool for researching heart failure and related cardiovascular conditions. Its unique mechanism may provide insights into therapeutic strategies for managing heart health. -
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. -
M2 Cholinoceptors Allosteric Modulator
W-84 dibromide is a potent allosteric modulator of M2 cholinoceptors, effectively retarding the dissociation of [3H]N-methylscopolamine. This compound stabilizes the complexes formed between cholinergic antagonists and receptors, exhibiting non-competitive antagonism at muscarinic acetylcholine receptors. W-84 dibromide demonstrates protective effects against organophosphate intoxication when administered in conjunction with atropine, making it a valuable tool in neuropharmacological research and studies related to cholinergic signaling. -
Muscarinic Receptor Antagonist
Velufenacin is a muscarinic receptor antagonist that selectively blocks the activity of muscarinic acetylcholine receptors. This compound demonstrates significant biological activity in various in vitro and in vivo models, making it a valuable tool for studying the role of cholinergic signaling in physiological processes. Velufenacin is applicable in research focused on neurological disorders, respiratory conditions, and other diseases where modulation of the muscarinic receptor pathway is critical. -
Actin Agonist
NGX-267 is a selective agonist of the actin M1 receptor, demonstrating high selectivity among the five actin receptor subtypes, particularly favoring M1 over M3. This compound exhibits distinct affinity profiles for dopamine D2 and 5-HT2B receptors, highlighting its unique pharmacological properties. NGX-267 is valuable for research applications focused on actin receptor modulation and its implications in cellular dynamics and neurobiology. -
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. -
Steroids
Smilagenin acetate is a sapogenin derivative that targets steroid pathways. It has been shown to enhance the expression of acetylcholine M2 receptors, making it a valuable tool for research into dementia and related neurodegenerative disorders. This compound can facilitate studies aimed at understanding cholinergic signaling and its implications in cognitive function. -
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. -
M4 Inhibitor
VU6008055 is a potent, selective allosteric modulator targeting the M4 muscarinic acetylcholine receptor, with EC50 values of 73.4 nM for human M4 and 19.5 nM for rat M4. This compound is capable of crossing the blood-brain barrier and exhibits oral bioactivity, making it a valuable tool for neuropharmacological research. VU6008055 demonstrates antipsychotic-like effects, contributing to its potential applications in studying psychiatric disorders and related therapeutic approaches. -
Probe Metabolites
5-Hydroxytryptophol-O-glucuronide is a glucuronide standard utilized as a probe metabolite. It is specifically designed to assess the enzymatic activity of human UGT1A6 in various in vitro systems, including human liver microsomes and recombinant UGT1A6 assays. This compound serves as an essential tool for pharmacokinetic studies and the evaluation of drug metabolism. -
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. -
Neuroprotective Agent
Fentonium bromide is a neuroprotective agent that functions primarily as an anticholinergic, providing relief from gastrointestinal spasms and peptic ulcer symptoms. Its biological activity makes it a valuable compound for studying neurological disorders, particularly those involving bladder instability and dysfunction. Researchers can utilize Fentonium bromide to explore its therapeutic potential in neuroprotection and related pathways. -
M1 Muscarinic Receptor Agonist
Nebracetam hydrochloride is an orally active agonist of the M1 muscarinic receptor. It facilitates an increase in intracellular Ca2+ concentration, characterized by an EC50 value of 1.59 mM. This compound demonstrates neuroprotective properties and has potential to enhance cognitive function, making it relevant for research focused on neurological disorders, including Alzheimer's disease. -
M1 Receptor Antagonist
Nitrocaramiphen hydrochloride is a selective antagonist of the M1 muscarinic acetylcholine receptor, exhibiting a Ki value of 5.5 nM. This compound effectively blocks the hyperpolarizing effects induced by muscarine on muscle fibers, making it a valuable tool for research on cholinergic signaling and receptor pharmacology. Its application extends to studies on neuromuscular transmission and the physiological roles of M1 receptors in various systems. -
Muscarinic Receptor Antagonist
(R)-Oxybutynin hydrochloride is a muscarinic receptor antagonist exhibiting potent antimuscarinic, antispasmodic, and anticholinergic properties. It effectively competes with Carbachol to inhibit induced contractions, making it valuable for studying neurogenic bladder dysfunction and incontinence. Additionally, (R)-Oxybutynin hydrochloride features an alkyne group that allows for copper-catalyzed azide-alkyne cycloaddition (CuAAc), facilitating research in click chemistry applications. -
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. -
Muscarinic M4 Receptor PAM
Direclidine is a selective allosteric modulator of the muscarinic acetylcholine M4 receptor, known for its minimal affinity for M1, M2, M3, and M5 receptors. By non-covalently binding to the orthosteric site, Direclidine activates the M4 receptor, leading to the inhibition of acetylcholine release from striatal cholinergic interneurons. This mechanism helps to modulate the dopaminergic system and alleviate psychiatric symptoms linked to excessive dopamine activity. Direclidine is primarily utilized in research exploring neuropsychiatric disorders such as schizophrenia. -
Muscarinic Receptor Antagonist
(R)-Oxybutynin is a potent muscarinic receptor antagonist employed in the investigation of neurogenic bladder dysfunction. This compound exhibits antispasmodic, antimuscarinic, and anticholinergic properties, effectively inhibiting carbachol-induced contractions. It serves as a valuable tool for studying urinary incontinence and related conditions. -
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. -
Anticholinergic Agent
Penehyclidine is an anticholinergic agent that selectively antagonizes M1 and M3 receptors. This compound is known to activate NF-kB in lung tissue, leading to the inhibition of inflammatory factor release. Penehyclidine demonstrates potential in alleviating pulmonary inflammatory responses, particularly in models of chronic obstructive pulmonary disease (COPD) during mechanical ventilation. Its mechanistic action supports further research in respiratory disorders and inflammatory conditions. -
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. -
M2/4 Muscarinic Receptor Antagonist
TD-6301 is a potent antagonist of the M2 and M4 muscarinic receptors, demonstrating high selectivity and strong affinity for the human M2 receptor (Ki = 0.36 nM). This compound effectively inhibits volume-induced bladder contractions (ID50 = 0.075 mg/kg), making it a valuable tool in the study of overactive bladder conditions. Its specificity for bladder tissues presents opportunities for targeted therapeutic research in urology and related fields. -
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. -
Muscarinic Receptor Antagonist
Solifenacin D5 hydrochloride is a deuterium-labeled derivative of Solifenacin hydrochloride, acting as a muscarinic receptor antagonist. With pKis of 7.6, 6.9, and 8.0 for M1, M2, and M3 receptors respectively, it is effective in modulating receptor activity. This compound is primarily utilized in pharmacological research related to bladder control and the treatment of overactive bladder conditions. -
Muscarinic Acetylcholine Receptor Enhancer
VU6007678 is a muscarinic acetylcholine receptor enhancer that primarily acts as a potentiator of acetylcholine signaling. This compound enhances receptor activity at human M1, M3, and M5, as well as rat M1, M3, M4, and M5 muscarinic acetylcholine receptors. VU6007678 is a valuable tool for research investigations into Alzheimer's disease, schizophrenia, and ischemic stroke, facilitating studies of cognitive function and neuropharmacology. -
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. -
Muscarinic Receptor Agonist
Milameline hydrochloride is a nonselective, partial agonist of muscarinic receptors, demonstrated to enhance cognitive function. It exhibits comparable affinity across various human muscarinic receptor subtypes, with IC50 values of 1.3 µM for M1, 1.1 µM for M2, 1.5 µM for M3, and 1.9 µM for M4 receptors. Milameline hydrochloride produces both central and peripheral cholinergic effects and effectively reverses cognitive deficits induced by scopolamine. This compound serves as a valuable tool for research related to Alzheimer's disease and cognitive impairment. -
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. -
Muscarinic M3 Antagonist
AZD-9164 bromide is a long-acting antagonist of the muscarinic M3 receptor. It demonstrates significant potential for modulating airway smooth muscle contraction and has applications in the study of respiratory diseases, including chronic obstructive pulmonary disease (COPD) and asthma. Researchers may utilize AZD-9164 bromide to explore mechanisms underlying bronchoconstriction and to develop targeted therapies for these conditions.
