Catalog No.
Product Name
Application
Product Information
Citations
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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. -
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. -
Muscarinic Receptor Blocker
Ethybenztropine is a muscarinic receptor blocker, functioning primarily as an anticholinergic agent. It inhibits the action of acetylcholine at muscarinic receptors, thereby exerting antihistaminergic effects. This compound is utilized in research applications that explore cholinergic signaling pathways and the role of muscarinic receptors in various biological processes. -
Cholinergic Receptor
L-(-)-Neopterin (L-erythro-Neopterin) is a competitive antagonist of cholinergic receptors, mitigating the inhibitory effects of pteridine diuretics on the growth of Crithidia fasciculata. This compound is valuable in studies investigating nervous system functions and purine metabolism, providing insights into neurochemical pathways and potential therapeutic applications. -
M1 Positive Allosteric Modulator
VU6052254 is a selective, potent positive allosteric modulator of the muscarinic M1 acetylcholine receptor, exhibiting an EC50 of 59 nM. This compound demonstrates no activity on M2-5 receptors, ensuring specificity in its mechanism of action. VU6052254 enhances memory recognition and effectively reverses cognitive impairments induced by scopolamine at a minimum effective dose of 1 mg/kg. It is a valuable tool for researching neurological disorders, including Alzheimer's disease, facilitating investigations into cognitive enhancement strategies. -
Muscarinic Receptor Blocker
Ethybenztropine hydrobromide is a muscarinic receptor blocker with notable antiparkinsonian activity. This anticholinergic agent functions to alleviate symptoms associated with Parkinson's disease, potentially enhancing dopaminergic signaling by acting as a dopamine reuptake inhibitor. It is widely utilized in research exploring therapeutic strategies for managing Parkinson’s disease and related movement disorders. -
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. -
Muscarinic M3 Receptor Antagonist
Muscarinic M3 receptor antagonist-2 is a selective antagonist of the muscarinic M3 receptor, crucial in mediating various physiological responses. This compound demonstrates potency in inhibiting M3 receptor activity, making it valuable for research into disorders related to cholinergic signaling and smooth muscle contraction. Its application is particularly relevant in studies focused on airway diseases, gastrointestinal motility, and other conditions associated with M3 receptor dysregulation. -
M1 Receptor Agonist
Lu AE51090 is a selective agonist of the muscarinic M1 receptor, designed to penetrate the blood-brain barrier. This compound activates the human M1 receptor with an EC50 of 61 nM and demonstrates minimal activity at M2 to M5 receptors. Lu AE51090 has been shown to produce procognitive effects in murine models and is relevant for research into Alzheimer’s disease and cognitive impairments associated with schizophrenia. -
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. -
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. -
Anticholinergic Agent
Homatropine hydrochloride is an anticholinergic agent that primarily targets muscarinic acetylcholine receptors. It effectively induces pupil dilation and exerts cycloplegic effects, making it valuable in ophthalmologic studies. Additionally, it demonstrates antitussive properties, contributing to research in respiratory conditions. This compound is suitable for investigations into eye diseases and cough-related disorders.
