Catalog No.
Product Name
Application
Product Information
Citations
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mAChR Control
Tolterodine dimer acts as a muscarinic acetylcholine receptor (mAChR) antagonist. It serves as an impurity of Tolterodine, a compound known for its potent activity against mAChRs. This reagent is primarily utilized in research applications aimed at investigating cholinergic signaling pathways and evaluating potential therapeutic strategies for bladder control and related disorders. -
mAChR Agonist
NNC 11-1607 is a selective agonist for the M1 and M4 subtypes of muscarinic acetylcholine receptors (mAChR). It effectively inhibits Forskolin-stimulated cAMP accumulation in human M2 and M4 mAChR-expressing Chinese hamster ovary cells. This compound shows potential for investigating central nervous system disorders, including Alzheimer’s disease and schizophrenia, making it a valuable tool for related research applications. -
mAChR Antagonist
Atropine oxide hydrochloride is a competitive antagonist of muscarinic acetylcholine receptors, including M1, M2, M3, M4, and M5. It demonstrates key biological activity in antagonizing acetylcholine's effects, making it valuable in research focused on neurotransmission and receptor signaling. This reagent is particularly significant for studies involving the therapeutic applications in specific nerve agent and pesticide poisonings. -
Stable Isotope
Rac-Fesoterodine-d14 fumarate is a stable isotope-labeled version of the racemic muscarinic receptor antagonist Fesoterodine. It exhibits competitive inhibition across multiple mAChR subtypes, with pKivalues of 8.0, 7.7, 7.4, 7.3, and 7.5 for M1, M2, M3, M4, and M5 receptors, respectively. This compound is primarily utilized in research applications focusing on the pharmacological characterization and monitoring of overactive bladder treatments. -
mAChR
Revefenacin impurity 4 is an intermediate compound associated with Revefenacin, targeting the human M3 muscarinic acetylcholine receptor. This impurity demonstrates significant binding affinity with a Ki value of 55 nM, highlighting its potential as a pharmacological agent. It is useful for research applications involving muscarinic receptor modulation and the study of cholinergic signaling pathways. -
mAChR Control
(Rac)-5-Carboxy tolterodine is an inactive metabolite of the muscarinic acetylcholine receptor antagonist Tolterodine. It serves as a valuable control in studies involving muscarinic receptors, particularly in the context of acetylcholine modulation. This compound is useful for researchers investigating the pharmacokinetics and metabolic pathways of Tolterodine and related drugs. -
mAChR Antagonist
5-Hydroxymethyl tolterodine formate is a potent antagonist of muscarinic acetylcholine receptors (mAChR). This active metabolite, derived from tolterodine and fesoterodine through the action of CYP2D6 and plasma esterases respectively, has significant implications in the study of urinary disorders. Researchers can utilize 5-Hydroxymethyl tolterodine formate in pharmacological investigations of cholinergic signaling and its effects on smooth muscle activity, contributing to the understanding of treatment options for overactive bladder and related conditions. -
mAChR Antagonist
Alvameline maleate is a muscarinic acetylcholine receptor (mAChR) antagonist with selective activity at the M2 and M3 subtypes, while acting as a partial agonist for the M1 subtype. This compound has demonstrated the ability to competitively inhibit contractions in human detrusor muscle induced by ammonium chloride and electrical field stimulation, highlighting its potential for applications in bladder function regulation. Furthermore, alvameline maleate has shown promise in enhancing cognitive function following traumatic brain injury in rodent models, making it a valuable tool for research in both urology and neuropharmacology. -
mAChR Antagonist
Temiverine hydrochloride is a mAChR antagonist exhibiting anticholinergic activity. This compound is also a versatile click chemistry reagent, featuring an alkyne group that enables the copper-catalyzed azide-alkyne cycloaddition (CuAAC) with azide-containing molecules. Its applications extend to chemical biology, facilitating the development of novel therapeutics and biochemical probes. -
mAChR Antagonist
Ambutonium bromide is a selective antagonist of the muscarinic acetylcholine receptors (mAChRs). By inhibiting the action of acetylcholine, it plays a significant role in modulating cholinergic signaling pathways. This compound is primarily utilized in research applications aimed at studying the effects of mAChR inhibition in various physiological and pathological contexts. -
mAChR Agonist
ENS-163 phosphate is a selective muscarinic acetylcholine receptor (mAChR) M1 agonist. It exhibits significant biological activity by modulating M1 receptor signaling pathways, which are implicated in cognitive processes. This compound is valuable for research applications related to neuropsychological disorders and the exploration of potential therapeutic targets in Alzheimer's disease and other cognitive impairments. -
mAChR Antagonist
Rispenzepine is an antimuscarinic compound that selectively antagonizes M1 and M3 muscarinic acetylcholine receptors (mAChRs). This compound exhibits significant biological activity in modulating cholinergic signaling pathways, making it valuable for research on neurological disorders and other conditions influenced by mAChR activity. Its specific receptor selectivity positions Rispenzepine as a useful tool in studies focused on receptor function and the development of therapeutic interventions. -
mAChR Agonist
Muscarine tosylate is a potent agonist of the muscarinic acetylcholine receptors (mAChRs). This compound selectively stimulates the parasympathetic nervous system, leading to various physiological effects. Muscarine tosylate is widely utilized in research applications focusing on neuropharmacology and the modulation of cholinergic signaling pathways. -
Metabolite of Oxybutynin
N-Desethyloxybutynin hydrochloride is an active metabolite of Oxybutynin, primarily targeting muscarinic acetylcholine receptors (mAChRs). This compound demonstrates significant binding affinity in isolated human bladder and parotid gland tissues, with pKi values of 8.2 and 8.7, respectively. It is useful in research exploring bladder function, salivary secretion, and the pharmacological effects of anticholinergic agents. -
Stable Isotope
(R)-Hydroxytolterodine-d14 is a deuterated form of Desfesoterodine, a selective antagonist of muscarinic acetylcholine receptors (mAChRs). This compound exhibits high potency, with a KB value of 0.84 nM and a pA2 of 9.14. As a significant metabolite of Tolterodine and Fesoterodine, it has demonstrated efficacy in models of cerebral infarction-induced detrusor overactivity in rats, making it valuable for research in urology and neurology. -
mAChR Antagonist
WIN 62,577 is a selective antagonist of muscarinic acetylcholine receptors (mAChRs), specifically targeting M1 to M4 subtypes. This compound acts as an allosteric enhancer of acetylcholine affinity at the M3 receptor, making it a valuable tool for studying cholinergic signaling. Its unique properties allow for exploration of mAChR-related pathways and their implications in various physiological and pathological conditions. Suitable for research applications in neurobiology and pharmacology, WIN 62,577 facilitates investigations into receptor functions and potential therapeutic targets. -
mAChR Antagonist
Cyclodrine hydrochloride is a potent antagonist of muscarinic acetylcholine receptors (mAChRs). It is primarily utilized in research to investigate cholinergic signaling pathways and the role of mAChR in various physiological and pathological processes. This compound may aid in the exploration of potential therapeutic targets for disorders influenced by cholinergic activity. -
mAChR Agonist
CDD0102 is a potent agonist of the M1 muscarinic acetylcholine receptor (mAChR). It demonstrates significant biological activity in promoting M1 receptor signaling pathways, making it valuable for research into neurobiology and cognitive function. CDD0102 is essential for studies investigating the role of muscarinic receptors in various physiological and pathological processes. -
mAChR Inhibitor
Tematropium is a selective muscarinic acetylcholine receptor (mAChR) inhibitor known for its soft anticholinergic properties. It demonstrates significant biological activity in modulating bronchoconstriction and respiratory secretions. Tematropium is commonly used in research focused on respiratory diseases, exploring its potential in the treatment of asthma and chronic obstructive pulmonary disease (COPD). -
mAChR Modulator
BTM-1086 is a potent muscarinic acetylcholine receptor (mAChR) modulator, primarily functioning as an anti-ulcer agent. It demonstrates significant inhibitory activity against gastric secretion, making it valuable for research in gastrointestinal disorders. BTM-1086 can be utilized in studies focused on receptor signaling and the pharmacological management of gastric-related conditions. -
mAChR Antagonist
YM-46303 is an antagonist of muscarinic acetylcholine receptors (mAChR), demonstrating high affinity for both M1 and M3 subtypes, with notable selectivity for the M3 receptor over the M2 receptor. This compound is valuable in the study of receptor signaling pathways and can be utilized in research involving neurological disorders, smooth muscle contraction, and other cholinergic system-related investigations. Its specificity makes it a useful tool for elucidating the roles of mAChR subtypes in various biological processes. -
mAChR Inhibitor
Timepidium bromide is a muscarinic acetylcholine receptor (mAChR) inhibitor that exhibits anticholinergic properties. It is primarily utilized in research investigating acetylcholine signaling pathways and the role of mAChR in various physiological and pathological processes. This compound is valuable for studying conditions influenced by cholinergic activity, including respiratory and gastrointestinal disorders. -
mAChR Activator
Vinconate is an indolonaphthyridine derivative that acts as an activator of the muscarinic acetylcholine receptor (mAChR). This compound is utilized in research to investigate cholinergic signaling pathways and their implications in neurological and cognitive functions. Its ability to modulate mAChR activity makes it a valuable tool for exploring potential therapeutic applications in neurodegenerative diseases and cognitive disorders. -
mAChR Antagonist
Atropine is a competitive antagonist of muscarinic acetylcholine receptors (mAChR), exhibiting IC50 values of 0.39 nM for human mAChR M4 and 0.71 nM for chicken mAChR M4. This compound effectively inhibits acetylcholine-induced relaxations in human pulmonary veins. Atropine is utilized in research focused on anti-myopia and the treatment of bradycardia. -
mAChR Agonist
Betovumeline hydrochloride is an agonist of muscarinic acetylcholine receptors (mAChRs), which play a critical role in various neurological functions. This compound is valuable for research into neurological disorders, facilitating the study of receptor activation and signaling pathways. Its ability to selectively engage mAChRs makes it a useful tool in pharmacological investigations and potential therapeutic applications. -
M1/M4 receptor Agonist
Xanomeline is a selective agonist of the muscarinic M1 and M4 receptors, known to enhance neuronal excitability. This compound is primarily used in research focused on neurological disorders, including schizophrenia, and offers potential insights into the modulation of cholinergic signaling pathways in the central nervous system. -
M1/M4 Receptor Agonist
Xanomeline tartrate is a potent agonist of the muscarinic M1 and M4 receptors, exhibiting antipsychotic-like activity. This compound enhances neuronal excitability and is primarily utilized in research focused on schizophrenia. Its mechanism provides valuable insights into potential therapeutic approaches for neuropsychiatric conditions. -
mAChR Superagonist
Iperoxo is a potent superagonist of muscarinic acetylcholine receptors (mAChR), effectively activating M1, M2, and M3 subtypes with pEC50 values of 9.87, 10.1, and 9.78, respectively. This compound is valuable for investigating activation-related conformational transitions in muscarinic receptors, particularly when labeled with tritium. Its strong receptor activity makes Iperoxo suitable for research in neurotransmission and receptor pharmacology. -
Muscarinic M4 Receptor Modulator
Emraclidine is a positive allosteric modulator of the muscarinic M4 receptor, designed to enhance receptor activity. This compound has shown potential in the study of neurological diseases, providing insights into cholinergic signaling pathways and their implications in various disorders. Researchers may utilize Emraclidine to explore novel therapeutic approaches targeting the M4 receptor in neuropharmacology. -
hM3Dq Agonist
DREADD agonist 21 dihydrochloride is a highly potent agonist of the human muscarinic acetylcholine M3 receptor (hM3Dq), with an EC50 value of 1.7 nM. This compound selectively activates hM3Dq, facilitating the study of neuronal signaling pathways in various research applications. Its utility in chemogenetics allows for precise modulation of cellular activity, making it an invaluable tool for investigating the roles of specific neuronal circuits in behavior and disease models. -
Muscarinic Receptor Agonist
Pilocarpine nitrate is a potent agonist of the M3 muscarinic acetylcholine receptor. It effectively stimulates muscarinic receptors, leading to increased salivation and glandular secretions. This compound is widely utilized in pharmacological research related to the treatment of dry mouth and glaucoma, as well as in studies of neurodegenerative diseases. -
M1 Antagonist
VU 0255035 is a highly selective and competitive antagonist of the M1 muscarinic acetylcholine receptor (mAChR). It effectively inhibits M1 mAChR signaling, which contributes to the reduction of epileptic seizures and the modulation of neuronal membrane potential. This compound is valuable for research applications focused on central nervous system disorders, including epilepsy, Parkinson's disease, and dystonia. -
BChE/NMDA/mAChR Antagonist
Ethopropazine hydrochloride is a potent and selective inhibitor of butyrylcholinesterase (BChE) and acts as a non-selective antagonist at muscarinic acetylcholine receptors (mAChR) and N-methyl-D-aspartate receptors (NMDA). This compound exhibits anticholinergic, antihistamine, and antiadrenergic activities, making it valuable in studying its effects on neuropathic pain conditions such as thermal hyperalgesia. Ethopropazine hydrochloride is particularly relevant in research related to Parkinson's disease, providing insights into cholinergic system modulation and receptor interactions. -
mAChR Antagonist
Otenzepad is a selective, competitive antagonist of the M2 muscarinic acetylcholine receptor, exhibiting IC50 values of 640 nM in rabbit peripheral lung tissue and 386 nM in rat heart tissue. This compound plays a significant role in modulating cholinergic signaling and has applications in research focused on respiratory and cardiovascular physiology. Its use aids in the study of receptor-mediated pathways and potential therapeutic targets in related disorders. -
mAChR Agonist
Oxotremorine sesquifumarate is an agonist of muscarinic acetylcholine receptors (mAChRs), primarily activating the M2 subtype. This compound is instrumental in neurological research, facilitating the study of cholinergic signaling and its implications in various neurological disorders. Its ability to modulate M2 receptor activity makes it valuable for investigating the physiological and pathophysiological roles of these receptors in the nervous system. -
M1 mAChR Antagonist
Pirenzepine is a selective antagonist of the M1 muscarinic acetylcholine receptor (mAChR) with limited ability to cross the blood-brain barrier. This compound is primarily utilized for its ability to inhibit gastric acid secretion and alleviate muscle spasm, making it relevant in the study of peptic ulcers. Additionally, Pirenzepine exhibits anti-proliferative properties in various cancer cell lines, providing valuable insights for cancer research applications. -
Vesicular Acetylcholine Transporter Inhibitor
(-)-Vesamicol is a vesicular acetylcholine transporter inhibitor that exerts its action by reversibly and non-competitively inhibiting the transport of acetylcholine into synaptic vesicles. This compound effectively blocks the activity of vesicular acetylcholine transporters in medial amygdala neurons, making it a valuable tool for studies related to neurotransmission and neurodevelopmental disorders. Its specific application is in research focused on central precocious puberty, providing insights into the role of acetylcholine transport in this condition. -
mAChR Modulator
Aceclidine, a modulator of muscarinic acetylcholine receptors, primarily targets the M3 receptor while also acting as an M1 receptor agonist (EC50: 40 μM). This compound serves as a cycloplegic agent, surfactant, tonicity adjustor, and can enhance viscosity and provide antioxidant effects. It is applicable in research focusing on conditions such as refractive errors of the eye, xerostomia, Sjögren's syndrome, glaucoma, conjunctivitis, lacrimal gland disorders, and esotropia. -
M1 PAM
VU0453595 is a highly selective positive allosteric modulator (PAM) for the M1 muscarinic acetylcholine receptor, with an EC50 of 2140 nM. This compound has shown potential in modulating M1 receptor activity, making it a valuable tool for investigations into schizophrenia and related cognitive disorders. Its systemic activity enhances the understanding of M1 receptor function and its role in neuropsychiatric conditions. -
M5 mAChR Antagonist
VU6019650 is a potent and selective orthosteric antagonist of the M5 muscarinic acetylcholine receptor (IC50 = 36 nM). This compound is being investigated for its potential in alleviating opioid use disorder by modulating the mesolimbic dopaminergic reward circuitry. VU6019650 effectively reduces neuronal firing rates in midbrain dopamine neurons of the ventral tegmental area in response to Oxotremorine M iodide, offering insights into its pharmacological application in neuropsychiatric research. -
mAChR Antagonist
(Rac)-5-Hydroxymethyl Tolterodine is a mAChR antagonist with high affinity for M1, M2, M3, M4, and M5 receptors, exhibiting Ki values of 2.3 nM, 2 nM, 2.5 nM, 2.8 nM, and 2.9 nM, respectively. This active metabolite of Tolterodine is valuable for investigating the pathophysiology and treatment of overactive bladder conditions. Its selective inhibition of muscarinic acetylcholine receptors allows for exploration of therapeutic strategies targeting bladder hyperactivity. -
DREADD Agonist
JHU37160 is a potent DREADD agonist that selectively targets hM3Dq and hM4Di receptors with EC50 values of 18.5 nM and 0.2 nM, respectively, in HEK-293 cells. This compound exhibits significant brain penetration and selectively displaces [3H]Clozapine from DREADD sites without affecting other Clozapine-binding sites in murine brain tissue. JHU37160 is valuable for research applications involving chemogenetics, neurobiology, and the exploration of neural circuits. -
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. -
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.
