Catalog No.
Product Name
Application
Product Information
Citations
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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. -
M3 Receptor PAM
ASP8302 is a positive allosteric modulator of the muscarinic M3 receptor. It has demonstrated efficacy in enhancing voiding efficiency and decreasing residual urine volume in models of voiding dysfunction. ASP8302 is suitable for research applications focused on underactive bladder conditions. -
M1 Receptor Positive Modulator
PQCA is a selective and potent positive allosteric modulator of the muscarinic M1 receptor. With EC50 values of 49 nM and 135 nM for the rhesus and human M1 receptors, respectively, PQCA demonstrates high specificity, showing inactivity towards other muscarinic receptors. This compound has significant potential in addressing cognitive deficits associated with Alzheimer's disease, making it a valuable tool for research into therapeutic strategies for neurodegenerative disorders. -
M1 Positive Allosteric Modulator
VU0467319 is a highly selective, orally active M1 positive allosteric modulator (PAM) with a blood-brain barrier permeability and an EC50 of 492 nM. It demonstrates significant selectivity over M2-5 (EC50 > 30 μM) in both human and rat models. This compound enhances cognitive function through central M1 muscarinic receptors, making it a promising candidate for research into Alzheimer's disease without causing cholinergic adverse reactions. VU0467319 holds potential for advancing understanding and treatment strategies in cognitive impairments associated with neurodegenerative disorders. -
Anticholinergic Agent
Sofpironium bromide is an anticholinergic agent that primarily targets M3 muscarinic receptors in eccrine glands, effectively reducing sweating. This compound is utilized in research focused on primary axillary hyperhidrosis (PAH). Additionally, it demonstrates a high affinity for M1, M2, M4, and M5 muscarinic receptor subtypes, making it a valuable tool for studying various cholinergic pathways and their physiological effects. -
mAChR Antagonist
Fesoterodine is a competitive antagonist of muscarinic acetylcholine receptors (mAChR), exhibiting pKi values of 8.0, 7.7, 7.4, 7.3, and 7.5 for the M1, M2, M3, M4, and M5 subtypes, respectively. This orally active compound is primarily utilized in the treatment of overactive bladder (OAB) conditions. Its broad receptor targeting allows for effective modulation of bladder function, making it a valuable tool in urological research and therapy development. -
Relative Configuration of VU6021625
rel-VU6021625, a derivative of VU6021625, serves as a potent and selective antagonist of the mAChR M4 receptor, exhibiting IC50 values of 0.44 nM for human M4 and 57 nM for rat M4. This compound demonstrates significant potential in neurological research, particularly in the study of disorders related to cholinergic signaling. Its use can aid in understanding mAChR M4 functions and therapeutic applications targeting this receptor. -
mAChR Activator
VU0238441 is a positive allosteric modulator targeting pan muscarinic acetylcholine receptors (mAChRs), demonstrating EC50 values of 3.2 μM, 2.8 μM, 2.2 μM, 2.1 μM for M1, M2, M3, and M5, respectively, while maintaining minimal activity against M4 (>10 μM). This compound enhances the receptor activity in a pharmacologically relevant manner and is valuable for exploring the role of mAChRs in neurological and cognitive research. Its applications include drug discovery and the study of receptor signaling pathways associated with cholinergic systems. -
M5 mAChR PAM
ML380 is a selective positive allosteric modulator (PAM) targeting the M5 muscarinic acetylcholine receptor (mAChR) with EC50 values of 190 nM for human and 610 nM for rat receptors. It demonstrates moderate selectivity over the M1 and M3 mAChR subtypes. By enhancing the affinity of acetylcholine for the M5 mAChR, ML380 may play a significant role in research focused on neurological and cognitive functions, offering potential avenues for the study of related disorders. -
mAChR M5 Orthosteric Antagonist
ML381 is a selective orthosteric antagonist of the mAChR M5 receptor, with an IC50 of 450 nM and a Ki value of 340 nM. This compound is known for its ability to penetrate the central nervous system, making it a valuable tool for investigating the role of mAChR M5 in neurological research. Due to its instability in rat plasma, ML381 is primarily utilized as a molecular probe for in vitro studies and electrophysiological applications. -
mAChR Antagonist
Ipratropium bromide hydrate is a muscarinic acetylcholine receptor (mAChR) antagonist, exhibiting IC50 values of 2.9 nM, 2 nM, and 1.7 nM for M1, M2, and M3 receptors, respectively. This compound effectively induces relaxation of smooth muscle, making it valuable for research applications in chronic obstructive pulmonary disease (COPD) and asthma. Its selective inhibition of mAChRs contributes to its therapeutic potential in respiratory disorders. -
mAChR Antagonist
Tiotropium bromide monohydrate is a long-acting antagonist of muscarinic acetylcholine receptors (mAChRs). It exhibits significant bronchodilator activity, making it effective in the management of chronic obstructive pulmonary disease (COPD) and asthma. This compound is widely utilized in research studies investigating respiratory pharmacology and cholinergic signaling pathways. -
M4 mAChR Antagonist
VU6028418 is a potent and highly selective antagonist of the M4 muscarinic acetylcholine receptor (mAChR), exhibiting an IC50 of 4.1 nM against the human M4 receptor. This compound demonstrates promise in the modulation of cholinergic signaling pathways, making it an invaluable tool for research on neuropharmacology and therapeutic interventions in disorders linked to M4 mAChR activity. Its oral bioavailability further supports its use in in vivo studies, aiding in the exploration of its potential effects on cognition and metabolic processes. -
Antiacetylcholine Compound
Oxyphenonium bromide is an antiacetylcholine compound that functions as a muscarinic acetylcholine receptor (mAChR) antagonist. It effectively mitigates bronchial obstruction by blocking acetylcholine's action, thereby reducing airway constriction. This compound is primarily utilized in research investigating respiratory conditions and the modulation of cholinergic signaling pathways. -
mAChR M1/3/5 PAM
VU0119498 is a positive allosteric modulator of muscarinic acetylcholine receptors M1, M3, and M5, showing EC50 values of 6.04 µM, 6.38 µM, and 4.08 µM, respectively. This compound exhibits significant antidiabetic activity, making it a valuable tool for studying metabolic disorders and receptor signaling pathways related to glucose homeostasis. Its modulation of mAChR activity provides insights into therapeutic strategies for diabetes and other related conditions. -
Muscarinic Receptors Antagonist
Cyclopentolate hydrochloride is a muscarinic receptor antagonist, exhibiting a pKB value of 7.8 on the circular ciliary muscle. This anti-muscarinic agent is primarily utilized in ophthalmology for its ability to induce mydriasis and cycloplegia. It serves as a valuable tool in various research applications related to eye physiology and pharmacology. -
mAChR Inhibitor
Arborine is a potent mAChR inhibitor that modulates the peripheral actions of acetylcholine, leading to a significant reduction in blood pressure. This compound is particularly valuable in research applications focused on cardiovascular physiology and the mechanistic study of cholinergic signaling pathways. Its ability to influence blood pressure dynamics makes it an important tool for investigating therapeutic interventions in hypertension and related disorders.
