Catalog No.
Product Name
Application
Product Information
Citations
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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. -
nAChR Desensitizer
Anagyrine hydrochloride is a quinolizidine alkaloid that serves as a desensitizer of nicotinic acetylcholine receptors (nAChR). It exhibits potent binding to muscarinic acetylcholine receptors with an IC50 value of 132 µM and a weaker interaction with nAChR at 2096 µM. This compound effectively desensitizes nAChR without requiring metabolic conversion, making it valuable for research involving cholinergic signaling and receptor function studies. -
M3 mAChR Antagonist
YM-58790 free base is a potent antagonist of the muscarinic acetylcholine receptors (mAChR), specifically targeting the M3 subtype with a Ki value of 15 nM, along with M1 and M2 subtypes at 28 nM and 260 nM, respectively. This compound demonstrates significant inhibitory effects on bladder pressure during reflexly-evoked rhythmic contractions in rat studies. YM-58790 free base is used in research focused on neuropharmacology and the modulation of cholinergic signaling pathways, particularly in relation to bladder function and potential therapeutic applications in urological disorders. -
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. -
mAChR Agonist
Arecaidine-propargyl ester tosylate acts as a potent agonist of muscarinic acetylcholine receptors (mAChR). Its primary biological activity includes stimulation of mAChR, which is critical for neuropharmacological research and studies related to the central nervous system. This compound is useful for exploring the role of muscarinic signaling in various physiological processes and developing potential therapeutic strategies targeting mAChR pathways. -
Muscarinic Acetylcholine Receptor M3 Antagonist
Muscarinic M3 receptor antagonist-1 functions as an antagonist of the muscarinic acetylcholine receptor M3. It plays a crucial role in the study of inflammatory and obstructive airway diseases, providing insights into potential therapeutic interventions. This reagent aids in the exploration of M3 receptor-mediated pathways and their implications in respiratory conditions. -
Muscarinic Antagonist
Tiquizium bromide is a nonselective muscarinic antagonist that acts as an atropine-type spasmolytic agent. It effectively inhibits the development of gastric and duodenal lesions, while also inducing mydriasis and reducing salivation induced by pilocarpine. This compound is useful in pharmacological studies aimed at exploring muscarinic receptor modulation and its physiological effects. -
mAChR Inhibitor
(Rac)-Sabcomeline hydrochloride is a selective agonist of the M1 muscarinic acetylcholine receptor (mAChR). It exhibits potential neuroprotective effects and is of significant interest in research related to Alzheimer's disease and cognitive disorders. This compound is utilized in studies aimed at understanding the role of muscarinic receptors in synaptic plasticity and memory function. -
M1 Receptor Agonist
Tazomeline is a selective agonist of the M1 muscarinic receptor, demonstrating significant inhibitory effects on twitch height in the rabbit vas deferens with an IC50 of 0.001 nM. This compound is primarily utilized in research focused on neuropsychiatric disorders, offering insights into the modulation of cholinergic signaling and potential therapeutic applications. -
mAChR Modulator
(E/Z)-VU0029767 is an allosteric modulator of M1 muscarinic acetylcholine receptors (mAChRs), enhancing receptor activity by increasing agonist affinity. This compound exhibits distinct properties across various experimental conditions, including its interaction with mutant M1 receptors and effects on downstream signaling pathways. (E/Z)-VU0029767 is employed in research to explore mAChR function and develop therapeutic strategies targeting related neurological disorders. -
mAChR Antagonist
Parapenzolate bromide is an orally active antagonist of muscarinic acetylcholine receptors (mAChRs). As an anticholinergic agent, it demonstrates antispasmodic properties, making it useful for studies related to gastrointestinal motility and smooth muscle relaxation. This compound is valuable in research applications focusing on the modulation of cholinergic signaling and its effects on various physiological processes. -
M1 Receptor Antagonist
Trihexyphenidyl is a selective M1 muscarinic receptor antagonist, with an IC50 of 3.7 nM for rat cerebral cortex M1 receptors. It modulates cholinergic activity, effectively countering acetylcholine supersensitivity in neural pathways. Trihexyphenidyl is utilized in research for Parkinson's disease and demonstrates efficacy in improving movement disorders, as well as inhibiting vagally-induced bradycardia and vasodilation. Its inhibition of McN-A-343-induced pressor responses highlights its potential in studying neurophysiological effects. -
Muscarinic Receptor Ligand
Emepronium bromide is a muscarinic receptor ligand that acts as an antispasmodic agent for the bladder, exhibiting an IC50 of 236 nM. This compound is valuable for research focused on bladder diseases, allowing for the exploration of muscarinic receptor mechanisms and the development of therapeutic strategies targeting bladder dysfunction. -
M3 Antagonist
MK-0969 is an M3 muscarinic acetylcholine receptor antagonist. It exhibits biological activity relevant to the modulation of smooth muscle tone, making it useful in the study of conditions such as chronic obstructive pulmonary disease and urinary incontinence. Researchers can employ MK-0969 to investigate the therapeutic potential of M3 receptor inhibition in respiratory and urological disorders. -
Anticholinergic Agent
Ilmetropium iodide is an anticholinergic agent that selectively antagonizes M-cholinergic receptors in bronchial smooth muscle. This selective blockade effectively reduces or prevents bronchoconstriction triggered by cholinergic stimuli and various bronchospasm-inducing factors. With a superior strength and selectivity compared to other anticholinergics, ilmetropium iodide is a valuable tool in respiratory research and the development of novel therapeutic strategies for conditions like asthma and COPD. -
mAChR Antagonist
Sintropium bromide is a muscarinic acetylcholine receptor (mAChR) antagonist that exerts notable anticholinergic effects. Its primary biological activity includes alleviating pain and reducing muscle spasms, making it a valuable tool for research in pain management and neuromuscular studies. -
M1 muscarinic/σ1 Receptor Agonist
(Rac)-AF710B is a potent allosteric agonist targeting M1 muscarinic and σ1 receptors. This compound exhibits selective interactions that are valuable for elucidating the role of these receptors in neurological pathways. Its application in research focuses primarily on Alzheimer's disease, making it a significant reagent for studying potential therapeutic strategies. -
M4 mAChR PAM
VU6009453 is a positive allosteric modulator (PAM) of the M4 muscarinic acetylcholine receptor (mAChR), exhibiting an EC50 of 383 nM. This compound effectively enhances M4 receptor activity and is valuable for research focused on neurological disorders. Its ability to penetrate the blood-brain barrier makes it a pertinent tool in studies investigating potential therapeutic strategies for conditions related to M4 mAChR function. -
Muscarinic Receptor Ligand
PTAC oxalate is a selective ligand for muscarinic receptors, functioning as a partial agonist at M2 and M4 receptors while acting as an antagonist at M1, M3, and M5 receptors, with Ki values ranging from 0.2 to 2.8 nM in CHO cells. This compound demonstrates significant biological activity by alleviating mechanical allodynia associated with neuropathic pain and exhibiting potential antidepressant effects. PTAC oxalate serves as a valuable tool for research into muscarinic receptor function and the development of therapeutics for pain and mood disorders. -
Antimuscarinic Agent
Prifinium bromide is an antimuscarinic agent that acts by selectively inhibiting muscarinic acetylcholine receptors. It exhibits antispasmodic and antiemetic effects, making it useful in the management of gastrointestinal disorders. This compound is relevant for research applications involving smooth muscle relaxation and the modulation of vomiting reflex pathways. -
M4 mAChR PAM
M4 mAChR Modulator-2 is a selective positive allosteric modulator (PAM) of the M4 muscarinic acetylcholine receptor (M4 mAChR) with an EC50 of 513 nM. This compound exhibits a high degree of target selectivity, demonstrating minimal affinity for non-target receptors, such as D1R/D2R/D3R, various 5-HT subtypes, opioid receptors, and M1/M2 receptors. M4 mAChR Modulator-2 is effective in reversing hyperlocomotion induced by Dizocilpine (MK-801) in murine models and is utilized in research focused on schizophrenia. -
M3 Muscarinic Receptor Antagonist
J-104129 is a selective antagonist of the M3 muscarinic receptor, exhibiting a Ki value of 4.2 nM. This compound demonstrates significant bronchodilatory effects, making it useful in studying respiratory disorders. Its oral bioactivity supports its application in pharmacological research focusing on muscarinic receptor modulation. -
M4 Receptor Positive Allosteric Modulator
Muscarinic M4 modulator-1 is a positive allosteric modulator of the M4 muscarinic receptor. It enhances receptor activity with allosteric potencies indicated by EC50 values of 14 nM in CHO-K1 cells and 3 nM in HEK293 cells. This compound exhibits antipsychotic-like effects, making it a valuable tool for research into psychiatric and neurological disorders. -
Muscarinic-3 Agonist
Methacholine iodide is a potent agonist of the muscarinic-3 (M3) receptor. By directly stimulating acetylcholine receptors on smooth muscle, it induces bronchoconstriction and airway narrowing. Methacholine iodide is particularly effective for assessing bronchial hyperresponsiveness (BHR) and is utilized as a diagnostic tool in evaluating airway hyperreactivity in patients with asthma-like symptoms and normal resting expiratory flow rates. -
M1 mAChR PAM
ML169 is a potent and selective positive allosteric modulator (PAM) of the M1 muscarinic acetylcholine receptor (mAChR), demonstrating an EC50 of 1.38 µM. This compound exhibits significant brain penetrance and is a valuable tool for research in Alzheimer's disease. Its modulation of M1 mAChR enhances cholinergic signaling, making it an important probe for studying cognitive function and potential therapeutic strategies in neurodegenerative disorders. -
mAChR Inhibitor
BTM-1042 is a selective muscarinic acetylcholine receptor (mAChR) inhibitor with notable antispasmodic properties. It effectively inhibits electrical stimulation-induced contraction in the guinea pig ileum and demonstrates a dose-dependent reduction in spontaneous movement of the rabbit stomach. BTM-1042 displays similar activity to atropine in blocking muscarinic receptors while having a minimal impact on other receptor types. Additionally, it suppresses ileal responses triggered by nicotine and 5-hydroxytryptamine, highlighting its potential utility in gastrointestinal research applications and studies related to smooth muscle contraction modulation. -
Stable Isotope
Fesoterodine-d7 fumarate is a deuterium-labeled derivative of Fesoterodine fumarate, serving as a stable isotope for research applications. Fesoterodine fumarate acts as a competitive antagonist of muscarinic acetylcholine receptors (mAChRs), demonstrating non-subtype selectivity with pKi values of 8.0, 7.7, 7.4, 7.3, and 7.5 for M1, M2, M3, M4, and M5, respectively. It is primarily utilized in studies related to overactive bladder (OAB) and provides valuable insight into muscarinic receptor function and pharmacology. -
M1/M2/M4 Muscarinic Agonist
M1/M2/M4 muscarinic agonist 3 is a selective agonist for muscarinic acetylcholine receptors M1, M2, and M4, exhibiting EC50 values of 3.2 nM, 32 nM, and 1.7 nM, respectively. This compound is effective in modulating neurotransmission and has significant implications for research in cognitive function, neuropharmacology, and potential therapeutic applications in neurological disorders. Its activity profile makes it a valuable tool for studying muscarinic signaling pathways and receptor interactions. -
M1 mAChR Agonist
GSK1034702 hydrochloride is a potent allosteric agonist of the M1 muscarinic acetylcholine receptor (mAChR), with a pEC50 value of 8.1, capable of crossing the blood-brain barrier. This compound activates the Gq/11 protein-mediated signaling pathway, leading to enhanced neuronal firing and long-term potentiation (LTP) in the hippocampal CA1 region. GSK1034702 hydrochloride is valuable for investigating cognitive impairments associated with neurological conditions, such as Alzheimer's disease, and demonstrates pro-cognitive effects in animal models, especially relevant in studies of nicotine withdrawal-induced cognitive dysfunction. Potential side effects related to peripheral M receptor activation, such as gastrointestinal reactions, should be considered in research applications. -
mAChR Antagonist
Oxyphencyclimine is an orally active antagonist of muscarinic acetylcholine receptors (mAChR). This compound is demonstrated to reduce ulceration index and enhance pepsin activity in rat models of gastric ulcers. Oxyphencyclimine is suitable for investigation in studies related to peptic ulcer disease and gastrointestinal spasms, providing a valuable tool for understanding these conditions. -
M Cholinergic Receptor Antagonist
Petiline is a steroidal alkaloid that serves as a selective antagonist of M cholinergic receptors. By competitively inhibiting these receptors, Petiline demonstrates significant anticholinergic effects, including a reduction in vagal influence on cardiac function. Additionally, it exhibits central excitatory, cardiotonic, and spasmolytic activities, making it a valuable tool for investigating cholinergic system-related disorders such as arrhythmias and intestinal spasms. -
Muscarinic Receptor Agonist
Milameline is a nonselective, partial agonist of muscarinic receptors, demonstrating significant potential in cognitive enhancement. It exhibits balanced affinity across various human muscarinic receptor subtypes, with IC50 values of approximately 1.3 µM for M1, 1.1 µM for M2, 1.5 µM for M3, and 1.9 µM for M4 receptors. In addition to its central and peripheral cholinergic effects, Milameline counteracts cognitive deficits induced by Scopolamine. This compound is valuable for researching Alzheimer's Disease and other cognitive disorders. -
mAChR Antagonist
Atropine hydrobromide is a competitive antagonist of muscarinic acetylcholine receptors (mAChRs), demonstrating IC50 values of 0.39 nM and 0.71 nM for human mAChR M4 and chicken mAChR M4, respectively. It effectively inhibits acetylcholine-induced relaxations in human pulmonary veins. This compound is valuable for research applications related to anti-myopia and the treatment of bradycardia. -
Muscarinic Receptor Antagonist
Biperiden lactate is a non-selective muscarinic receptor antagonist that competitively interacts with M1 muscarinic receptors. This compound inhibits acetylcholine activity, thus enhancing dopamine signaling within the central nervous system. Biperiden lactate is particularly useful for research into Parkinson's disease and related psychiatric disorders, providing insights into therapeutic strategies aimed at managing these conditions. -
Detrusor Muscle Contraction Inhibitor
FK 584 is a potent detrusor muscle contraction inhibitor that primarily exhibits antimuscarinic activity alongside weak calcium channel blocking properties. This compound has shown significant efficacy in inhibiting detrusor muscle contractions across various experimental models, making it a valuable tool for research on overactive bladder (OAB). FK 584 presents a manageable risk of mydriasis, enabling detailed exploration of its therapeutic potential in bladder function studies. -
Anticholinergic Agent
(R,R)-Glycopyrrolate is an anticholinergic agent that selectively inhibits the action of acetylcholine on muscarinic receptors. This compound is primarily utilized for its efficacy in reducing excessive salivation, particularly in individuals with developmental disabilities. Its application extends to various research contexts, including the assessment of cholinergic modulation in neurological studies. -
M1/M2 Receptor Agonist
Lu 26-046 is a selective agonist for the muscarinic M1 and M2 receptors, with reported affinities (Ki values) of 0.51 nM and 26 nM, respectively, while exhibiting weak antagonistic activity at the M3 receptor (Ki 5 nM). This compound demonstrates a specific stimulating effect that has been recognized in behavioral assays with rats. Lu 26-046 serves as a valuable tool in research investigating cholinergic signaling pathways and receptor subtype functions. -
AChE/mAChR Antagonist
CI-1002, a potent antagonist of acetylcholinesterase (AChE) and muscarinic acetylcholine receptors (mAChR), is utilized in neuroscience research. Its ability to inhibit AChE activity makes it particularly valuable for investigating the underlying mechanisms of cognitive dysfunction associated with Alzheimer’s disease. CI-1002 serves as a crucial tool for studying neurodegenerative processes and potential therapeutic strategies. -
M1 Muscarinic Receptor Agonist
Nebracetam is an orally active agonist of the M1 muscarinic receptor, known for its ability to increase intracellular Ca2+ concentration, demonstrated with an EC50 value of 1.59 mM. This compound exhibits neuroprotective properties and has been shown to improve cognitive impairment. Nebracetam is applicable in research focused on neurological conditions, including Alzheimer's disease, making it a valuable tool for understanding and developing potential therapeutic strategies. -
Muscarinic Antagonist
Caramiphen hydrochloride is a muscarinic antagonist that exhibits anticonvulsant properties. It provides partial protection against seizures and neuropathological effects induced by Soman exposure. This compound is valuable for research focused on exploring therapeutic strategies for seizure disorders and understanding the underlying mechanisms of muscarinic receptor modulation. -
mAChR Antagonist
AF-DX 384 methanesulfonate is a selective antagonist of M2 and M4 muscarinic acetylcholine receptors, with inhibitory constants of 6.03 nM and 10 nM, respectively. This compound has demonstrated the ability to reverse cognitive deficits in novel object recognition and passive avoidance assays in both aged rats and young rats subjected to scopolamine-induced impairments. It serves as a valuable tool in neuroscientific research focused on memory and learning processes. -
Antiarrhythmic Agent
Pirmenol is an orally active antiarrhythmic agent that primarily targets the muscarinic acetylcholine receptor (mAChR), leading to the inhibition of the I(K.ACh) current (IC50: 0.1 μM). It demonstrates significant antiarrhythmic properties, making it valuable for investigating cardiovascular disorders, particularly atrial fibrillation. Pirmenol serves as a useful tool for research aimed at understanding and developing treatments for cardiac arrhythmias.
