Search by product name, CAS, target or catalog number. Press Down Arrow to reach product suggestions, Tab to move between links, and Escape to close suggestions.
Muscarinic acetylcholine receptors (mAChRs) are a class of G protein-coupled receptors (GPCRs) found in the central and peripheral nervous systems, as well as in various other tissues and organs throughout the body. These receptors are named after muscarine, a natural alkaloid compound found in certain mushrooms, which was one of the first substances discovered to activate them.
There are five subtypes of muscarinic receptors, designated as M1 through M5, each with distinct tissue distribution and functions. Here's an overview of their roles:
Muscarinic receptors are activated by the neurotransmitter acetylcholine and play a vital role in regulating a wide range of physiological processes, including heart rate, smooth muscle contraction, glandular secretion, and neurotransmitter release. They are targets for various drugs, including anticholinergic agents, which block their activity, and drugs used to treat conditions like bradycardia and neurodegenerative disorders.
Understanding the functions and regulation of muscarinic acetylcholine receptors is essential for developing therapies that modulate their activity and for advancing our knowledge of how they contribute to various physiological and pathological processes in the body.
PF-06767832 is a selective positive allosteric modulator of the muscarinic M1 receptor, exhibiting an EC50 value of 60 nM. This compound demonstrates favorable penetration into the central nervous system, enhancing M1 receptor signaling. It is primarily used in research focused on neuropharmacology, cognition, and potential treatments for cognitive disorders.
VU6000918 is a positive allosteric modulator of the muscarinic acetylcholine receptor M4, demonstrating an EC50 of 19 nM for human M4. This compound enhances the receptor's activity in response to acetylcholine, making it a valuable tool for studying M4 receptor function. VU6000918 can be utilized in research related to neurological disorders and cognitive functions, providing insights into the therapeutic potential of modulating M4 receptor signaling.
LY 2033298 is a selective positive allosteric modulator of the muscarinic M4 receptor, enhancing the receptor's activity. This compound is valuable for investigating psychiatric disorders and related neurobiological pathways, providing insights into the potential therapeutic mechanisms for disorders associated with M4 receptor dysfunction.
VU6004256 is a potent and selective positive allosteric modulator of the M1 muscarinic receptor, exhibiting an EC50 value of 155 nM. This compound enhances M1 receptor activity and shows promise in addressing cognitive deficits associated with schizophrenia. It is a valuable tool for research into therapeutic strategies targeting muscarinic receptors in neuropsychiatric disorders.
VU0152099 is a selective positive allosteric modulator of the mAChR M4 receptor, exhibiting an EC50 of 0.4 µM for the rat M4 receptor. This compound demonstrates significant brain penetrance and is inactive against other mAChR subtypes and GPCRs. VU0152099 does not possess agonist activity; instead, it enhances the response of M4 to acetylcholine, making it a valuable tool for research into neuropharmacology and the modulation of cholinergic signaling.
Synonyms: ML253
VU0448088 is a potent positive allosteric modulator targeting the M4 muscarinic acetylcholine receptor, demonstrating EC50 values of 56 nM and 176 nM for human and rat receptors, respectively. This tricyclic compound effectively crosses the blood-brain barrier, making it a valuable tool for investigating neuropsychiatric conditions, particularly those related to psychosis. Its ability to enhance M4 receptor activity highlights its potential in research applications focused on neuromodulation and cognitive function.
BAY-2413555 is an orally active modulator of the muscarinic acetylcholine receptor M2, primarily targeting cardiac function. This compound demonstrates protective effects on the heart and enhances cardiac performance, making it a valuable tool for researching heart failure and related cardiovascular conditions. Its unique mechanism may provide insights into therapeutic strategies for managing heart health.
(R)-VU 6008667 acts as a negative allosteric modulator (NAM) of the muscarinic acetylcholine receptor subtype M5. This compound has demonstrated potential in modulating M5 receptor-mediated pathways, which are implicated in various neurological conditions. Its selectivity and pharmacological profile make it a valuable research tool for studying M5 receptor functions and associated signaling mechanisms.
Synonyms: HDMPPA
W-84 dibromide is a potent allosteric modulator of M2 cholinoceptors, effectively retarding the dissociation of [3H]N-methylscopolamine. This compound stabilizes the complexes formed between cholinergic antagonists and receptors, exhibiting non-competitive antagonism at muscarinic acetylcholine receptors. W-84 dibromide demonstrates protective effects against organophosphate intoxication when administered in conjunction with atropine, making it a valuable tool in neuropharmacological research and studies related to cholinergic signaling.
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.
Synonyms: AF98943
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.
Synonyms: NBI-1117568; HTL-0016878
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.
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.
Synonyms: N-Desmethylquazepam
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.
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.
Out of stock
All 3 sizes
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.
Out of stock
All 3 sizes
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.
Out of stock
All 3 sizes
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.
(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.
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.
Out of stock
All 3 sizes
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.
Out of stock
All 3 sizes
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.
Out of stock
All 3 sizes
Synonyms: VU0405652
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.
VU6009048 is a positive allosteric modulator of the M4 muscarinic acetylcholine receptor (mAChR4) that exhibits effective central nervous system penetration. This compound is useful for investigating neurological disorders such as Parkinson's disease, Huntington's disease, and schizophrenia, facilitating the exploration of therapeutic options targeting cholinergic signaling pathways. Its mechanism of action enhances receptor activity, making it a valuable tool for research in neuropharmacology.
Out of stock
All 3 sizes
M3 mAChR agonist 1 is a positive allosteric modulator (PAM) specifically targeting the M3 and M5 muscarinic acetylcholine receptors. This compound exhibits notable selectivity over other muscarinic subtypes, including M1, M2, and M4. M3 mAChR agonist 1 enhances the contraction of isolated rat bladder strips by modulating M3 receptor activity, thus promoting signaling pathways associated with bladder function. This reagent is suitable for research applications in endocrinology and related fields.
Out of stock
All 3 sizes