mAChR

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:

  • M1 Receptors: Predominantly found in the central nervous system, particularly in regions associated with cognitive functions. Activation of M1 receptors is linked to memory and learning.
  • M2 Receptors: Found in the heart, where they play a crucial role in regulating heart rate and cardiac contractility. Activation of M2 receptors slows heart rate and reduces the force of cardiac contractions.
  • M3 Receptors: Present in smooth muscle tissues, such as those in the gastrointestinal tract, urinary bladder, and bronchial airways. Activation of M3 receptors leads to smooth muscle contraction.
  • M4 Receptors: Distributed mainly in the central nervous system and involved in modulating neurotransmitter release. Their role in cognition and neuropsychiatric disorders is of interest.
  • M5 Receptors: Located in certain areas of the brain and implicated in the modulation of dopamine release. Research suggests they may be relevant to Parkinson's disease and addiction.

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.

Items 151-175 of 399

  • ML375
    Cat. No.
    A61286

    ML375

    Synonyms: VU0483253

    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.

    5 mg
    $90.00
    10 mg
    $155.00
    All 5 sizes
  • PD 102807
    Cat. No.
    A61288

    PD 102807

    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.

    1 mg
    $40.00
    5 mg
    $100.00
    All 6 sizes
  • ASP8302
    Cat. No.
    A61289

    ASP8302

    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.

    1 mg
    $290.00
    5 mg
    $755.00
    All 6 sizes
  • PQCA
    Cat. No.
    A61290

    PQCA

    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.

    1 mg
    $40.00
    5 mg
    $95.00
    All 6 sizes
  • VU0467319
    Cat. No.
    A61291

    VU0467319

    Synonyms: VU319

    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.

    5 mg
    $90.00
    10 mg
    $150.00
    All 5 sizes
  • Sofpironium bromide
    Cat. No.
    A61292

    Sofpironium bromide

    Synonyms: BBI 4000

    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.

    1 mg
    $55.00
    5 mg
    $135.00
    All 7 sizes
  • Fesoterodine
    Cat. No.
    A61293

    Fesoterodine

    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.

    5 mg
    $40.00
    10 mg
    $65.00
    All 5 sizes
  • rel-VU6021625
    Cat. No.
    A61294

    rel-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.

    5 mg
    $415.00
    10 mg
    $635.00
    All 3 sizes
  • VU0238441
    Cat. No.
    A61296

    VU0238441

    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.

    5 mg
    $20.00
    10 mg
    $25.00
    All 5 sizes
  • ML380
    Cat. No.
    A61297

    ML380

    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.

    2 mg
    $35.00
    5 mg
    $55.00
    All 7 sizes
  • ML381
    Cat. No.
    A61299

    ML381

    Synonyms: VU0488130

    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.

    1 mg
    $75.00
    5 mg
    $185.00
    All 6 sizes
  • Ipratropium bromide hydrate
    Cat. No.
    A61300

    Ipratropium bromide hydrate

    Synonyms: Sch 1000 bromide hydrate

    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.

    50 mg
    $20.00
    100 mg
    $25.00
    All 4 sizes
  • Tiotropium bromide monohydrate
    Cat. No.
    A61301

    Tiotropium bromide monohydrate

    Synonyms: BA-679 BR monohydrate

    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.

    25 mg
    $30.00
    50 mg
    $45.00
    All 4 sizes
  • VU6028418
    Cat. No.
    A61302

    VU6028418

    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.

    5 mg
    $475.00
    10 mg
    $880.00
    All 5 sizes
  • Oxyphenonium bromide
    Cat. No.
    A61303

    Oxyphenonium bromide

    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.

    10 mg
    $35.00
    25 mg
    $50.00
    All 4 sizes
  • VU0119498
    Cat. No.
    A61304

    VU0119498

    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.

    5 mg
    $20.00
    10 mg
    $25.00
    All 6 sizes
  • Cyclopentolate hydrochloride
    Cat. No.
    A61305

    Cyclopentolate hydrochloride

    Synonyms: DL-Cyclopentolate hydrochloride

    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.

    5 mg
    $20.00
    10 mg
    $35.00
    All 5 sizes
  • Arborine
    Cat. No.
    A61306

    Arborine

    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.

    1 mg
    $25.00
    5 mg
    $65.00
    All 5 sizes
  • (±)-Darifenacin
    Cat. No.
    A61307

    (±)-Darifenacin ((±)-UK-88525)

    Synonyms: (±)-UK-88525

    (±)-Darifenacin is a selective antagonist of the M3 muscarinic acetylcholine receptor (mAChR), functioning primarily by inhibiting receptor activation. This compound demonstrates potent activity in modulating smooth muscle contraction and glandular secretion, making it particularly useful for research in gastrointestinal disorders and urinary incontinence. Applications include studies on the mechanism of muscarinic receptor signaling and the development of therapeutic strategies targeting mAChR-related conditions.

    5 mg
    $35.00
    10 mg
    $55.00
    All 5 sizes
  • M4 mAChR agonist-1
    Cat. No.
    A61309

    M4 mAChR agonist-1

    M4 mAChR agonist-1 is a selective agonist targeting the M4 muscarinic acetylcholine receptor. This compound exhibits potent activation of the M4 receptor with an EC50 greater than 10 μM in human cell systems. It is valuable for research applications focused on studying cholinergic signaling and neuropharmacology.

    2 mg
    $30.00
    5 mg
    $50.00
    All 7 sizes
  • Pentoxyverine
    Cat. No.
    A61310

    Pentoxyverine

    Synonyms: Carbetapentane

    Pentoxyverine is an orally active sigma-1 receptor agonist, exhibiting affinity with Kis of 41 nM for σ1, 894 nM for σ2, and 75 nM for guinea-pig brain membran σ1. This compound acts as a muscarinic antagonist and demonstrates significant biological activities, including antitussive, anticonvulsant, and spasmolytic effects. Pentoxyverine is utilized in research for its potential to inhibit bronchial interceptors, diminish the cough reflex, induce relaxation of bronchial smooth muscle, and reduce airway resistance in various pulmonary conditions.

    5 mg
    $25.00
    10 mg
    $35.00
    All 6 sizes
  • LY593093
    Cat. No.
    A61311

    LY593093

    LY593093 is a selective agonist of the muscarinic M1 receptor, demonstrating an EC50 of 22.8 nM. This compound is orally active and effectively penetrates the blood-brain barrier, making it a valuable tool for investigating mechanisms underlying Alzheimer's disease. Its selectivity for the muscarinic M1 receptor positions LY593093 as a promising reagent for research in neurodegenerative disorders.

    5 mg
    $985.00
    10 mg
    $1,510.00
    All 5 sizes
  • Zamifenacin fumarate
    Cat. No.
    A61312

    Zamifenacin fumarate

    Synonyms: UK-76654 fumarate

    Zamifenacin fumarate is a potent antagonist of the muscarinic M3 receptor, primarily targeting the gastrointestinal system. It demonstrates significant efficacy in reducing colonic motility, making it relevant for research in conditions such as irritable bowel syndrome. This compound is essential for studies exploring gut motility modulation and the pharmacological mechanisms underlying gastrointestinal disorders.

    2 mg
    $25.00
    5 mg
    $40.00
    All 7 sizes
  • VU0467485
    Cat. No.
    A61313

    VU0467485

    Synonyms: AZ13713945

    VU0467485 is a potent and selective positive allosteric modulator of the muscarinic acetylcholine receptor 4 (M4). It enhances acetylcholine activity at M4 receptors, exhibiting EC50 values of 26.6 nM in rat and 78.8 nM in human systems. VU0467485 shows high selectivity for M4 over the other muscarinic receptor subtypes (M1, M2, M3, and M5) in both human and rat samples. This compound also demonstrates moderate to high central nervous system penetration and possesses antipsychotic-like properties, making it a valuable tool for the study of neurological disorders.

    1 mg
    $35.00
    5 mg
    $80.00
    All 6 sizes
  • Cycrimine
    Cat. No.
    A61314

    Cycrimine

    Cycrimine is an orally active antagonist of the muscarinic acetylcholine receptor M1, effectively inhibiting acetylcholine levels in models of Parkinson's disease. Its antispasmodic properties make Cycrimine a valuable tool for research in behavioral and mental disorders, providing insights into cholinergic signaling pathways. This compound is suitable for studies aimed at understanding the role of mAChRs in neurodegenerative conditions and related therapeutic interventions.

    1 mg
    $130.00
    5 mg
    $310.00
    All 6 sizes

Items 151-175 of 399

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