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 201-225 of 399

  • Velufenacin
    Cat. No.
    A61342

    Velufenacin

    Synonyms: DA-8010

    Velufenacin is a muscarinic receptor antagonist that selectively blocks the activity of muscarinic acetylcholine receptors. This compound demonstrates significant biological activity in various in vitro and in vivo models, making it a valuable tool for studying the role of cholinergic signaling in physiological processes. Velufenacin is applicable in research focused on neurological disorders, respiratory conditions, and other diseases where modulation of the muscarinic receptor pathway is critical.

    1 mg
    $35.00
    5 mg
    $85.00
    All 7 sizes
  • NGX-267
    Cat. No.
    A61343

    NGX-267

    Synonyms: AF-267B

    NGX-267 is a selective agonist of the actin M1 receptor, demonstrating high selectivity among the five actin receptor subtypes, particularly favoring M1 over M3. This compound exhibits distinct affinity profiles for dopamine D2 and 5-HT2B receptors, highlighting its unique pharmacological properties. NGX-267 is valuable for research applications focused on actin receptor modulation and its implications in cellular dynamics and neurobiology.

    5 mg
    $350.00
    10 mg
    $540.00
    All 5 sizes
  • Terodiline hydrochloride
    Cat. No.
    A61344

    Terodiline hydrochloride

    Terodiline hydrochloride is an M1-selective muscarinic acetylcholine receptor (mAChR) antagonist, exhibiting binding affinities of 15 nM for M1, 160 nM for M2, and 280 nM for M3 receptors, with further action as a calcium channel blocker. This compound is primarily used in the treatment of urinary frequency and urge incontinence. Its ability to selectively inhibit specific mAChR subtypes makes it a valuable reagent for investigating the pharmacological modulation of urinary tract function.

    5 mg
    $350.00
    25 mg
    $1,025.00
    All 4 sizes
  • VU10010
    Cat. No.
    A61345

    VU10010

    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.

    2 mg
    $25.00
    5 mg
    $40.00
    All 7 sizes
  • Smilagenin acetate
    Cat. No.
    A61346

    Smilagenin acetate

    Smilagenin acetate is a sapogenin derivative that targets steroid pathways. It has been shown to enhance the expression of acetylcholine M2 receptors, making it a valuable tool for research into dementia and related neurodegenerative disorders. This compound can facilitate studies aimed at understanding cholinergic signaling and its implications in cognitive function.

    2 mg
    $25.00
    5 mg
    $45.00
    All 7 sizes
  • mAChR antagonist 1
    Cat. No.
    A61347

    mAChR antagonist 1

    mAChR antagonist 1 is a selective antagonist for muscarinic acetylcholine receptors (mAChRs), exhibiting Ki values of 255 nM, 121 nM, 158 nM, and 255 nM for the M1, M3, M4, and M5 subtypes, respectively. This compound is useful for studies investigating the role of mAChR signaling in various physiological and pathological processes. Its application extends to neuropharmacology and drug development, making it a valuable tool for exploring mAChR-related pathways.

    5 mg
    $45.00
    10 mg
    $80.00
    All 6 sizes
  • Oxyphencyclimine hydrochloride
    Cat. No.
    A61348

    Oxyphencyclimine hydrochloride

    Oxyphencyclimine hydrochloride is a tertiary amine that acts as a muscarinic acetylcholine receptor (mAChR) antagonist. It primarily targets the peripheral parasympathetic nervous system, exhibiting key biological activities related to the inhibition of smooth muscle contraction. This compound is utilized in research focused on gastrointestinal motility and the modulation of parasympathetic responses.

    2 mg
    $25.00
    5 mg
    $40.00
    All 6 sizes
  • VU6008055
    Cat. No.
    A61349

    VU6008055

    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.

    5 mg
    $400.00
    10 mg
    $655.00
    All 5 sizes
  • 5-Hydroxytryptophol-O-glucuronide
    Cat. No.
    A61350

    5-Hydroxytryptophol-O-glucuronide

    Synonyms: UGT1A6

    5-Hydroxytryptophol-O-glucuronide is a glucuronide standard utilized as a probe metabolite. It is specifically designed to assess the enzymatic activity of human UGT1A6 in various in vitro systems, including human liver microsomes and recombinant UGT1A6 assays. This compound serves as an essential tool for pharmacokinetic studies and the evaluation of drug metabolism.

    1 mg
    $280.00
    5 mg
    $1,065.00
    All 2 sizes
  • Tigloidin
    Cat. No.
    A61352

    Tigloidin

    Synonyms: Tigloyl pseudotropine; Tiglylpseudotropine; Tiglyssin

    Tigloidin is an antagonist of muscarinic acetylcholine receptors (mAChRs) with notable anticholinergic activity. This compound has potential implications in research related to neuropharmacology and the modulation of cholinergic signaling pathways. Its ability to inhibit mAChR activity makes it a valuable tool for investigating conditions influenced by acetylcholine activity.

    5 mg
    $165.00
    10 mg
    $295.00
    All 5 sizes
  • Fentonium bromide
    Cat. No.
    A61353

    Fentonium bromide

    Fentonium bromide is a neuroprotective agent that functions primarily as an anticholinergic, providing relief from gastrointestinal spasms and peptic ulcer symptoms. Its biological activity makes it a valuable compound for studying neurological disorders, particularly those involving bladder instability and dysfunction. Researchers can utilize Fentonium bromide to explore its therapeutic potential in neuroprotection and related pathways.

    5 mg
    $190.00
    10 mg
    $285.00
    All 5 sizes
  • Nebracetam hydrochloride
    Cat. No.
    A61354

    Nebracetam hydrochloride

    Synonyms: WEB 1881 FU hydrochloride

    Nebracetam hydrochloride is an orally active agonist of the M1 muscarinic receptor. It facilitates an increase in intracellular Ca2+ concentration, characterized by an EC50 value of 1.59 mM. This compound demonstrates neuroprotective properties and has potential to enhance cognitive function, making it relevant for research focused on neurological disorders, including Alzheimer's disease.

    5 mg
    $25.00
    10 mg
    $40.00
    All 5 sizes
  • Nitrocaramiphen hydrochloride
    Cat. No.
    A61355

    Nitrocaramiphen hydrochloride

    Nitrocaramiphen hydrochloride is a selective antagonist of the M1 muscarinic acetylcholine receptor, exhibiting a Ki value of 5.5 nM. This compound effectively blocks the hyperpolarizing effects induced by muscarine on muscle fibers, making it a valuable tool for research on cholinergic signaling and receptor pharmacology. Its application extends to studies on neuromuscular transmission and the physiological roles of M1 receptors in various systems.

    5 mg
    $25.00
    10 mg
    $40.00
    All 6 sizes
  • (R)-Oxybutynin hydrochloride
    Cat. No.
    A61356

    (R)-Oxybutynin hydrochloride

    Synonyms: Aroxybutynin hydrochloride

    (R)-Oxybutynin hydrochloride is a muscarinic receptor antagonist exhibiting potent antimuscarinic, antispasmodic, and anticholinergic properties. It effectively competes with Carbachol to inhibit induced contractions, making it valuable for studying neurogenic bladder dysfunction and incontinence. Additionally, (R)-Oxybutynin hydrochloride features an alkyne group that allows for copper-catalyzed azide-alkyne cycloaddition (CuAAc), facilitating research in click chemistry applications.

    5 mg
    $115.00
    10 mg
    $200.00
    All 5 sizes
  • 4-Piperidyl N-(2-biphenyl)carbamate
    Cat. No.
    A61358

    4-Piperidyl N-(2-biphenyl)carbamate

    4-Piperidyl N-(2-biphenyl)carbamate is a competitive antagonist of muscarinic acetylcholine receptors (mAChR), exhibiting notable selectivity for the M2 and M3 subtypes. With pKi values of 7.33 for M2 and 7.51 for M3, this compound demonstrates a markedly higher affinity compared to β2 adrenergic receptors, which has a pKi of 4.94. This specificity makes it a valuable tool for research into mAChR-related signaling pathways and potential therapeutic applications in various neurological disorders.

    1 g
    $20.00
    5 g
    $55.00
    All 4 sizes
  • Bethanechol
    Cat. No.
    A61359

    Bethanechol

    Synonyms: Carbamyl-β-methylcholine

    Bethanechol is a selective agonist for muscarinic acetylcholine receptors (mAChRs), specifically targeting subtypes M1, M2, M3, M4, and M5. This parasympathomimetic compound promotes various parasympathetic responses, making it valuable in studies related to gastrointestinal motility, urinary retention, and other conditions influenced by parasympathetic activation. Research applications include evaluating the physiological effects of mAChR stimulation and investigating therapeutic strategies for disorders involving cholinergic transmission.

    Out of stock

    All 3 sizes
  • Nuvenzepine
    Cat. No.
    A61360

    Nuvenzepine

    Nuvenzepine is an mAChR antagonist that demonstrates potential therapeutic applications in the treatment of gastrospasm. By selectively inhibiting muscarinic acetylcholine receptors, Nuvenzepine may help alleviate symptoms associated with gastrointestinal motility disorders. This compound is of particular interest in pharmacological research focused on gastrointestinal therapies.

    1 mg
    $145.00
    5 mg
    $395.00
    All 6 sizes
  • Oxitropium Bromide
    Cat. No.
    A61361

    Oxitropium Bromide

    Oxitropium Bromide is a muscarinic acetylcholine receptor (mAChR) antagonist that serves as an effective anticholinergic bronchodilator. It is primarily utilized in the management of asthma and chronic obstructive pulmonary disease (COPD), where it helps alleviate bronchoconstriction and improve airflow. This compound is essential for research focused on respiratory health and the development of treatments for airway obstructive disorders.

    Out of stock

    All 3 sizes
  • VU6036864
    Cat. No.
    A61362

    VU6036864

    VU6036864 is a selective antagonist of the M5 muscarinic acetylcholine receptor (mAChR) with an IC50 of 20 nM for human M5. This compound exhibits over 500-fold selectivity against human M1-4 receptors, making it a valuable tool for studying M5 receptor functions in both in vitro and in vivo settings. VU6036864 is characterized by its ability to penetrate the blood-brain barrier and demonstrate high oral bioavailability, providing a promising avenue for research in neuropharmacology and related fields.

    Out of stock

    All 3 sizes
  • Direclidine
    Cat. No.
    A61363

    Direclidine

    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.

    5 mg
    $1,105.00
    10 mg
    $1,595.00
    All 5 sizes
  • (R)-Oxybutynin
    Cat. No.
    A61364

    (R)-Oxybutynin

    Synonyms: Aroxybutynin

    (R)-Oxybutynin is a potent muscarinic receptor antagonist employed in the investigation of neurogenic bladder dysfunction. This compound exhibits antispasmodic, antimuscarinic, and anticholinergic properties, effectively inhibiting carbachol-induced contractions. It serves as a valuable tool for studying urinary incontinence and related conditions.

    25 mg
    $1,800.00
    50 mg
    $2,285.00
    All 3 sizes
  • Arecoline hydrochloride
    Cat. No.
    A61365

    Arecoline hydrochloride

    Arecoline hydrochloride is a partial agonist of nicotinic and muscarinic acetylcholine receptors (nAChR/mAChR). This psychoactive alkaloid demonstrates stimulation, increased alertness, anxiolytic effects, and possesses anti-parasitic properties. Additionally, Arecoline hydrochloride can induce oxidative stress, making it a valuable compound for research in neuropharmacology and parasitology.

    Out of stock

    All 3 sizes
  • VU6021625
    Cat. No.
    A61366

    VU6021625

    VU6021625 is a selective antagonist of the M4 muscarinic acetylcholine receptor (mAChR), exhibiting an IC50 of 0.44 nM for human M4 and 57 nM for rat M4. This compound is valuable for studies exploring the role of M4 receptors in neurological processes and potential therapeutic targets for neurodegenerative diseases. Its selectivity and potency make it an important tool for researchers investigating cholinergic signaling pathways.

    Out of stock

    All 3 sizes
  • Penehyclidine
    Cat. No.
    A61367

    Penehyclidine

    Penehyclidine is an anticholinergic agent that selectively antagonizes M1 and M3 receptors. This compound is known to activate NF-kB in lung tissue, leading to the inhibition of inflammatory factor release. Penehyclidine demonstrates potential in alleviating pulmonary inflammatory responses, particularly in models of chronic obstructive pulmonary disease (COPD) during mechanical ventilation. Its mechanistic action supports further research in respiratory disorders and inflammatory conditions.

    25 mg
    $1,275.00
    All 1 sizes
  • (Rac)-5-Hydroxymethyl Tolterodine-d14
    Cat. No.
    A61368

    (Rac)-5-Hydroxymethyl Tolterodine-d14

    Synonyms: (Rac)-Desfesoterodine-d14; (Rac)-PNU-200577-d14

    (Rac)-5-Hydroxymethyl Tolterodine-d14 is a deuterium-labeled derivative of (Rac)-5-Hydroxymethyl Tolterodine, a potent muscarinic acetylcholine receptor (mAChR) antagonist. It exhibits high affinity with Ki values of 2.3 nM, 2 nM, 2.5 nM, 2.8 nM, and 2.9 nM for M1, M2, M3, M4, and M5 receptors, respectively. This stable isotope is instrumental in studies related to overactive bladder syndrome and facilitates pharmacokinetic research by enabling sensitive detection and quantification in biological samples.

    Out of stock

    All 3 sizes

Items 201-225 of 399

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