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 276-300 of 399

  • M1/M2/M4 muscarinic agonist 3
    Cat. No.
    A61428

    M1/M2/M4 muscarinic agonist 3

    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.

    Out of stock

    All 3 sizes
  • GSK1034702 hydrochloride
    Cat. No.
    A61429

    GSK1034702 hydrochloride

    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.

    25 mg
    $1,275.00
    50 mg
    $1,625.00
    All 3 sizes
  • Oxyphencyclimine
    Cat. No.
    A61430

    Oxyphencyclimine

    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.

    25 mg
    $1,275.00
    50 mg
    $1,625.00
    All 3 sizes
  • Petiline
    Cat. No.
    A61431

    Petiline

    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.

    Out of stock

    All 3 sizes
  • Milameline
    Cat. No.
    A61432

    Milameline

    Synonyms: CI-979; RU35926

    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.

    25 mg
    $1,275.00
    50 mg
    $1,625.00
    All 3 sizes
  • Atropine hydrobromide
    Cat. No.
    A61433

    Atropine hydrobromide

    Synonyms: Tropine tropate hydrobromide; DL-Hyoscyamine hydrobromide

    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.

    25 mg
    $1,275.00
    50 mg
    $1,625.00
    All 3 sizes
  • Biperiden lactate
    Cat. No.
    A61434

    Biperiden lactate

    Synonyms: KL 373 lactate

    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.

    25 mg
    $1,275.00
    50 mg
    $1,625.00
    All 3 sizes
  • FK 584
    Cat. No.
    A61435

    FK 584

    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.

    Out of stock

    All 3 sizes
  • (R,R)-Glycopyrrolate
    Cat. No.
    A61436

    (R,R)-Glycopyrrolate

    Synonyms: (R,R)-Glycopyrronium bromide; (R,R)-Glycopyrrolate bromide

    (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.

    25 mg
    $1,275.00
    50 mg
    $1,625.00
    All 3 sizes
  • Lu 26-046
    Cat. No.
    A61437

    Lu 26-046

    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.

    25 mg
    $2,035.00
    50 mg
    $2,610.00
    All 3 sizes
  • CI-1002
    Cat. No.
    A61438

    CI-1002

    Synonyms: PD 142676

    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.

    25 mg
    $1,275.00
    50 mg
    $1,625.00
    All 3 sizes
  • Nebracetam
    Cat. No.
    A61439

    Nebracetam

    Synonyms: WEB 1881 FU

    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.

    25 mg
    $1,275.00
    50 mg
    $1,625.00
    All 3 sizes
  • Caramiphen hydrochloride
    Cat. No.
    A61440

    Caramiphen hydrochloride

    Synonyms: Parpanil hydrochloride

    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.

    25 mg
    $1,275.00
    50 mg
    $1,625.00
    All 3 sizes
  • AF-DX 384 methanesulfonate
    Cat. No.
    A61441

    AF-DX 384 methanesulfonate

    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.

    25 mg
    $1,275.00
    50 mg
    $1,625.00
    All 3 sizes
  • Pirmenol
    Cat. No.
    A61442

    Pirmenol

    Synonyms: (±)-Pirmenol; CI-845 free base

    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.

    5 mg
    $20.00
    10 mg
    $30.00
    All 5 sizes
  • LU-25-077
    Cat. No.
    A61443

    LU-25-077

    LU-25-077 is a brain-penetrant N-demethyl metabolite of Lu 25-109, functioning primarily as a partial agonist of the M1 muscarinic acetylcholine receptor while exhibiting antagonistic properties toward M2 and M3 receptors. This compound is valuable for neurological research, enabling the exploration of cholinergic modulation in various pathophysiological conditions. It provides an important tool for studying cognitive processes and potential therapeutic strategies for neurodegenerative disorders.

    Out of stock

    All 3 sizes
  • Tiemonium iodide
    Cat. No.
    A61444

    Tiemonium iodide

    Tiemonium iodide is a muscarinic acetylcholine receptor (mAChR) antagonist that exhibits antispasmodic properties. It is primarily utilized in research related to the nervous system, where it helps investigate the modulation of cholinergic signaling and its effects on smooth muscle contraction. This reagent serves as a valuable tool for understanding the physiological and pharmacological roles of mAChRs in various biological contexts.

    Out of stock

    All 3 sizes
  • (S)-Tolterodine
    Cat. No.
    A61445

    (S)-Tolterodine

    (S)-Tolterodine is a selective muscarinic acetylcholine receptor (mAChR) inhibitor, exhibiting an IC50 value of 588 nM. This compound is primarily used in studies related to bladder overactivity and other cholinergic signaling pathways. Its pharmacological properties make it a valuable tool for investigating the mechanisms of mAChR modulation in both clinical and preclinical research.

    Out of stock

    All 3 sizes
  • Darotropium bromide
    Cat. No.
    A61446

    Darotropium bromide

    Synonyms: GSK233705

    Darotropium bromide is a long-acting muscarinic antagonist that targets muscarinic acetylcholine receptors. Its primary biological activity is the blockade of these receptors, resulting in bronchodilation and reduced airway resistance. This compound is primarily used in research related to chronic obstructive pulmonary disease (COPD), aiding in the investigation of its therapeutic potential and effects on pulmonary function.

    1 mg
    $60.00
    5 mg
    $155.00
    All 7 sizes
  • AC-42
    Cat. No.
    A61447

    AC-42

    AC-42 is a selective allosteric agonist for the M1 muscarinic receptor, exhibiting potent activity with EC50 values of 805 nM for the human wild-type and 220 nM for the Y381A mutant receptor. This compound enhances inositol phosphate (IP) accumulation and calcium mobilization in CHO cells, making it a valuable tool for studying M1 receptor signaling pathways. Its unique mechanism of action facilitates research into neuropharmacology and cognitive function modulation.

    25 mg
    $1,275.00
    50 mg
    $1,625.00
    All 3 sizes
  • M1 ligand 1
    Cat. No.
    A61448

    M1 ligand 1

    M1 ligand 1 is a selective ligand for the muscarinic acetylcholine receptor M1. It is an N-desmethyl derivative of arecoline, designed for use in research applications focused on neurological studies. M1 ligand 1 serves as a potential PET (positron emission tomography) radiotracer, providing insights into receptor activity and distribution in brain imaging studies.

    25 mg
    $1,275.00
    50 mg
    $1,625.00
    All 3 sizes
  • Cyclodrine
    Cat. No.
    A61449

    Cyclodrine

    Cyclodrine is a selective antagonist of muscarinic acetylcholine receptors (mAChR). It exhibits biological activity by inhibiting cholinergic signaling, which has implications in neuropharmacology and the study of various neurological disorders. Research applications include exploring cholinergic system modulation and assessing the role of mAChR in cognitive function and behavior.

    1 mg
    $55.00
    5 mg
    $130.00
    All 7 sizes
  • J 104129 fumarate
    Cat. No.
    A61450

    J 104129 fumarate

    J 104129 fumarate is a selective muscarinic M3 antagonist, demonstrating a Ki value of 4.2 nM for M3 and 490 nM for M2, indicating a high degree of selectivity. This compound effectively antagonizes acetylcholine-induced bronchoconstriction, making it a valuable tool for investigating obstructive airway diseases. Its oral activity and specificity present opportunities for research in pulmonary pharmacology and the treatment of respiratory conditions.

    1 mg
    $160.00
    5 mg
    $410.00
    All 3 sizes
  • Bencycloquidium bromide
    Cat. No.
    A61451

    Bencycloquidium bromide

    Bencycloquidium bromide is a muscarinic M(3) receptor antagonist that functions as an anticholinergic bronchodilator. It shows significant potential in modulating airway smooth muscle tone and can be utilized in research focusing on respiratory conditions such as rhinitis. This compound is valuable for exploring therapeutic strategies aimed at relieving bronchoconstriction and improving airflow in pulmonary studies.

    25 mg
    $3,195.00
    50 mg
    $4,065.00
    All 3 sizes
  • Propiverine
    Cat. No.
    A61452

    Propiverine

    Propiverine is a potent antimuscarinic agent that targets muscarinic receptors in the urinary bladder. By inhibiting cellular calcium influx, it reduces muscle spasms, demonstrating both neurotropic and musculotropic effects on smooth muscle. Propiverine is primarily utilized in research related to overactive bladder (OAB) and offers insights into bladder dysfunction therapies.

    25 mg
    $1,275.00
    50 mg
    $1,625.00
    All 3 sizes

Items 276-300 of 399

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