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 176-200 of 399

  • PCS1055
    Cat. No.
    A61315

    PCS1055

    PCS1055 is a selective competitive antagonist of the muscarinic M4 receptor, exhibiting an IC50 of 18.1 nM and a Kd of 5.72 nM. It effectively inhibits radioligand [3H]-NMS binding to the M4 receptor with a Ki of 6.5 nM. Additionally, PCS1055 demonstrates inhibitory activity against acetylcholinesterase (AChE), with IC50 values of 22 nM for electric eel AChE and 120 nM for human AChE. This compound is valuable for research focused on muscarinic receptor signaling and cholinergic modulation.

    5 mg
    $190.00
    10 mg
    $300.00
    All 5 sizes
  • Arecaidine but-2-ynyl ester tosylate
    Cat. No.
    A61316

    Arecaidine but-2-ynyl ester tosylate

    Synonyms: ABET

    Arecaidine but-2-ynyl ester tosylate is a selective agonist of the mAChR M2 receptor, known to induce dose-dependent reductions in mean arterial pressure and heart rate in rodent models. This compound serves as a valuable tool in cardiovascular disease research, elucidating the role of mAChR M2 in cardiac function. Additionally, as a click chemistry reagent, Arecaidine but-2-ynyl ester tosylate contains an alkyne functional group, enabling its application in copper-catalyzed azide-alkyne cycloaddition reactions with azide-containing molecules for further synthetic applications.

    5 mg
    $100.00
    10 mg
    $165.00
    All 5 sizes
  • Zamifenacin
    Cat. No.
    A61317

    Zamifenacin

    Synonyms: UK-76654

    Zamifenacin is a potent antagonist of the muscarinic M3 receptor, demonstrating gut-selective activity. This compound effectively reduces colonic motility, making it a valuable tool in the study of irritable bowel syndrome and related gastrointestinal disorders. Its mechanism of action provides insights into the modulation of gastrointestinal function and potential therapeutic applications in digestive health.

    5 mg
    $80.00
    10 mg
    $125.00
    All 5 sizes
  • Muscarine iodide
    Cat. No.
    A61318

    Muscarine iodide

    Synonyms: (+)-Muscarine iodide

    Muscarine iodide is a potent agonist of the muscarinic acetylcholine receptors (mAChR). It actively stimulates the parasympathetic nervous system, making it a valuable tool in studying cholinergic signaling pathways. This compound is commonly utilized in research focused on neuropharmacology and the physiological effects of muscarinic receptor activation.

    1 mg
    $150.00
    5 mg
    $395.00
    All 3 sizes
  • VU0486846
    Cat. No.
    A61319

    VU0486846

    VU0486846 is a selective positive allosteric modulator of the M1 muscarinic acetylcholine receptor. This compound enhances receptor activity in a manner dependent on the presence of the endogenous ligand. VU0486846 is utilized in research to explore its potential therapeutic effects in cognitive disorders and neurodegenerative diseases. Its oral bioavailability makes it a valuable tool for in vivo studies of M1 modulation.

    1 mg
    $145.00
    5 mg
    $370.00
    All 2 sizes
  • PF-06767832
    Cat. No.
    A61320

    PF-06767832

    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.

    5 mg
    $460.00
    10 mg
    $755.00
    All 5 sizes
  • LASSBio-873
    Cat. No.
    A61321

    LASSBio-873

    LASSBio-873 is a potent muscarinic acetylcholine receptor (mAChR) agonist that effectively crosses the blood-brain barrier. It exhibits significant analgesic properties in models of acute and inflammatory pain. Research indicates that the analgesic effects of LASSBio-873 can be antagonized by the M2 receptor inhibitor methoctramine, making it a valuable tool for studying pain mechanisms and mAChR signaling pathways.

    1 mg
    $45.00
    5 mg
    $105.00
    All 5 sizes
  • VU6000918
    Cat. No.
    A61322

    VU6000918

    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.

    5 mg
    $205.00
    10 mg
    $335.00
    All 5 sizes
  • DAU 5884 hydrochloride
    Cat. No.
    A61323

    DAU 5884 hydrochloride

    DAU 5884 hydrochloride is a potent antagonist of the muscarinic M3 receptor. It effectively inhibits methacholine-induced cellular proliferation and muscle contractility, making it a valuable tool for research into muscarinic signaling pathways and related physiological effects. This compound is useful for studies investigating respiratory physiology and disorders associated with muscarinic receptor activation.

    5 mg
    $260.00
    10 mg
    $425.00
    All 3 sizes
  • L-Hyoscyamine sulfate
    Cat. No.
    A61324

    L-Hyoscyamine sulfate

    Synonyms: Daturine sulfate

    L-Hyoscyamine sulfate is a competitive antagonist of muscarinic acetylcholine receptors (mAChRs). This natural tropane alkaloid demonstrates significant biological activity by inhibiting mAChRs, making it useful in research applications focused on neuropharmacology and the modulation of cholinergic signaling. Its structural similarity to atropine further emphasizes its relevance in studies related to anticholinergic effects and the exploration of receptor interaction mechanisms.

    5 mg
    $25.00
    10 mg
    $40.00
    All 6 sizes
  • LY 2033298
    Cat. No.
    A61325

    LY 2033298

    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.

    1 mg
    $70.00
    5 mg
    $175.00
    All 7 sizes
  • Tridihexethyl chloride
    Cat. No.
    A61326

    Tridihexethyl chloride

    Synonyms: Pathilon chloride

    Tridihexethyl chloride is an anticholinergic agent that acts as a muscarinic acetylcholine receptor (mAChR) antagonist. It exhibits significant antimuscarinic and antisecretory properties, providing pronounced antispasmodic effects on the gastrointestinal system. This compound is valuable for research related to peptic ulcer disease and acquired nystagmus, facilitating studies on gastrointestinal motility and secretion modulation.

    1 mg
    $135.00
    25 mg
    $830.00
    All 4 sizes
  • Thiochrome
    Cat. No.
    A61327

    Thiochrome

    Thiochrome is a selective enhancer of muscarinic acetylcholine receptor subtype M4. As a natural oxidation product and metabolite of thiamine, Thiochrome exhibits neutral cooperativity with acetylcholine at M1 to M3 receptors. This compound is valuable for studying the modulation of cholinergic signaling and its implications in neuropharmacology and therapeutic research.

    2 mg
    $20.00
    5 mg
    $25.00
    All 3 sizes
  • CHF5407
    Cat. No.
    A61328

    CHF5407

    CHF5407 is a selective, competitive antagonist of the muscarinic M3 receptor, exhibiting subnanomolar affinities for human muscarinic receptors M1, M2, and M3. This compound demonstrates prolonged antibronchospastic activity, making it a valuable tool for research into bronchial hyperreactivity and related respiratory conditions. CHF5407 is suitable for studies investigating the role of muscarinic receptors in various biological processes and potential therapeutic applications.

    1 mg
    $120.00
    5 mg
    $255.00
    All 6 sizes
  • Tiotropium-d6 bromide
    Cat. No.
    A61329

    Tiotropium-d6 bromide

    Synonyms: BA679 BR-d6

    Tiotropium-d6 bromide is a deuterium-labeled analogue of Tiotropium, primarily targeting muscarinic acetylcholine receptors (mAChR). As a potent mAChR antagonist, it effectively inhibits the binding of acetylcholine, preventing the activation of ligand-gated ion channels. This reagent is valuable for studies involving receptor binding assays, pharmacokinetics, and metabolic pathway analysis.

    1 mg
    $695.00
    All 1 sizes
  • JHU37152
    Cat. No.
    A61330

    JHU37152

    JHU37152 is a potent agonist for Designer Receptors Exclusively Activated by Designer Drugs (DREADDs), specifically targeting the hM3Dq and hM4Di receptors with EC50 values of 5 nM and 0.5 nM, respectively, in HEK-293 cells. This compound demonstrates selective displacement of [3H]Clozapine from DREADD sites without affecting other Clozapine-binding sites in mouse brain tissue. JHU37152 is valuable for research applications involving neural circuit manipulation and the study of neuropharmacology.

    5 mg
    $20.00
    10 mg
    $25.00
    All 6 sizes
  • Hexocyclium methylsulfate
    Cat. No.
    A61331

    Hexocyclium methylsulfate

    Hexocyclium methylsulfate is a potent antagonist of muscarinic acetylcholine receptors (mAChR), exhibiting pKi values of 8.9, 7.7, 8.4, and 8.8 for the M1, M2, M3, and M4 subtypes, respectively. This compound demonstrates significant biological activity in modulating cholinergic signaling pathways. It is valuable in research applications related to gastrointestinal conditions such as duodenal ulcers and irritable bowel syndrome.

    5 mg
    $140.00
    10 mg
    $225.00
    All 5 sizes
  • VU6004256
    Cat. No.
    A61332

    VU6004256

    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.

    5 mg
    $255.00
    10 mg
    $420.00
    All 5 sizes
  • VU0152099
    Cat. No.
    A61334

    VU0152099

    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.

    5 mg
    $20.00
    10 mg
    $30.00
    All 6 sizes
  • VU0448088
    Cat. No.
    A61335

    VU0448088

    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.

    5 mg
    $90.00
    10 mg
    $145.00
    All 5 sizes
  • Guvacoline hydrobromide
    Cat. No.
    A61337

    Guvacoline hydrobromide

    Guvacoline hydrobromide is a pyridine alkaloid that functions as a full activator of muscarinic receptors. It exhibits biological activity as a weak full agonist of both atrial and ileal muscarinic acetylcholine receptors (mAChR). This compound is valuable for research applications involving cholinergic signaling and receptor pharmacology.

    1 mg
    $30.00
    5 mg
    $105.00
    All 6 sizes
  • BAY-2413555
    Cat. No.
    A61338

    BAY-2413555

    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.

    1 mg
    $155.00
    5 mg
    $280.00
    All 6 sizes
  • (R)-VU 6008667
    Cat. No.
    A61339

    (R)-VU 6008667

    (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.

    5 mg
    $150.00
    10 mg
    $275.00
    All 5 sizes
  • (Rac)-5-Hydroxymethyl Tolterodine hydrochloride
    Cat. No.
    A61340

    (Rac)-5-Hydroxymethyl Tolterodine hydrochloride

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

    (Rac)-5-Hydroxymethyl Tolterodine hydrochloride is an mAChR antagonist, demonstrating Ki values of 2.3 nM, 2.0 nM, 2.5 nM, 2.8 nM, and 2.9 nM for M1, M2, M3, M4, and M5 muscarinic receptors, respectively. This active metabolite of Tolterodine is primarily utilized in research related to overactive bladder conditions. Its selective inhibition of muscarinic acetylcholine receptors provides a valuable tool for investigating bladder dysfunction and potential therapeutic interventions.

    2 mg
    $20.00
    100 mg
    $25.00
    All 4 sizes
  • W-84 dibromide
    Cat. No.
    A61341

    W-84 dibromide

    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.

    2 mg
    $25.00
    5 mg
    $40.00
    All 7 sizes

Items 176-200 of 399

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