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 26-50 of 399

  • Arecoline hydrobromide
    Cat. No.
    A11815

    Arecoline hydrobromide

    Synonyms: methyl 1,2,5,6-tetrahydro-1-methyl-3-pyridinecarboxylate hydrobromide

    Arecoline hydrobromide is a partial agonist of nicotinic (nAChR) and muscarinic acetylcholine receptors (mAChR). This naturally occurring psychoactive alkaloid possesses brain-penetrant properties and is known for its stimulation, alertness enhancement, anxiolytic effects, and anti-parasitic activity. Additionally, Arecoline hydrobromide can induce oxidative stress, making it valuable for research in neuropharmacology and related fields.

    100 mg
    $25.00
    200 mg
    $30.00
    All 5 sizes
  • Oxybutynin chloride
    Cat. No.
    A11899

    Oxybutynin chloride

    Oxybutynin chloride is a competitive antagonist of muscarinic acetylcholine receptors (mAChRs), exhibiting binding affinities with Ki values of 14.3 nM and 5.55 nM for [3H]NMS in mouse bladder and cerebral cortex, respectively. It effectively inhibits vascular Kv channels with an IC50 of 11.51 μM, independent of its anticholinergic effects. Oxybutynin chloride is primarily utilized for the management of overactive bladder syndrome (OAB) and alleviating bladder and urinary tract muscle spasms. Additionally, it serves as a click chemistry reagent due to its alkyne functionality, enabling copper-catalyzed azide-alkyne cycloaddition (CuAAc) reactions with azide-containing molecules.

    100 mg
    $25.00
    500 mg
    $45.00
    All 4 sizes
  • Darifenacin
    Cat. No.
    A11987

    Darifenacin

    Darifenacin works by blocking the M3 muscarinic acetylcholine receptor, which is primarily responsible for bladder muscle contractions.

    1 mg
    $25.00
    5 mg
    $55.00
    All 6 sizes
  • Catharanthine sulfate
    Cat. No.
    A12161

    Catharanthine sulfate

    Catharanthine sulfate is a vinblastine-type alkaloid precursor with antitumor activity. It inhibits AChR by ion channel blocking and desensitization.

    25 mg
    $20.00
    50 mg
    $25.00
    All 5 sizes
  • AC260584
    Cat. No.
    A12264

    AC260584

    AC260584 is an M1 muscarinic receptor allosteric agonist with a pEC50 of 7.6.

    1 mg
    $110.00
    5 mg
    $320.00
    All 7 sizes
  • Darenzepine
    Cat. No.
    A12333

    Darenzepine

    Darenzepine is a muscarinic receptor inhibitor extracted from patent US 20170095465 A1.

    1 mg
    $220.00
    5 mg
    $440.00
    All 7 sizes
  • Beperidium iodide
    Cat. No.
    A12382

    Beperidium iodide

    Synonyms: SX 810

    Beperidium iodide shows a competitive antagonistic effect against acetylcholine receptor with a pA2 of 7.93.

    1 mg
    $85.00
    5 mg
    $345.00
    All 6 sizes
  • Smilagenin
    Cat. No.
    A12599

    Smilagenin

    Smilagenin (SMI) is a lipid-soluble small-molecule steroidal sapogenin from Rhizoma anemarrhenae and Radix asparagi widely used in traditional Chinese medicine for treating chronic neurodegeneration diseases.

    2 mg
    $40.00
    5 mg
    $65.00
    All 7 sizes
  • Glycopyrrolate
    Cat. No.
    A12641

    Glycopyrrolate

    Synonyms: Glycopyrrolate bromide; Glycopyrronium bromide

    Glycopyrrolate is a muscarinic competitive antagonist used as an antispasmodic.

    5 mg
    $25.00
    10 mg
    $35.00
    All 7 sizes
  • MK7622
    Cat. No.
    A12835

    MK7622

    MK7622 is a muscarinic M1 receptor positive allosteric modulator.

    2 mg
    $40.00
    5 mg
    $65.00
    All 6 sizes
  • Flavoxate
    Cat. No.
    A12900

    Flavoxate

    Synonyms: BML-278; Urispas; Bladuril; Spasuret; Uronid

    Flavoxate binds and inhibits muscarinic receptors, thereby suppressing the micturition reflex and increases urinary bladder capacity by modifying the micturition center in the brain stem.

    10 mg
    $70.00
    25 mg
    $145.00
    All 3 sizes
  • Arecoline
    Cat. No.
    A13071

    Arecoline

    Arecoline is a cholinergic alkaloid from seeds of the betel nut palm Areca catechu.

    50 mg
    $25.00
    100 mg
    $45.00
    All 3 sizes
  • Xanomeline oxalate
    Cat. No.
    A13685

    Xanomeline oxalate

    Synonyms: LY246708

    Xanomeline oxalate is a potent agonist of muscarinic acetylcholine receptors (EC50 values are 0.3, 92.5, 5, 52, and 42 nM for M1, M2, M3, M4, and M5, respectively).

    5 mg
    $25.00
    10 mg
    $45.00
    All 7 sizes
  • AF-DX 384
    Cat. No.
    A13856

    AF-DX 384

    AF-DX 384 is a drug which acts as a selective antagonist of the muscarinic acetylcholine receptors.

    1 mg
    $75.00
    5 mg
    $200.00
    All 5 sizes
  • Atropine methyl nitrate
    Cat. No.
    A13857

    Atropine methyl nitrate

    Synonyms: Methylatropine nitrate

    Atropine methyl nitrate is a muscarinic acetylcholine receptor (mAChR) antagonist, primarily utilized for its ability to induce pupil dilation (mydriasis) during ophthalmic examinations. This quaternary ammonium derivative is specifically formulated for the treatment of pyloric spasms in infants due to its high polarity, which limits its central nervous system penetration compared to its parent compound, atropine. Research applications include studying cholinergic signaling pathways and exploring therapeutic strategies for gastrointestinal disorders.

    5 mg
    $130.00
    10 mg
    $215.00
    All 5 sizes
  • TBPB
    Cat. No.
    A14205

    TBPB

    TBPB is an allosteric M1 mAChR agonist with EC50 value of 89 nM that regulates amyloid processing and produces antipsychotic-like activity in rats.

    5 mg
    $30.00
    10 mg
    $55.00
    All 6 sizes
  • Diphenidol HCl
    Cat. No.
    A14244

    Diphenidol HCl

    Diphenidol HCl is a potent antagonist of muscarinic M2 and M3 receptor with pKb of 6.72 and 7.02.

    100 mg
    $40.00
    200 mg
    $60.00
    All 4 sizes
  • Peimisine
    Cat. No.
    A14657

    Peimisine

    Synonyms: Ebeiensine

    Peimisine and peiminine production by endophytic fungus Fusarium sp. isolated from Fritillaria unibracteata var. wabensis.

    1 mg
    $30.00
    5 mg
    $75.00
    All 7 sizes
  • Umeclidinium bromide
    Cat. No.
    A15268

    Umeclidinium bromide

    Synonyms: GSK573719A

    Umeclidinium bromide(GSK573719A) is a muscarinic receptor antagonist which is useful in treatment of chronic obstructive pulmonary disease (COPD).

    1 mg
    $25.00
    2 mg
    $40.00
    All 8 sizes
  • Imidafenacin
    Cat. No.
    A15490

    Imidafenacin

    Synonyms: KRP-197; ONO-8025

    Imidafenacin is a potent and selective inhibitor of M3 receptors with Kb of 0.317 nM; less potent for M2 receptors(IC50=4.13 nM).

    10 mg
    $25.00
    25 mg
    $55.00
    All 6 sizes
  • L-Hyoscyamine
    Cat. No.
    A15560

    L-Hyoscyamine

    Synonyms: Hyoscyamine

    L-Hyoscyamine is a potent and competitive antagonist of muscarinic acetylcholine receptors (mAChRs). As a natural tropane alkaloid, it exerts significant biological activity that makes it valuable in pharmacological research. L-Hyoscyamine is utilized in studies investigating the modulation of cholinergic signaling and related therapeutic applications.

    25 mg
    $35.00
    50 mg
    $60.00
    All 3 sizes
  • Revefenacin
    Cat. No.
    A15986

    Revefenacin

    Synonyms: TD4208; GSK1160724

    Revefenacin is potent and selective muscarinic receptor antagonist in development for the treatment of COPD.

    1 mg
    $30.00
    5 mg
    $75.00
    All 7 sizes

Items 26-50 of 399

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