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 326-350 of 399

  • Phenglutarimid
    Cat. No.
    A61482

    Phenglutarimid

    Synonyms: Ciba 10870; Phenglutarimide

    Phenglutarimid is a muscarinic acetylcholine receptor (mAChR) inhibitor that exhibits anticholinergic properties. It is primarily utilized in research related to Parkinson's disease and other cholinergic dysfunctions. Its ability to modulate neurotransmitter activity makes it a valuable tool for investigating the therapeutic mechanisms underlying movement disorders.

    25 mg
    $1,405.00
    50 mg
    $1,790.00
    All 3 sizes
  • M1/M2/M4 muscarinic agonist 1
    Cat. No.
    A61483

    M1/M2/M4 muscarinic agonist 1

    M1/M2/M4 Muscarinic Agonist 1 is a selective agonist targeting muscarinic M4, M1, and M2 receptors, with EC50 values of 6.5 nM, 26 nM, and 210 nM, respectively. This compound facilitates receptor activation, making it valuable in studying cholinergic signaling and its implications in neurological conditions. Research applications include investigations into mental disorders such as schizophrenia and delusions, providing insights into therapeutic approaches for these conditions.

    Out of stock

    All 3 sizes
  • Methantheline bromide
    Cat. No.
    A61484

    Methantheline bromide

    Methantheline bromide is a quaternary ammonium derivative that exhibits anticholinergic activity. It is known to significantly reduce axillary sweat production, making it useful in studies related to hyperhidrosis. Additionally, Methantheline bromide serves as a valuable tool in research investigating intractable peptic ulcers, contributing to the understanding of gastrointestinal disorders.

    25 mg
    $1,275.00
    50 mg
    $1,625.00
    All 3 sizes
  • M3 mAChR agonist 1
    Cat. No.
    A61485

    M3 mAChR agonist 1

    M3 mAChR agonist 1 is a positive allosteric modulator (PAM) specifically targeting the M3 and M5 muscarinic acetylcholine receptors. This compound exhibits notable selectivity over other muscarinic subtypes, including M1, M2, and M4. M3 mAChR agonist 1 enhances the contraction of isolated rat bladder strips by modulating M3 receptor activity, thus promoting signaling pathways associated with bladder function. This reagent is suitable for research applications in endocrinology and related fields.

    Out of stock

    All 3 sizes
  • PF-06827443
    Cat. No.
    A61486

    PF-06827443

    PF-06827443 is a selective positive allosteric modulator (PAM) of the M1 muscarinic acetylcholine receptor. This compound exhibits high potency and oral bioavailability while effectively penetrating the central nervous system. PF-06827443 has been shown to enhance cholinergic signaling, leading to cholinergic adverse effects and convulsions. It is a valuable tool for researchers investigating M1 receptor functions and their roles in neurological conditions.

    Out of stock

    All 3 sizes
  • VU0090157
    Cat. No.
    A61487

    VU0090157

    VU0090157 is a positive allosteric modulator of the M1 muscarinic acetylcholine receptor (mAChR). By binding to an allosteric site, VU0090157 enhances the affinity of acetylcholine, thereby influencing neurotransmission. This compound is valuable for research in neuropsychiatric disorders such as schizophrenia and Alzheimer's disease, facilitating the exploration of therapeutic strategies that target mAChRs.

    25 mg
    $1,275.00
    50 mg
    $1,625.00
    All 3 sizes
  • PSD-506
    Cat. No.
    A61488

    PSD-506

    Synonyms: RO 3202904

    PSD-506 is a muscarinic M2/M3 antagonist that effectively inhibits the activity of these receptors. This compound demonstrates notable potential in researching bladder overactivity and urinary incontinence. Its specific targeting of M2 and M3 receptors makes PSD-506 a valuable tool for studying related therapeutic avenues and advancing understanding of related physiological mechanisms.

    25 mg
    $1,655.00
    50 mg
    $2,115.00
    All 3 sizes
  • Butropium bromide
    Cat. No.
    A61489

    Butropium bromide

    Butropium bromide is a competitive antagonist of muscarinic acetylcholine receptors (mAChRs). It effectively inhibits acetylcholine-induced glandular secretion and smooth muscle contraction, thereby reducing salivary gland secretion and alleviating respiratory smooth muscle spasms. This compound is valuable for studying conditions related to excessive salivation and could aid in research on respiratory function modulation.

    Out of stock

    All 3 sizes
  • Ethybenztropine hydrochloride
    Cat. No.
    A61490

    Ethybenztropine hydrochloride

    Synonyms: Ponalid hydrochloride; UK 738 hydrochloride

    Ethybenztropine hydrochloride is a potent muscarinic receptor blocker with established anticholinergic properties. This compound demonstrates significant antiparkinsonian activity, effectively improving motor symptoms in patients with Parkinson's disease. Additionally, Ethybenztropine hydrochloride may exhibit dopamine reuptake inhibitory effects, contributing to its therapeutic efficacy. It is utilized in research applications focused on neuropharmacology and the modulation of neurotransmitter balance.

    25 mg
    $1,275.00
    50 mg
    $1,625.00
    All 3 sizes
  • Imidafenacin hydrochloride
    Cat. No.
    A61493

    Imidafenacin hydrochloride

    Synonyms: KRP-197 (hydrochloride); ONO-8025 (hydrochloride)

    Imidafenacin hydrochloride is an orally active inhibitor of muscarinic M1 and M3 receptors. It effectively inhibits bladder contraction in vivo, demonstrating significant antidiuretic effects through the enhancement of vasopressin signaling. This compound is particularly relevant for research focused on overactive bladder and related conditions, making it a valuable tool in the study of urinary disorders.

    Out of stock

    All 3 sizes
  • PF-06764427
    Cat. No.
    A61494

    PF-06764427

    PF-06764427 is a selective positive allosteric modulator of the M1 muscarinic acetylcholine receptor. It demonstrates significant agonist activity at the M1 receptor, enhancing cholinergic signaling. This compound is valuable for research applications pertaining to Alzheimer's disease and schizophrenia, providing insights into cognitive function and neuropharmacology.

    Out of stock

    All 3 sizes
  • Methacholine bromide
    Cat. No.
    A61495

    Methacholine bromide

    Synonyms: Acetyl-β-methylcholine bromide

    Methacholine bromide is a potent agonist of the muscarinic-3 (M3) receptor. Its primary action induces bronchoconstriction by directly stimulating acetylcholine receptors on smooth muscle, resulting in airway narrowing. This compound is particularly sensitive for identifying bronchial hyperresponsiveness (BHR) and is utilized in clinical settings to assess airway hyperresponsiveness (AHR) in patients presenting with asthma-like symptoms, especially those with normal resting expiratory flow rates.

    25 mg
    $1,800.00
    50 mg
    $2,285.00
    All 3 sizes
  • Betovumeline
    Cat. No.
    A61496

    Betovumeline

    Betovumeline is a selective agonist for muscarinic acetylcholine receptors (mAChRs). This compound plays a key role in modulating cholinergic signaling and demonstrates potential biological activity in various neurological disorders. It is widely utilized in research applications focused on understanding the mechanisms underlying cognitive function and neurodegenerative diseases.

    Out of stock

    All 3 sizes
  • VU0455691
    Cat. No.
    A61497

    VU0455691

    VU0455691 is a selective orthosteric antagonist of the M1 muscarinic acetylcholine receptor (mAChR) with a pIC50 of 6.64 and an IC50 of 0.23 µM for human M1. This compound is useful in investigating the physiological and pathological roles of M1 mAChR in various neurological disorders. Its ability to selectively inhibit M1 mAChR activation makes it a valuable tool for research into cholinergic signaling pathways and potential therapeutic interventions.

    25 mg
    $1,275.00
    50 mg
    $1,625.00
    All 3 sizes
  • Mazaticol
    Cat. No.
    A61498

    Mazaticol

    Mazaticol is an anticholinergic agent targeting muscarinic acetylcholine receptors. It effectively blocks cholinergic nerve activity and serves as a potent inhibitor of 3H-QNB and 3H-PZ binding, demonstrating high affinity for M2 receptors. Additionally, Mazaticol exhibits inhibitory effects on dopamine uptake in striatal nerve terminals, making it valuable for research into parkinsonian syndromes.

    25 mg
    $1,800.00
    50 mg
    $2,285.00
    All 3 sizes
  • UH-AH 37
    Cat. No.
    A61500

    UH-AH 37

    UH-AH 37 is a selective antagonist of muscarinic acetylcholine receptors (mAChR). It demonstrates enhanced potency in inhibiting muscarinic responses in intestinal tissue compared to cardiac tissue. This compound is valuable for research into gastrointestinal motility disorders and the pharmacological modulation of mAChR signaling pathways.

    25 mg
    $1,275.00
    50 mg
    $1,625.00
    All 3 sizes
  • VU6008677
    Cat. No.
    A61501

    VU6008677

    VU6008677 is a positive allosteric modulator of the M4 muscarinic acetylcholine receptor, with an EC50 value of 120 nM for hM4. This compound enhances receptor activity and is valuable for studying M4 receptor functions and related signaling pathways. Additionally, VU6008677 demonstrates inhibition of cytochrome P450 and possesses favorable pharmacokinetic properties in rat models, making it suitable for in vivo research applications.

    25 mg
    $1,275.00
    50 mg
    $1,625.00
    All 3 sizes
  • Flutropium bromide
    Cat. No.
    A61502

    Flutropium bromide

    Synonyms: Ba 598Br; Flubron

    Flutropium bromide is a potent bronchospasmolytic agent that exerts its effects through anticholinergic action. It is effective in suppressing bronchospasms and is primarily utilized in research related to asthma and chronic obstructive pulmonary disease (COPD). This compound provides valuable insights into respiratory mechanisms and potential therapeutic interventions for obstructive airway disorders.

    Out of stock

    All 3 sizes
  • SM-21 maleate
    Cat. No.
    A61503

    SM-21 maleate

    SM-21 maleate serves as a presynaptic cholinergic modulator and binds to central muscarinic receptors with an affinity of 0.174 μM. This compound exhibits significant biological activity related to cholinergic signaling, making it a valuable tool for studying synaptic transmission and neuropharmacology. Its application in research may provide insights into cholinergic dysfunctions and potential therapeutic targets for neurological disorders.

    5 mg
    $220.00
    10 mg
    $365.00
    All 3 sizes
  • Cyclobuxine D
    Cat. No.
    A61504

    Cyclobuxine D

    Cyclobuxine D is a steroidal alkaloid that functions as a muscarinic acetylcholine receptor (mAChR) inhibitor. It exhibits a notable bradycardic effect in rat models and effectively inhibits contractions induced by acetylcholine and Ba++ in isolated rabbit jejunum muscle. Due to its biological activities, Cyclobuxine D is valuable for research in pharmacology and cardiovascular studies.

    Out of stock

    All 3 sizes
  • Tolterodine-d14 hydrochloride
    Cat. No.
    A61506

    Tolterodine-d14 hydrochloride

    Synonyms: (R)-(+)-Tolterodine-d14 hydrochloride; (+)-Tolterodine-d14 hydrochloride; (R)-Tolterodine-d14 hydrochloride; PNU-200583-d14 hydrochloride

    Tolterodine-d14 hydrochloride is a deuterium-labeled version of Tolterodine hydrochloride, a potent muscarinic acetylcholine receptor (mAChR) inhibitor. This compound competitively binds to acetylcholine, thereby reducing involuntary bladder muscle contractions and modulating sympathetic nervous activity. In addition to its role in managing overactive bladder and urinary tract infections, Tolterodine has been shown to restore the Nrf2/NF-κB signaling pathway, offering protective effects against inflammation and ferroptosis. Its applications extend to studies involving reactive oxygen species and lipid oxidation.

    1 mg
    $335.00
    All 1 sizes
  • Muscarinic M1 receptor agonist-1
    Cat. No.
    A61507

    Muscarinic M1 receptor agonist-1

    Muscarinic M1 receptor agonist-1 is a selective agonist targeting the muscarinic M1 receptor. This compound plays a significant role in modulating neurotransmission and is of particular interest in the study of psychiatric disorders, including schizophrenia. Its ability to activate the M1 receptor may provide insights into therapeutic strategies for managing cognitive dysfunction associated with these conditions.

    Out of stock

    All 3 sizes
  • DAU 5884
    Cat. No.
    A61510

    DAU 5884

    DAU 5884 is a selective antagonist of muscarinic acetylcholine receptors (mAChRs), with particular potency towards the M1 receptor subtype while exhibiting discrimination between M4 and M2 subtypes. This compound demonstrates significant biological activity in modulating signaling pathways associated with mAChR, making it a valuable tool for research in neuropharmacology and potential therapeutic applications in disorders related to cholinergic signaling. Functional assays and radioligand binding studies characterize its subtype specificity and efficacy.

    25 mg
    $1,275.00
    50 mg
    $1,625.00
    All 3 sizes
  • KTX-005
    Cat. No.
    A61511

    KTX-005

    KTX-005 is a selective agonist of the muscarinic acetylcholine receptor (mAChR), which modulates the signaling pathways associated with acetylcholine neurotransmission. This compound is primarily utilized in research focused on neuropsychiatric disorders, specifically schizophrenia. KTX-005's effects on mAChR activity make it a valuable tool for studying synaptic transmission and receptor dynamics in neurological contexts.

    Out of stock

    All 3 sizes
  • RLH-033
    Cat. No.
    A61513

    RLH-033

    RLH-033 is a potent and selective ligand for the sigma 1 recognition site. It exhibits high affinity for sigma 1 sites labeled by [3H](+)-pentazocine, demonstrating a Ki value of 50 pM. This compound is valuable for research applications targeting sigma 1 receptor functions, contributing to the understanding of its roles in neuroprotection and various pathophysiological conditions.

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

Items 326-350 of 399

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