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 51-59 of 59

  • 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
  • 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
  • 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
  • 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
  • Dimethyl-W84 dibromide
    Cat. No.
    A61521

    Dimethyl-W84 dibromide

    Dimethyl-W84 dibromide is a modulator of M2 muscarinic acetylcholine receptors. This compound exhibits significant regulatory activity on mAChRs, making it a valuable tool in the study of nervous system functions and disorders. Its application in research can help elucidate the role of acetylcholine signaling in various neurological conditions.

    1 mg
    $100.00
    5 mg
    $255.00
    All 2 sizes
  • BTM-1086
    Cat. No.
    A61560

    BTM-1086

    BTM-1086 is a potent muscarinic acetylcholine receptor (mAChR) modulator, primarily functioning as an anti-ulcer agent. It demonstrates significant inhibitory activity against gastric secretion, making it valuable for research in gastrointestinal disorders. BTM-1086 can be utilized in studies focused on receptor signaling and the pharmacological management of gastric-related conditions.

    25 mg
    $1,275.00
    50 mg
    $1,625.00
    All 3 sizes
  • VU6007496
    Cat. No.
    A67693

    VU6007496

    VU6007496 is a selective positive allosteric modulator (PAM) of the M1 muscarinic acetylcholine receptor. It enhances receptor activity, contributing to potential improvements in cognitive function and memory processing. Its favorable pharmacokinetics support its use in central nervous system studies and drug discovery related to neurodegenerative diseases. Researchers may explore VU6007496 in preclinical models to investigate its therapeutic effects on cognitive disorders.

    25 mg
    $1,405.00
    50 mg
    $1,790.00
    All 3 sizes
  • VU0366369
    Cat. No.
    A78837

    VU0366369

    Synonyms: ML137

    VU0366369 is a selective positive allosteric modulator (PAM) of the muscarinic acetylcholine receptor subtype M1, exhibiting an EC50 value of 830 nM. This compound has demonstrated potential for enhancing M1 receptor function, making it a valuable tool in the study of central nervous system disorders. Researchers may utilize VU0366369 to explore therapeutic strategies for conditions such as Alzheimer's disease and schizophrenia, focusing on cholinergic signaling pathways.

    5 mg
    $50.00
    10 mg
    $75.00
    All 6 sizes

Items 51-59 of 59

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