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 1-25 of 77

  • LY2119620
    Cat. No.
    A14217

    LY2119620

    Synonyms: LY-2219620

    LY2119620 is a specific, and allosteric agonist of human M2 and M4 muscarinic acetylcholine receptors.

    1 mg
    $45.00
    5 mg
    $95.00
    All 7 sizes
  • Bethanechol chloride
    Cat. No.
    A10180

    Bethanechol chloride

    Bethanechol is a parasympathomimetic choline carbamate that selectively stimulates muscarinic receptors without any effect on nicotinic receptors.

    200 mg
    $20.00
    500 mg
    $25.00
    All 5 sizes
  • Cevimeline
    Cat. No.
    A11372

    Cevimeline (AF-102B)

    Synonyms: AF102B

    Cevimeline (AF-102B) is a parasympathomimetic and muscarinic agonist, with particular effect on M3 receptors; used in the treatment of dry mouth associated with sjogren's syndrome.

    5 mg
    $580.00
    10 mg
    $980.00
    All 3 sizes
  • Metanicotine
    Cat. No.
    A11545

    Metanicotine

    Synonyms: Rivanicline; RJR 2403

    Metanicotine is a neuronal nicotinic receptor agonist, showing high selectivity for the α4β2 subtype (Ki=26 nM); > 1,000 fold selectivity than ??7 receptors(Ki= 36000 nM).

    5 mg
    $400.00
    10 mg
    $620.00
    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
  • 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
  • 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
  • Pilocarpine Hydrochloride
    Cat. No.
    A16669

    Pilocarpine Hydrochloride

    Synonyms: Pilocarpine HCl; NSC 5746 HCl; (+)-Pilocarpine hydrochloride

    Pilocarpine Hydrochloride is a selective agonist for the M3 muscarinic acetylcholine receptor (mAChR). It plays a significant role in stimulating glandular secretion, particularly in the treatment of dry mouth and glaucoma. This compound is valuable in research focused on neuropharmacology, as well as studies investigating cholinergic signaling and its implications in various physiological processes.

    500 mg
    $25.00
    1 g
    $50.00
    All 4 sizes
  • Methacholine chloride
    Cat. No.
    A17285

    Methacholine chloride

    Synonyms: Acetyl-beta-methylcholine chloride; Provocholine; Mecholyl chloride; Amechol; Methapharma Brand of Methacholine Chloride; Provokit; Roche Brand of Methacholine Chloride

    Methacholine chloride is a synthetic choline ester that acts as a non-selective muscarinic receptor agonist in the parasympathetic nervous system.

    100 mg
    $50.00
    200 mg
    $80.00
    All 4 sizes
  • Cevimeline hydrochloride
    Cat. No.
    A18092

    Cevimeline hydrochloride

    Synonyms: Evoxac; Cevimeline HCl

    Cevimeline (Evoxac) Hcl is a parasympathomimetic and muscarinic agonist, with particular effect on M3 receptors; used in the treatment of dry mouth associated with sjogren's syndrome.

    2 mg
    $50.00
    5 mg
    $60.00
    All 4 sizes
  • Talsaclidine
    Cat. No.
    A18571

    Talsaclidine

    Talsaclidine is a muscarinic agonist with preferential neuron-stimulating properties. Talsaclidine is a full agonist at the M1 subtype, and as a partial agonist at the M2 and M3 subtypes.

    1 mg
    $240.00
    5 mg
    $560.00
    All 5 sizes
  • Alvameline
    Cat. No.
    A19271

    Alvameline

    Synonyms: Lu 25-109

    Alvameline (Lu25-109) is a partial M1 agonist and M2/M3 antagonist.

    1 mg
    $200.00
    5 mg
    $500.00
    All 6 sizes
  • Blarcamesine
    Cat. No.
    A21095

    Blarcamesine (AVex-73)

    Synonyms: AE-37; AVex-73; Anavex-2-73

    Blarcamesine, also known as AVex-73 and AE-37, is a muscarinic M1 agonist potentially for the treatment of Alzheimer's disease. It is an ς receptor ligand.

    5 mg
    $35.00
    10 mg
    $50.00
    All 6 sizes
  • Perlapine
    Cat. No.
    A22204

    Perlapine

    Perlapine is a potent and selective hM3Dq DREADD agonist (EC50 = 2.8 nM). This drug exhibits >10,000-fold selectivity for hM3Dq over hM3.

    1 mg
    $35.00
    5 mg
    $115.00
    All 4 sizes
  • VU0364572 TFA
    Cat. No.
    A57573

    VU0364572 TFA

    VU0364572 TFA is a selective allosteric agonist of the M1 muscarinic receptor, exhibiting an EC50 of 0.11 μM. This compound demonstrates neuroprotective properties, making it a potential candidate for mitigating memory impairments and alleviating neuropathology associated with Alzheimer's Disease. Additionally, VU0364572 TFA is capable of penetrating the central nervous system, thus enabling its application in neurological research.

    5 mg
    $215.00
    10 mg
    $380.00
    All 5 sizes
  • VU0364572
    Cat. No.
    A57576

    VU0364572

    VU0364572 is a selective allosteric agonist of the M1 muscarinic receptor, exhibiting an EC50 of 0.11 μM. It demonstrates neuroprotective effects, making it a valuable tool in investigating memory impairments and neuropathological changes associated with Alzheimer’s Disease. Additionally, VU0364572 is orally bioactive and capable of penetrating the central nervous system, enhancing its utility in neuropharmacological research.

    25 mg
    $1,275.00
    50 mg
    $1,625.00
    All 3 sizes
  • Clozapine N-oxide dihydrochloride
    Cat. No.
    A59853

    Clozapine N-oxide dihydrochloride

    Clozapine N-oxide dihydrochloride is a selective agonist for designer receptors exclusively activated by designer drugs (DREADDs), specifically targeting hM3Dq and hM4Di. This compound plays a crucial role in neuronal circuit manipulation for experimental purposes. It is notable for its inability to cross the blood-brain barrier, making it useful for in vivo studies to modulate neuronal activity without central nervous system effects. Clozapine N-oxide dihydrochloride is integral in research applications related to neuroscience, enabling the dissection of gene function and behavior in animal models.

    2 mg
    $25.00
    5 mg
    $40.00
    All 6 sizes
  • Sabcomeline hydrochloride
    Cat. No.
    A59871

    Sabcomeline hydrochloride

    Synonyms: SB-202026 hydrochloride; Memric hydrochloride

    Sabcomeline hydrochloride is a muscarinic receptor agonist with the ability to penetrate the blood-brain barrier. It exhibits strong affinity for human muscarinic receptor subtypes hM1 to hM5 (pKi=6.72-7.23) and functions as a near-full agonist at the hM3 receptor, leading to extracellular acidification. This compound also influences dopamine D2 receptor binding kinetics via neural network modulation, while exhibiting minimal effects on cardiovascular parameters. Sabcomeline hydrochloride is valuable in research related to Alzheimer's disease and other neurodegenerative disorders, especially for investigating its effects on spatial memory and taste aversion in rodent models.

    2 mg
    $400.00
    5 mg
    $410.00
    All 6 sizes
  • Betovumeline hydrochloride
    Cat. No.
    A61259

    Betovumeline hydrochloride

    Betovumeline hydrochloride is an agonist of muscarinic acetylcholine receptors (mAChRs), which play a critical role in various neurological functions. This compound is valuable for research into neurological disorders, facilitating the study of receptor activation and signaling pathways. Its ability to selectively engage mAChRs makes it a useful tool in pharmacological investigations and potential therapeutic applications.

    1 mg
    $95.00
    5 mg
    $240.00
    All 6 sizes
  • Xanomeline
    Cat. No.
    A61261

    Xanomeline

    Synonyms: LY-246708

    Xanomeline is a selective agonist of the muscarinic M1 and M4 receptors, known to enhance neuronal excitability. This compound is primarily used in research focused on neurological disorders, including schizophrenia, and offers potential insights into the modulation of cholinergic signaling pathways in the central nervous system.

    2 mg
    $25.00
    5 mg
    $40.00
    All 6 sizes

Items 1-25 of 77

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