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 126-150 of 399

  • Atropine
    Cat. No.
    A61258

    Atropine

    Synonyms: Tropine tropate; DL-Hyoscyamine

    Atropine is a competitive antagonist of muscarinic acetylcholine receptors (mAChR), exhibiting IC50 values of 0.39 nM for human mAChR M4 and 0.71 nM for chicken mAChR M4. This compound effectively inhibits acetylcholine-induced relaxations in human pulmonary veins. Atropine is utilized in research focused on anti-myopia and the treatment of bradycardia.

    100 mg
    $50.00
    500 mg
    $80.00
    All 4 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
  • Xanomeline tartrate
    Cat. No.
    A61262

    Xanomeline tartrate

    Synonyms: LY 246708 tartrate

    Xanomeline tartrate is a potent agonist of the muscarinic M1 and M4 receptors, exhibiting antipsychotic-like activity. This compound enhances neuronal excitability and is primarily utilized in research focused on schizophrenia. Its mechanism provides valuable insights into potential therapeutic approaches for neuropsychiatric conditions.

    2 mg
    $25.00
    5 mg
    $40.00
    All 6 sizes
  • Iperoxo
    Cat. No.
    A61263

    Iperoxo

    Iperoxo is a potent superagonist of muscarinic acetylcholine receptors (mAChR), effectively activating M1, M2, and M3 subtypes with pEC50 values of 9.87, 10.1, and 9.78, respectively. This compound is valuable for investigating activation-related conformational transitions in muscarinic receptors, particularly when labeled with tritium. Its strong receptor activity makes Iperoxo suitable for research in neurotransmission and receptor pharmacology.

    1 mg
    $35.00
    5 mg
    $90.00
    All 8 sizes
  • Emraclidine
    Cat. No.
    A61264

    Emraclidine

    Synonyms: CVL-231

    Emraclidine is a positive allosteric modulator of the muscarinic M4 receptor, designed to enhance receptor activity. This compound has shown potential in the study of neurological diseases, providing insights into cholinergic signaling pathways and their implications in various disorders. Researchers may utilize Emraclidine to explore novel therapeutic approaches targeting the M4 receptor in neuropharmacology.

    1 mg
    $105.00
    2 mg
    $155.00
    All 7 sizes
  • DREADD agonist 21 dihydrochloride
    Cat. No.
    A61265

    DREADD agonist 21 dihydrochloride

    DREADD agonist 21 dihydrochloride is a highly potent agonist of the human muscarinic acetylcholine M3 receptor (hM3Dq), with an EC50 value of 1.7 nM. This compound selectively activates hM3Dq, facilitating the study of neuronal signaling pathways in various research applications. Its utility in chemogenetics allows for precise modulation of cellular activity, making it an invaluable tool for investigating the roles of specific neuronal circuits in behavior and disease models.

    5 mg
    $90.00
    10 mg
    $135.00
    All 5 sizes
  • Pilocarpine nitrate
    Cat. No.
    A61266

    Pilocarpine nitrate

    Pilocarpine nitrate is a potent agonist of the M3 muscarinic acetylcholine receptor. It effectively stimulates muscarinic receptors, leading to increased salivation and glandular secretions. This compound is widely utilized in pharmacological research related to the treatment of dry mouth and glaucoma, as well as in studies of neurodegenerative diseases.

    50 mg
    $25.00
    100 mg
    $30.00
    All 3 sizes
  • VU 0255035
    Cat. No.
    A61267

    VU 0255035

    Synonyms: VU 255035

    VU 0255035 is a highly selective and competitive antagonist of the M1 muscarinic acetylcholine receptor (mAChR). It effectively inhibits M1 mAChR signaling, which contributes to the reduction of epileptic seizures and the modulation of neuronal membrane potential. This compound is valuable for research applications focused on central nervous system disorders, including epilepsy, Parkinson's disease, and dystonia.

    1 mg
    $25.00
    5 mg
    $55.00
    All 7 sizes
  • Ethopropazine hydrochloride
    Cat. No.
    A61268

    Ethopropazine hydrochloride

    Synonyms: Isothazine

    Ethopropazine hydrochloride is a potent and selective inhibitor of butyrylcholinesterase (BChE) and acts as a non-selective antagonist at muscarinic acetylcholine receptors (mAChR) and N-methyl-D-aspartate receptors (NMDA). This compound exhibits anticholinergic, antihistamine, and antiadrenergic activities, making it valuable in studying its effects on neuropathic pain conditions such as thermal hyperalgesia. Ethopropazine hydrochloride is particularly relevant in research related to Parkinson's disease, providing insights into cholinergic system modulation and receptor interactions.

    5 mg
    $20.00
    10 mg
    $35.00
    All 5 sizes
  • Otenzepad
    Cat. No.
    A61269

    Otenzepad

    Synonyms: AF-DX 116

    Otenzepad is a selective, competitive antagonist of the M2 muscarinic acetylcholine receptor, exhibiting IC50 values of 640 nM in rabbit peripheral lung tissue and 386 nM in rat heart tissue. This compound plays a significant role in modulating cholinergic signaling and has applications in research focused on respiratory and cardiovascular physiology. Its use aids in the study of receptor-mediated pathways and potential therapeutic targets in related disorders.

    1 mg
    $30.00
    5 mg
    $60.00
    All 7 sizes
  • Oxotremorine sesquifumarate
    Cat. No.
    A61270

    Oxotremorine sesquifumarate

    Oxotremorine sesquifumarate is an agonist of muscarinic acetylcholine receptors (mAChRs), primarily activating the M2 subtype. This compound is instrumental in neurological research, facilitating the study of cholinergic signaling and its implications in various neurological disorders. Its ability to modulate M2 receptor activity makes it valuable for investigating the physiological and pathophysiological roles of these receptors in the nervous system.

    5 mg
    $45.00
    10 mg
    $80.00
    All 5 sizes
  • Pirenzepine
    Cat. No.
    A61271

    Pirenzepine

    Synonyms: LS 519 free base; Pirenzepin; Gastrozepin

    Pirenzepine is a selective antagonist of the M1 muscarinic acetylcholine receptor (mAChR) with limited ability to cross the blood-brain barrier. This compound is primarily utilized for its ability to inhibit gastric acid secretion and alleviate muscle spasm, making it relevant in the study of peptic ulcers. Additionally, Pirenzepine exhibits anti-proliferative properties in various cancer cell lines, providing valuable insights for cancer research applications.

    25 mg
    $25.00
    50 mg
    $45.00
    All 4 sizes
  • (-)-Vesamicol
    Cat. No.
    A61272

    (-)-Vesamicol

    Synonyms: (-)-AH5183

    (-)-Vesamicol is a vesicular acetylcholine transporter inhibitor that exerts its action by reversibly and non-competitively inhibiting the transport of acetylcholine into synaptic vesicles. This compound effectively blocks the activity of vesicular acetylcholine transporters in medial amygdala neurons, making it a valuable tool for studies related to neurotransmission and neurodevelopmental disorders. Its specific application is in research focused on central precocious puberty, providing insights into the role of acetylcholine transport in this condition.

    5 mg
    $100.00
    10 mg
    $150.00
    All 5 sizes
  • Aceclidine
    Cat. No.
    A61273

    Aceclidine

    Synonyms: Quinuclidin-3-yl acetate

    Aceclidine, a modulator of muscarinic acetylcholine receptors, primarily targets the M3 receptor while also acting as an M1 receptor agonist (EC50: 40 μM). This compound serves as a cycloplegic agent, surfactant, tonicity adjustor, and can enhance viscosity and provide antioxidant effects. It is applicable in research focusing on conditions such as refractive errors of the eye, xerostomia, Sjögren's syndrome, glaucoma, conjunctivitis, lacrimal gland disorders, and esotropia.

    100 mg
    $20.00
    200 mg
    $25.00
    All 7 sizes
  • VU0453595
    Cat. No.
    A61274

    VU0453595

    VU0453595 is a highly selective positive allosteric modulator (PAM) for the M1 muscarinic acetylcholine receptor, with an EC50 of 2140 nM. This compound has shown potential in modulating M1 receptor activity, making it a valuable tool for investigations into schizophrenia and related cognitive disorders. Its systemic activity enhances the understanding of M1 receptor function and its role in neuropsychiatric conditions.

    2 mg
    $30.00
    5 mg
    $50.00
    All 6 sizes
  • VU6019650
    Cat. No.
    A61275

    VU6019650

    VU6019650 is a potent and selective orthosteric antagonist of the M5 muscarinic acetylcholine receptor (IC50 = 36 nM). This compound is being investigated for its potential in alleviating opioid use disorder by modulating the mesolimbic dopaminergic reward circuitry. VU6019650 effectively reduces neuronal firing rates in midbrain dopamine neurons of the ventral tegmental area in response to Oxotremorine M iodide, offering insights into its pharmacological application in neuropsychiatric research.

    5 mg
    $100.00
    10 mg
    $165.00
    All 5 sizes
  • (Rac)-5-Hydroxymethyl Tolterodine
    Cat. No.
    A61277

    (Rac)-5-Hydroxymethyl Tolterodine

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

    (Rac)-5-Hydroxymethyl Tolterodine is a mAChR antagonist with high affinity for M1, M2, M3, M4, and M5 receptors, exhibiting Ki values of 2.3 nM, 2 nM, 2.5 nM, 2.8 nM, and 2.9 nM, respectively. This active metabolite of Tolterodine is valuable for investigating the pathophysiology and treatment of overactive bladder conditions. Its selective inhibition of muscarinic acetylcholine receptors allows for exploration of therapeutic strategies targeting bladder hyperactivity.

    100 mg
    $25.00
    500 mg
    $45.00
    All 3 sizes
  • JHU37160
    Cat. No.
    A61278

    JHU37160

    JHU37160 is a potent DREADD agonist that selectively targets hM3Dq and hM4Di receptors with EC50 values of 18.5 nM and 0.2 nM, respectively, in HEK-293 cells. This compound exhibits significant brain penetration and selectively displaces [3H]Clozapine from DREADD sites without affecting other Clozapine-binding sites in murine brain tissue. JHU37160 is valuable for research applications involving chemogenetics, neurobiology, and the exploration of neural circuits.

    10 mg
    $35.00
    25 mg
    $65.00
    All 4 sizes
  • GSK1034702
    Cat. No.
    A61279

    GSK1034702

    GSK1034702 is an allosteric agonist of the M1 muscarinic acetylcholine receptor (mAChR) with a pEC50 of 8.1 and the capability to cross the blood-brain barrier. It activates the Gq/11 protein-mediated signaling pathway, promoting neuronal firing and enhancing long-term potentiation (LTP) in the hippocampal CA1 region. This compound is valuable for investigating cognitive impairment mechanisms, including those related to Alzheimer's disease, and has demonstrated pro-cognitive effects in models of nicotine withdrawal cognitive dysfunction. Additionally, GSK1034702 may elicit certain side effects associated with peripheral M receptor activation, including gastrointestinal reactions.

    1 mg
    $55.00
    5 mg
    $135.00
    All 7 sizes
  • Telenzepine dihydrochloride
    Cat. No.
    A61281

    Telenzepine dihydrochloride

    Telenzepine dihydrochloride is a selective antagonist of the muscarinic M1 receptor, exhibiting a Ki value of 0.94 nM. This compound effectively inhibits gastric acid secretion and demonstrates significant antiulcer properties, making it a valuable tool for research into gastrointestinal disorders and therapeutic interventions in related conditions.

    2 mg
    $25.00
    5 mg
    $40.00
    All 6 sizes
  • Fesoterodine L-mandelate
    Cat. No.
    A61282

    Fesoterodine L-mandelate

    Fesoterodine L-mandelate is a competitive antagonist of muscarinic acetylcholine receptors (mAChR), demonstrating non-subtype selectivity with pKi values of 8.0, 7.7, 7.4, 7.3, and 7.5 for M1, M2, M3, M4, and M5 receptors, respectively. This orally active compound is primarily utilized in the treatment of overactive bladder (OAB). Its inhibition of mAChRs contributes to a reduction in bladder contractions, providing therapeutic benefits for managing urinary incontinence.

    2 mg
    $25.00
    5 mg
    $40.00
    All 7 sizes
  • Dipeptide diaminobutyroyl benzylamide diacetate
    Cat. No.
    A61283

    Dipeptide diaminobutyroyl benzylamide diacetate

    Dipeptide diaminobutyroyl benzylamide diacetate functions as a muscarinic acetylcholine receptor (mAChR) antagonist. It induces muscle relaxation, making it relevant in studies related to skin aging and facial wrinkles, including crow's feet and periorbital creases. This compound can be utilized in research focused on dermatological applications and the physiological mechanisms underlying muscle tone regulation in the skin.

    50 mg
    $25.00
    100 mg
    $40.00
    All 3 sizes
  • Guvacoline hydrochloride
    Cat. No.
    A61284

    Guvacoline hydrochloride

    Guvacoline hydrochloride is a muscarinic receptor full activator, primarily targeting atrial and ileal muscarinic receptors. As a pyridine alkaloid derived from Areca triandra, it demonstrates the ability to act as a weak full agonist at these receptors. Guvacoline hydrochloride is utilized in research applications focusing on muscarinic receptor activation and its physiological implications.

    5 mg
    $35.00
    10 mg
    $45.00
    All 5 sizes
  • VU0357017 hydrochloride
    Cat. No.
    A61285

    VU0357017 hydrochloride

    Synonyms: CID-25010775

    VU0357017 hydrochloride is a selective allosteric agonist of the M1 muscarinic acetylcholine receptor, demonstrating a potent efficacy with an EC50 of 477 nM. This compound exhibits high selectivity for the M1 receptor, showing no activity at M2-M5 subtypes even at concentrations up to 30 μM. VU0357017 hydrochloride is valuable for research applications related to Alzheimer's disease and schizophrenia.

    5 mg
    $30.00
    10 mg
    $45.00
    All 6 sizes

Items 126-150 of 399

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