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.

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  1. Methoctramine hydrate is a selective M2 muscarinic receptor antagonist at nM concentrations
  2. (-)-Nicotine ditartrate is a potent agonist of AChR (nicotinic acetylcholine recepto).
  3. M2/M4 AChR agonist

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

    Atropine is a competitive antagonist for the muscarinic acetylcholine receptor types M1, M2, M3, M4 and M5.
  5. muscarinic receptor antagonist

    Biperiden hydrochloride is a muscarinic receptor antagonist that displays some selectivity for the M1 subtype
  6. Muscarinic receptor agonist

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

    Fesoterodine fumarate is a medicine which is used in urinary urgency, reducing the frequency of passing urine and urge urinary incontinence
  8. mAChR M2 antagonist

    Gallamine Triethiodide is a mAChR M2 antagonist with pronounced cardioselectivity.
  9. Ipratropium bromide is a muscarinic antagonist, bronchodilator, N-Isopropyl salt of atropine.
  10. Rsogladine is an anti-gastric ulcer agent that facilitates gap-junctional intercellular communication through M1 muscarininc acetylcholine receptor binding.
  11. Methscopolamine bromide is a competitive antimuscarinic agent that blocks the binding of acetylcholine at muscarinic acetylcholine receptors (mAChR M).
  12. Oxybutynin(Ditropan) is an anticholinergic medication used to relieve urinary and bladder difficulties.
  13. AchR antagonist

    Rocuronium Bromide is a competitive AchR antagonist, used in modern anaesthesia.
  14. muscarinic receptor antagonist

    SVT-40776 is a novel M3 muscarinic receptor antagonist, for the treatment of overactive bladder.
  15. muscarinic acetylcholine receptor (mAChR) antagonist

    Tiotropium Bromide (BA679 BR) is a muscarinic acetylcholine receptor (mAChR) antagonist that blocks the binding of the acetylcholine ligand and subsequent opening of the ligand-gated ion channel.
  16. muscarinic receptor antagonist

    Tolterodine tartrate (Detrol LA) is a muscarinic receptor antagonist which is used for the treatment of urinary incontinence.
  17. muscarinic acetylcholine receptor antagonist

    Benzetimide hydrochloride is a muscarinic acetylcholine receptor antagonist.
  18. mAChR antagonist

    Nor-benzetimide is a major metabolite of Benzetimide. Benzetimide is a mAChR antagonist with anticholinergic activity.
  19. mAChR Agonist

    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.
  20. Anticholinergic agent

    Penehyclidine hydrochloride (also known as Penequinine hydrochloride) is a selective anticholinergic agent that acts as an antagonist of muscarinic M1 and M3 receptors. It exerts anti-inflammatory effects by modulating immune signaling in lung tissue, notably through activation of the NF-κB pathway and inhibition of pro-inflammatory cytokine release. In preclinical studies, Penehyclidine hydrochloride has been shown to alleviate pulmonary inflammation in rat models of chronic obstructive pulmonary disease (COPD), particularly under conditions of mechanical ventilation. These properties suggest its potential utility in managing respiratory inflammatory conditions and improving outcomes in mechanically ventilated patients with COPD.
  21. PDE Inhibitor

    Flavoxate hydrochloride is a competitive inhibitor of phosphodiesterase (PDE), providing significant antispasmodic effects through its action as a muscarinic acetylcholine receptor (mAChR) antagonist. In addition to its PDE inhibition, it exhibits moderate calcium antagonistic properties and local anesthetic effects. Flavoxate hydrochloride is utilized in research focused on overactive bladder (OAB) and related lower urinary tract infections, contributing to a better understanding of these conditions and potential therapeutic approaches.
  22. mAChR Agonist

    Isopteropodine is a positive modulator that selectively targets muscarinic acetylcholine receptors (mAChRs), exhibiting notable agonistic activity. It demonstrates an EC50 of 9.92 μM for acetylcholine and 14.5 μM for 5-hydroxytryptamine (5-HT), highlighting its potential in neuroscience research related to cognitive function. Additionally, Isopteropodine displays antibacterial efficacy against Gram-positive bacteria, with minimum inhibitory concentrations (MICs) of 150 μg/mL for Staphylococcus aureus and 250 μg/mL for Bacillus subtilis, making it suitable for studies in antimicrobial activity and cognitive impairment.
  23. M3 mAChR Antagonist

    p-F-HHSiD hydrochloride is a potent and selective antagonist of the M3 muscarinic acetylcholine receptor (mAChR). This compound also demonstrates antagonistic properties towards other mAChR subtypes and the alpha1-adrenoceptor. p-F-HHSiD hydrochloride is useful for research applications involving cancer, metabolic disorders, neurological conditions, and cardiovascular diseases, including colon cancer, Alzheimer’s disease, and diabetes.
  24. mAChR Antagonist

    Batefenterol Succinate is an inhaled bifunctional bronchodilator that acts as a muscarinic acetylcholine receptor (mAChR) antagonist and a beta2-adrenoceptor agonist. This dual mechanism results in effective smooth muscle relaxation, enhancing respiratory function. Batefenterol Succinate is primarily utilized in research focused on chronic obstructive pulmonary disease (COPD) and other respiratory conditions, providing insights into therapeutic strategies for airway obstruction.
  25. mAChR/Adrenergic Receptor Antagonist

    Muscarinic toxin 3 (MT3) is a selective and non-competitive antagonist of muscarinic acetylcholine receptors (mAChRs) and adrenergic receptors. It exhibits high potency with pIC50 values of 6.71, 8.79, 8.86, 7.57, 8.13, and 8.49 against M1, M4, α1A, α1B, α1D, α2A, α2B, and α2C receptors, respectively, highlighting its prominent adrenoceptor activity. This compound is valuable in studying receptor signaling pathways and has potential applications in pharmacological research focused on nervous system disorders and cardiovascular diseases.
  26. M3 mAChR Antagonist

    p-F-HHSiD (p-Fluorohexahydrosiladifenidol) functions as a selective antagonist of the M3 muscarinic acetylcholine receptor (mAChR). This compound exhibits antagonistic activity against various muscarinic receptor subtypes as well as the alpha-1 adrenergic receptor. p-F-HHSiD is valuable for research in cancer, metabolic disorders, neurological pathologies, and cardiovascular diseases, including colon cancer, Alzheimer's disease, and diabetes.
  27. mAChR Antagonist

    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.
  28. mAChR Agonist

    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.
  29. mAChR Regulator

    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.
  30. mAChR Control

    Tolterodine dimer acts as a muscarinic acetylcholine receptor (mAChR) antagonist. It serves as an impurity of Tolterodine, a compound known for its potent activity against mAChRs. This reagent is primarily utilized in research applications aimed at investigating cholinergic signaling pathways and evaluating potential therapeutic strategies for bladder control and related disorders.
  31. mAChR Agonist

    NNC 11-1607 is a selective agonist for the M1 and M4 subtypes of muscarinic acetylcholine receptors (mAChR). It effectively inhibits Forskolin-stimulated cAMP accumulation in human M2 and M4 mAChR-expressing Chinese hamster ovary cells. This compound shows potential for investigating central nervous system disorders, including Alzheimer’s disease and schizophrenia, making it a valuable tool for related research applications.
  32. mAChR Antagonist

    Atropine oxide hydrochloride is a competitive antagonist of muscarinic acetylcholine receptors, including M1, M2, M3, M4, and M5. It demonstrates key biological activity in antagonizing acetylcholine's effects, making it valuable in research focused on neurotransmission and receptor signaling. This reagent is particularly significant for studies involving the therapeutic applications in specific nerve agent and pesticide poisonings.
  33. Stable Isotope

    Rac-Fesoterodine-d14 fumarate is a stable isotope-labeled version of the racemic muscarinic receptor antagonist Fesoterodine. It exhibits competitive inhibition across multiple mAChR subtypes, with pKivalues of 8.0, 7.7, 7.4, 7.3, and 7.5 for M1, M2, M3, M4, and M5 receptors, respectively. This compound is primarily utilized in research applications focusing on the pharmacological characterization and monitoring of overactive bladder treatments.
  34. mAChR

    Revefenacin impurity 4 is an intermediate compound associated with Revefenacin, targeting the human M3 muscarinic acetylcholine receptor. This impurity demonstrates significant binding affinity with a Ki value of 55 nM, highlighting its potential as a pharmacological agent. It is useful for research applications involving muscarinic receptor modulation and the study of cholinergic signaling pathways.
  35. mAChR Control

    (Rac)-5-Carboxy tolterodine is an inactive metabolite of the muscarinic acetylcholine receptor antagonist Tolterodine. It serves as a valuable control in studies involving muscarinic receptors, particularly in the context of acetylcholine modulation. This compound is useful for researchers investigating the pharmacokinetics and metabolic pathways of Tolterodine and related drugs.
  36. mAChR Antagonist

    5-Hydroxymethyl tolterodine formate is a potent antagonist of muscarinic acetylcholine receptors (mAChR). This active metabolite, derived from tolterodine and fesoterodine through the action of CYP2D6 and plasma esterases respectively, has significant implications in the study of urinary disorders. Researchers can utilize 5-Hydroxymethyl tolterodine formate in pharmacological investigations of cholinergic signaling and its effects on smooth muscle activity, contributing to the understanding of treatment options for overactive bladder and related conditions.
  37. mAChR Antagonist

    Alvameline maleate is a muscarinic acetylcholine receptor (mAChR) antagonist with selective activity at the M2 and M3 subtypes, while acting as a partial agonist for the M1 subtype. This compound has demonstrated the ability to competitively inhibit contractions in human detrusor muscle induced by ammonium chloride and electrical field stimulation, highlighting its potential for applications in bladder function regulation. Furthermore, alvameline maleate has shown promise in enhancing cognitive function following traumatic brain injury in rodent models, making it a valuable tool for research in both urology and neuropharmacology.
  38. mAChR Antagonist

    Temiverine hydrochloride is a mAChR antagonist exhibiting anticholinergic activity. This compound is also a versatile click chemistry reagent, featuring an alkyne group that enables the copper-catalyzed azide-alkyne cycloaddition (CuAAC) with azide-containing molecules. Its applications extend to chemical biology, facilitating the development of novel therapeutics and biochemical probes.
  39. mAChR Antagonist

    Ambutonium bromide is a selective antagonist of the muscarinic acetylcholine receptors (mAChRs). By inhibiting the action of acetylcholine, it plays a significant role in modulating cholinergic signaling pathways. This compound is primarily utilized in research applications aimed at studying the effects of mAChR inhibition in various physiological and pathological contexts.
  40. mAChR Agonist

    ENS-163 phosphate is a selective muscarinic acetylcholine receptor (mAChR) M1 agonist. It exhibits significant biological activity by modulating M1 receptor signaling pathways, which are implicated in cognitive processes. This compound is valuable for research applications related to neuropsychological disorders and the exploration of potential therapeutic targets in Alzheimer's disease and other cognitive impairments.
  41. mAChR Antagonist

    Rispenzepine is an antimuscarinic compound that selectively antagonizes M1 and M3 muscarinic acetylcholine receptors (mAChRs). This compound exhibits significant biological activity in modulating cholinergic signaling pathways, making it valuable for research on neurological disorders and other conditions influenced by mAChR activity. Its specific receptor selectivity positions Rispenzepine as a useful tool in studies focused on receptor function and the development of therapeutic interventions.
  42. mAChR Agonist

    Muscarine tosylate is a potent agonist of the muscarinic acetylcholine receptors (mAChRs). This compound selectively stimulates the parasympathetic nervous system, leading to various physiological effects. Muscarine tosylate is widely utilized in research applications focusing on neuropharmacology and the modulation of cholinergic signaling pathways.
  43. Metabolite of Oxybutynin

    N-Desethyloxybutynin hydrochloride is an active metabolite of Oxybutynin, primarily targeting muscarinic acetylcholine receptors (mAChRs). This compound demonstrates significant binding affinity in isolated human bladder and parotid gland tissues, with pKi values of 8.2 and 8.7, respectively. It is useful in research exploring bladder function, salivary secretion, and the pharmacological effects of anticholinergic agents.
  44. Stable Isotope

    (R)-Hydroxytolterodine-d14 is a deuterated form of Desfesoterodine, a selective antagonist of muscarinic acetylcholine receptors (mAChRs). This compound exhibits high potency, with a KB value of 0.84 nM and a pA2 of 9.14. As a significant metabolite of Tolterodine and Fesoterodine, it has demonstrated efficacy in models of cerebral infarction-induced detrusor overactivity in rats, making it valuable for research in urology and neurology.
  45. mAChR Antagonist

    WIN 62,577 is a selective antagonist of muscarinic acetylcholine receptors (mAChRs), specifically targeting M1 to M4 subtypes. This compound acts as an allosteric enhancer of acetylcholine affinity at the M3 receptor, making it a valuable tool for studying cholinergic signaling. Its unique properties allow for exploration of mAChR-related pathways and their implications in various physiological and pathological conditions. Suitable for research applications in neurobiology and pharmacology, WIN 62,577 facilitates investigations into receptor functions and potential therapeutic targets.
  46. mAChR Antagonist

    Cyclodrine hydrochloride is a potent antagonist of muscarinic acetylcholine receptors (mAChRs). It is primarily utilized in research to investigate cholinergic signaling pathways and the role of mAChR in various physiological and pathological processes. This compound may aid in the exploration of potential therapeutic targets for disorders influenced by cholinergic activity.
  47. mAChR Agonist

    CDD0102 is a potent agonist of the M1 muscarinic acetylcholine receptor (mAChR). It demonstrates significant biological activity in promoting M1 receptor signaling pathways, making it valuable for research into neurobiology and cognitive function. CDD0102 is essential for studies investigating the role of muscarinic receptors in various physiological and pathological processes.
  48. mAChR Inhibitor

    Tematropium is a selective muscarinic acetylcholine receptor (mAChR) inhibitor known for its soft anticholinergic properties. It demonstrates significant biological activity in modulating bronchoconstriction and respiratory secretions. Tematropium is commonly used in research focused on respiratory diseases, exploring its potential in the treatment of asthma and chronic obstructive pulmonary disease (COPD).
  49. mAChR Modulator

    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.
  50. mAChR Antagonist

    YM-46303 is an antagonist of muscarinic acetylcholine receptors (mAChR), demonstrating high affinity for both M1 and M3 subtypes, with notable selectivity for the M3 receptor over the M2 receptor. This compound is valuable in the study of receptor signaling pathways and can be utilized in research involving neurological disorders, smooth muscle contraction, and other cholinergic system-related investigations. Its specificity makes it a useful tool for elucidating the roles of mAChR subtypes in various biological processes.

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