2. シグナル伝達
  3. GPCR/G Protein
    Neuronal Signaling
  4. mAChR
  5. mAChR2 Isoform

mAChR2

The M2 muscarinic acetylcholine receptor (mAChR2) functions as a G protein-coupled receptor that regulates acetylcholine signaling in both neuronal and non-neuronal cells[1]. Mechanistically, M2 modulates presynaptic neurotransmitter release via coupling to protein kinase C (PKC) and PDK1, selectively influencing PKCβI and PKCε isoforms and downstream SNARE machinery[2]. In the neuromuscular junction, M2 participates in developmental synapse elimination by regulating activity-dependent acetylcholine release, coordinating with M1/M4 mAChRs and adenosine receptors[3][4]. Beyond the nervous system, M2 receptors control epithelial and immune cell functions, including endocytosis-mediated receptor trafficking and signaling regulation[1]. In cardiac myocytes, M2 activation triggers endothelial nitric oxide synthase (eNOS)-dependent nitration of p190A RhoGAP, enhancing RhoA activity and altering cytoskeletal dynamics[5]. In disease models, down-regulation of M2 adversely affects Alzheimer’s disease-relevant genes, including BACE1, and disrupts amyloid precursor protein processing[6][7]. Compared with related muscarinic isoforms, M2 uniquely suppresses BACE1 expression, whereas M1 activation increases it[7]. Pharmacologically, selective M2 inhibitors, such as methoctramine, can block agonist-induced signaling in smooth muscle and macrophages, providing tools for dissecting M2-specific pathways[8][9]. These characteristics render M2 a critical target for experimental modulation in studies of synaptic plasticity, neurodegeneration, cardiac physiology, and immune regulation[1][2][5].

References:

mAChR2 関連製品 (57):

製品番号 製品名 製品効果 純度
  • HY-17360
    Tiotropium Bromide Antagonist 99.91%
    Tiotropium bromide (BA-679 BR) is a long-acting anticholinergic bronchodilator. Tiotropium bromide blocks the action of acetylcholine at muscarinic M1, M2, and M3 receptors, prevents bronchoconstriction, and dilates bronchial airways. Tiotropium bromide is applicable to research related to chronic obstructive pulmonary disease and asthma.
  • HY-107647
    (S)-(+)-Dimethindene maleate Antagonist 99.80%
    (S)-(+)-Dimethindene maleate, an enantiomer, is a potent M2-selective muscarinic receptor antagonist (pA2 = 7.86/7.74; pKi = 7.78). (S)-(+)-Dimethindene maleate shows lower affinities for the muscarinic M1 (pA2 = 6.83/6.36; pKi = 7.08), the M3 (pA2 = 6.92/6.96; pKi = 6.70) and the M4 receptors (pKi = 7.00), respectively. (S)-(+)-Dimethindene maleate also is a histamine H1 receptor antagonist (pA2 = 7.48).
  • HY-122743
    Iperoxo Agonist 99.48%
    Iperoxo is a potent superagonist of muscarinic acetylcholine receptor (mAChR) that activates M1, M2 and M3 receptors with pEC50 of 9.87, 10.1 and 9.78. Iperoxo can be used for direct probing activation-related conformational transitions of muscarinic receptors when labeled with tritium.
  • HY-101381
    Otenzepad Antagonist 99.93%
    Otenzepad (AF-DX 116) is a selective and competitive M2 muscarinic acetylcholine receptor antagonist, with IC50 values of 640 nM and 386 nM for rabbit peripheral lung and rat heart, respectively.
  • HY-B0461
    Trospium chloride Antagonist 99.93%
    Trospium chloride is an orally active, specific and competitive antagonist of muscarinic cholinergic receptors (mAChRs), with antimuscarinic activity. Trospium chloride binds to muscarinic receptors M1, M2 and M3 with high affinity, but not nicotinic, cholinergic receptors.
  • HY-183144
    Vedaclidine Modulator
    Vedaclidine is an orally active muscarinic acetylcholine receptor (mAChR) modulator with mixed receptor activity, which activates muscarinic M2 and M4 receptors and blocks muscarinic M1, M3 and M5 receptors. Vedaclidine exerts its activity through interaction with spinal M4 muscarinic receptors, and does not induce hypothermia or excessive salivation. Vedaclidine can be used in research related to pain, neuropathic pain and inflammatory pain states.
  • HY-180358
    Gallamine Antagonist
    Gallamine is an allosteric, selective muscarinic M2 acetylcholine receptor antagonist (EC50: 130 nM for [3H]NMS dissociation from porcine muscarinic M2 receptors). Gallamine is also an acetylcholinesterase inhibitor (IC50s : 1070 μM, 1480 μM, 235  μM for EeAChE, hAChE, hBChE, respectively (in the absence of MeCN)). Gallamine increases free norepinephrine levels. Gallamine can be used as a muscle relaxant.
  • HY-137388
    p-F-HHSiD Antagonist
    p-F-HHSiD (p-Fluorohexahydrosiladifenidol) is a potent and selective M3 mAChR antagonist. p-F-HHSiD has antagonistic effects on other subtypes of the M receptor and the alpha1-adrenoceptor. p-F-HHSiD can be used for the researches of cancer, metabolic, neurological and cardiovascular disease such as, colon cancer, Alzheimer’s disease and diabetes.
  • HY-101239
    Oxotremorine sesquifumarate Agonist 98.0%
    Oxotremorine sesquifumarate is a mAChR agonist that mainly activates M2 receptors. Oxotremorine sesquifumarate can be used for neurological research.
  • HY-B0241
    Ipratropium bromide Antagonist 99.92%
    Ipratropium bromide (Sch 1000) is a muscarinic receptor antagonist, with IC50s of 2.9 nM, 2 nM, and 1.7 nM for M1, M2, and M3 receptors, respectively. Ipratropium bromide relaxes smooth muscle, can be used in the research for COPD (chronic obstructive pulmonary disease) and asthma.
  • HY-A0082
    Diphenidol hydrochloride Antagonist 99.06%
    Diphenidol hydrochloride (Difenidol hydrochloride) is a non-selective muscarinic M1-M4 receptor antagonist, has anti-arrhythmic activity. Diphenidol hydrochloride is also a potent non-specific blocker of voltage-gated ion channels (Na+, K+, and Ca2+) in neuronal cells. Diphenidol hydrochloride can be used in the study of antivertigo and antinausea.
  • HY-A0034
    Solifenacin Antagonist 99.77%
    Solifenacin (YM905 free base) is a novel muscarinic receptor antagonist with pKis of 7.6, 6.9 and 8.0 for M1, M2 and M3 receptors, respectively.
  • HY-116294A
    Methoctramine tetrahydrochloride Antagonist 98.72%
    Methoctramine tetrahydrochloride is a potent and cardioselectivity antagonist of M2 muscarinic receptor. Methoctramine tetrahydrochloride can inhibit Muscarine (HY-121404)-induced bradycardia in vivo. Methoctramine tetrahydrochloride can be used in the study of cardiovascular diseases.
  • HY-15885
    LY2119620 Agonist 99.74%
    LY2119620 is a high-affinity muscarinic M2/M4 receptor agonist.
  • HY-N0340
    Scopolamine butylbromide Antagonist 99.97%
    Scopolamine butylbromide (Hyoscine butylbromide) is an orally active anticholinergic agent and spasmolytic. Scopolamine butylbromide binds with high affinity to rat cardiac M2 (Ki 83 nmol/L), hM2 (Ki 233 nmol/L), rat intestinal M3 (Ki 290 nmol/L) and hM3 (Ki 643 nmol/L) muscarinic receptors. Scopolamine butylbromide exerts a dose-dependent antagonistic effect on Carbachol-induced gastrointestinal smooth muscle spasm. Scopolamine butylbromide can be used for the research of abdominal colic and pain associated with gastrointestinal spasm, functional abdominal pain, chronic gastropathy and gastric ulcer.
  • HY-12980
    Batefenterol Antagonist 99.72%
    Batefenterol (GSK961081;TD-5959) is a novel muscarinic receptor antagonist and β2-adrenoceptor agonist; displays high affinity for hM2, hM3 muscarinic and hβ2-adrenoceptor with Ki values of 1.4, 1.3 and 3.7 nM, respectively.
  • HY-B1339
    Dicyclomine hydrochloride Inhibitor 98.09%
    Dicyclomine hydrochloride is a potent and orally active muscarinic cholinergic receptors antagonist. Dicyclomine hydrochloride shows high affinity for muscarinic M1 receptor subtype (Ki=5.1 nM) and M2 receptor subtype (Ki=54.6 nM) in brush-border membrane and basal plasma membranes, respectively. Dicyclomine is an antispasmodic agent and relieves smooth muscle spasm of the gastrointestinal tract in vivo.
  • HY-A0002
    Solifenacin Succinate Antagonist 99.91%
    Solifenacin Succinate (YM905) is a novel muscarinic receptor antagonist with pKis of 7.6, 6.9 and 8.0 for M1, M2 and M3 receptors, respectively.
  • HY-B0460
    Tiotropium bromide monohydrate Antagonist 99.68%
    Tiotropium bromide monohydrate (BA-679 BR monohydrate) is a long-acting anticholinergic bronchodilator. Tiotropium bromide monohydrate blocks the action of acetylcholine at muscarinic M1, M2, and M3 receptors, prevents bronchoconstriction, and dilates bronchial airways. Tiotropium bromide monohydrate is applicable to research related to chronic obstructive pulmonary disease and asthma.
  • HY-I0230
    Solifenacin hydrochloride Antagonist 98.86%
    Solifenacin hydrochloride (YM905 hydrochloride) is a muscarinic receptor antagonist, with pKis of 7.6, 6.9 and 8.0 for M1, M2 and M3 receptors, respectively.