Date published: 2026-4-5

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mAChR M2 Inhibitors

Muscarinic acetylcholine receptor M2 (mAChR M2) inhibitors are a class of chemical compounds that specifically target and modulate the activity of the M2 subtype of muscarinic acetylcholine receptors. The M2 receptor is a G protein-coupled receptor (GPCR) that is predominantly coupled to the Gi/o family of G proteins, which inhibit adenylate cyclase activity, reduce cyclic AMP (cAMP) levels, and modulate ion channel conductance, particularly potassium channels. By inhibiting the M2 receptor, mAChR M2 inhibitors can disrupt this signaling pathway, leading to alterations in downstream signaling events, including changes in cAMP concentrations and ion flux. These alterations can have significant consequences for cellular function, particularly in tissues where the M2 receptor is densely expressed, such as cardiac and smooth muscle tissues, as well as in certain neural circuits. The specificity of these inhibitors for the M2 subtype, as opposed to other muscarinic receptor subtypes (M1, M3, M4, M5), is crucial for understanding their role in modulating specific physiological processes. At the molecular level, mAChR M2 inhibitors typically bind to the orthosteric or allosteric sites of the M2 receptor, leading to conformational changes that either directly block the receptor's ability to bind acetylcholine or modulate the receptor's signaling efficacy. These binding interactions are often characterized by high affinity and selectivity, which are essential for their specific inhibitory actions on the M2 subtype. The structural diversity among mAChR M2 inhibitors allows for a range of binding modes and mechanisms of action, from competitive antagonism at the orthosteric site to non-competitive modulation at allosteric sites. This diversity is further reflected in the varying physicochemical properties of these inhibitors, including their lipophilicity, molecular weight, and the presence of functional groups that contribute to receptor binding. The study of mAChR M2 inhibitors is thus a complex field that intersects with various aspects of molecular pharmacology, receptor biology, and biochemistry, offering insights into the fundamental mechanisms of GPCR signaling modulation.

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Items 1 to 10 of 17 total

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Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

AF-DX 384

118290-27-0sc-203498
sc-203498A
10 mg
50 mg
$129.00
$548.00
(0)

AF-DX 384 acts as a selective antagonist of the M2 muscarinic acetylcholine receptor, characterized by its unique ability to disrupt receptor conformational states. Its structural features allow for specific hydrogen bonding and hydrophobic interactions with key amino acids, influencing receptor desensitization. The compound exhibits a distinctive kinetic profile, enabling it to modulate receptor activity with precision, thereby affecting downstream signaling cascades.

AQ-RA 741

123548-16-3sc-203517
sc-203517A
10 mg
50 mg
$135.00
$575.00
(0)

AQ-RA 741 functions as a modulator of the M2 muscarinic acetylcholine receptor, distinguished by its capacity to stabilize specific receptor conformations. Its unique molecular architecture facilitates intricate electrostatic interactions and steric hindrance with critical residues, impacting receptor activation dynamics. The compound's reaction kinetics reveal a nuanced binding affinity, allowing for selective engagement with the receptor's allosteric sites, thereby influencing intracellular signaling pathways.

Atropine

51-55-8sc-252392
5 g
$204.00
2
(1)

Atropine, a tropane alkaloid, inhibits mAChR M2 by competitively binding to its acetylcholine binding site. This hinders acetylcholine from binding to the receptor, preventing downstream signaling. The blockade of mAChR M2 signaling leads to a reduction in parasympathetic nervous system activity.

Biperiden hydrochloride

1235-82-1sc-203846
sc-203846A
10 mg
50 mg
$160.00
$505.00
(0)

Biperiden hydrochloride acts as a selective antagonist at the M2 muscarinic acetylcholine receptor, characterized by its ability to disrupt acetylcholine binding through competitive inhibition. Its structural features enable it to form specific hydrogen bonds and hydrophobic interactions with receptor domains, altering conformational states. This modulation affects downstream signaling cascades, showcasing its role in fine-tuning receptor activity and influencing neurotransmitter release dynamics.

Gallamine Triethiodide

65-29-2sc-200175
sc-200175A
1 g
5 g
$145.00
$300.00
1
(0)

Gallamine Triethiodide, a non-depolarizing neuromuscular blocking agent, indirectly inhibits mAChR M2 by blocking the action of acetylcholine at the neuromuscular junction. This results in reduced activation of mAChR M2 and subsequent inhibition of parasympathetic responses in smooth muscle.

AF-DX 116

102394-31-0sc-223772
5 mg
$109.00
3
(0)

AF-DX 116 is a selective antagonist of the M2 muscarinic acetylcholine receptor, exhibiting unique binding characteristics that enhance its specificity. Its molecular structure facilitates distinct electrostatic interactions and steric hindrance, effectively blocking acetylcholine access. This compound influences receptor conformational dynamics, leading to altered intracellular signaling pathways. The kinetics of its binding suggest a rapid onset of action, contributing to its nuanced modulation of cholinergic transmission.

Telenzepine dihydrochloride

147416-96-4sc-204332
sc-204332A
10 mg
25 mg
$63.00
$131.00
(0)

Telenzepine dihydrochloride acts as a selective modulator of the M2 muscarinic acetylcholine receptor, characterized by its unique allosteric binding site interactions. This compound exhibits a distinctive ability to stabilize specific receptor conformations, thereby influencing downstream signaling cascades. Its reaction kinetics reveal a slow dissociation rate, allowing for prolonged receptor engagement. Additionally, Telenzepine dihydrochloride's hydrophilic nature enhances solubility, facilitating effective receptor interaction.

PD 102807

23062-91-1sc-203659
sc-203659A
1 mg
10 mg
$202.00
$950.00
2
(0)

PD 102807 is a selective antagonist of the M2 muscarinic acetylcholine receptor, distinguished by its unique binding affinity that alters receptor dynamics. This compound exhibits a rapid onset of action, with kinetic profiles indicating swift receptor occupancy. Its structural features promote specific hydrogen bonding interactions, enhancing selectivity. Furthermore, PD 102807's lipophilic characteristics contribute to its membrane permeability, influencing its pharmacokinetic behavior.

(S)-(+)-Dimethindene maleate

121367-05-3sc-361329
sc-361329A
10 mg
50 mg
$240.00
$979.00
1
(0)

(S)-(+)-Dimethindene maleate acts as a selective modulator of the M2 muscarinic acetylcholine receptor, characterized by its unique stereochemistry that influences receptor conformation. This compound demonstrates a distinctive interaction profile, facilitating allosteric modulation that fine-tunes receptor signaling pathways. Its hydrophobic regions enhance membrane interaction, while specific electrostatic interactions promote targeted binding, affecting downstream cellular responses and receptor desensitization kinetics.

Oxybutynin Chloride

1508-65-2sc-208141
2.5 g
$265.00
(0)

Oxybutynin Chloride exhibits a unique affinity for the M2 muscarinic acetylcholine receptor, engaging in specific hydrogen bonding and hydrophobic interactions that stabilize its binding. This compound's structural features allow it to influence receptor dynamics, leading to altered signaling cascades. Its kinetic behavior showcases a rapid association and slower dissociation, which may impact receptor desensitization and subsequent cellular activity, highlighting its intricate role in modulating cholinergic pathways.