Date published: 2025-11-1

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mAChR M1 Inhibitors

Muscarinic acetylcholine receptor (mAChR) M1 inhibitors are a class of chemical compounds that specifically target and inhibit the activity of the M1 subtype of muscarinic acetylcholine receptors. These receptors belong to the G protein-coupled receptor (GPCR) superfamily, which is widely involved in various physiological processes through their interaction with acetylcholine, a neurotransmitter. The M1 subtype of mAChR is primarily expressed in the central nervous system, particularly in regions such as the hippocampus, cortex, and striatum. This receptor subtype is coupled to the Gq/11 protein, which upon activation, triggers a cascade of intracellular signaling pathways including the activation of phospholipase C, increased production of inositol triphosphate (IP3), and the subsequent release of calcium from intracellular stores. M1 receptors are involved in the modulation of various intracellular processes such as phosphoinositide metabolism, calcium signaling, and the activation of mitogen-activated protein kinase (MAPK) pathways. Inhibitors of the M1 receptor function by binding to the receptor and preventing its activation by endogenous acetylcholine. This inhibition leads to a reduction in the downstream signaling processes typically initiated by M1 receptor activation. The chemical structures of mAChR M1 inhibitors can vary significantly, ranging from small organic molecules to more complex structures, each with distinct binding affinities and selectivity profiles. These compounds often interact with the orthosteric or allosteric sites of the receptor, which can either completely block the receptor's function or modulate its activity to a lesser degree. The design and study of mAChR M1 inhibitors require a deep understanding of the receptor's structure, particularly its ligand-binding domains, and the dynamics of its conformational states. Advances in computational modeling and structural biology have been instrumental in identifying key interactions between these inhibitors and the receptor, guiding the development of compounds with enhanced selectivity and potency for the M1 subtype.

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Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

AQ-RA 741

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

AQ-RA 741 is a selective antagonist of the M1 muscarinic acetylcholine receptor, distinguished by its ability to stabilize receptor conformations that inhibit signaling. Its unique binding affinity is attributed to specific hydrophobic interactions and hydrogen bonding with key amino acid residues, which modulate receptor activity. The compound exhibits a distinctive kinetic profile, characterized by a slow off-rate, allowing for prolonged receptor occupancy and nuanced modulation of cholinergic pathways.

Diphenhydramine hydrochloride

147-24-0sc-204729
sc-204729A
sc-204729B
10 g
25 g
100 g
$51.00
$82.00
$122.00
4
(1)

Diphenhydramine hydrochloride acts as a non-selective antagonist at the M1 muscarinic acetylcholine receptor, exhibiting a complex interaction profile. Its binding involves both electrostatic and hydrophobic forces, influencing receptor dynamics. The compound's unique structural features facilitate allosteric modulation, altering receptor conformation and downstream signaling pathways. Additionally, its reaction kinetics reveal a rapid association rate, contributing to its multifaceted impact on cholinergic neurotransmission.

Atropine

51-55-8sc-252392
5 g
$200.00
2
(1)

Atropine is a competitive antagonist for the muscarinic acetylcholine receptors and may decrease expression by inhibiting receptor activation.

Biperiden hydrochloride

1235-82-1sc-203846
sc-203846A
10 mg
50 mg
$112.00
$422.00
(0)

Biperiden hydrochloride selectively targets the M1 muscarinic acetylcholine receptor, showcasing a unique binding affinity that stabilizes specific receptor conformations. Its molecular structure promotes distinct hydrogen bonding interactions, enhancing receptor-ligand specificity. The compound exhibits notable reaction kinetics, characterized by a moderate dissociation rate, which influences the duration of its receptor engagement. This dynamic behavior contributes to its nuanced modulation of cholinergic signaling pathways.

Scopolamine

51-34-3sc-473216
sc-473216A
sc-473216B
100 mg
500 mg
1 g
$169.00
$496.00
$771.00
2
(0)

As a non-selective muscarinic antagonist, scopolamine may downregulate receptor expression by blocking the receptor and reducing its activity.

AF-DX 116

102394-31-0sc-223772
5 mg
$107.00
3
(0)

AF-DX 116 is a selective antagonist of the M1 muscarinic acetylcholine receptor, exhibiting a unique interaction profile that alters receptor dynamics. Its molecular architecture facilitates specific electrostatic interactions, enhancing binding precision. The compound demonstrates rapid association kinetics, allowing for swift modulation of receptor activity. This behavior influences downstream signaling cascades, providing insights into cholinergic system regulation and receptor functionality.

Telenzepine dihydrochloride

147416-96-4sc-204332
sc-204332A
10 mg
25 mg
$62.00
$128.00
(0)

Telenzepine dihydrochloride acts as a selective modulator of the M1 muscarinic acetylcholine receptor, characterized by its ability to stabilize receptor conformations. Its unique structural features promote distinct hydrogen bonding and hydrophobic interactions, which fine-tune receptor activation. The compound exhibits a notable affinity for allosteric sites, influencing receptor signaling pathways and enhancing the understanding of cholinergic neurotransmission dynamics.

(S)-(+)-Dimethindene maleate

121367-05-3sc-361329
sc-361329A
10 mg
50 mg
$235.00
$960.00
1
(0)

(S)-(+)-Dimethindene maleate is a selective antagonist of the M1 muscarinic acetylcholine receptor, exhibiting unique stereochemical properties that influence its binding affinity. Its molecular structure facilitates specific electrostatic interactions and steric hindrance, which modulate receptor activity. The compound's kinetic profile reveals a rapid onset of action, with distinct conformational changes in the receptor that alter downstream signaling cascades, providing insights into cholinergic modulation.

Oxybutynin Chloride

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

Oxybutynin Chloride acts as a selective modulator of the M1 muscarinic acetylcholine receptor, characterized by its ability to induce conformational shifts in the receptor's structure. This compound engages in specific hydrogen bonding and hydrophobic interactions, enhancing its binding efficacy. Its unique kinetic behavior allows for a nuanced regulation of receptor-mediated pathways, influencing downstream cellular responses and contributing to the complexity of cholinergic signaling.

4-DAMP

1952-15-4sc-200167
50 mg
$192.00
5
(1)

4-DAMP is a potent antagonist of the M1 muscarinic acetylcholine receptor, exhibiting a high affinity for the receptor's orthosteric site. Its unique structure facilitates specific electrostatic interactions, which stabilize the receptor-ligand complex. The compound's kinetic profile reveals rapid association and dissociation rates, allowing for dynamic modulation of receptor activity. This behavior underscores its role in fine-tuning cholinergic signaling pathways, impacting various cellular processes.