Date published: 2025-12-5

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mAChR M1 Activators

Muscarinic acetylcholine receptors (mAChRs) are a class of G-protein-coupled receptors (GPCRs) found in various tissues throughout the body, including the central nervous system, peripheral nervous system, and other organs. Among the subtypes of mAChRs, M1 receptors hold a unique position due to their predominant expression in the central nervous system, particularly in regions associated with cognition and memory, making them an attractive target for pharmacological research. mAChR M1 activators are a class of compounds that specifically target and activate these M1 receptors.The M1 subtype of mAChRs is primarily responsible for mediating the effects of the neurotransmitter acetylcholine in the brain. When activated, M1 receptors stimulate intracellular signaling pathways, notably the phosphoinositide hydrolysis cascade, which leads to an increase in intracellular calcium and the activation of protein kinase C. These signaling events play a crucial role in modulating synaptic transmission, memory, and cognitive processes. Therefore, compounds designed to activate M1 receptors selectively are of particular interest for understanding the physiological and pathological roles of these receptors in the brain. Researchers have developed a variety of M1 activators, which can serve as valuable tools for studying the functional consequences of M1 receptor activation.

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Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

Cevimeline Hydrochloride Salt

107220-28-0sc-207420
5 mg
$330.00
(0)

Cevimeline Hydrochloride Salt acts as a potent agonist at the M1 muscarinic acetylcholine receptor, characterized by its ability to induce specific allosteric changes in receptor conformation. This compound engages in unique electrostatic interactions with key amino acid residues, enhancing receptor activation. Its distinct pharmacokinetic properties allow for rapid receptor binding and prolonged activity, influencing intracellular signaling cascades and promoting nuanced physiological responses.

cis-2-Methyl-5-trimethylammoniummethyl-1,3-oxathiolane iodide

76541-57-6sc-252614
5 mg
$199.00
(0)

Cis-2-Methyl-5-trimethylammoniummethyl-1,3-oxathiolane iodide functions as a selective modulator of the M1 muscarinic acetylcholine receptor, exhibiting unique ligand-receptor dynamics. Its quaternary ammonium structure facilitates strong ionic interactions with the receptor, promoting a specific conformational shift. This compound's kinetic profile reveals a rapid association and dissociation rate, allowing for fine-tuned modulation of downstream signaling pathways, thereby influencing cellular responses with precision.

N-Desmethylclozapine

6104-71-8sc-201113
sc-201113A
5 mg
25 mg
$98.00
$364.00
2
(0)

N-Desmethylclozapine acts as a modulator of the M1 muscarinic acetylcholine receptor, characterized by its ability to engage in unique hydrogen bonding interactions. This compound exhibits a distinct allosteric effect, altering receptor conformation and enhancing ligand affinity. Its interaction kinetics are notable for a prolonged duration of action, which may lead to sustained receptor activation. Additionally, its lipophilicity contributes to effective membrane permeability, influencing its bioavailability in cellular environments.

Oxotremorine Sesquifumarate

17360-35-9sc-200170
sc-200170A
100 mg
500 mg
$66.00
$255.00
(0)

Oxotremorine Sesquifumarate selectively targets the M1 muscarinic acetylcholine receptor, showcasing a unique binding profile that stabilizes receptor states. Its interaction involves specific electrostatic and hydrophobic contacts, facilitating a nuanced modulation of signaling pathways. The compound exhibits rapid kinetics, allowing for swift receptor activation, while its structural features promote effective integration into lipid bilayers, enhancing its interaction with cellular membranes.

Milameline hydrochloride

139886-32-1sc-204085
sc-204085A
10 mg
50 mg
$137.00
$564.00
1
(0)

Milameline hydrochloride exhibits a distinctive affinity for the M1 muscarinic acetylcholine receptor, characterized by its ability to induce conformational changes that enhance receptor activity. The compound engages in specific hydrogen bonding and hydrophobic interactions, which fine-tune downstream signaling cascades. Its kinetic profile reveals a balanced rate of receptor binding and dissociation, allowing for sustained modulation of cholinergic pathways, while its solubility properties facilitate effective cellular uptake.

tert-Butyl peroxybenzoate

614-45-9sc-258210
100 ml
$38.00
(0)

Allosteric agonist, selectively activates M1 receptors enhancing receptor response to acetylcholine.

Xanomeline oxalate

141064-23-5sc-204402
10 mg
$155.00
(0)

Xanomeline oxalate selectively targets the M1 muscarinic acetylcholine receptor, demonstrating unique allosteric modulation that alters receptor dynamics. Its molecular structure allows for intricate electrostatic interactions and pi-stacking with aromatic residues, enhancing receptor activation. The compound exhibits a rapid association rate with the receptor, coupled with a prolonged dissociation phase, promoting persistent signaling. Additionally, its solubility characteristics support efficient membrane permeability, influencing bioavailability.

VU 0357017 hydrochloride

1135242-13-5sc-362818
sc-362818A
5 mg
25 mg
$90.00
$364.00
(0)

VU 0357017 hydrochloride is a selective modulator of the M1 muscarinic acetylcholine receptor, exhibiting unique binding kinetics that facilitate receptor activation. Its structural conformation enables specific hydrogen bonding and hydrophobic interactions with key amino acid residues, enhancing receptor affinity. The compound's dynamic behavior includes a fast onset of action, followed by a gradual dissociation, which sustains receptor engagement. Furthermore, its physicochemical properties contribute to favorable membrane interactions, optimizing its functional profile.

McN-A-343

55-45-8sc-200186A
sc-200186
10 mg
50 mg
$26.00
$77.00
4
(0)

McN-A-343 is a potent allosteric modulator of the M1 muscarinic acetylcholine receptor, characterized by its ability to stabilize receptor conformations that promote signaling. It engages in specific electrostatic interactions with charged residues, enhancing receptor selectivity. The compound exhibits a unique dual-action mechanism, facilitating both receptor activation and desensitization. Its lipophilic nature aids in membrane penetration, influencing its pharmacokinetic behavior and receptor modulation efficiency.

(2S)-2-Ethyl-8-methyl-1-thia-4,8-diazaspiro[4,5]decan-3-one

503431-81-0sc-206582
5 mg
$330.00
(0)

(2S)-2-Ethyl-8-methyl-1-thia-4,8-diazaspiro[4,5]decan-3-one acts as a selective modulator of the M1 muscarinic acetylcholine receptor, exhibiting unique binding dynamics that favor specific receptor conformations. Its structural features allow for intricate hydrogen bonding and hydrophobic interactions, enhancing receptor affinity. The compound's spirocyclic framework contributes to its distinct conformational flexibility, influencing its interaction kinetics and overall receptor modulation profile.