Date published: 2025-10-15

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mAChR M3 Activators

Muscarinic Acetylcholine Receptors (mAChRs) are a class of G protein-coupled receptors (GPCRs) that play a crucial role in mediating the effects of the neurotransmitter acetylcholine (ACh) in the central nervous system (CNS) and peripheral tissues. These receptors are named after muscarine, a natural alkaloid compound found in certain mushrooms, which can selectively activate them. There are five subtypes of mAChRs, designated as M1 through M5, each encoded by a distinct gene. These receptor subtypes exhibit distinct anatomical distribution patterns and signaling mechanisms, allowing for diverse physiological responses to acetylcholine. mAChRs are integral membrane proteins composed of seven transmembrane helices (TMHs) connected by intracellular and extracellular loops. They are primarily found on the plasma membrane of postsynaptic neurons, smooth muscles, and other cell types throughout the body. Additionally, some mAChRs are also present in presynaptic terminals, where they regulate neurotransmitter release. Upon binding acetylcholine, mAChRs undergo conformational changes that activate their intracellular signaling pathways. Activation of mAChRs leads to the dissociation of the heterotrimeric G proteins into Gα and Gβγ subunits. The different mAChR subtypes display varying affinities for acetylcholine and selective agonists or antagonists. For instance, M1, M3, and M5 subtypes primarily couple to Gq/11 proteins, which activate phospholipase Cβ (PLCβ) and subsequently elevate intracellular calcium levels and activate protein kinase C (PKC). On the other hand, M2 and M4 subtypes predominantly couple to Gi/o proteins, which inhibit adenylate cyclase (AC) and reduce cyclic AMP (cAMP) levels, leading to downstream effects mediated by cAMP-dependent protein kinase (PKA). Due to their extensive distribution and involvement in various physiological processes, mAChRs have profound effects on the nervous, cardiovascular, respiratory, gastrointestinal, and urinary systems.

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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 muscarinic receptor agonist, demonstrating a unique affinity for M3 receptors. Its molecular architecture facilitates specific hydrogen bonding and hydrophobic interactions, enhancing receptor activation. The compound exhibits rapid kinetics, leading to swift receptor engagement and downstream signaling. Additionally, its solubility characteristics allow for effective interaction in various environments, influencing cellular responses and physiological pathways.

Carbamyl-β-methylcholine chloride

590-63-6sc-234279
5 g
$132.00
(0)

Bethanechol, a muscarinic agonist, directly activates mAChR M3 by binding and stimulating receptor activity. Its cholinergic effects contribute to smooth muscle contraction and glandular secretion, exemplifying direct activation of mAChR M3 without involvement of other proteins.

Oxotremorine Sesquifumarate

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

Oxotremorine Sesquifumarate serves as a selective activator of muscarinic M3 receptors, characterized by its unique structural conformation that promotes effective receptor binding. The compound engages in specific electrostatic interactions, enhancing its affinity and selectivity. Its dynamic reaction kinetics facilitate rapid activation of signaling cascades, while its distinct solubility profile allows for versatile interactions within biological systems, influencing various cellular mechanisms.

Milameline hydrochloride

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

Milameline hydrochloride functions as a potent activator of muscarinic M3 receptors, distinguished by its unique ability to stabilize receptor conformations through specific hydrogen bonding and hydrophobic interactions. This compound exhibits a remarkable capacity for modulating intracellular signaling pathways, leading to enhanced receptor responsiveness. Its favorable partitioning characteristics enable efficient membrane penetration, promoting swift engagement with target sites and influencing downstream cellular activities.

Xanomeline oxalate

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

Xanomeline oxalate serves as a selective modulator of muscarinic M3 receptors, characterized by its ability to induce distinct allosteric changes in receptor structure. This compound engages in unique electrostatic interactions that facilitate receptor activation, enhancing ligand binding affinity. Its kinetic profile reveals rapid onset and prolonged action, allowing for sustained receptor engagement. Additionally, its solubility properties contribute to effective distribution within biological systems, optimizing its interaction dynamics.

Pilocarpine

92-13-7sc-479256
100 mg
$250.00
1
(0)

Pilocarpine, another muscarinic agonist, directly activates mAChR M3 by binding to the receptor and promoting downstream signaling. Through its cholinergic actions, pilocarpine induces smooth muscle contraction and glandular secretion, illustrating direct activation of mAChR M3.

Cevimeline-d4 Hydrochloride Salt

107220-28-0 (unlabeled)sc-217875
sc-217875B
sc-217875A
1 mg
25 mg
10 mg
$290.00
$3500.00
$2200.00
(0)

Cevimeline-d4 Hydrochloride Salt acts as a potent modulator of muscarinic M3 receptors, exhibiting unique conformational dynamics that promote receptor activation. Its isotopic labeling enhances tracking in metabolic studies, providing insights into receptor-ligand interactions. The compound demonstrates distinctive binding kinetics, characterized by a swift association and a gradual dissociation, which may influence downstream signaling pathways. Its hydrophilic nature aids in solvation, facilitating effective molecular interactions.

Cevimeline

107233-08-9sc-353133
25 mg
$1800.00
(0)

Cevimeline, a muscarinic agonist, directly activates mAChR M3 by binding to the receptor and eliciting cholinergic responses. Its actions include stimulating smooth muscle contraction and glandular secretion, demonstrating direct activation of mAChR M3 without involvement of other proteins.

Oxotremorine M

63939-65-1sc-203656
100 mg
$148.00
3
(1)

Oxotremorine M, a muscarinic agonist, directly activates mAChR M3 by binding to the receptor and initiating downstream signaling. Its cholinergic effects, such as smooth muscle contraction and glandular secretion, exemplify direct activation of mAChR M3 without engaging other proteins.

Arecoline

63-75-2sc-210836
10 mg
$153.00
2
(0)

Arecoline, a muscarinic agonist, directly activates mAChR M3 by binding and initiating receptor-mediated responses. Its cholinergic actions, including smooth muscle contraction and glandular secretion, demonstrate direct activation of mAChR M3 without reliance on other proteins or signaling pathways.