Date published: 2025-10-11

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mAChR M4 Inhibitors

The class of mAChR M4 inhibitors encompasses a diverse array of chemical compounds that exert their inhibitory effects on the receptor through various mechanisms. Tropicamide, an example within this class, directly interferes with mAChR M4 by binding to its acetylcholine binding site, preventing the receptor's normal activation. This direct inhibition disrupts downstream signaling pathways associated with mAChR M4, modulating cellular responses. Additionally, methoctramine acts as a selective mAChR M4 antagonist, achieving inhibition through binding to the receptor's allosteric site, inducing conformational changes that hinder its interaction with acetylcholine. Scopolamine, another member of this class, competitively binds to the orthosteric site of mAChR M4, impeding the receptor's interaction with acetylcholine and disrupting downstream signaling pathways. These inhibitors, including pirenzepine, darifenacin, and himbacine, further contribute to the specificity of mAChR M4 modulation by targeting the receptor directly and interfering with its normal functioning. Notably, telenzepine achieves inhibition through binding to the receptor, showcasing the versatility within this chemical class.AF-DX 384, a potent and selective mAChR M4 antagonist, distinguishes itself by targeting the receptor's allosteric site, inducing conformational changes that impede acetylcholine binding. Ipratropium bromide competitively binds to the orthosteric site, disrupting the normal activation of mAChR M4 and modulating downstream signaling pathways. AQRA 741, with its selectivity for mAChR M4, binds to the receptor and interferes with acetylcholine binding, providing a targeted means of influencing receptor function. Pilocarpine introduces an indirect mechanism within this class, stimulating muscarinic receptors M1 and M3, leading to increased acetylcholine release. This, in turn, activates negative feedback mechanisms inhibiting acetylcholine release at the M4 receptor. The indirect inhibition of mAChR M4 by pilocarpine showcases the diversity of approaches within this class.

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Items 1 to 10 of 15 total

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Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

Tropicamide

1508-75-4sc-202371
100 mg
$31.00
3
(1)

Tropicamide acts as a selective antagonist at muscarinic M4 receptors, exhibiting unique binding dynamics that disrupt typical receptor activation. Its molecular interactions involve competitive inhibition, leading to altered signaling pathways. The compound's affinity for the M4 subtype is notable, as it influences downstream effects on neurotransmitter release. Tropicamide's rapid kinetics facilitate transient modulation of receptor activity, making it a key player in the regulation of cholinergic signaling.

AF-DX 384

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

AF-DX 384 is a selective antagonist for muscarinic M4 receptors, characterized by its unique allosteric modulation of receptor conformation. This compound engages in specific hydrogen bonding and hydrophobic interactions, which stabilize the inactive state of the receptor. Its kinetic profile reveals a fast association and dissociation rate, allowing for precise temporal control over cholinergic signaling pathways. The distinct selectivity for M4 enhances its role in fine-tuning neural communication.

Biperiden hydrochloride

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

Biperiden hydrochloride acts as a modulator of muscarinic M4 receptors, exhibiting a unique binding affinity that influences receptor dynamics. Its molecular structure facilitates specific electrostatic interactions, promoting a conformational shift that alters receptor activity. The compound's reaction kinetics demonstrate a notable balance between rapid binding and prolonged receptor occupancy, enabling nuanced regulation of cholinergic pathways. This selectivity underscores its potential in influencing synaptic transmission.

Methoctramine

104807-46-7sc-257709B
sc-257709
sc-257709A
5 mg
10 mg
25 mg
$163.00
$306.00
$444.00
1
(1)

Methoctramine acts as a selective antagonist for mAChR M4. It impedes the receptor′s function by binding to its allosteric site, inducing a conformational change that hinders its interaction with acetylcholine. Consequently, this inhibition disrupts the intracellular signaling cascades associated with mAChR M4, particularly those involved in neurotransmission and cellular responses.

AF-DX 116

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

AF-DX 116 selectively targets muscarinic M4 receptors, showcasing a distinct interaction profile characterized by its ability to stabilize receptor conformations. The compound engages in specific hydrogen bonding and hydrophobic interactions, enhancing its binding affinity. Its kinetic behavior reveals a rapid association rate coupled with a slow dissociation, allowing for sustained receptor modulation. This unique dynamic contributes to its role in fine-tuning cholinergic signaling pathways.

PD 102807

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

PD 102807 exhibits a selective affinity for muscarinic M4 receptors, demonstrating unique allosteric modulation capabilities. Its binding induces conformational changes that enhance receptor activity through specific electrostatic interactions. The compound's reaction kinetics are marked by a moderate association rate and prolonged retention at the receptor site, facilitating nuanced regulation of neurotransmitter release. This behavior underscores its potential in influencing cholinergic neurotransmission dynamics.

Scopolamine

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

Scopolamine, an alkaloid found in plants, acts as a potent mAChR M4 inhibitor by competitively binding to the receptor's orthosteric site. This binding prevents acetylcholine from effectively engaging with the receptor, leading to the inhibition of downstream signaling pathways.

(S)-(+)-Dimethindene maleate

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

(S)-(+)-Dimethindene maleate selectively engages with muscarinic M4 receptors, showcasing distinct binding characteristics that promote receptor stabilization. Its molecular interactions involve hydrophobic contacts and hydrogen bonding, which fine-tune receptor conformation. The compound exhibits a unique kinetic profile, characterized by a slow dissociation rate, allowing for sustained receptor activation. This prolonged engagement may influence downstream signaling pathways, highlighting its intricate role in modulating cholinergic activity.

4-DAMP

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

4-DAMP is a selective antagonist of muscarinic M4 receptors, exhibiting unique binding dynamics that enhance receptor specificity. Its molecular structure facilitates strong hydrophobic interactions and strategic electrostatic contacts, which contribute to its affinity. The compound's kinetic behavior is marked by a rapid association rate, leading to effective receptor occupancy. This interaction profile may alter receptor desensitization processes, impacting cholinergic signaling pathways in a nuanced manner.

Himbacine

6879-74-9sc-200181
sc-200181A
1 mg
5 mg
$77.00
$315.00
3
(1)

Himbacine acts as a selective modulator of muscarinic M4 receptors, characterized by its unique allosteric binding site interactions. The compound exhibits a distinctive conformational flexibility that allows it to stabilize receptor states, influencing downstream signaling cascades. Its kinetic profile reveals a slow dissociation rate, promoting prolonged receptor engagement. This behavior may lead to altered receptor dynamics, potentially affecting the overall cholinergic network in intricate ways.