mAChR4 Agonist

mAChR4 Agonists (22):

Cat. No.	Product Name	Effect	Purity

HY-17366

Clozapine N-oxide	Agonist	99.98%
Clozapine N-oxide is a major metabolite of Clozapine and a human muscarinic designer receptors (DREADDs) agonist. Clozapine N-oxide activates the DREADD receptor hM3Dq and hM4Di. Clozapine N-oxide can't cross the blood-brain barrier. Clozapine is a potent dopamine antagonist and also a potent and selective muscarinic M4 receptor (EC₅₀=11 nM) agonist.

HY-42110

Deschloroclozapine	Agonist	99.93%
Deschloroclozapine, a metabolite of Clozapine, is a highly potent muscarinic DREADDs agonist, with blood-brain barrier permeability. Deschloroclozapine binds to DREADD receptor subtypes hM3Dq and hM4Di with K_i of 6.3 and 4.2 nM, respectively. [¹¹C]-Deschloroclozapine is developed as a promising PET tracer for DREADD imaging.

HY-17366A

Clozapine N-oxide dihydrochloride	Agonist	99.74%
Clozapine N-oxide dihydrochloride is a major metabolite of Clozapine and a human muscarinic designer receptors (DREADDs) agonist. Clozapine N-oxide dihydrochloride activates the DREADD receptor hM3Dq and hM4Di. Clozapine N-oxide dihydrochloride cannot cross the blood-brain barrier. Clozapine is a potent dopamine antagonist and also a potent and selective muscarinic M4 receptor (EC₅₀=11 nM) agonist.

HY-119363

VU6009453	Agonist
VU6009453 (compound 15q) is a brain-penetrant M4 mAChR positive allosteric modulator (PAM) with an EC₅₀ of 383 nM. VU6009453 can be used for research on neurological diseases.

HY-105182

Xanomeline	Agonist	99.80%
Xanomeline, as an effective and selective muscarinic type 1 and type 4 (M1/M4) receptor agonist, increases neuronal excitability. Xanomeline can be used for the research of neurological disorders, such as schizophrenia.

HY-B0406A

Bethanechol chloride	Agonist	99.56%
Bethanechol chloride (Carbamyl-β-methylcholine chloride), a parasympathomimetic agent, is a mAChR agonist that exerts its effects via directly stimulating the mAChR (M1, M2, M3, M4, and M5) of the parasympathetic nervous system.

HY-112209

VU0467154	Agonist	99.23%
VU0467154 is a positive allosteric modulator of the M4 muscarinic acetylcholine receptor (mAChR), potentiating the response to ACh with pEC₅₀s of 7.75, 6.2 and 6 for rat, human and cynomolgus monkey M4 receptor, respectively.

HY-131881

JHU37160	Agonist	99.98%
JHU37160 is a potent and brain-penetrant DREADD agonist, with EC₅₀s of 18.5 nM and 0.2 nM for hM3Dq and hM4Di DREADDs in HEK-293 cells, respectively. JHU37160 exhibits selective [³H]Clozapine displacement from DREADDs and not from other Clozapine-binding sites in mice brain tissue.

HY-106432A

Sabcomeline hydrochloride	Agonist	99.81%
Sabcomeline (SB-202026; Memric) hydrochloride is a muscarinic receptor agonist capable of crossing the blood-brain barrier. Sabcomeline hydrochloride exhibits affinity for all hM1 to hM5 subtypes (pK_i=6.72-7.23), and shows near-full agonism at the hM3 receptor, inducing extracellular acidification. Sabcomeline hydrochloride alters the binding kinetics of dopamine D2 receptors through neural network regulation. Sabcomeline hydrochloride also causes minimal cardiovascular changes, effectively reverses spatial memory deficits in rodents and induces conditioned taste aversion. Sabcomeline hydrochloride is an important tool compound in studies of Alzheimer's disease and related neurodegenerative diseases.

HY-15885

LY2119620	Agonist	99.74%
LY2119620 is a high-affinity muscarinic M₂/M₄ receptor agonist.

HY-131891

JHU37152	Agonist	99.45%
JHU37152 is a potent and brain-penetrant DREADD agonist, with EC₅₀s of 5 nM and 0.5 nM for hM3Dq and hM4Di DREADDs in HEK-293 cells, respectively. JHU37152 exhibits selective [³H]Clozapine displacement from DREADDs and not from other Clozapine-binding sites in mice brain tissue.

HY-120184

VU0467485	Agonist	99.29%
VU0467485 (AZ13713945) is a potent, selective, and orally bioavailable muscarinic acetylcholine receptor 4 (M4) positive allosteric modulator (PAM). VU0467485 (AZ13713945) potentiates activity of ACh at M4 with EC₅₀s of 26.6 nM and 78.8 nM at rat and human M4 receptors, respectively. VU0467485 (AZ13713945) shows selectivity for M4 over human and rat M1/2/3/5. VU0467485 (AZ13713945) displays moderate to high CNS penetration. VU0467485 (AZ13713945) has antipsychotic-like activity.

HY-159829

Direclidine	Agonist
Direclidine (NBI-1117568, HTL-0016878) is a selective orthosteric agonist targeting the muscarinic acetylcholine M4 receptor, exhibiting very low affinity for M1, M2, M3, and M5 receptors. It binds to the orthosteric site of the M4 receptor in a non-covalent, competitive manner. Direclidine specifically activates the M4 receptor, inhibiting the release of acetylcholine from striatal cholinergic interneurons, thereby regulating the balance of the dopaminergic system and reducing psychiatric symptoms associated with excessive dopamine release. Direclidine can improve symptoms associated with neuropsychiatric disorders and is used in research on schizophrenia and other neuropsychiatric disorders.

HY-B0406

Bethanechol	Agonist
Bethanechol (Carbamyl-β-methylcholine), a parasympathomimetic agent, is a mAChR agonist that exerts its effects via directly stimulating the mAChR (M1, M2, M3, M4, and M5) of the parasympathetic nervous system.

HY-107650

Milameline hydrochloride	Agonist
Milameline (CI 979; RU35926) hydrochloride is a nonselective, partical and orally active muscarinic receptor agonist that improves cognition. Milameline hydrochloride has equal affinity for different subtypes of human muscarinic receptors with IC₅₀ of 1.3 µM for M1-, 1.1 µM for M2-, 1.5 µM for M3-, and 1.9 µM for M4-muscarinic receptors. Milameline hydrochloride has a higher affinity for sites [³H]CMD (IC₅₀ = 20 nM), than [³H]QNB, (IC₅₀ = 3059 nM). Milameline hydrochloride produces both central and peripheral cholinergic effects and reverses the cognitive deficits induced by Scopolamine (HY-N0296). Milameline hydrochloride can be used for the study of Alzheimer’s Disease.

HY-149702

M1/M4 muscarinic agonist 1	Agonist
M1/M4 muscarinic agonist 1 (compound 41) is a selective muscarinic M4/M1 agonist with EC₅₀ values of 14 and 55 nM for M4 and M1, respectively. M1/M4 muscarinic agonist 1 can be used for research on mental diseases, such as schizophrenia, delusional disorder, etc.

HY-118363

Lu AE51090	Agonist	99.51%
Lu AE51090 is selective muscarinic M1 receptor agonist with blood-brain barrier penetration. Lu AE51090 activates human M1 receptor with EC₅₀ of 61 nM, while showing no significant agonism at M2-M5 receptors. Lu AE51090 exerts procognitive effects in mice. Lu AE51090 can be used for the study of Alzheimer’s disease (AD) and cognitive impairment associated with schizophrenia (CIAS).

HY-135460

Milameline	Agonist
Milameline (CI-979; RU35926) is a nonselective, partical and orally active muscarinic receptor agonist that improves cognition. Milameline has equal affinity for different subtypes of human muscarinic receptors with IC₅₀ of 1.3 µM for M1-, 1.1 µM for M2-, 1.5 µM for M3-, and 1.9 µM for M4-muscarinic receptors. Milameline has a higher affinity for sites [³H]CMD (IC₅₀ = 20 nM), than [³H]QNB, (IC₅₀ = 3059 nM). Milameline produces both central and peripheral cholinergic effects and reverses the cognitive deficits induced by Scopolamine (HY-N0296). Milameline can be used for the study of Alzheimer’s Disease.

HY-B0406AS

Bethanechol-d₆ chloride	Agonist
Bethanechol-d₆ (chloride) is the deuterium labeled Bethanechol chloride. Bethanechol chloride (Carbamyl-β-methylcholine chloride), a parasympathomimetic agent, is a mAChR agonist that exerts its effects via directly stimulating the mAChR (M1, M2, M3, M4, and M5) of the parasympathetic nervous system.

HY-107650A

Milameline hydroiodide	Agonist
Milameline (CI 979; RU35926) hydroiodide is a nonselective, partical and orally active muscarinic receptor agonist that improves cognition. Milameline hydroiodide has equal affinity for different subtypes of human muscarinic receptors with IC₅₀ of 1.3 µM for M1-, 1.1 µM for M2-, 1.5 µM for M3-, and 1.9 µM for M4-muscarinic receptors. Milameline hydroiodide has a higher affinity for sites [³H]CMD (IC₅₀ = 20 nM), than [³H]QNB, (IC₅₀ = 3059 nM). Milameline hydroiodide produces both central and peripheral cholinergic effects and reverses the cognitive deficits induced by Scopolamine (HY-N0296). Milameline hydroiodide can be used for the study of Alzheimer’s Disease.

Name
Email *

	Sorry, but the email address you supplied was invalid.