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Results for "

muscarinic M1/M4 receptor

" in MedChemExpress (MCE) Product Catalog:

By Targets:	mAChR (57) 5-HT Receptor (10) Adrenergic Receptor (10) Apoptosis (8) Autophagy (4) Cholinesterase (ChE) (1) Dopamine Receptor (6) Dopamine Transporter (4) Histamine Receptor (11) IKK (4) Isotope-Labeled Compounds (9) Keap1-Nrf2 (4) Ligands for E3 Ligase (1) mTOR (4) p62 (4) Parasite (1) Potassium Channel (4) Pyroptosis (4) Reference Standards (10) Serotonin Transporter (4) Sigma Receptor (1) Sodium Channel (8) Trk Receptor (4)
By Research Areas:	Cancer (6) Cardiovascular Disease (1) Endocrinology (4) Inflammation/Immunology (8) Metabolic Disease (12) Neurological Disease (49)

By Targets:

mAChR (57)

5-HT Receptor (10)

Adrenergic Receptor (10)

Apoptosis (8)

Autophagy (4)

Cholinesterase (ChE) (1)

Dopamine Receptor (6)

Dopamine Transporter (4)

Histamine Receptor (11)

IKK (4)

Isotope-Labeled Compounds (9)

Keap1-Nrf2 (4)

Ligands for E3 Ligase (1)

mTOR (4)

p62 (4)

Parasite (1)

Potassium Channel (4)

Pyroptosis (4)

Reference Standards (10)

Serotonin Transporter (4)

Sigma Receptor (1)

Sodium Channel (8)

Trk Receptor (4)

By Research Areas:

Cancer (6)

Cardiovascular Disease (1)

Endocrinology (4)

Inflammation/Immunology (8)

Metabolic Disease (12)

Neurological Disease (49)

Inhibitors & Agonists

Peptides

Isotope-Labeled Compounds

Targets Recommended: mAChR

Cat. No.	상품명	Target	연구분야	Chemical Structure

HY-14539

Clozapine Maximum Cited Publications 11 Publications Verification HF 1854; ZINC000019796155	Dopamine Receptor mAChR Adrenergic Receptor 5-HT Receptor Ligands for E3 Ligase	Neurological Disease Cancer
Clozapine (HF 1854) is an antipsychotic used for the research of schizophrenia. Clozapine has high affinity for a number of neuroreceptors. Clozapine is a potent antagonist of dopamine D2 with a K_i of 75 nM. Clozapine inhibits the **muscarinic M1 receptor** and serotonin 5HT2A receptor with K_is of 9.5 nM and 4 nM, respectively . Clozapine is also a potent and selective agonist at the **muscarinic M4 receptor (EC₅₀**=11 nM) .

HY-B0298A

Clemastine fumarate Maximum Cited Publications 11 Publications Verification HS-592 fumarate; Meclastine fumarate	Histamine Receptor Apoptosis mAChR Pyroptosis Keap1-Nrf2 p62 Autophagy mTOR IKK	Neurological Disease Metabolic Disease
Clemastine (HS-592; Meclastine) fumarate is an orally active, blood-brain barrier-permeable H1 histamine receptor (H1 histamine receptor) antagonist with potent antiallergic effects. Clemastine fumarate also antagonizes muscarinic acetylcholine receptors (mAChR), particularly the M1 and M4 subtypes. In addition to antihistamine effects, Clemastine fumarate exhibits multiple pharmacological activities, especially in promoting central nervous system remyelination, activating autophagy and pyroptosis, exerting anti-apoptotic and neuroprotective effects, and suppressing inflammation .

HY-105182

Xanomeline 5+ Cited Publications LY-246708	mAChR	Neurological Disease
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-B0527A

Amitriptyline hydrochloride 5+ Cited Publications	Serotonin Transporter 5-HT Receptor mAChR Histamine Receptor Adrenergic Receptor Trk Receptor Sodium Channel Potassium Channel Dopamine Transporter Apoptosis	Neurological Disease Inflammation/Immunology Endocrinology
Amitriptyline hydrochloride is an orally active tricyclic antidepressant (TCA). Amitriptyline hydrochloride mainly exerts its antidepressant effect by blocking SERT (K_i = 3.45 nM) and NET (K_i = 13.3 nM), thereby increasing the concentrations of 5-hydroxytryptamine (5-HT) and norepinephrine (NE) in the synaptic cleft. Amitriptyline hydrochloride is also an agonist at α2A and TrkA/TrkB receptors, thereby exerting analgesic and neurotrophic activities (inhibiting cell apoptosis). Amitriptyline hydrochloride can reduce inflammation, angiogenesis and fibrosis. Amitriptyline hydrochloride binds to DAT (with K_i = 2.58 μM). Amitriptyline hydrochloride has high affinity for a series of receptors and can antagonize muscarinic cholinergic receptors (M1/M2/M3/M4/M5 receptors) (K_i = 11-24 nM), H1 receptors (K_i = 0.5-1.1 nM), adrenergic α1 receptors (K_i = 4.4 nM), etc., resulting in a series of side effects. Amitriptyline hydrochloride can block sodium channels and hERG potassium channel (IC₅₀ = 4.78 μM) and it has cardiotoxicity .

HY-B0527

Amitriptyline 5+ Cited Publications	Serotonin Transporter Trk Receptor Sodium Channel 5-HT Receptor Histamine Receptor Adrenergic Receptor mAChR Potassium Channel Dopamine Transporter Apoptosis	Neurological Disease Inflammation/Immunology Endocrinology
Amitriptyline is an orally active tricyclic antidepressant (TCA). Amitriptyline mainly exerts its antidepressant effect by blocking SERT (K_i = 3.45 nM) and NET (K_i = 13.3 nM), thereby increasing the concentrations of 5-hydroxytryptamine (5-HT) and norepinephrine (NE) in the synaptic cleft. Amitriptyline is also an agonist at α2A and TrkA/TrkB receptors, thereby exerting analgesic and neurotrophic activities (inhibiting cell apoptosis). Amitriptyline can reduce inflammation, angiogenesis and fibrosis. Amitriptyline binds to DAT (with K_i = 2.58 μM). Amitriptyline has high affinity for a series of receptors and can antagonize muscarinic cholinergic receptors (M1/M2/M3/M4/M5 receptors) (K_i = 11-24 nM), H1 receptors (K_i = 0.5-1.1 nM), adrenergic α1 receptors (K_i = 4.4 nM), etc., resulting in a series of side effects. Amitriptyline can block sodium channels and hERG potassium channel (IC₅₀ = 4.78 μM) and it has cardiotoxicity .

HY-105182A

Xanomeline tartrate 5+ Cited Publications LY 246708 tartrate	mAChR	Neurological Disease
Xanomeline (LY 246708) is the potent agonist of muscarinic *M1/M4* receptor with antipsychotic-like activity. Xanomeline (LY 246708) increases neuronal excitability. Xanomeline (LY 246708) can be used for the research of schizophrenia .

HY-A0030

Fesoterodine fumarate	mAChR	Neurological Disease Metabolic Disease Cancer
Fesoterodine Fumarate is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pK_i values of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively. Fesoterodine Fumarate is used for the overactive bladder (OAB) .

HY-B0298

Clemastine Maximum Cited Publications 11 Publications Verification HS-592; Meclastine	Histamine Receptor mAChR Autophagy Apoptosis Keap1-Nrf2 p62 mTOR Pyroptosis IKK	Cardiovascular Disease Neurological Disease Inflammation/Immunology
Clemastine (HS-592; Meclastine) is an orally active, blood-brain barrier-permeable H1 histamine receptor (H1 histamine receptor) antagonist with potent antiallergic effects. Clemastine also antagonizes muscarinic acetylcholine receptors (mAChR), particularly the M1 and M4 subtypes. In addition to antihistamine effects, Clemastine exhibits multiple pharmacological activities, especially in promoting central nervous system remyelination, activating autophagy and pyroptosis, exerting anti-apoptotic and neuroprotective effects, and suppressing inflammation .

HY-107646

PD 102807	mAChR	Neurological Disease
PD 102807 is a M4 muscarinic receptor antagonist with an IC₅₀ of 90.7 nM. PD 102807 inhibits M1, M2, M3, M5 muscarinic receptor with IC₅₀s of 6558.7, 3440.7, 950.0, and 7411.7 nM, respectively . Antidyskinetic effect.

HY-A0082

Diphenidol hydrochloride Difenidol hydrochloride	mAChR Sodium Channel	Neurological Disease
Diphenidol hydrochloride (Difenidol hydrochloride) is a non-selective **muscarinic M₁-M₄ receptor** antagonist, has anti-arrhythmic activity. Diphenidol hydrochloride is also a potent non-specific blocker of voltage-gated ion channels (Na ⁺, K ⁺, and Ca ²⁺) in neuronal cells. Diphenidol hydrochloride can be used in the study of antivertigo and antinausea .

HY-70053

Fesoterodine	mAChR	Neurological Disease Metabolic Disease
Fesoterodine is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pK_i values of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively. Fesoterodine is used for the overactive bladder (OAB) .

HY-107647

(S)-(+)-Dimethindene maleate 1 Publications Verification	mAChR Histamine Receptor	Inflammation/Immunology
(S)-(+)-Dimethindene maleate, an enantiomer, is a potent M₂-selective muscarinic receptor antagonist (pA₂ = 7.86/7.74; pK_i = 7.78). (S)-(+)-Dimethindene maleate shows lower affinities for the muscarinic M₁ (pA₂ = 6.83/6.36; pK_i = 7.08), the M₃ (pA₂ = 6.92/6.96; pK_i = 6.70) and the M₄ receptors (pK_i = 7.00), respectively. (S)-(+)-Dimethindene maleate also is a histamine H₁ receptor antagonist (pA₂ = 7.48) .

HY-159829

Direclidine NBI-1117568; HTL-0016878	mAChR	Neurological Disease
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-109013

Sofpironium bromide BBI 4000	mAChR	Neurological Disease
Sofpironium bromide (BBI 4000) is an anticholinergic agent used in the study of primary axillary hyperhidrosis (PAH). Sofpironium bromide reduces sweating by inhibiting M3 muscarinic receptors in eccrine glands at the application site. Sofpironium bromide also has a high afnity for the M1, M2, M4 and M5 subtypes .

HY-122203

PCS1055 dihydrochloride 2 Publications Verification	mAChR Cholinesterase (ChE)	Neurological Disease
PCS1055 dihydrochloride is a potent, selective and competitive **muscarinic M4 receptor antagonist with an IC₅₀ of 18.1 nM and a K_d** of 5.72 nM. PCS1055 dihydrochloride inhibits radioligand [ ³H]-NMS binding to the M4 receptor with a K_i of 6.5 nM. PCS1055 dihydrochloride exhibits >100-fold selectivity over M1-, M3-, and M5-receptors and 30-fold selectivity at the M2 receptor. PCS1055 dihydrochloride is also a potent AChE inhibitor with IC₅₀ s of 22 nM and 120 nM for electric eel and human AChE, respectively .

HY-N7247

Thiochrome	mAChR	Metabolic Disease
Thiochrome, a natural oxidation product and metabolite of thiamine, is a selective *M4 muscarinic* receptor of acetylcholine (ACh)** affinity enhancer. Thiochrome has neutral cooperativity with ACh at M1 to M3 receptors .

HY-14539A

Clozapine hydrochloride Maximum Cited Publications 11 Publications Verification HF 1854 hydrochloride	Dopamine Receptor mAChR Adrenergic Receptor 5-HT Receptor	Neurological Disease
Clozapine hydrochloride (HF 1854 hydrochloride) is an antipsychotic used for the research of schizophrenia. Clozapine hydrochloride has high affinity for a number of neuroreceptors. Clozapine hydrochloride is a potent antagonist of dopamine D2 with a K_i of 75 nM. Clozapine hydrochloride inhibits the **muscarinic M1 receptor** and serotonin 5HT2A receptor with K_is of 9.5 nM and 4 nM, respectively . Clozapine hydrochloride is also a potent and selective agonist at the **muscarinic M4 receptor (EC₅₀**=11 nM) .

HY-14539R

Clozapine (Standard) Maximum Cited Publications 11 Publications Verification HF 1854 (Standard)	Reference Standards Dopamine Receptor mAChR Adrenergic Receptor 5-HT Receptor	Neurological Disease
Clozapine (Standard) is the analytical standard of Clozapine. This product is intended for research and analytical applications. Clozapine (HF 1854) is an antipsychotic used for the research of schizophrenia. Clozapine has high affinity for a number of neuroreceptors. Clozapine is a potent antagonist of dopamine D2 with a K_i of 75 nM. Clozapine inhibits the **muscarinic M1 receptor** and serotonin 5HT2A receptor with K_is of 9.5 nM and 4 nM, respectively . Clozapine is also a potent and selective agonist at the **muscarinic M4 receptor (EC₅₀**=11 nM) .

HY-70053A

Fesoterodine L-mandelate	mAChR	Neurological Disease Metabolic Disease Cancer
Fesoterodine L-mandelate is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pK_i values of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively. Fesoterodine L-mandelate is used for the overactive bladder (OAB) .

HY-B0527AR

Amitriptyline hydrochloride (Standard) 4 Publications Verification	Reference Standards Serotonin Transporter 5-HT Receptor Histamine Receptor mAChR Adrenergic Receptor Trk Receptor Sodium Channel Potassium Channel Dopamine Transporter Apoptosis	Neurological Disease Inflammation/Immunology Endocrinology
Amitriptyline hydrochloride (Standard) is the analytical standard of Amitriptyline hydrochloride (HY-B0527A). This product is intended for research and analytical applications. Amitriptyline hydrochloride is an orally active tricyclic antidepressant (TCA). Amitriptyline hydrochloride mainly exerts its antidepressant effect by blocking SERT (K_i = 3.45 nM) and NET (K_i = 13.3 nM), thereby increasing the concentrations of 5-hydroxytryptamine (5-HT) and norepinephrine (NE) in the synaptic cleft. Amitriptyline hydrochloride is also an agonist at α2A and TrkA/TrkB receptors, thereby exerting analgesic and neurotrophic activities (inhibiting cell apoptosis). Amitriptyline hydrochloride can reduce inflammation, angiogenesis and fibrosis. Amitriptyline hydrochloride binds to DAT (with K_i = 2.58 μM). Amitriptyline hydrochloride has high affinity for a series of receptors and can antagonize muscarinic cholinergic receptors (M1/M2/M3/M4/M5 receptors) (K_i = 11-24 nM), H1 receptors (K_i = 0.5-1.1 nM), adrenergic α1 receptors (K_i = 4.4 nM), etc., resulting in a series of side effects. Amitriptyline hydrochloride can block sodium channels and hERG potassium channel (IC₅₀ = 4.78 μM) and it has cardiotoxicity.

HY-105182S1

Xanomeline-d3 LY-246708-d₃	Isotope-Labeled Compounds mAChR	Neurological Disease
Xanomeline-d₃ (LY-246708-d₃) is deuterium labeled Xanomeline. 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-B0527AS

Amitriptyline-d6 hydrochloride	Isotope-Labeled Compounds Serotonin Transporter 5-HT Receptor Histamine Receptor mAChR Adrenergic Receptor Trk Receptor Sodium Channel Potassium Channel Dopamine Transporter Apoptosis	Neurological Disease Inflammation/Immunology Endocrinology
Amitriptyline-d₆ hydrochloride is the deuterium labeled Amitriptyline hydrochloride (HY-B0527A). Amitriptyline hydrochloride is an orally active tricyclic antidepressant (TCA). Amitriptyline hydrochloride mainly exerts its antidepressant effect by blocking SERT (K_i = 3.45 nM) and NET (K_i = 13.3 nM), thereby increasing the concentrations of 5-hydroxytryptamine (5-HT) and norepinephrine (NE) in the synaptic cleft. Amitriptyline hydrochloride is also an agonist at α2A and TrkA/TrkB receptors, thereby exerting analgesic and neurotrophic activities (inhibiting cell apoptosis). Amitriptyline hydrochloride can reduce inflammation, angiogenesis and fibrosis. Amitriptyline hydrochloride binds to DAT (with K_i = 2.58 μM). Amitriptyline hydrochloride has high affinity for a series of receptors and can antagonize muscarinic cholinergic receptors (M1/M2/M3/M4/M5 receptors) (K_i = 11-24 nM), H1 receptors (K_i = 0.5-1.1 nM), adrenergic α1 receptors (K_i = 4.4 nM), etc., resulting in a series of side effects. Amitriptyline hydrochloride can block sodium channels and hERG potassium channel (IC₅₀ = 4.78 μM) and it has cardiotoxicity.

HY-107656

PTAC oxalate	mAChR	Neurological Disease
PTAC oxalate is a selective **muscarinic receptor ligand. PTAC oxalate is an partial agonist of M2 and M4 but antagonist of M1, M3, and M5 (K_i** values of 0.2-2.8 nM for hM1-5 in CHO cells). PTAC oxalate alleviates the mechanical allodynia on the neuropathic pain and has antidepression effects .

HY-A0030S

Fesoterodine-d7 fumarate	mAChR	Metabolic Disease
Fesoterodine-d₇ (fumarate) is the deuterium labeled Fesoterodine fumarate . Fesoterodine Fumarate is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pKi values of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively. Fesoterodine Fumarate is used for the overactive bladder (OAB) .

HY-105182AR

Xanomeline tartrate (Standard) LY 246708 tartrate (Standard)	Reference Standards mAChR	Neurological Disease
Xanomeline (tartrate) (Standard) is the analytical standard of Xanomeline (tartrate). This product is intended for research and analytical applications. Xanomeline (LY 246708) is the potent agonist of muscarinic M1/M4 receptor with antipsychotic-like activity. Xanomeline (LY 246708) increases neuronal excitability. Xanomeline (LY 246708) can be used for the research of schizophrenia .

HY-A0270

Diphenidol	mAChR Sodium Channel	Neurological Disease
Diphenidol is a non-selective **muscarinic M₁-M₄ receptor** antagonist, has anti-arrhythmic activity. Diphenidol is also a potent non-specific blocker of voltage-gated ion channels (Na ⁺, K ⁺, and Ca ²⁺) in neuronal cells. Diphenidol can be used in the study of antivertigo and antinausea .

HY-175532

M4 mAChR Modulator-2	mAChR	Neurological Disease
M4 mAChR Modulator-2 is an orally active, selective, brain-penetrant positive allosteric modulator (PAM) of the M4 muscarinic acetylcholine receptor (M4 mAChR) (EC₅₀ = 513 nM). M4 mAChR Modulator-2 exhibits high target selectivity, showing negligible affinity and low inhibition rates for non-target receptors (D1R/D2R/D3R, 5-HT subtypes, κ/δ/μ opioid receptors, H1, M1/M2) while specifically binding to M4 mAChR with a K_i of 377 nM and an inhibition rate of 62.8%. M4 mAChR Modulator-2 reverses Dizocilpine (MK-801) (HY-15084B)-induced hyperlocomotion in mice. M4 mAChR Modulator-2 can be used for the study of schizophrenia

HY-12158

VU0238441	mAChR	Neurological Disease
VU0238441 is a pan muscarinic acetylcholine receptor (mAChR) positive allosteric modulator (PAM) with EC₅₀s of 3.2 μM, 2.8 μM, 2.2 μM, 2.1 μM, >10 μM for M1, M2, M3, M5 and M4, respectively .

HY-A0030R

Fesoterodine fumarate (Standard)	Reference Standards mAChR	Neurological Disease Metabolic Disease Cancer
Fesoterodine (fumarate) (Standard) is the analytical standard of Fesoterodine (fumarate). This product is intended for research and analytical applications. Fesoterodine Fumarate is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pKi values of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively. Fesoterodine Fumarate is used for the overactive bladder (OAB) .

HY-120792

DAU 5884	mAChR	Others
DAU 5884 is a muscarinic receptor antagonist with activity that discriminates between different muscarinic receptor subtypes. DAU 5884 discriminates between M4 and M2 receptor sites and is a highly potent M1-selective antagonist with specific activity at different muscarinic receptors characterized by radioligand binding studies and functional assays.

HY-122510

Atropine oxide Atropine oxidation	Parasite	Neurological Disease
Atropine Oxide (Atropine oxidation), a derivative of Atropine, acts as a competitive antagonist to the muscarinic acetylcholine receptors M1, M2, M3, M4, and M5, and is utilized in the treatment of specific nerve agent and pesticide poisonings.

HY-119333

NNC 11-1607	mAChR	Neurological Disease
NNC 11-1607 is a selective M1/M4 muscarinic acetylcholine receptor (mAChR) agonist. NNC 11-1607 inhibits Forskolin (HY-15371)-stimulated cAMP accumulation in Chinese hamster ovary cells expressing the human M2 or M4 mAChR. NNC 11-1607 is promising for research of central nervous system disorders, such as Alzheimer’s disease and schizophrenia .

HY-122510A

Atropine oxide hydrochloride Atropine oxidation hydrochloride	mAChR
Atropine Oxide (Atropine oxidation) hydrochloride, a derivative of Atropine, acts as a competitive antagonist to the muscarinic acetylcholine receptors M1, M2, M3, M4, and M5, and is utilized in the treatment of specific nerve agent and pesticide poisonings .

HY-183144

Vedaclidine	mAChR	Neurological Disease Inflammation/Immunology
Vedaclidine is an orally active muscarinic acetylcholine receptor (mAChR) modulator with mixed receptor activity, which activates muscarinic M2 and M4 receptors and blocks muscarinic M1, M3 and M5 receptors. Vedaclidine exerts its activity through interaction with spinal M4 muscarinic receptors, and does not induce hypothermia or excessive salivation. Vedaclidine can be used in research related to pain, neuropathic pain and inflammatory pain states .

HY-105182R

Xanomeline (Standard) LY-246708 (Standard)	Reference Standards mAChR	Neurological Disease
Xanomeline (Standard) is the analytical standard of Xanomeline. This product is intended for research and analytical applications. 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-120184

VU0467485 AZ13713945	mAChR	Neurological Disease
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 EC₅₀*s 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-N7247R

Thiochrome (Standard)	Reference Standards mAChR	Metabolic Disease
Thiochrome (Standard) is the analytical standard of Thiochrome. This product is intended for research and analytical applications. Thiochrome, a natural oxidation product and metabolite of thiamine, is a selective M4 muscarinic receptor of acetylcholine (ACh) affinity enhancer. Thiochrome has neutral cooperativity with ACh at M1 to M3 receptors .

HY-167849

Sofpironium tosylate BBI-4000 tosylate	mAChR	Neurological Disease
Sofpironium (BBI 4000) tosylate is an anticholinergic agent used in the study of primary axillary hyperhidrosis (PAH). Sofpironium tosylate reduces sweating by inhibiting M3 muscarinic receptors in eccrine glands at the application site. Sofpironium tosylate also has a high afnity for the M1, M2, M4 and M5 subtypes .

HY-14539B

Clozapine dihydrochloride HF 1854 dihydrochloride	Dopamine Receptor mAChR Adrenergic Receptor 5-HT Receptor	Neurological Disease Cancer
Clozapine (HF 1854) dihydrochloride is an antipsychotic used for the research of schizophrenia. Clozapine has high affinity for a number of neuroreceptors. Clozapine is a potent antagonist of dopamine D2 with a K_i of 75 nM. Clozapine inhibits the **muscarinic M1 receptor** and serotonin 5HT2A receptor with K_is of 9.5 nM and 4 nM, respectively . Clozapine is also a potent and selective agonist at the **muscarinic M4 receptor (EC₅₀**=11 nM) .

HY-A0082R

Diphenidol hydrochloride (Standard) Difenidol hydrochloride (Standard)	Reference Standards mAChR Sodium Channel	Neurological Disease
Diphenidol (hydrochloride) (Standard) is the analytical standard of Diphenidol (hydrochloride). This product is intended for research and analytical applications. Diphenidol hydrochloride (Difenidol hydrochloride) is a non-selective muscarinic M1-M4 receptor antagonist, has anti-arrhythmic activity. Diphenidol hydrochloride is also a potent non-specific blocker of voltage-gated ion channels (Na+, K+, and Ca2+) in neuronal cells. Diphenidol hydrochloride can be used in the study of antivertigo and antinausea [4] .

HY-70053S

rac-Fesoterodine-d14 fumarate	Isotope-Labeled Compounds mAChR	Neurological Disease Metabolic Disease
(Rac)-Fesoterodine-d₁₄ fumarate is a labelled racemic Fesoterodine. Fesoterodine is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pK_ivalues of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively. Fesoterodine is used for the overactive bladder (OAB) .

HY-A0082S

Diphenidol-d10 hydrochloride Difenidol hydrochloride-d₁₀	Isotope-Labeled Compounds Sodium Channel mAChR	Neurological Disease
Diphenidol-d₁₀ (hydrochloride) (Difenidol hydrochloride-d₁₀) is deuterium labeled Diphenidol (hydrochloride). Diphenidol hydrochloride (Difenidol hydrochloride) is a non-selective **muscarinic M₁-M₄ receptor** antagonist, has anti-arrhythmic activity. Diphenidol hydrochloride is also a potent non-specific blocker of voltage-gated ion channels (Na ⁺, K ⁺, and Ca ²⁺) in neuronal cells. Diphenidol hydrochloride can be used in the study of antivertigo and antinausea .

HY-W720879

Fesoterodine-d3	Isotope-Labeled Compounds mAChR	Metabolic Disease
Fesoterodine-d₃ is the deuterium labeled Fesoterodine (HY-70053). Fesoterodine is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pKi values of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively. Fesoterodine is used for the overactive bladder (OAB) .

HY-14539S3

Clozapine-d3 HF 1854-d₃	Isotope-Labeled Compounds 5-HT Receptor Adrenergic Receptor Dopamine Receptor mAChR	Neurological Disease Cancer
Clozapine-d₃ (HF 1854-d₃) is deuterium labeled Clozapine. Clozapine (HF 1854) is an antipsychotic used for the research of schizophrenia. Clozapine has high affinity for a number of neuroreceptors. Clozapine is a potent antagonist of dopamine D2 with a K_i of 75 nM. Clozapine inhibits the **muscarinic M1 receptor** and serotonin 5HT2A receptor with K_is of 9.5 nM and 4 nM, respectively . Clozapine is also a potent and selective agonist at the **muscarinic M4 receptor (EC₅₀**=11 nM) .

HY-107650

Milameline hydrochloride CI 979 hydrochloride; RU 35926 hydrochloride	mAChR	Neurological Disease
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-135460

Milameline CI-979; RU35926	mAChR	Neurological Disease
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-P5846

Muscarinic toxin 3 MT3	mAChR Adrenergic Receptor	Neurological Disease
Muscarinic toxin 3 (MT3) is a potent and non-competitive mAChR and adrenoceptors antagonist with pIC₅₀s of 6.71, 8.79, 8.86, 7.57, 8.13, 8.49, <6.5, 7.29 against M₁, M₄, α_1A, α_1B, α_1D,α_2A,α_2B and α_2C receptors, respectively. Muscarinic toxin 3 displays prominent adrenoceptor activity .

HY-B0298AS

Clemastine-d5 fumarate 1 Publications Verification HS-592-d5 fumarate; Meclastine-d5 fumarate	Isotope-Labeled Compounds Histamine Receptor Apoptosis mAChR Pyroptosis Keap1-Nrf2 p62 Autophagy mTOR IKK	Neurological Disease Metabolic Disease
Clemastine (HS-592; Meclastine)-d₅ fumarate is the deuterium labeled Clemastine fumarate. Clemastine fumarate is an orally active, blood-brain barrier-permeable H1 histamine receptor (H1 histamine receptor) antagonist with potent antiallergic effects. Clemastine fumarate also antagonizes muscarinic acetylcholine receptors (mAChR), particularly the M1 and M4 subtypes. In addition to antihistamine effects, Clemastine fumarate exhibits multiple pharmacological activities, especially in promoting central nervous system remyelination, activating autophagy and pyroptosis, exerting anti-apoptotic and neuroprotective effects, and suppressing inflammation .

HY-B0298AR

Clemastine fumarate (Standard) HS-592 fumarate (Standard); Meclastine fumarate (Standard)	Reference Standards Histamine Receptor Apoptosis mAChR Pyroptosis Keap1-Nrf2 p62 Autophagy mTOR IKK	Neurological Disease Metabolic Disease
Clemastine (HS-592; Meclastine) fumarate (Standard) is the analytical standard of Clemastine fumarate. This product is intended for research and analytical applications. Clemastine fumarate is an orally active, blood-brain barrier-permeable H1 histamine receptor (H1 histamine receptor) antagonist with potent antiallergic effects. Clemastine fumarate also antagonizes muscarinic acetylcholine receptors (mAChR), particularly the M1 and M4 subtypes. In addition to antihistamine effects, Clemastine fumarate exhibits multiple pharmacological activities, especially in promoting central nervous system remyelination, activating autophagy and pyroptosis, exerting anti-apoptotic and neuroprotective effects, and suppressing inflammation .

HY-123778

VU6007678	mAChR	Neurological Disease
VU6007678 is a CNS-penetrant muscarinic acetylcholine receptor (mAChR) modulator. VU6007678 potentiates acetylcholine-mediated signaling at human M1, M3, M5 and rat M1, M3, M4, M5 muscarinic acetylcholine receptors. VU6007678 is applicable to research related to Alzheimer's disease, schizophrenia, and ischemic stroke .

Cat. No.	상품명	Target	Research Area

HY-P5846

Muscarinic toxin 3 MT3	mAChR Adrenergic Receptor	Neurological Disease
Muscarinic toxin 3 (MT3) is a potent and non-competitive mAChR and adrenoceptors antagonist with pIC₅₀s of 6.71, 8.79, 8.86, 7.57, 8.13, 8.49, <6.5, 7.29 against M₁, M₄, α_1A, α_1B, α_1D,α_2A,α_2B and α_2C receptors, respectively. Muscarinic toxin 3 displays prominent adrenoceptor activity .

Cat. No.	상품명	Chemical Structure

HY-105182S1

Xanomeline-d3
Xanomeline-d₃ (LY-246708-d₃) is deuterium labeled Xanomeline. 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-B0527AS

Amitriptyline-d6 hydrochloride

Amitriptyline-d₆ hydrochloride is the deuterium labeled Amitriptyline hydrochloride (HY-B0527A). Amitriptyline hydrochloride is an orally active tricyclic antidepressant (TCA). Amitriptyline hydrochloride mainly exerts its antidepressant effect by blocking SERT (K_i = 3.45 nM) and NET (K_i = 13.3 nM), thereby increasing the concentrations of 5-hydroxytryptamine (5-HT) and norepinephrine (NE) in the synaptic cleft. Amitriptyline hydrochloride is also an agonist at α2A and TrkA/TrkB receptors, thereby exerting analgesic and neurotrophic activities (inhibiting cell apoptosis). Amitriptyline hydrochloride can reduce inflammation, angiogenesis and fibrosis. Amitriptyline hydrochloride binds to DAT (with K_i = 2.58 μM). Amitriptyline hydrochloride has high affinity for a series of receptors and can antagonize muscarinic cholinergic receptors (M1/M2/M3/M4/M5 receptors) (K_i = 11-24 nM), H1 receptors (K_i = 0.5-1.1 nM), adrenergic α1 receptors (K_i = 4.4 nM), etc., resulting in a series of side effects. Amitriptyline hydrochloride can block sodium channels and hERG potassium channel (IC₅₀ = 4.78 μM) and it has cardiotoxicity.

HY-A0030S

Fesoterodine-d7 fumarate
Fesoterodine-d₇ (fumarate) is the deuterium labeled Fesoterodine fumarate . Fesoterodine Fumarate is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pKi values of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively. Fesoterodine Fumarate is used for the overactive bladder (OAB) .

HY-70053S

rac-Fesoterodine-d14 fumarate
(Rac)-Fesoterodine-d₁₄ fumarate is a labelled racemic Fesoterodine. Fesoterodine is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pK_ivalues of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively. Fesoterodine is used for the overactive bladder (OAB) .

HY-A0082S

Diphenidol-d10 hydrochloride

Diphenidol-d₁₀ (hydrochloride) (Difenidol hydrochloride-d₁₀) is deuterium labeled Diphenidol (hydrochloride). Diphenidol hydrochloride (Difenidol hydrochloride) is a non-selective muscarinic M₁-M₄ receptor antagonist, has anti-arrhythmic activity. Diphenidol hydrochloride is also a potent non-specific blocker of voltage-gated ion channels (Na ⁺, K ⁺, and Ca ²⁺) in neuronal cells. Diphenidol hydrochloride can be used in the study of antivertigo and antinausea .

HY-W720879

Fesoterodine-d3
Fesoterodine-d₃ is the deuterium labeled Fesoterodine (HY-70053). Fesoterodine is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pKi values of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively. Fesoterodine is used for the overactive bladder (OAB) .

HY-14539S3

Clozapine-d3

Clozapine-d₃ (HF 1854-d₃) is deuterium labeled Clozapine. Clozapine (HF 1854) is an antipsychotic used for the research of schizophrenia. Clozapine has high affinity for a number of neuroreceptors. Clozapine is a potent antagonist of dopamine D2 with a K_i of 75 nM. Clozapine inhibits the muscarinic M1 receptor and serotonin 5HT2A receptor with K_is of 9.5 nM and 4 nM, respectively . Clozapine is also a potent and selective agonist at the muscarinic M4 receptor (EC₅₀=11 nM) .

HY-B0298AS

Clemastine-d5 fumarate

1 Publications Verification

Clemastine (HS-592; Meclastine)-d₅ fumarate is the deuterium labeled Clemastine fumarate. Clemastine fumarate is an orally active, blood-brain barrier-permeable H1 histamine receptor (H1 histamine receptor) antagonist with potent antiallergic effects. Clemastine fumarate also antagonizes muscarinic acetylcholine receptors (mAChR), particularly the M1 and M4 subtypes. In addition to antihistamine effects, Clemastine fumarate exhibits multiple pharmacological activities, especially in promoting central nervous system remyelination, activating autophagy and pyroptosis, exerting anti-apoptotic and neuroprotective effects, and suppressing inflammation .

HY-105182S

Xanomeline-d11
Xanomeline-d₁₁ (LY-246708-d₁₁) is the deuterium labeled Xanomeline (HY-105182). 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-109013S

Sofpironium-13C,d3 bromide

Sofpironium- ¹³C,d₃ bromide (BBI 4000- ¹³C,d₃) is the deuterium and ¹³C-labeled Sofpironium bromide (HY-109013). Sofpironium bromide (BBI 4000) is an anticholinergic agent used in the study of primary axillary hyperhidrosis (PAH). Sofpironium bromide reduces sweating by inhibiting M3 muscarinic receptors in eccrine glands at the application site. Sofpironium bromide also has a high afnity for the M1, M2, M4 and M5 subtypes .

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