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muscle-relaxant

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (2) Adrenergic Receptor (9) Akt (7) Apoptosis (14) Autophagy (2) Biochemical Assay Reagents (2) Calcium Channel (11) Caspase (2) Cholinesterase (ChE) (9) COX (5) Cytochrome P450 (3) DNA Methyltransferase (5) Drug Derivative (6) Drug Intermediate (2) Drug Metabolite (5) Endogenous Metabolite (7) Environmental Pollutants (1) ERK (1) GABA Receptor (19) Glutathione Reductase (GR) (1) Heme Oxygenase (HO) (1) Histamine Receptor (2) iGluR (14) Isotope-Labeled Compounds (21) Keap1-Nrf2 (1) mAChR (9) MEK (1) MMP (1) nAChR (9) NF-κB (4) NO Synthase (5) P2X Receptor (1) Parasite (1) PGC-1α (4) PGE synthase (5) Phosphodiesterase (PDE) (1) PI3K (1) Platelet-activating Factor Receptor (PAFR) (1) Potassium Channel (8) Prostaglandin Receptor (1) Ras (1) Reactive Oxygen Species (ROS) (6) Reference Standards (27) Sodium Channel (7) Wnt (6) β-catenin (6)
By Research Areas:	Cancer (20) Cardiovascular Disease (11) Endocrinology (6) Infection (1) Inflammation/Immunology (28) Metabolic Disease (5) Neurological Disease (107)

By Targets:

5-HT Receptor (2)

Adrenergic Receptor (9)

Akt (7)

Apoptosis (14)

Autophagy (2)

Biochemical Assay Reagents (2)

Calcium Channel (11)

Caspase (2)

Cholinesterase (ChE) (9)

COX (5)

Cytochrome P450 (3)

DNA Methyltransferase (5)

Drug Derivative (6)

Drug Intermediate (2)

Drug Metabolite (5)

Endogenous Metabolite (7)

Environmental Pollutants (1)

ERK (1)

GABA Receptor (19)

Glutathione Reductase (GR) (1)

Heme Oxygenase (HO) (1)

Histamine Receptor (2)

iGluR (14)

Isotope-Labeled Compounds (21)

Keap1-Nrf2 (1)

mAChR (9)

MEK (1)

MMP (1)

nAChR (9)

NF-κB (4)

NO Synthase (5)

P2X Receptor (1)

Parasite (1)

PGC-1α (4)

PGE synthase (5)

Phosphodiesterase (PDE) (1)

PI3K (1)

Platelet-activating Factor Receptor (PAFR) (1)

Potassium Channel (8)

Prostaglandin Receptor (1)

Ras (1)

Reactive Oxygen Species (ROS) (6)

Reference Standards (27)

Sodium Channel (7)

Wnt (6)

β-catenin (6)

By Research Areas:

Cancer (20)

Cardiovascular Disease (11)

Endocrinology (6)

Infection (1)

Inflammation/Immunology (28)

Metabolic Disease (5)

Neurological Disease (107)

132

Inhibitors & Agonists

Biochemical Assay Reagents

Natural
Products

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-17440

Rocuronium Bromide 2 Publications Verification ORG 9426 Bromide	nAChR	Neurological Disease Inflammation/Immunology Cancer
Rocuronium Bromide (ORG 9426 Bromide) is an aminosteroid non-depolarizing neuromuscular blocker or muscle relaxant used in modern anaesthesia, to facilitate endotracheal intubation and to provide skeletal musclerelaxation during surgery or mechanical ventilation.

HY-B0118A

Vecuronium bromide ORG NC 45	nAChR	Neurological Disease Cancer
Vecuronium (ORG NC 45) bromide is a non-depolarizing neuromuscular blocking agent that also acts as a nicotinic acetylcholine receptor (nAChR) inhibitor, a muscle relaxant, and can be used for pre-surgical anesthesia .

HY-B0499A

Otilonium bromide 3 Publications Verification Octylonium bromide; SP63	mAChR	Neurological Disease
Otilonium bromide (OB) is an orally active mAChR inhibitor and smooth muscle relaxant which can interfere with the mobilization of calcium in intestinal smooth muscle, OB can be used for research of irritable bowel syndrome .

HY-W016221

6-Hydroxy Chlorzoxazone 1 Publications Verification	Drug Metabolite	Inflammation/Immunology
6-Hydroxy Chlorzoxazone is a metabolite of Chlorzoxazone (HY-B1462). Chlorzoxazone is a centrally acting muscle relaxant used to treat muscle spasm and the resulting pain or discomfort .

HY-B1139

Tolperisone hydrochloride 2 Publications Verification	Apoptosis	Neurological Disease
Tolperisone hydrochloride is a centrally acting muscle relaxant studied in neurological disorders causing pathological rhabdomyosclerosis (pyramidal tract injury, multiple sclerosis, myelopathy, encephalomyelitis), spastic paralysis, and other muscle dystonia-related Encephalopathy. Tolperisone hydrochloride also has antiviral activity .

HY-B0262

Methocarbamol 1 Publications Verification	Sodium Channel	Neurological Disease
Methocarbamol is an orally active central muscle relaxant and blocks muscular Nav1.4 channel. Methocarbamol reversibly affects voltage dependence of inactivation of Nav1.4 channel. Methocarbamol has the potential for muscle spasms and pain syndromes research .

HY-B1833

Afloqualone HQ-495	GABA Receptor	Neurological Disease
Afloqualone (HQ-495) is an orally active central muscle relaxant and antivertiginous agent that can increase the sensitivity of GABA receptors in neurons of the lateral vestibular nucleus. Afloqualone (HQ-495) can be used in the research of low back pain and neck-arm-shoulder syndrome .

HY-B0353

Chlormezanone	GABA Receptor	Neurological Disease
Chlormezanone resembles benzodiazepine. The action of Chlormezanone is similar to benzodiazepine-type agents. Chlormezanone is used as an anxiolytic and a muscle relaxant.

HY-N0301

Thiocolchicoside	GABA Receptor	Neurological Disease Inflammation/Immunology
Thiocolchicoside is a competitive γ-aminobutyric acid type A (GAB_AA) receptor antagonist and glycine receptor agonist in the central nervous system. Thiocolchicoside is a semisynthetic sulfur derivative of colchicoside. Thiocolchicoside is a muscle relaxant and has anti-inflammatory, and analgesic properties .

HY-B1700A

Mivacurium dichloride	nAChR	Neurological Disease
Mivacurium dichloride is a benzylisoquinoline derivative and is a short-acting non-depolarizing neuromuscular blocking agent and skeletal muscle relaxant. Mivacurium dichloride couples with the nAChR to reduce or inhibit the depolarizing effect of acetylcholine on the terminal disc of the muscle cell .

HY-107944

Chlorphenesin carbamate Maolate; U 19646	Drug Derivative	Neurological Disease
Chlorphenesin carbamate is a centrally acting skeletal muscle relaxant, as well as a derivate of Chlorphenesin (HY-A0133). Chlorphenesin carbamate can be used for the research of pain and discomfort related to skeletal muscle trauma and inflammation . Chlorphenesin carbamate is a selective blocker of polysynaptic pathways at the spinal and supra-spinal levels . Antinociceptive effect .

HY-101237

DHBP dibromide Diheptylviologen dibromide	Calcium Channel	Cardiovascular Disease Neurological Disease
DHBP dibromide is an inhibitor for calcium release and a muscle relaxant.

HY-B0416

Gallamine Triethiodide	mAChR Adrenergic Receptor	Neurological Disease
Gallamine Triethiodide is a blood-brain barrier-permeable skeletal muscle relaxant. Gallamine Triethiodide induces skeletal muscle paralysis by blocking acetylcholine. Gallamine Triethiodide directly stimulates intracardiac β receptors. Gallamine Triethiodide prolongs the duration of afterdischarge in the cat cerebral cortex. Gallamine Triethiodide can be used in studies related to convulsive disorders .

HY-B1343

Pridinol mesylate	Cholinesterase (ChE)	Neurological Disease
Pridinol mesylate is an orally active, blood-brain permeable, muscarinic acetylcholine receptor (mAChR)-directed muscle relaxant. Pridinol mesylate reduces the conduction of impulses to spinal motor neurons and exerts muscle relaxant activity. Pridinol mesylate inhibits skeletal muscle contractures in diseases of both central and peripheral origin and can be used in research in the field of musculoskeletal diseases .

HY-B0570

Decamethonium Bromide 1 Publications Verification	nAChR	Neurological Disease
Decamethonium Bromide is an acetylcholine receptor inhibitor and muscle relaxant. Decamethonium Bromide first induces depolarization of skeletal muscles, and then binds to postsynaptic acetylcholine receptors to induce persistent paralysis .\n

HY-113920A

Azumolene 3 Publications Verification EU4093 free base	Calcium Channel	Metabolic Disease
Azumolene (EU4093 free base), a Dantrolene analog, is a muscle relaxant. Azumolene is a ryanodine receptor (RyR) modulator and inhibits the calcium-release through ryanodine receptor. Azumolene can be used for malignant hyperthermia research .

HY-N4323

14-Deoxyandrographolide 1 Publications Verification	Calcium Channel Apoptosis Caspase	Neurological Disease Metabolic Disease
14-Deoxyandrographolide is a diterpene with calcium channel blocking activity and acts as a uterine smooth muscle relaxant. 14-Deoxyandrographolide stimulates the release of nitric oxide (NO) in endothelial cells. 14-Deoxyandrographolide gradually desensitizes liver cells to TNF-α mediated apoptosis by inducing the release of TNFRSF1A .

HY-126112

Mephenoxalone	Drug Derivative	Neurological Disease
Mephenoxalone is a muscle relaxant with anti-anxiety activity. Mephenoxalone has neuropharmacologic activity in vivo. Mephenoxalone inhibits neuron transmission and can relax skeletal muscles by inhibiting the reflex arc .

HY-N2005

Cycleanine	Calcium Channel Apoptosis	Cardiovascular Disease Inflammation/Immunology Cancer
Cycleanine is a potent vascular selective Calcium antagonist. Cycleanine has analgesic, muscle relaxant and anti-inflammatory activities. Cycleanine has potential for anti-ovarian cancer acting through the apoptosis pathway .

HY-B2112

Valethamate bromide	mAChR	Neurological Disease
Valethamate bromide is an ester, serving as an effective rapidly acting anticholinergic antispasmodic and muscle relaxant. Valethamate bromide accelerates labor by improving cervical dilation. Valethamate bromide can significantly shorten the labor process and have fewer side effects .

HY-W016414

Triethyl phosphate	Environmental Pollutants Endogenous Metabolite	Cardiovascular Disease
Triethyl phosphate is a versatile phosphate ester compound. Triethyl phosphate induces rapid and short-acting anesthesia, and exhibits hypotensive, smooth muscle relaxant, and cardiac inhibitory effects. Triethyl phosphate also modulates cholinergic toxicity; its anesthetic effect shows sex- and age-dependency in rodents, and it interacts with SKF 525-A (HY-B1311) to alter the duration of anesthesia .

HY-B1230

Camylofine	mAChR	Neurological Disease
Camylofin is an antimuscarinic, is a smooth muscle relaxant

HY-B1462S1

Chlorzoxazone-13C	Cytochrome P450	Inflammation/Immunology
Chlorzoxazone- ¹³C is the ¹³C labeled Chlorzoxazone . Chlorzoxazone is a centrally acting muscle relaxant used to treat muscle spasm and the resulting pain or discomfort .

HY-B1283

Mephenesin	iGluR	Neurological Disease
Mephenesin is an NMDA receptor antagonist. Mephenesin is also a central muscle relaxant with antianxiety, muscle-paralyzing and anticonvulsant effects. Mephenesin acts directly on the skeletal muscle fibres to produce skeletal muscle relaxation. Mephenesin is promising for research of spasticity or painful muscle spasm .

HY-B1462S

Chlorzoxazone-d3	Cytochrome P450	Inflammation/Immunology
Chlorzoxazone-d₃ is the deuterium labeled Chlorzoxazone. Chlorzoxazone is a centrally acting muscle relaxant used to treat muscle spasm and the resulting pain or discomfort. It acts on the spinal cord by depressing reflexes.Chlorzoxazone is currently being used as a marker substrate in vitro/vivo studies to quantify cytochrome P450 2E1 (CYP2E1) activity in humans.

HY-121340

Emylcamate	Others	Neurological Disease
Emylcamate is a potent muscle relaxant. Emylcamate has the potential for the research of neurological diseases .

HY-17033

Rocuronium Org-9426	nAChR	Neurological Disease Cancer
Rocuronium (Org-9426) is an aminosteroid non-depolarizing neuromuscular blocker or muscle relaxant used in modern anaesthesia.

HY-128891

Eperisone	P2X Receptor	Neurological Disease
Eperisone ((±)-Eperisone) is an antispasmodic agent and centrally acting *muscle relaxant* useful in the study of diseases characterized by muscle stiffness and pain. Eperisone acts by relaxing skeletal and vascular smooth muscle, resulting in vasodilation, decreased muscle tone, improved circulation, and inhibition of pain reflexes. Eperisone is also a potent P2X7 receptor antagonist .

HY-B1833R

Afloqualone (Standard) HQ-495 (Standard)	Reference Standards GABA Receptor	Neurological Disease
Afloqualone (Standard) is the analytical standard of Afloqualone. This product is intended for research and analytical applications. Afloqualone (HQ-495) is an orally active central muscle relaxant and antivertiginous agent that can increase the sensitivity of GABA receptors in neurons of the lateral vestibular nucleus. Afloqualone (HQ-495) can be used in the research of low back pain and neck-arm-shoulder syndrome .

HY-106888

CS-722 Free base	Endogenous Metabolite	Neurological Disease
CS-722 Free base is a synthesized centrally acting muscle relaxant, and has a muscle relaxant activity and depressant effectson the spinal reflex . CS-722 Free base inhibits spontaneous inhibitory postsynaptic currents and excitatory postsynaptic currents in hippocampal cultures probably by an inhibition of both sodium and calcium currents .

HY-B1343A

Pridinol	Cholinesterase (ChE)	Neurological Disease
Pridinol is an orally active, blood-brain permeable, muscarinic acetylcholine receptor (mAChR)-directed muscle relaxant. Pridinol reduces the conduction of impulses to spinal motor neurons and exerts muscle relaxant activity. Pridinol inhibits skeletal muscle contractures in diseases of both central and peripheral origin and can be used in research in the field of musculoskeletal diseases .

HY-A0258A

Metubine Metocurine iodide; Dimethylchondrocurarine iodide	nAChR	Neurological Disease
Metubine (Metocurine iodide) is a non-depolarizing muscle relaxant. Metubine has neuromuscular blocking activities .

HY-W748379

Fenyramidol (±)-Phenyramidol	Drug Derivative	Neurological Disease
Fenyramidol is an Aminopyridine derivative. Fenyramidol can be used as a moderately potent, non-narcotic muscle relaxant with concomitant analgesic activity .

HY-B0740S

Cyclobenzaprine-d3 hydrochloride MK130-d3 hydrochloride	Isotope-Labeled Compounds 5-HT Receptor	Neurological Disease
Cyclobenzaprine-d₃ (hydrochloride) is the deuterium labeled Cyclobenzaprine hydrochloride. Cyclobenzaprine hydrochloride (MK130 hydrochloride) is a skeletal muscle relaxant and a central nervous system (CNS) depressant.

HY-B1343R

Pridinol mesylate (Standard)	Reference Standards Cholinesterase (ChE)	Neurological Disease
Pridinol mesylate (Standard) is the analytical standard of Pridinol mesylate (HY-B1343). This product is intended for research and analytical applications. Pridinol mesylate is an orally active, blood-brain permeable, muscarinic acetylcholine receptor (mAChR)-directed muscle relaxant. Pridinol mesylate reduces the conduction of impulses to spinal motor neurons and exerts muscle relaxant activity. Pridinol mesylate inhibits skeletal muscle contractures in diseases of both central and peripheral origin and can be used in research in the field of musculoskeletal diseases .

HY-172338

Chlorzoxazone-N-glucuronide CHZ-N-Glc	Endogenous Metabolite	Others
Chlorzoxazone-N-glucuronide is a phase II metabolite of the skeletal muscle relaxant – Chlorzoxazone. Chlorzoxazone-N-glucuronide can be synthesized via glucuronidation of chlorozoxazone by UGT1A9 .

HY-N0301R

Thiocolchicoside (Standard)	Reference Standards GABA Receptor	Neurological Disease Inflammation/Immunology
Thiocolchicoside (Standard) is the analytical standard of Thiocolchicoside. This product is intended for research and analytical applications. Thiocolchicoside is a competitive γ-aminobutyric acid type A (GAB_AA) receptor antagonist and glycine receptor agonist in the central nervous system. Thiocolchicoside is a semisynthetic sulfur derivative of colchicoside. Thiocolchicoside is a muscle relaxant and has anti-inflammatory, and analgesic properties .

HY-B0499AR

Otilonium bromide (Standard) Octylonium bromide (Standard); SP63 (Standard)	Reference Standards mAChR	Neurological Disease
Otilonium (bromide) (Standard) is the analytical standard of Otilonium (bromide). This product is intended for research and analytical applications. Otilonium bromide (OB) is an orally active mAChR inhibitor and smooth muscle relaxant which can interfere with the mobilization of calcium in intestinal smooth muscle, OB can be used for research of irritable bowel syndrome .

HY-B0262R

Methocarbamol (Standard)	Reference Standards Sodium Channel	Neurological Disease
Methocarbamol (Standard) is the analytical standard of Methocarbamol. This product is intended for research and analytical applications. Methocarbamol is an orally active central muscle relaxant and blocks muscular Nav1.4 channel. Methocarbamol reversibly affects voltage dependence of inactivation of Nav1.4 channel. Methocarbamol has the potential for muscle spasms and pain syndromes research .

HY-N4323R

14-Deoxyandrographolide (Standard)	Reference Standards Calcium Channel Apoptosis Caspase	Neurological Disease Metabolic Disease
14-Deoxyandrographolide (Standard) is the analytical standard of 14-Deoxyandrographolide. 14-Deoxyandrographolide is a diterpene with calcium channel blocking activity and acts as a uterine smooth muscle relaxant. 14-Deoxyandrographolide stimulates the release of nitric oxide (NO) in endothelial cells. 14-Deoxyandrographolide gradually desensitizes liver cells to TNF-α mediated apoptosis by inducing the release of TNFRSF1A .

HY-B1901S

Eperisone-d10 hydrochloride	Isotope-Labeled Compounds	Neurological Disease
Eperisone-d₁₀ (hydrochloride) is the deuterium labeled Eperisone hydrochloride. Eperisone Hydrochloride ((±)-Eperisone hydrochloride) is an antispastic agent used for treatment of diseases characterized by muscle stiffness and pain. It works by relaxing both skeletal muscles and vascularsmooth muscles, thus demonstrating avariety of effects such as reduction ofmyotonia, improvement of circulationand suppression of the pain reflex. Eperisone Hydrochloride ((±)-Eperisone hydrochloride) is a centrally acting muscle relaxant inhibiting the pain reflex pathway, having a vasodilator effect [2 .

HY-100159

Ipenoxazone MLV-6976; NC-1200	Phosphodiesterase (PDE)	Neurological Disease
Ipenoxazone is a potent and centrally acting muscle relaxant.

HY-100159A

Ipenoxazone hydrochloride MLV-6976 hydrochloride; NC-1200 hydrochloride	iGluR	Neurological Disease
Ipenoxazone (MLV-6976) hydrochloride is a potent and centrally acting muscle relaxant.

HY-101808

Doxefazepam SAS-643	GABA Receptor	Neurological Disease
Doxefazepam is a benzodiazepine derivative. It possesses anxiolytic, anticonvulsan and skeletal muscle relaxant properties.

HY-B1139A

Tolperisone	Sodium Channel	Neurological Disease
Tolperisone, a centrally acting muscle relaxant, is utilized for alleviating symptoms of spasticity and muscle spasms.

HY-14895B

Fabomotizole dihydrochloride CM346 dihydrochloride	Endogenous Metabolite	Neurological Disease
Fabomotizole dihydrochloride is an anxiolytic agent. Fabomotizole dihydrochloride produces anxiolytic and neuroprotective effects without any muscle relaxant actions.

HY-165544

Decamethonium chloride	Others	Neurological Disease
Decamethonium chloride is a depolarizing neuromuscular blocking agent that can be used to study the mechanism of action of muscle relaxants .

HY-167650

Fletazepam	GABA Receptor	Neurological Disease
Fletazepam is a benzodiazepine derivative with sedative, anxiolytic and muscle relaxant effects. Fletazepam can be utilized in neurological research .

HY-128469

Inaperisone	GABA Receptor	Neurological Disease
Inaperisone is a centrally acting muscle relaxant. Inaperisone can inhibit the micturition reflex by acting indirectly on GABAB receptors in the brainstem .

HY-169470

Pridinol hydrochloride	Cholinesterase (ChE)	Neurological Disease
Pridinol hydrochloride is the hydrochloride salt form of Pridinol (HY-B1343A). Pridinol hydrochloride is an orally active anticholinergic agent, and acts as muscle relaxant .

Cat. No.	Product Name	Type

HY-77785

2-Amino-5-chlorobenzophenone 1 Publications Verification 5-Chloro-2-aminobenzophenone	Biochemical Assay Reagents
2-Amino-5-chlorobenzophenone (5-Chloro-2-aminobenzophenone) is a chemical intermediate. Derivatives of 2-Amino-5-chlorobenzophenone serve as skeletal muscle relaxants. 2-Amino-5-chlorobenzophenone acts as a starting material for the synthesis of anti-biofilm 2-amino-5-chlorobenzophenone Schiff bases. 2-Amino-5-chlorobenzophenone is applicable to research related to bacterial infections .\n

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N4323

14-Deoxyandrographolide 1 Publications Verification	Structural Classification Acanthaceae Simsia foetida (Cav.) S.F.Blake Terpenoids Diterpenoids Plants Source Classification	Calcium Channel Apoptosis Caspase
14-Deoxyandrographolide is a diterpene with calcium channel blocking activity and acts as a uterine smooth muscle relaxant. 14-Deoxyandrographolide stimulates the release of nitric oxide (NO) in endothelial cells. 14-Deoxyandrographolide gradually desensitizes liver cells to TNF-α mediated apoptosis by inducing the release of TNFRSF1A .

HY-N2005

Cycleanine	Alkaloids Classification of Application Fields Plants Cissampelos pareira Menispermaceae Inflammation/Immunology Disease Research Fields Alkaloid Dimers Source Classification	Calcium Channel Apoptosis
Cycleanine is a potent vascular selective Calcium antagonist. Cycleanine has analgesic, muscle relaxant and anti-inflammatory activities. Cycleanine has potential for anti-ovarian cancer acting through the apoptosis pathway .

HY-106888

CS-722 Free base	Structural Classification Natural Products Neurological Disease Classification of Application Fields Endogenous metabolite Disease Research Fields Source Classification	Endogenous Metabolite
CS-722 Free base is a synthesized centrally acting muscle relaxant, and has a muscle relaxant activity and depressant effectson the spinal reflex . CS-722 Free base inhibits spontaneous inhibitory postsynaptic currents and excitatory postsynaptic currents in hippocampal cultures probably by an inhibition of both sodium and calcium currents .

HY-N4323R

14-Deoxyandrographolide (Standard)	Structural Classification Acanthaceae Simsia foetida (Cav.) S.F.Blake Terpenoids Diterpenoids Plants Source Classification	Reference Standards Calcium Channel Apoptosis Caspase
14-Deoxyandrographolide (Standard) is the analytical standard of 14-Deoxyandrographolide. 14-Deoxyandrographolide is a diterpene with calcium channel blocking activity and acts as a uterine smooth muscle relaxant. 14-Deoxyandrographolide stimulates the release of nitric oxide (NO) in endothelial cells. 14-Deoxyandrographolide gradually desensitizes liver cells to TNF-α mediated apoptosis by inducing the release of TNFRSF1A .

Cat. No.	Product Name	Chemical Structure

HY-B1462S1

Chlorzoxazone-13C
Chlorzoxazone- ¹³C is the ¹³C labeled Chlorzoxazone . Chlorzoxazone is a centrally acting muscle relaxant used to treat muscle spasm and the resulting pain or discomfort .

HY-B1462S

Chlorzoxazone-d3
Chlorzoxazone-d₃ is the deuterium labeled Chlorzoxazone. Chlorzoxazone is a centrally acting muscle relaxant used to treat muscle spasm and the resulting pain or discomfort. It acts on the spinal cord by depressing reflexes.Chlorzoxazone is currently being used as a marker substrate in vitro/vivo studies to quantify cytochrome P450 2E1 (CYP2E1) activity in humans.

HY-B0194S

Tizanidine-d4

Tizanidine-d₄ is the deuterium labeled Tizanidine (HY-B0194). Tizanidine, a skeletal muscle relaxant, is an orally effective central α₂-adrenoceptor agonist (IC₅₀ = 6.9 nmol). Tizanidine primarily exerts muscle relaxation effects by inhibiting the release of excitatory amino acids (glutamate and aspartate) from the presynaptic terminals of spinal cord interneurons. Tizanidine has anti-injury activity and can inhibit gastrointestinal (GI) transport. Tizanidine can inhibit the proliferation, migration, and invasion of lung cancer cells and induce cell apoptosis by upregulating Nischarin and inhibiting the AKT and Wnt3a/β-catenin signaling pathways. Tizanidine can be used to treat spasticity caused by diseases such as multiple sclerosis (MS), stroke, and spinal cord injury (SCI).

HY-B0464S1

Hydralazine-d5 hydrochloride

Hydralazine-d₅ (hydrochloride) is deuterium-labeled Hydralazine (hydrochloride) (HY-B0464). Hydralazine hydrochloride is an orally active, blood-brain barrier-permeable DNA methyltransferase inhibitor with vasodilatory, arterial smooth muscle relaxant and hypotensive activities. Hydralazine hydrochloride reactivates silenced tumor suppressor genes via mediating DNA demethylation, while exerting neuroprotective and anti-inflammatory properties. Hydralazine hydrochloride inhibits NOS-2 (iNOS) and COX-2, and reduces the production of NO and PGE_E2; meanwhile, Hydralazine hydrochloride scavenges reactive oxygen species and inhibits macrophage activation. Hydralazine hydrochloride alleviates motor dysfunction, neuropathic inflammatory pain, and formalin-induced somatic and emotional pain responses. In addition, Hydralazine hydrochloride directly induces DNA strand breaks and sister chromatid exchange, exhibiting certain mutagenic characteristics. Hydralazine hydrochloride has been widely used in studies on hypertension, various cancers (such as cervical cancer, leukemia), spinal cord injury and the mechanisms of inflammatory pain .

HY-B0464S

Hydralazine-d4 hydrochloride

Hydralazine-d4 hydrochloride is the deuterium labeled Hydralazine hydrochloride. Hydralazine hydrochloride is an orally active, blood-brain barrier-permeable DNA methyltransferase inhibitor with vasodilatory, arterial smooth muscle relaxant and hypotensive activities. Hydralazine hydrochloride reactivates silenced tumor suppressor genes via mediating DNA demethylation, while exerting neuroprotective and anti-inflammatory properties. Hydralazine hydrochloride inhibits NOS-2 (iNOS) and COX-2, and reduces the production of NO and PGE_E2; meanwhile, Hydralazine hydrochloride scavenges reactive oxygen species and inhibits macrophage activation. Hydralazine hydrochloride alleviates motor dysfunction, neuropathic inflammatory pain, and formalin-induced somatic and emotional pain responses. In addition, Hydralazine hydrochloride directly induces DNA strand breaks and sister chromatid exchange, exhibiting certain mutagenic characteristics. Hydralazine hydrochloride has been widely used in studies on hypertension, various cancers (such as cervical cancer, leukemia), spinal cord injury and the mechanisms of inflammatory pain .

HY-B0740S

Cyclobenzaprine-d3 hydrochloride
Cyclobenzaprine-d₃ (hydrochloride) is the deuterium labeled Cyclobenzaprine hydrochloride. Cyclobenzaprine hydrochloride (MK130 hydrochloride) is a skeletal muscle relaxant and a central nervous system (CNS) depressant.

HY-B1901S

Eperisone-d10 hydrochloride

Eperisone-d₁₀ (hydrochloride) is the deuterium labeled Eperisone hydrochloride. Eperisone Hydrochloride ((±)-Eperisone hydrochloride) is an antispastic agent used for treatment of diseases characterized by muscle stiffness and pain. It works by relaxing both skeletal muscles and vascularsmooth muscles, thus demonstrating avariety of effects such as reduction ofmyotonia, improvement of circulationand suppression of the pain reflex. Eperisone Hydrochloride ((±)-Eperisone hydrochloride) is a centrally acting muscle relaxant inhibiting the pain reflex pathway, having a vasodilator effect [2 .

HY-B1343AS

Pridinol-d5

Pridinol-d₅ is deuterium labeled Pridinol (HY-B1343A) . Pridinol is an orally active, blood-brain permeable, muscarinic acetylcholine receptor (mAChR)-directed muscle relaxant. Pridinol reduces the conduction of impulses to spinal motor neurons and exerts muscle relaxant activity. Pridinol inhibits skeletal muscle contractures in diseases of both central and peripheral origin and can be used in research in the field of musculoskeletal diseases .

HY-B0262S

Methocarbamol-d5
Methocarbamol-d₅ is deuterium labeled Methocarbamol. Methocarbamol is an orally active central muscle relaxant and blocks muscular Nav1.4 channel .

HY-B0262S1

Methocarbamol-d3
Methocarbamol-d₃ is the deuterium labeled Methocarbamol. Methocarbamol is an orally active central muscle relaxant and blocks muscular Nav1.4 channel. Methocarbamol reversibly affects voltage dependence of inactivation of Nav1.4 channel. Methocarbamol has the potential for muscle spasms and pain syndromes research .

HY-W016221S1

6-Hydroxy Chlorzoxazone-15N,d2
6-Hydroxy Chlorzoxazone- ¹⁵N,d₂ is the ¹⁵N and deuterium labeled 6-Hydroxy Chlorzoxazone (HY-W016221). 6-Hydroxy Chlorzoxazone is a metabolite of Chlorzoxazone (HY-B1462). Chlorzoxazone is a centrally acting muscle relaxant used to treat muscle spasm and the resulting pain or discomfort .

HY-B1283S

Mephenesin-d3
Mephenesin-d₃ is deuterium labeled Mephenesin. Mephenesin is an NMDA receptor antagonist. Mephenesin is also a central muscle relaxant with antianxiety, muscle-paralyzing and anticonvulsant effects. Mephenesin acts directly on the skeletal muscle fibres to produce skeletal muscle relaxation. Mephenesin is promising for research of spasticity or painful muscle spasm .

HY-B0262S2

Methocarbamol-13C,d3
Methocarbamol- ¹³C,d₃ is the ¹³C- and deuterium labeled Methocarbamol. Methocarbamol is an orally active central muscle relaxant and blocks muscular Nav1.4 channel. Methocarbamol reversibly affects voltage dependence of inactivation of Nav1.4 channel. Methocarbamol has the potential for muscle spasms and pain syndromes research .

HY-12542S

Dantrolene-13C3

Dantrolene- ¹³C₃ is the ¹³C₃ labeled Dantrolene. Dantrolene (F368), a muscle relaxant, non-competitively inhibits human erythrocyte glutathione reductase. Ki and IC50 values are 111.6 μM and 52.3 μM, respectively. Dantrolene is a ryanodine receptor antagonist and Ca2+ signaling stabilizer. Dantrolene can be used for the research of muscle spasticity, malignant hyperthermia, Huntington's disease and other neuroleptic malignant syndrome.

HY-B1833S

Afloqualone-d7
Afloqualone-d₇ (HQ-495-d₇) is deuterium labeled Afloqualone. Afloqualone (HQ-495) is an orally active central muscle relaxant and antivertiginous agent that can increase the sensitivity of GABA receptors in neurons of the lateral vestibular nucleus. Afloqualone (HQ-495) can be used in the research of low back pain and neck-arm-shoulder syndrome .

HY-B0678S

Metaxalone-d3

Metaxalone-d₃ is the deuterium labeled Metaxalone. Metaxalone (AHR438; NSC170959) is an FDA-approved muscle relaxant. Metaxalone acts mainly on the central nervous system and achieves muscle relaxation by inhibiting polysynaptic reflex arcs. In addition, Metaxalone is an inhibitor of MAO-A, which has anti-inflammatory and antioxidant effects. Metaxalone inhibits IL-1β-induced inflammatory phenotype, modulates NF-κB and other related signaling pathways, and decreases MAO-A expression and activity in IL-1β-treated microglia .

HY-B0678S1

Metaxalone-d6

Metaxalone-d₆ is deuterium labeled Metaxalone. Metaxalone (AHR438; NSC170959) is an FDA-approved muscle relaxant. Metaxalone acts mainly on the central nervous system and achieves muscle relaxation by inhibiting polysynaptic reflex arcs. In addition, Metaxalone is an inhibitor of MAO-A, which has anti-inflammatory and antioxidant effects. Metaxalone inhibits IL-1β-induced inflammatory phenotype, modulates NF-κB and other related signaling pathways, and decreases MAO-A expression and activity in IL-1β-treated microglia .

HY-B0194AS

Tizanidine-d4 hydrochloride

Tizanidine-d₄ hydrochloride is deuterium labeled Tizanidine hydrochloride (HY-B0194A). Tizanidine hydrochloride, a skeletal muscle relaxant, is an orally effective central α₂-adrenoceptor agonist (IC₅₀ = 6.9 nmol). Tizanidine hydrochloride primarily exerts muscle relaxation effects by inhibiting the release of excitatory amino acids (glutamate and aspartate) from the presynaptic terminals of spinal cord interneurons. Tizanidine hydrochloride has anti-injury activity and can inhibit gastrointestinal (GI) transport. Tizanidine hydrochloride can inhibit the proliferation, migration, and invasion of lung cancer cells and induce cell apoptosis by upregulating Nischarin and inhibiting the AKT and Wnt3a/β-catenin signaling pathways. Tizanidine hydrochloride can be used to treat spasticity caused by diseases such as multiple sclerosis (MS), stroke, and spinal cord injury (SCI).

HY-W016221S

6-Hydroxy Chlorzoxazone-d2
6-Hydroxy Chlorzoxazone-d₂ is deuterium labeled 6-Hydroxy Chlorzoxazone. 6-Hydroxy Chlorzoxazone is a metabolite of Chlorzoxazone (HY-B1462). Chlorzoxazone is a centrally acting muscle relaxant used to treat muscle spasm and the resulting pain or discomfort .

HY-B1139S

Tolperisone-d10 hydrochloride

Tolperisone-d₁₀ (hydrochloride) is the deuterium labeled Tolperisone hydrochloride. Tolperisone hydrochloride is a centrally acting muscle relaxant, is indicated for use in the treatment of pathologically increased tone of the cross-striated muscle caused by neurological diseases (damage of the pyramidal tract, multiple sclerosis, myelopathy, encephalomyelitis) and of spastic paralysis and other encephalopathies manifested with muscular dystonia.

HY-W709349S

Flupirtine-d6 hydrochloride

Flupirtine-d₆ (D 9998-d₆) hydrochloride is the deuterium labeled Flupirtine hydrochloride (HY-W709349). Flupirtine hydrochloride is an orally active, blood-brain barrier-crossing non-opioid analgesic and neuroprotective agent. Flupirtine hydrochloride is a neuronal potassium channel opener (Kv7 activator), a NMDA receptor antagonist and a GABA receptor activator. Flupirtine hydrochloride stabilizes blood-brain-barrier integrity, reduces oxidative stress and brain leukocyte infiltration, enhances angioneurogenesis, suppresses calcium influx, stabilizes neuronal resting membrane potential, and counteracts focal cerebral ischemia. Flupirtine hydrochloride exhibits analgesic, muscle relaxant properties, protects neurons from excitotoxic, ischemic, or cytokine-mediated death. Flupirtine hydrochloride functions as a non-opioid analgesic without antipyretic or antiphlogistic properties, shows no relevant affinity to opiate receptor. Flupirtine hydrochloride can be used for the research of focal cerebral ischemia, pain, Alzheimer’s disease, or multiple sclerosis .

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