Search Result
Results for "
cholinergic activity
" in MedChemExpress (MCE) Product Catalog:
2
Biochemical Assay Reagents
8
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-B0282
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ACh chloride
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nAChR
Calcium Channel
Endogenous Metabolite
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Infection
Neurological Disease
Cancer
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Acetylcholine chloride (ACh chloride), a neurotransmitter, is a potent and BBB-permeable cholinergic agonist. Acetylcholine chloride is a modulator of the activity of dopaminergic (DAergic) neurons through the stimulation of nicotinic acetylcholine receptors (nAChRs) . Acetylcholine chloride inhibits p53 mutant peptide aggregation in vitro .
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- HY-B0527A
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Serotonin Transporter
5-HT Receptor
mAChR
Histamine Receptor
Adrenergic Receptor
Trk Receptor
Sodium Channel
Potassium Channel
Dopamine Transporter
Apoptosis
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Neurological Disease
Inflammation/Immunology
Endocrinology
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Amitriptyline hydrochloride is an orally active tricyclic antidepressant (TCA). Amitriptyline hydrochloride mainly exerts its antidepressant effect by blocking SERT (Ki = 3.45 nM) and NET (Ki = 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 Ki = 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) (Ki = 11-24 nM), H1 receptors (Ki = 0.5-1.1 nM), adrenergic α1 receptors (Ki = 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 .
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- HY-B0527
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Serotonin Transporter
Trk Receptor
Sodium Channel
5-HT Receptor
Histamine Receptor
Adrenergic Receptor
mAChR
Potassium Channel
Dopamine Transporter
Apoptosis
|
Neurological Disease
Inflammation/Immunology
Endocrinology
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|
Amitriptyline is an orally active tricyclic antidepressant (TCA). Amitriptyline mainly exerts its antidepressant effect by blocking SERT (Ki = 3.45 nM) and NET (Ki = 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 Ki = 2.58 μM). Amitriptyline has high affinity for a series of receptors and can antagonize muscarinic cholinergic receptors (M1/M2/M3/M4/M5 receptors) (Ki = 11-24 nM), H1 receptors (Ki = 0.5-1.1 nM), adrenergic α1 receptors (Ki = 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 .
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- HY-B0461
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mAChR
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Neurological Disease
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Trospium chloride is an orally active, specific and competitive antagonist of muscarinic cholinergic receptors (mAChRs), with antimuscarinic activity. Trospium chloride binds to muscarinic receptors M1, M2 and M3 with high affinity, but not nicotinic, cholinergic receptors .
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- HY-B0282S
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ACh-d4 chloride
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nAChR
Calcium Channel
Endogenous Metabolite
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Neurological Disease
Cancer
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Acetylcholine-d4 (chloride) is the deuterium labeled Acetylcholine chloride. Acetylcholine chloride (ACh chloride), a neurotransmitter, is a potent and BBB-permeable cholinergic agonist. Acetylcholine chloride is a modulator of the activity of dopaminergic (DAergic) neurons through the stimulation of nicotinic acetylcholine receptors (nAChRs) . Acetylcholine chloride inhibits p53 mutant peptide aggregation in vitro .
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- HY-B1277
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mAChR
Cholinesterase (ChE)
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Neurological Disease
|
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Trihexyphenidyl hydrochloride is a selective and orally active M1 muscarinic receptor antagonist with an IC50 of 3.7 nM for rat cerebral cortex M1 muscarinic receptors. Trihexyphenidyl hydrochloride modulates cholinergic activity, countering acetylcholine supersensitivity in neural pathways. Trihexyphenidyl hydrochloride improves movement disorder, inhibits McN-A-343 (HY-107648)-induced pressor responses, vagally-induced bradycardia and vasodilatation. Trihexyphenidyl hydrochloride can be used for the research of Parkinson's disease. .
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- HY-B1693
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Methotrimeprazine
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5-HT Receptor
Dopamine Receptor
Histamine Receptor
Autophagy
Enterovirus
Calcium Channel
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Infection
Neurological Disease
Inflammation/Immunology
|
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Levomepromazine (Methotrimeprazine) is an orally active antipsychotic compound and Ca 2+ release inducer. Levomepromazine inhibits SERCA pump and induces an increase in cytoplasmic Ca 2+ levels. Levomepromazine has antagonistic effects on a variety of neurotransmitter receptors, including dopamine, cholinergic, serotonin, and histamine receptors. Levomepromazine can induce adaptive ER stress and autophagy. In addition, Levomepromazine has antiviral, anti-inflammatory, neuroprotective and analgesic, sedative and anti-injurious activities. Levomepromazine can be used in the study psychiatric disorders and relieving nausea and vomiting .
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- HY-B0170A
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Azatadine maleate
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Histamine Receptor
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Inflammation/Immunology
Endocrinology
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Azatadine dimaleate (Azatadine maleate) is an inhibitor of histamine and cholinergic with an IC50 of 6. Azatadine dimaleate has additional antiserotonin activity. Azatadine dimaleate can be studied in research on perennial allergic rhinitis .
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- HY-B0282S1
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ACh-d9 chloride
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nAChR
Calcium Channel
Endogenous Metabolite
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Neurological Disease
Cancer
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Acetylcholine-d9 (chloride) is the deuterium labeled Acetylcholine chloride. Acetylcholine chloride (ACh chloride), a neurotransmitter, is a potent and BBB-permeable cholinergic agonist. Acetylcholine chloride is a modulator of the activity of dopaminergic (DAergic) neurons through the stimulation of nicotinic acetylcholine receptors (nAChRs) . Acetylcholine chloride inhibits p53 mutant peptide aggregation in vitro .
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- HY-NP143
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Biochemical Assay Reagents
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Neurological Disease
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Nerve Growth Factor 2.5S, murine submaxillary gland is a neurotrophic polypeptide required for normal growth and development of sympathetic and embryonic sensory neurons and certain cholinergic neurons in the central nervous system. Nerve Growth Factor 2.5S, murine submaxillary gland has only β-subunit , and shows nerve growth-promoting activity .
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- HY-B0282R
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ACh chloride (Standard)
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Reference Standards
nAChR
Calcium Channel
Endogenous Metabolite
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Neurological Disease
Cancer
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Acetylcholine (chloride) (Standard) is the analytical standard of Acetylcholine (chloride). This product is intended for research and analytical applications. Acetylcholine chloride (ACh chloride), a neurotransmitter, is a potent and BBB-permeable cholinergic agonist. Acetylcholine chloride is a modulator of the activity of dopaminergic (DAergic) neurons through the stimulation of nicotinic acetylcholine receptors (nAChRs) . Acetylcholine chloride inhibits p53 mutant peptide aggregation in vitro .
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- HY-B0461R
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mAChR
Reference Standards
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Neurological Disease
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Trospium (chloride) (Standard) is the analytical standard of Trospium (chloride). This product is intended for research and analytical applications. Trospium chloride is an orally active, specific and competitive antagonist of muscarinic cholinergic receptors (mAChRs), with antimuscarinic activity. Trospium chloride binds to muscarinic receptors M1, M2 and M3 with high affinity, but not nicotinic, cholinergic receptors .
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- HY-W127699
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N,N,N-Trimethyl-2-(propionyloxy)ethanaminium (p-toluenesulfonate)
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Biochemical Assay Reagents
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Others
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Propionylcholine (p-toluenesulfonate) is an organic compound commonly used in biochemical research and neuroscience research. It can be used to study cholinergic signal transduction and esterase activity, and is widely used in biomedical research and pharmacological research. In addition, this compound is also used as a substrate or catalyst in certain biochemical reactions.
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- HY-N0801
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MMP
Cholinesterase (ChE)
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Neurological Disease
Inflammation/Immunology
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Polygalacic acid, is a triterpene, isolated from the root of Polygala tenuifolia Willd. Polygalacic acid inhibits MMP expression. Polygalacic acid may have a therapeutic effect in Osteoarthritis (OA) treatment .
Polygalacic acid exerts a significant neuroprotective effect on cognitive impairment, PA improves cholinergic system reactivity by inhibiting acetylcholinesterase (AChE) activity, increasing choline acetyltransferase (ChAT) activity, and elevating levels of acetylcholine (Ach) in the hippocampus and frontal cortex .
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- HY-B0527AR
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Reference Standards
Serotonin Transporter
5-HT Receptor
Histamine Receptor
mAChR
Adrenergic Receptor
Trk Receptor
Sodium Channel
Potassium Channel
Dopamine Transporter
Apoptosis
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Neurological Disease
Inflammation/Immunology
Endocrinology
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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 (Ki = 3.45 nM) and NET (Ki = 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 Ki = 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) (Ki = 11-24 nM), H1 receptors (Ki = 0.5-1.1 nM), adrenergic α1 receptors (Ki = 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.
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- HY-B2198
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Actinomin chloride
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Cholinesterase (ChE)
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Neurological Disease
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Carpronium (Actinomin) chloride is an orally active cholinergic agonist, local vasodilator and parasympathomimetic agent. Carpronium chloride is structurally similar to acetylcholine. Carpronium chloride promotes hair growth, and oral overdose induces cholinergic crisis. Carpronium chloride is applicable to research related to alopecia areata .
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- HY-B0461S
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Isotope-Labeled Compounds
mAChR
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Neurological Disease
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Trospium-d8 (chloride) is the deuterium labeled Trospium chloride. Trospium chloride is an orally active, specific and competitive antagonist of muscarinic cholinergic receptors (mAChRs), with antimuscarinic activity. Trospium chloride binds to muscarinic receptors M1, M2 and M3 with high affinity, but not nicotinic, cholinergic receptors .
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- HY-135483A
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nAChR
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Neurological Disease
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AR-R17779 hydrochloride is a potent and selective full agonist of nAChR, with Kis of 92 and 16000 nM for α7 and α4β2 subtype, respectively. AR-R17779 hydrochloride can improve learning and memory in rats. AR-R17779 hydrochloride also has anxiolytic activity. AR-R17779 hydrochloride can reduce inflammation by activating antiinflammatory cholinergic (vagal) pathways .
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- HY-W987949
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Others
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Neurological Disease
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Z-4105 is an orally active nootropic agent. Z-4105 reverses the amnesic effects of electroconvulsive shock (ECS) and methylazoxymethanol acetate (MAM), and improves learning and memory functions. Z-4105 enhances the activity of the brain cholinergic system without affecting other neurotransmitter systems. Z-4105 significantly alleviates neuropathic pain in rats. Z-4105 can be used in the research of neuropathic pain and brain dysfunction .
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- HY-B0527AS
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Isotope-Labeled Compounds
Serotonin Transporter
5-HT Receptor
Histamine Receptor
mAChR
Adrenergic Receptor
Trk Receptor
Sodium Channel
Potassium Channel
Dopamine Transporter
Apoptosis
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Neurological Disease
Inflammation/Immunology
Endocrinology
|
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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 (Ki = 3.45 nM) and NET (Ki = 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 Ki = 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) (Ki = 11-24 nM), H1 receptors (Ki = 0.5-1.1 nM), adrenergic α1 receptors (Ki = 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.
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- HY-114899
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Environmental Pollutants
Cholinesterase (ChE)
Insecticide
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Infection
Neurological Disease
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Azamethiphos is an acetylcholinesterase inhibitor and insecticide. Azamethiphos covalently binds to acetylcholinesterase via phosphorylation, inhibits its activity, causes acetylcholine to accumulate in cholinergic synapses, triggers uncontrolled excitation of cholinergic sites, induces paralysis and leads to death. Azamethiphos can be used as a bath insecticide in salmonid aquaculture to control sea lice infestations, and it exerts acute toxicity to European lobster larvae, including mortality and movement disorders .
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- HY-105170B
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nAChR
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Neurological Disease
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ABT-418 hydrochloride is a potent and selective agonist of nAChRs with cognitive enhancing and anxiolytic activities. ABT-418 hydrochloride activates cholinergic channel and can be used for research of Alzheimer's disease .
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- HY-119918
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mAChR
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Neurological Disease
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Cycrimine is an orally active muscarinic cholinergic receptor (mAChR) M1 antagonist, reduces the acetylcholine levels in parkinson model. Cycrimine shows antispasmodic activity, can be used in studies of behavioral and mental disorder .
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- HY-120004
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mAChR
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Infection
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PF-06827443 is a potent, low-clearance, orally bioavailable, and CNS-penetrant M1-selective positive allosteric modulator (PAM) with minimal agonist activity. PF-06827443 induce cholinergic AEs and convulsion .
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- HY-B1277A
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mAChR
Cholinesterase (ChE)
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Cardiovascular Disease
Neurological Disease
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Trihexyphenidyl is a selective and orally active M1 muscarinic receptor antagonist with an IC50 of 3.7 nM for rat cerebral cortex M1 muscarinic receptors. Trihexyphenidyl modulates cholinergic activity, countering acetylcholine supersensitivity in neural pathways. Trihexyphenidyl improves movement disorder, inhibits McN-A-343 (HY-107648)-induced pressor responses, vagally-induced bradycardia and vasodilatation. Trihexyphenidyl can be used for the research of Parkinson's disease. .
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- HY-B1585B
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Parpanil (edisylate)
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iGluR
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Neurological Disease
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Caramiphen edisylate (Parpanil edisylate) is an anticholinergic agent with NMDA receptor antagonist activity. Caramiphen edisylate can be used to inhibit diseases related to cholinergic neurotransmission. Caramiphen edisylate exerts its pharmacological effects by blocking cholinergic effects .
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- HY-P3176
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Motilin Receptor
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Others
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Motilin, human, porcine is a gastrointestinal hormone, which is released during fasting and after eating, or by drinking water. Motilin, human, porcine promotes enteric cholinergic activity in human stomach with an EC50 of 33 nM, and thus modulates gastrointestinal motility function .
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- HY-120408
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Atroscine
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Adrenergic Receptor
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Neurological Disease
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(±)-Scopolamine (Atroscine) is the racemic modification of Scopolamine. (±)-Scopolamine inhibits α-adrenergic receptor activity. (±)-Scopolamine has Ki values of 33 μM and 7.25 nM for α1-adrenerg receptor and muscarinic cholinergic receptor, respectively .
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- HY-B1693A
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Methotrimeprazine hydrochloride
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5-HT Receptor
Dopamine Receptor
Histamine Receptor
Autophagy
Enterovirus
Calcium Channel
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Infection
Neurological Disease
Inflammation/Immunology
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Levomepromazine (Methotrimeprazine) hydrochloride is an orally active antipsychotic compound and Ca 2+ release inducer. Levomepromazine inhibits SERCA pump and induces an increase in cytoplasmic Ca 2+ levels. Levomepromazine hydrochloride has antagonistic effects on a variety of neurotransmitter receptors, including dopamine, cholinergic, serotonin, and histamine receptors. Levomepromazine hydrochloride can induce adaptive ER stress and autophagy. In addition, Levomepromazine hydrochloride has antiviral, anti-inflammatory, neuroprotective and analgesic, sedative and anti-injurious activities. Levomepromazine hydrochloride can be used in the study psychiatric disorders and relieving nausea and vomiting .
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- HY-B1693R
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Methotrimeprazine (Standard)
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Reference Standards
5-HT Receptor
Dopamine Receptor
Autophagy
Histamine Receptor
Enterovirus
Calcium Channel
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Infection
Neurological Disease
Inflammation/Immunology
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|
Levomepromazine (Standard) is the analytical standard of Levomepromazine. This product is intended for research and analytical applications. Levomepromazine (Methotrimeprazine) is an orally active antipsychotic compound and Ca 2+ release inducer. Levomepromazine inhibits SERCA pump and induces an increase in cytoplasmic Ca 2+ levels. Levomepromazine has antagonistic effects on a variety of neurotransmitter receptors, including dopamine, cholinergic, serotonin, and histamine receptors. Levomepromazine can induce adaptive ER stress and autophagy. In addition, Levomepromazine has antiviral, anti-inflammatory, neuroprotective and analgesic, sedative and anti-injurious activities. Levomepromazine can be used in the study psychiatric disorders and relieving nausea and vomiting .
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- HY-B1585
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Parpanil
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iGluR
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Neurological Disease
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Parpanil is an anticholinergic agent with NMDA receptor antagonist activity. Parpanil can be used to inhibit diseases related to cholinergic neurotransmission. Parpanil exerts its pharmacological effects by blocking cholinergic effects .
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- HY-N15736
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mAChR
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Neurological Disease
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Petiline is a steroidal alkaloid found in Petilium raddeanum, acting as a selective antagonist of M cholinergic receptors. Petiline exerts anticholinergic effects (e.g., reducing vagal influence on the heart) by competitively blocking M cholinergic receptors, and also has central excitatory, cardiotonic, and spasmolytic activities. Petiline is promising for research of cholinergic system-related diseases (e.g., arrhythmia, intestinal spasm) .
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- HY-167699
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mAChR
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Others
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Cyclodrine is a cholinergic receptor antagonist that exhibits biological activity by influencing both muscarinic and nicotinic receptors.
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- HY-14607
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HP 749
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Potassium Channel
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Neurological Disease
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Besipirdine (hydrochloride) is a potassium channel blocker with cholinergic and adrenergic activity. The cholinergic activity of Besipirdine (hydrochloride) involves stimulating phosphatidylinositol turnover and reducing potassium currents. The adrenergic activity of Besipirdine (hydrochloride) involves stimulating norepinephrine release, which is attributed to the inhibition of presynaptic α2-adrenergic receptors and the inhibition of norepinephrine uptake. Besipirdine (hydrochloride) may be used in research for Alzheimer's disease .
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- HY-U00085
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RU 47213
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Cholinesterase (ChE)
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Neurological Disease
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Itameline (RU 47213) is a prodrug with oral and long-lasting cholinergic activity. Itameline is a novel tetrahydropyridine-oxime that is cleaved in vivo to form an active metabolite, RU 35963. RU 35963 is a muscarinic receptor agonist that is nonselective with respect to receptor subtypes. Itameline possesses the capacity to reduce memory deficits induced by an impairment of cholinergic transmission in the rat .
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- HY-114899S
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Isotope-Labeled Compounds
Cholinesterase (ChE)
Insecticide
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Infection
Neurological Disease
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Azamethiphos-d6 is deuterated labeled Azamethiphos (HY-114899). Azamethiphos is an acetylcholinesterase inhibitor and insecticide. Azamethiphos covalently binds to acetylcholinesterase via phosphorylation, inhibits its activity, causes acetylcholine to accumulate in cholinergic synapses, triggers uncontrolled excitation of cholinergic sites, induces paralysis and leads to death. Azamethiphos can be used as a bath insecticide in salmonid aquaculture to control sea lice infestations, and it exerts acute toxicity to European lobster larvae, including mortality and movement disorders .
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- HY-114899R
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Reference Standards
Cholinesterase (ChE)
Insecticide
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Infection
Neurological Disease
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Azamethiphos (Standard) is the analytical standard of Azamethiphos (HY-114899). This product is intended for research and analytical applications. Azamethiphos is an acetylcholinesterase inhibitor and insecticide. Azamethiphos covalently binds to acetylcholinesterase via phosphorylation, inhibits its activity, causes acetylcholine to accumulate in cholinergic synapses, triggers uncontrolled excitation of cholinergic sites, induces paralysis and leads to death. Azamethiphos can be used as a bath insecticide in salmonid aquaculture to control sea lice infestations, and it exerts acute toxicity to European lobster larvae, including mortality and movement disorders .
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- HY-105545C
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(+)-Benzetimide hydrochloride; (S)-(+)-Dexetimide hydrochloride; Dexbenzetimide hydrochloride
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mAChR
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Neurological Disease
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Dexetimide hydrochloride ((+)-Benzetimide hydrochloride) is an antimuscarinic drug with the activity of suppressing neuroleptic-induced Parkinson's syndrome. Dexetimide hydrochloride is used to improve the symptoms of movement disorders caused by the use of neuroleptics. Dexetimide hydrochloride, as the (-)-enantiomer of (-)-Benzetimide, shows the ability to selectively inhibit cholinergic receptors .
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- HY-B0170AR
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Azatadine maleate (Standard)
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Histamine Receptor
Reference Standards
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Inflammation/Immunology
Endocrinology
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Azatadine (dimaleate) (Standard) is the analytical standard of Azatadine (dimaleate). This product is intended for research and analytical applications. Azatadine dimaleate (Azatadine maleate) is an inhibitor of histamine and cholinergic with an IC50 of 6. Azatadine dimaleate has additional antiserotonin activity. Azatadine dimaleate can be studied in research on perennial allergic rhinitis .
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- HY-105327
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Cholinesterase (ChE)
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Neurological Disease
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P11149 is a competitive, BBB-penetarated weakly, orally active and selective inhibitor of AChE. P11149 exhibits an IC50 of 1.3 μM for rat BChE/AChE. P11149, a Galanthamine derivative, demonstrates central cholinergic activity, behavioral efficacy and safety. P11149 is used in the study for Alzheimer's disease .
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- HY-114846
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Prostaglandin Receptor
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Cardiovascular Disease
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Ro 22-9194 inhibits aggregation and thromboxane Az (TXA2) synthetase activity in rabbit and human platelets. Ro 22-9194 has a potent inhibitory action against various types of model arrhythmias. Ro 22-9194 has non-cholinergic cardiac depressant properties with its vasodilating action .
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- HY-156031
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Cholinesterase (ChE)
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Neurological Disease
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BChE-IN-19 (Compound 7b) is a para-substituted derivative of indone (7b) with inhibitory activity of butyryl cholinesterase (BChE) (IC50=0.04 μM). BChE-IN-19 improves cholinergic scheduling in the nervous system. BChE-IN-19 can be used against Alzheimer's disease .
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- HY-105793
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mAChR
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Neurological Disease
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Mazaticol is an anticholinergic agent. Mazaticol blocks the muscarinic acetylcholine receptors and cholinergic nerve activity. Mazaticol is a potent 3H-QNB and 3H-PZ binding inhibitor, can bind to the M2 receptors with high affinity. Mazaticol exhibits inhibitory effects on dopamine uptake in the striatal nerve terminal. Mazaticol can be used for parkinsonian syndrome research .
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- HY-136625
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N-myristoyltransferase
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Cardiovascular Disease
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LY134046 is an inhibitor of norepinephrine N-methyltransferase (NMT) with cardiovascular activity. LY134046 causes sustained reductions in mean arterial blood pressure and heart rate, but no significant reductions in norepinephrine concentrations in the rat brain. LY134046 does not interact with adrenergic or cholinergic receptors, and its hypotensive and bradycardic effects do not require neurogenic tension. LY134046 (40 mg/kg/day) causes sustained and significant inhibition of hypothalamic and brainstem NMT activity, resulting in central norepinephrine depletion.
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- HY-172884
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Cholinesterase (ChE)
iGluR
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Neurological Disease
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MDAR IN-1 (Compound 5m) is a brain-penetrant inhibitor of acetylcholinesterase (AChE) and antagonist of the GluN1/GluN2B subtype of NMDAR receptor. MDAR IN-1 effectively inhibits AChE activity, enhances cholinergic neurotransmission, and blocks NMDAR, reducing excitatory neurotoxicity. MDAR IN-1 is promising for research of Alzheimer's disease .
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- HY-123934
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P-glycoprotein
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Neurological Disease
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VU6007477 is a brain-penetrant, selective M1 positive allosteric modulator (PAM) with an EC50 value of 230 nM. VU6007477 is also a human P-glycoprotein (P-gp) substrate with moderate permeability. VU6007477 displays improved central nervous system (CNS) penetration over the hydroxylated congeners. VU6007477 a pyranyl amide derivative, which is promising for research of robust cholinergic seizure activity .
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- HY-118056
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Cannabinoid Receptor
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ABD459 is a CB1 receptor antagonist with significant effects on regulating food intake and sleep-wake cycles. ABD459 completely displaces CB1 agonist CP99540 (Ki = 8.6 nM) and antagonizes CP55940-induced GTPγS binding (KB = 7.7 nM). ABD459 may specifically modulate endogenous cannabinoid release through cholinergic activity and plays a role in attention and arousal regulation. ABD459 is suitable for research in neurological disorders .
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- HY-B1277AS
-
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Isotope-Labeled Compounds
mAChR
Cholinesterase (ChE)
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Neurological Disease
|
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Trihexyphenidyl-d5 is deuterium labeled Trihexyphenidyl (HY-B1277A). Trihexyphenidyl is a selective and orally active M1 muscarinic receptor antagonist with an IC50 of 3.7 nM for rat cerebral cortex M1 muscarinic receptors. Trihexyphenidyl modulates cholinergic activity, countering acetylcholine supersensitivity in neural pathways. Trihexyphenidyl improves movement disorder, inhibits McN-A-343 (HY-107648)-induced pressor responses, vagally-induced bradycardia and vasodilatation. Trihexyphenidyl can be used for the research of Parkinson's disease. .
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-
- HY-136258
-
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nAChR
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Neurological Disease
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nAChR agonist CMPI hydrochloride is a potent and selective positive allosteric modulator (PAM) of nAChR containing a α4:α4 subunit interface. nAChR agonist CMPI hydrochloride enhances the response of (α4)3(β2)2 nAChR to ACh (10 µM) with an EC50 of 0.26 µM. nAChR agonist CMPI hydrochloride has potential for the research of nicotine dependence and many neuropsychiatric conditions associated with decreased brain cholinergic activity .
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- HY-B1277S
-
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Isotope-Labeled Compounds
mAChR
Cholinesterase (ChE)
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Neurological Disease
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Trihexyphenidyl-d5 hydrochloride is deuterium labeled Trihexyphenidyl hydrochloride (HY-B1277). Trihexyphenidyl hydrochloride is a selective and orally active M1 muscarinic receptor antagonist with an IC50 of 3.7 nM for rat cerebral cortex M1 muscarinic receptors. Trihexyphenidyl hydrochloride modulates cholinergic activity, countering acetylcholine supersensitivity in neural pathways. Trihexyphenidyl hydrochloride improves movement disorder, inhibits McN-A-343 (HY-107648)-induced pressor responses, vagally-induced bradycardia and vasodilatation. Trihexyphenidyl hydrochloride can be used for the research of Parkinson's disease. .
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- HY-B1277R
-
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Reference Standards
mAChR
Cholinesterase (ChE)
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Neurological Disease
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Trihexyphenidyl hydrochloride (Standard) is the analytical standard of Trihexyphenidyl hydrochloride (HY-B1277). This product is intended for research and analytical applications. Trihexyphenidyl is a selective and orally active M1 muscarinic receptor antagonist with an IC50 of 3.7 nM for rat cerebral cortex M1 muscarinic receptors. Trihexyphenidyl modulates cholinergic activity, countering acetylcholine supersensitivity in neural pathways. Trihexyphenidyl improves movement disorder, inhibits McN-A-343 (HY-107648)-induced pressor responses, vagally-induced bradycardia and vasodilatation. Trihexyphenidyl can be used for the research of Parkinson's disease. .
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- HY-165132
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(S)-Floramultine; (S)-Bechuanine; Merenderine
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Cholinesterase (ChE)
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Others
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Floramultine ((S)-Floramultine) is a compound isolated from plants with cholinergic activity. It is a moderately potent reversible inhibitor of cholinesterase and has a certain specificity for different cholinesterases.
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- HY-N8421
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Potassium Channel
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Cardiovascular Disease
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Tabernanthine is a negative chronotropic and negative inotropic agent that selectively acts on sinoatrial node receptors, regulating heart rhythm and myocardial contractility. Tabernanthine exhibits atropine resistance and direct non-cholinergic binding properties, acting directly on the sinoatrial node rather than relying on vagal nerve or cholinergic pathways to exert its key activity of slowing heart rate and weakening myocardial contractility. Tabernanthine is useful in cardiovascular pharmacology research, particularly in the areas of sinoatrial node function regulation, mechanisms related to bradycardia, and studies of cardiac receptor subtype differences .
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- HY-N18371
-
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Drug Derivative
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Others
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Decumbenine (2-1) is an isoquinoline alkaloid found in Corydalis decumbens (Thunb.) Pers .
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- HY-105170BR
-
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Reference Standards
nAChR
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Neurological Disease
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ABT-418 hydrochloride (Standard) is the analytical standard of ABT-418 hydrochloride (HY-105170B). This product is intended for research and analytical applications. ABT-418 hydrochloride is a potent and selective agonist of nAChRs with cognitive enhancing and anxiolytic activities. ABT-418 hydrochloride activates cholinergic channel and can be used for research of Alzheimer's disease .
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- HY-180382
-
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Cholinesterase (ChE)
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Cardiovascular Disease
|
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Trimethidinium methosulfate is an orally active ganglionic blocker with central antihypertensive activity. Trimethidinium methosulfate inhibits the conduction of sympathetic ganglia and reduces vascular contraction. Trimethidinium methosulfate acts on the cerebrovascular motor center and lowers peripheral vascular resistance. Trimethidinium methosulfate has cholinergic nerve inhibitory side effects, but they are relatively mild. Trimethidinium methosulfate can be used in hypertension research .
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- HY-168167
-
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Endogenous Metabolite
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Neurological Disease
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BuChE-IN-14 is a novel compound that selectively inhibits acetylcholinesterase (AChE) activity. BuChE-IN-14 showed a concentration-dependent inhibitory effect on AChE in rat brain in vitro experiments. BuChE-IN-14 can increase the extracellular acetylcholine (ACh) concentration in the rat hippocampus and striatum at a certain dose. BuChE-IN-14 may help improve memory impairment caused by cholinergic dysfunction .
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- HY-105327R
-
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Reference Standards
Cholinesterase (ChE)
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Neurological Disease
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P11149 (Standard) is the analytical standard of P11149 (HY-105327). This product is intended for research and analytical applications. P11149 is a competitive, BBB-penetarated weakly, orally active and selective inhibitor of AChE. P11149 exhibits an IC50 of 1.3 μM for rat BChE/AChE. P11149, a Galanthamine derivative, demonstrates central cholinergic activity, behavioral efficacy and safety. P11149 is used in the study for Alzheimer's disease .
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- HY-120042
-
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Carboxylesterase (CES)
Cholinesterase (ChE)
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Others
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Heptenophos is an inhibitor of AChE and plasma carboxylesterase (CES). By inhibiting AChE activity, Heptenophos causes the accumulation of acetylcholine at cholinergic synapses, thereby triggering typical symptoms of organophosphate poisoning. Heptenophos exhibits rapid lethal toxicity in male albino mice, but its toxic effects are effectively antagonized by obidoxime, and Memantine (HY-B0591) further enhances the detoxification efficacy of obidoxime. Therefore, Heptenophos is commonly used in studies related to the mechanism of organophosphate poisoning and detoxification strategies .
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- HY-101196
-
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Endogenous Metabolite
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Neurological Disease
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PG 9 maleate is a compound with analgesic and anti-memory loss activity. PG 9 maleate exerts analgesic effects by enhancing central cholinergic transmission. PG 9 maleate protects against memory loss caused by scopolamine or dicyclomine within a specific dose range. The affinity profile of PG 9 maleate indicates significant selectivity among the M4/M1 receptor subtypes, which may be the mechanism for its analgesic and anti-memory loss effects. PG 9 maleate can increase the release of acetylcholine, thereby improving its biological activity .
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- HY-116153
-
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Cholinesterase (ChE)
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Neurological Disease
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HUHS2002 is a free fatty acid derivative with the ability to enhance α7 cholinergic receptor activity. HUHS2002 enhances whole-cell membrane currents of α7 ACh receptors expressed in Xenopus oocytes in a concentration-dependent manner. The effects of HUHS2002 were blocked in the presence of the Ca2 /calmodulin-dependent protein kinase II (CaMKII) inhibitor KN-93. HUHS2002 activated CaMKII in cultured rodent hippocampal neurons, and this activation was abolished by KN-93. HUHS2002 also partially inhibited the activity of protein phosphatase 1 (PP1) in a cell-free PP1 activity assay .
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- HY-166562S
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Methotrimeprazine-d6 hydrochloride
|
Isotope-Labeled Compounds
Enterovirus
Histamine Receptor
Autophagy
5-HT Receptor
Calcium Channel
Dopamine Receptor
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Infection
Neurological Disease
Inflammation/Immunology
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Levomepromazine-d6 hydrochloride (Methotrimeprazine-d6 hydrochloride) is the deuterium labeled Levomepromazine hydrochloride. Levomepromazine (Methotrimeprazine) hydrochloride is an orally active antipsychotic compound and Ca 2+ release inducer. Levomepromazine inhibits SERCA pump and induces an increase in cytoplasmic Ca 2+ levels. Levomepromazine hydrochloride has antagonistic effects on a variety of neurotransmitter receptors, including dopamine, cholinergic, serotonin, and histamine receptors. Levomepromazine hydrochloride can induce adaptive ER stress and autophagy. In addition, Levomepromazine hydrochloride has antiviral, anti-inflammatory, neuroprotective and analgesic, sedative and anti-injurious activities. Levomepromazine hydrochloride can be used in the study psychiatric disorders and relieving nausea and vomiting .
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HY-L069
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2,065 compounds
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Alzheimer’s Disease (AD) is a progressive degenerative brain disease which causes mental and physical decline, gradually resulting in death. Despite the significant public health issue that it poses, only few medical treatments have been approved for Alzheimer’s Disease (AD) and these act to control symptoms rather than alter the course of the disease. Discovery of new therapeutic approaches depends on the study of pathology of AD. Recent research findings have led to greater understanding of disease neurobiology in Alzheimer's Disease (AD) and identification of unique targets for drug development. Several important mechanisms have been proposed to explain the underlying pathology of AD, such as Amyloid cascade hypothesis, Tau hypothesis and Cholinergic hypothesis, etc.
MCE offers a unique collection of 2,065 compounds with anti-Alzheimer’s Disease activities or targeting the unique targets of AD. MCE Anti-Alzheimer’s Disease Compound Library is a useful tool for exploring the mechanism of AD and discovering new drugs for AD.
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| Cat. No. |
Product Name |
Type |
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- HY-NP143
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Biochemical Assay Reagents
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Nerve Growth Factor 2.5S, murine submaxillary gland is a neurotrophic polypeptide required for normal growth and development of sympathetic and embryonic sensory neurons and certain cholinergic neurons in the central nervous system. Nerve Growth Factor 2.5S, murine submaxillary gland has only β-subunit , and shows nerve growth-promoting activity .
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- HY-W127699
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N,N,N-Trimethyl-2-(propionyloxy)ethanaminium (p-toluenesulfonate)
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Biochemical Assay Reagents
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Propionylcholine (p-toluenesulfonate) is an organic compound commonly used in biochemical research and neuroscience research. It can be used to study cholinergic signal transduction and esterase activity, and is widely used in biomedical research and pharmacological research. In addition, this compound is also used as a substrate or catalyst in certain biochemical reactions.
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| Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P3176
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Motilin Receptor
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Others
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Motilin, human, porcine is a gastrointestinal hormone, which is released during fasting and after eating, or by drinking water. Motilin, human, porcine promotes enteric cholinergic activity in human stomach with an EC50 of 33 nM, and thus modulates gastrointestinal motility function .
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| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
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- HY-B0282
-
-
-
- HY-B0282R
-
-
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- HY-N0801
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Triterpenes
Terpenoids
Polygalaceae
Plants
Polygala tenuifolia Willd.
Source Classification
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MMP
Cholinesterase (ChE)
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Polygalacic acid, is a triterpene, isolated from the root of Polygala tenuifolia Willd. Polygalacic acid inhibits MMP expression. Polygalacic acid may have a therapeutic effect in Osteoarthritis (OA) treatment .
Polygalacic acid exerts a significant neuroprotective effect on cognitive impairment, PA improves cholinergic system reactivity by inhibiting acetylcholinesterase (AChE) activity, increasing choline acetyltransferase (ChAT) activity, and elevating levels of acetylcholine (Ach) in the hippocampus and frontal cortex .
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- HY-120408
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-
-
- HY-N15736
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Alkaloids
other families
Other Alkaloids
Petilium raddeanum
Plants
Source Classification
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mAChR
|
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Petiline is a steroidal alkaloid found in Petilium raddeanum, acting as a selective antagonist of M cholinergic receptors. Petiline exerts anticholinergic effects (e.g., reducing vagal influence on the heart) by competitively blocking M cholinergic receptors, and also has central excitatory, cardiotonic, and spasmolytic activities. Petiline is promising for research of cholinergic system-related diseases (e.g., arrhythmia, intestinal spasm) .
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- HY-165132
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-
-
- HY-N8421
-
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Apocynaceae
Structural Classification
Alkaloids
Plants
Indole Alkaloids
Tabernanthe iboga Baill.
Source Classification
|
Potassium Channel
|
|
Tabernanthine is a negative chronotropic and negative inotropic agent that selectively acts on sinoatrial node receptors, regulating heart rhythm and myocardial contractility. Tabernanthine exhibits atropine resistance and direct non-cholinergic binding properties, acting directly on the sinoatrial node rather than relying on vagal nerve or cholinergic pathways to exert its key activity of slowing heart rate and weakening myocardial contractility. Tabernanthine is useful in cardiovascular pharmacology research, particularly in the areas of sinoatrial node function regulation, mechanisms related to bradycardia, and studies of cardiac receptor subtype differences .
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-
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- HY-N18371
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| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-B0282S
-
|
|
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Acetylcholine-d4 (chloride) is the deuterium labeled Acetylcholine chloride. Acetylcholine chloride (ACh chloride), a neurotransmitter, is a potent and BBB-permeable cholinergic agonist. Acetylcholine chloride is a modulator of the activity of dopaminergic (DAergic) neurons through the stimulation of nicotinic acetylcholine receptors (nAChRs) . Acetylcholine chloride inhibits p53 mutant peptide aggregation in vitro .
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- HY-B0282S1
-
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Acetylcholine-d9 (chloride) is the deuterium labeled Acetylcholine chloride. Acetylcholine chloride (ACh chloride), a neurotransmitter, is a potent and BBB-permeable cholinergic agonist. Acetylcholine chloride is a modulator of the activity of dopaminergic (DAergic) neurons through the stimulation of nicotinic acetylcholine receptors (nAChRs) . Acetylcholine chloride inhibits p53 mutant peptide aggregation in vitro .
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-
- HY-B0461S
-
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Trospium-d8 (chloride) is the deuterium labeled Trospium chloride. Trospium chloride is an orally active, specific and competitive antagonist of muscarinic cholinergic receptors (mAChRs), with antimuscarinic activity. Trospium chloride binds to muscarinic receptors M1, M2 and M3 with high affinity, but not nicotinic, cholinergic receptors .
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- HY-B0527AS
-
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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 (Ki = 3.45 nM) and NET (Ki = 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 Ki = 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) (Ki = 11-24 nM), H1 receptors (Ki = 0.5-1.1 nM), adrenergic α1 receptors (Ki = 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.
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-
-
- HY-114899S
-
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Azamethiphos-d6 is deuterated labeled Azamethiphos (HY-114899). Azamethiphos is an acetylcholinesterase inhibitor and insecticide. Azamethiphos covalently binds to acetylcholinesterase via phosphorylation, inhibits its activity, causes acetylcholine to accumulate in cholinergic synapses, triggers uncontrolled excitation of cholinergic sites, induces paralysis and leads to death. Azamethiphos can be used as a bath insecticide in salmonid aquaculture to control sea lice infestations, and it exerts acute toxicity to European lobster larvae, including mortality and movement disorders .
|
-
-
- HY-B1277AS
-
|
|
|
Trihexyphenidyl-d5 is deuterium labeled Trihexyphenidyl (HY-B1277A). Trihexyphenidyl is a selective and orally active M1 muscarinic receptor antagonist with an IC50 of 3.7 nM for rat cerebral cortex M1 muscarinic receptors. Trihexyphenidyl modulates cholinergic activity, countering acetylcholine supersensitivity in neural pathways. Trihexyphenidyl improves movement disorder, inhibits McN-A-343 (HY-107648)-induced pressor responses, vagally-induced bradycardia and vasodilatation. Trihexyphenidyl can be used for the research of Parkinson's disease. .
|
-
-
- HY-B1277S
-
|
|
|
Trihexyphenidyl-d5 hydrochloride is deuterium labeled Trihexyphenidyl hydrochloride (HY-B1277). Trihexyphenidyl hydrochloride is a selective and orally active M1 muscarinic receptor antagonist with an IC50 of 3.7 nM for rat cerebral cortex M1 muscarinic receptors. Trihexyphenidyl hydrochloride modulates cholinergic activity, countering acetylcholine supersensitivity in neural pathways. Trihexyphenidyl hydrochloride improves movement disorder, inhibits McN-A-343 (HY-107648)-induced pressor responses, vagally-induced bradycardia and vasodilatation. Trihexyphenidyl hydrochloride can be used for the research of Parkinson's disease. .
|
-
-
- HY-166562S
-
|
|
|
Levomepromazine-d6 hydrochloride (Methotrimeprazine-d6 hydrochloride) is the deuterium labeled Levomepromazine hydrochloride. Levomepromazine (Methotrimeprazine) hydrochloride is an orally active antipsychotic compound and Ca 2+ release inducer. Levomepromazine inhibits SERCA pump and induces an increase in cytoplasmic Ca 2+ levels. Levomepromazine hydrochloride has antagonistic effects on a variety of neurotransmitter receptors, including dopamine, cholinergic, serotonin, and histamine receptors. Levomepromazine hydrochloride can induce adaptive ER stress and autophagy. In addition, Levomepromazine hydrochloride has antiviral, anti-inflammatory, neuroprotective and analgesic, sedative and anti-injurious activities. Levomepromazine hydrochloride can be used in the study psychiatric disorders and relieving nausea and vomiting .
|
-
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