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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
224 Results for "
cholinergic
" in MedChemExpress (MCE) Product Catalog:
Products (224)
224 Results for "cholinergic" in MCE Product Catalog:
33
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Target:
Research Areas:
Infection Neurological Disease Inflammation/Immunology Cancer
Diphenhydramine is a first-generation histamine H1-receptor antagonist with anti-cholinergic effect. Diphenhydramine hydrochloride can across the ovine blood-brain barrier (BBB) .
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Target:
Research Areas:
Infection Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
Diphenhydramine hydrochloride is a first-generation histamine H1-receptor antagonist with anti-cholinergic effect. Diphenhydramine hydrochloride can across the ovine blood-brain barrier (BBB) .
9
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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Target:
Serotonin Transporter 5-HT Receptor mAChR Histamine Receptor Adrenergic Receptor Trk Receptor Sodium Channel Potassium Channel Dopamine Transporter Apoptosis
Research Areas:
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 .
7
7 Cited Publications
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Research Areas:
LM11A-31 dihydrochloride, a non-peptide p75 NTR (neurotrophin receptor p75) modulator, is an orally active and potent proNGF (nerve growth factor) antagonist. LM11A-31 dihydrochloride is an amino acid derivative with high blood-brain barrier permeability and blocks p75-mediated cell death. LM11A-31 dihydrochloride reverses cholinergic neurite dystrophy in Alzheimer's disease mouse models with mid- to late-stage disease progression .
7
7 Cited Publications
Target:
Research Areas:
LM11A-31, a non-peptide p75 NTR (neurotrophin receptor p75) modulator, is an orally active and potent proNGF (nerve growth factor) antagonist. LM11A-31 is an amino acid derivative with high blood-brain barrier permeability and blocks p75-mediated cell death. LM11A-31 reverses cholinergic neurite dystrophy in Alzheimer's disease mouse models with mid- to late-stage disease progression .
5
Category:
Flavonols Flavonoids Other Diseases Phenols Polyphenols Plants Apocynum venetum Linn. Disease Research Fields Apocynaceae Extract
Target:
4
4 Cited Publications
Synonyms: Pyrantel embonate
Pyrantel pamoate is an orally active antiparasitic agent. Pyrantel pamoate induces spastic paralysis in parasites via actions on neural and muscular cholinergic receptors as a nicotinic acetylcholine receptor (nAChR) agonist. Pyrantel pamoate eliminates both immature and mature endoparasites in horses. Pyrantel pamoate can be used in research related to parasitic infections .
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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. .
2
Target:
2
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Physostigmine salicylate (Eserine salicylate) is a reversible acetylcholinesterase (AChE) inhibitor. Physostigmine salicylate crosses the blood-brain barrier and stimulates central cholinergic neurotransmission. Physostigmine salicylate can reverse memory deficits in transgenic mice with Alzheimer's disease. Physostigmine salicylate is also an antidote for anticholinergic poisoning .
2
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Research Areas:
Physostigmine hemisulfate (Eserine hemisulfate) is a reversible acetylcholinesterase (AChE) inhibitor. Physostigmine hemisulfate can crosses the blood-brain barrier and stimulates central cholinergic neurotransmission. Physostigmine hemisulfate can reverse memory deficits in transgenic mice with Alzheimer's disease. Physostigmine hemisulfate is also an antidote for anticholinergic poisoning .
2
Research Areas:
Temephos (Temefos) is an orally active, blood-brain barrier-permeable organophosphate insecticide and AChE inhibitor. By irreversibly inhibiting AChE to induce cholinergic overactivation, Temephos effectively blocks larval development of Aedes aegypti (yellow fever mosquito) and Aedes albopictus (Asian tiger mosquito), and is commonly used in studies related to Dengue Virus, Zika Virus and other relevant pathogens. Temephos exhibits genotoxicity and neurodevelopmental toxicity, and may also cause liver injury, reproductive system abnormalities and cholinergic poisoning symptoms in mammals. Temephos tends to accumulate in adipose tissues and aquatic organisms, and is excreted via feces after metabolism through oxidation and hydrolysis. Note that CYP-mediated metabolic detoxification may reduce the actual larvicidal efficacy of Temephos against some mosquito species. Temephos can be used in research related to dengue fever, Zika virus disease, chikungunya and dracunculiasis .
1
1 Cited Publications
Research Areas:
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 .
1
1 Cited Publications
Pyrantel tartrate is an orally active antiparasitic agent. Pyrantel tartrate induces spastic paralysis in parasites via actions on neural and muscular cholinergic receptors as a nicotinic acetylcholine receptor (nAChR) agonist. Pyrantel tartrate eliminates both immature and mature endoparasites in horses. Pyrantel tartrate can be used in research related to parasitic infections .
1
1 Cited Publications
Cat. No.: HY-P1376A
Target:
Research Areas:
1
1 Cited Publications
Cat. No.: HY-17368
CAS No.: 123441-03-2
Synonyms: ENA 713 free base; SDZ-ENA 713 free base
Target:
Research Areas:
Rivastigmine (ENA 713 free base) is an orally active and potent cholinesterase (ChE) inhibitor and inhibits butyrylcholinesterase (BChE) and acetylcholinesteras (AChE) with IC50s of 0.037 μM , 4.15 μM, respectively. Rivastigmine can pass the blood brain barrier (BBB). Rivastigmine is a parasympathomimetic or cholinergic agent used for the research of mild to moderate dementia of the Alzheimer's type and dementia due to Parkinson's disease .
1
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Phosalone is an orally active, blood-brain barrier penetrant Insecticide and acaricide. Phosalone inhibits the activity of Acetylcholinesterase. Phosalone acts as a substrate for detoxifying esterases. Phosalone induces symptoms of cholinergic hyperactivity, toxic reactions, mortality, oxidative stress, and changes in pro-inflammatory protein levels, and exerts toxic effects on colonic tissues and cells. Phosalone controls pistachio psyllids. Phosalone can be used in studies related to colitis .
1
1 Cited Publications
Synonyms: ENA 713; SDZ-ENA 713
Target:
Research Areas:
Rivastigmine tartrate (ENA 713; SDZ-ENA 713) is an orally active and potent cholinesterase (ChE) inhibitor and inhibits butyrylcholinesterase (BChE) and acetylcholinesteras (AChE) with IC50s of 0.037 μM, 4.15 μM, respectively. Rivastigmine tartrate can pass the blood brain barrier (BBB). Rivastigmine tartrate is a parasympathomimetic or cholinergic agent used for the research of mild to moderate dementia of the Alzheimer's type and dementia due to Parkinson's disease .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
