Catalog No.
Product Name
Application
Product Information
Citations
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nAChR Agonist
Desformylflustrabromine HCl is a positive allosteric modulator of α4β2 and also a muscle-type nAChR inhibitor. -
COX and lipo-oxygenase inhibitor
Timegadine, a new antiinflammatory agent, is found to be a potent, competitive inhibitor of cyclo-oxygenase (COX) and lipo-oxygenase, with IC50s ranging from 5 nM (washed rabbit platelets) to 20 μM (rat brain) for COX and 100 μM for lipo-oxygenase both in the cytosol fraction of horse platelet homogenates, and in washed rabbit platelets. -
GABA receptor agonist
Afloqualone, also known as HQ-495, is a centrally acting muscle relaxant. Afloqualone inhibits vestibular nystagmus probably due to both inhibition of selective polysynaptic transmission and enhancement of the effects of GABA and glycine in the lateral vestibular nucleus (LVN), and its GABA-enhancing effect is thought to be attributable to the increased sensitivity of GABA receptors of the LVN neuron site. -
Muscarinic receptor agonist
Methacholine chloride is a synthetic choline ester that acts as a non-selective muscarinic receptor agonist in the parasympathetic nervous system. - L-Cycloserine ((S)-4-Amino-3-isoxazolidone) irreversibly inhibits GABA pyridoxal 5??-phosphate-dependent aminitransferase in E.
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nAChR agonist
Lobeline hydrochloride, a nicotinic receptor agonist, acting as a potent antagonist at both α3β2 and α4β2 neuronal nicotinic receptor subtypes. - (-)-Borneol is a bicyclic organic compound and a terpene derivative. The hydroxyl group in this compound is placed in an endo position. There are two different enantiomers of borneol. (-)-Borneol has a highly efficacious positive modulating action at GABA receptor with an EC50 of 237 μM.
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muscarinic antagonist
Anisotropine methylbromide is a muscarinic antagonist and antispasmodic. Anisotropine methylbromide is a quaternary ammonium compound. Its use as treatment adjunct in peptic ulcer has been replaced by the use of more effective agents. -
Muscarinic antagonist
Procyclidine hydrochloride is a muscarinic antagonist that crosses the blood-brain barrier and is used in the treatment of drug-induced extrapyramidal disorders and in Parkinsonism. -
AChE & butyrylcholinesterase inhibitor
Tacrine is a derivative of aminoacridine that functions as an inhibitor of both acetylcholinesterase (AChE) and butyrylcholinesterase (IC50s = 31 and 26.5 nM, respectively). -
Muscarinic antagonist
Mepenzolate Bromide is a muscarinic antagonist used to treat gastrointestinal disorders. It decreases the severity of elastase-induced airspace enlargement and respiratory dysfunction. -
B-type AChR activator
Bephenium hydroxynaphthoate is an anthelmintic agent formerly used in the treatment of hookworm infections and ascariasis; B-type AChR activator. -
Chloride Channel/GABA Receptor blocker
Picrotoxinin negatively modulate the action of GABA on GABAA receptors. -
COX-2 inhibitor
Aceclofenac is a cyclooxygenase-2 inhibitor used to treat osteoarthritis, rheumatoid arthritis and ankylosing spondylitis. -
NMDA receptor antagonist
Mephenesin is an NMDA receptor antagonist, is a centrally acting muscle relaxant. -
Acid pump antagonist
Revaprazan hydrochloride is a novel acid pump antagonist (APA). Revaprazan hydrochloride reduces COX-2 expression and has significant anti-inflammatory actions activities in H. pylori infection. -
insecticide
Azamethiphos is an organothiophosphate insecticide. It is a veterinary drug used in Atlantic salmon fish farming to control parasites. -
Cholinesterase Reactivator
Pralidoxime iodide is a Cholinesterase Reactivator. - Tiaprofenic acid is a non-steroidal anti-inflammatory drug (NSAID) of the arylpropionic acid (profen) class, used to treat pain, especially arthritic pain Long-term use of tiaprofenic acid is associated with severe cystitis, roughly 100 times more commonly than other NSAIDs. It is contraindicated in patients with cystitis and urinary tract infections.
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BChE inhibitor
Drofenine hydrochloride is a potent competitive inhibitor of BChE, and the ki values of Drofenine is calculated to be 3 uM. -
acetylcholinesterase inhibitor
Edrophonium Chloride, also known as Tensilon, is an acetylcholinesterase inhibitor used in cardiac arrhythmias and in the diagnosis of myasthenia gravis. Edrophonium Chloride has also been used as an antidote to curare principles. -
COX inhibitor
Diclofenac is a potent and nonselective anti-inflammatory agent, acts as a COX inhibitor, with IC50s of 4 nM, 1.3 nM for human COX-1 and COX-2 in CHO cells, and 5.1, 0.84 μM for ovine COX-1 and COX-2, respectively. -
nAChR antagonist
Mecamylamine hydrochloride is a nAChR antagonist previously used to treat hypertension. It displays a wide variety of activities, including reducing depression-like behaviors in subjects with Tourette's syndrome and improving rates of smoking cessation. -
M1 muscarinic receptor antagonist
Pirenzepine dihydrochloride (LS519) is a selective M1 muscarinic receptor antagonist. -
P2Y12 receptors inhibitor
Cangrelor Tetrasodium is a high-affinity, reversible inhibitor of P2Y12 receptors that causes almost complete inhibition of ADP-induced platelet aggregate. It is a modified ATP derivative stable to enzymatic degradation. Unlike clopidogrel (Plavix), which is a prodrug, cangrelor is an active drug not requiring metabolic conversion. -
GABA receptor agonist
Tramiprosate, also known as homotaurine, is a gamma-Aminobutyric acid (GABA) receptor agonist and a glycosaminoglycan mimetic used in the treatment of Alzheimer's disease. -
NMDA glutamate receptor co-agonist
(R)-Serine, an endogenous amino acid involved in glia-synapse interactions that has unique neurotransmitter characteristics, is a potent co-agonist at the NMDA glutamate receptor. - Pirmenol hydrochloride inhibits IK.ACh by blocking muscarinic receptors. The IC50 of Pirmenol for inhibition of Carbachol-induced IK.ACh is 0.1 μM.
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mAChR antagonist
Atropine methyl bromide, a muscarinic receptor (mAChR) antagonist, is a quaternary ammonium salt of atropine and a mydriatic for dilation of the pupil during ophthalmic examination. It is introduced for relieving pyloric spasm in infants for its highly polar nature. It penetrates less readily into the central nervous system than atropine. -
COX-2 inhibitor
Imrecoxib (BAP-909) is a novel and selective cyclooxygenase 2 (COX-2) inhibitor with an IC50 value of 18 nM, it also inhibits COX1- activity with an IC50 value of 115 nM. Imrecoxib (BAP-909) has anti-inflammatory effect. -
nAchR agonist
Pyrantel tartrate is an antinematodal thiophene nicotinic receptor agonist and can elicit spastic muscle paralysis in parasitic worms due to prolonged activation of the excitatory nicotinic acetylcholine (nACh) receptors on body wall muscle. -
mAChR agonist
Cevimeline (Evoxac) Hcl is a parasympathomimetic and muscarinic agonist, with particular effect on M3 receptors; used in the treatment of dry mouth associated with sjogren's syndrome. - Piperidolate hydrochloride is an antimuscarinic, Also a potential inhibitor of human glutathione transferase P1-1.
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COX-2 inhibitor
Bromfenac Sodium Sesquihydrate is a nonsteroidal anti-inflammatory drug (NSAID), which inhibits cyclooxygenase II (COX-2). -
alpha-1 adrenergic receptors / mAChRs inhibitor
Anisodamine is an inhibitor of alpha-1 adrenergic receptors and mAChRs isolated from Chinese solanacea plant.
