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non-selective ganglionic nicotinic-receptor antagonist (nAChR) antagonist
Hexamethonium Bromide is a non-selective ganglionic nicotinic-receptor antagonist (nAChR) antagonist, with mixed competitive and noncompetitive activity. -
NMDA receptor antagonist
Ifenprodil tartrate is the atypical N-methyl-D-aspartate (NMDA) receptor antagonist, inhibits NMDA-induced currents at NR1A/NR2B receptors with high affinity (IC50 = 0.34 μM). -
excitatory transmitter/agonist
L-Glutamic acid monosodium salt acts as an excitatory transmitter and an agonist at all subtypes of glutamate receptors (metabotropic, kainate, NMDA, and AMPA). (S)-Glutamic acid shows a direct activating effect on the release of DA from dopaminergic terminals. -
GABAB receptor agonist
(R)-Baclofen(STX209) is a selective GABAB receptor agonist. -
S6K inhibitor
Sodium Salicylate (Salicylic acid sodium salt) inhibits cyclo-oxygenase-2 (COX-2) activity independently of transcription factor (NF-κB) activation. Sodium Salicylate is also a S6K inhibitor.Sodium Salicylate is a NF-κB inhibitor that decreases inflammatory gene expression and improves repair in aged muscle. -
α3β4 nAChR ligand
AT-1001 is a tight junction regulator and reverses leaky junctions to their normally closed state. It is being studied in people with celiac disease - Edonerpic, also known as T-817, is a neuroprotectant. Edonerpic is a candidate therapeutic agent for Alzheimer's disease that inhibits oxidative stress and nitric oxide-induced neurotoxicity and acts as a neurotrophic factor.
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Muscarinic Receptor Antagonist
Solifenacin is a novel muscarinic receptor antagonist with pKis of 7.6, 6.9 and 8.0 for M1, M2 and M3 receptors, respectively. -
AChE and BChE inhibitor
Tacrine hydrochloride hydrate is an inhibitor of both acetyl (AChE) and butyryl-cholinestrase (BChE) with IC50s of 31 nM and 25.6 nM, respectively. -
acetylcholinesterase inhibitor
Pitofenone hydrochloride is an antispasmodic agent. It acts as a potent inhibitor of acetylcholinesterase activity. -
α7 Positive Modulator
NS 1738 is a α7 positive allosteric modulator.- Spencer R. Pierce, .et al. , Biomolecules, 2023, 13(4), 698 PMID: 37189445
- Hugo R Arias, .et al. , Br J Pharmacol, 2022, Sep 9 PMID: 36082615
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GABA receptor antagonist
(-)-Securinine is an alkaloid originally isolated from S. suffructicosa. Securinine, is a specific GABA receptor antagonist and has been found to have significant in vivo CNS activity. -
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. -
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.