|S2462||Donepezil HCl||5 mg/mL||<1 mg/mL||<1 mg/mL|
|S2547||Tiotropium Bromide hydrate||<1 mg/mL||8 mg/mL||<1 mg/mL|
|S2251||(-)-Huperzine A (HupA)||<1 mg/mL||0.66 mg/mL||<1 mg/mL|
|S2497||Pancuronium dibromide||100 mg/mL||100 mg/mL||100 mg/mL|
|S2550||Tolterodine tartrate||17 mg/mL||95 mg/mL||6 mg/mL|
|S3866||Galanthamine||57 mg/mL||100 mg/mL||-1 mg/mL|
|S3903||Lycorine||-1 mg/mL||57 mg/mL||-1 mg/mL|
|S3884||Jatrorrhizine||-1 mg/mL||67 mg/mL||-1 mg/mL|
|S3769||Palmatine||-1 mg/mL||70 mg/mL||-1 mg/mL|
|S3820||Dehydroevodiamine hydrochloride||-1 mg/mL||37 mg/mL||-1 mg/mL|
|S3835||Loganin||-1 mg/mL||78 mg/mL||-1 mg/mL|
|S3639||Tacrine hydrochloride hydrate||50 mg/mL||50 mg/mL||50 mg/mL|
|S3735||Umeclidinium bromide||<1 mg/mL||100 mg/mL||12 mg/mL|
|S3662||Pirenzepine dihydrochloride||84 mg/mL||1 mg/mL||<1 mg/mL|
|S3684||Methacholine chloride||39 mg/mL||39 mg/mL||39 mg/mL|
|S3701||Benactyzine hydrochloride||72 mg/mL||72 mg/mL||72 mg/mL|
|S2240||Fesoterodine Fumarate||100 mg/mL||100 mg/mL||100 mg/mL|
|S3005||Paroxetine HCl||1 mg/mL||73 mg/mL||35 mg/mL|
|S2629||PNU-120596||<1 mg/mL||62 mg/mL||1 mg/mL|
|S1754||Oxybutynin||<1 mg/mL||71 mg/mL||71 mg/mL|
|S2452||Amfebutamone (Bupropion) HCl||<1 mg/mL||8 mg/mL||<1 mg/mL|
|S3048||Solifenacin succinate||96 mg/mL||3 mg/mL||5 mg/mL|
|S1440||Varenicline Tartrate||72 mg/mL||1 mg/mL||<1 mg/mL|
|S1339||Galanthamine HBr||36 mg/mL||<1 mg/mL||<1 mg/mL|
|S1405||Vecuronium Bromide||4 mg/mL||100 mg/mL||100 mg/mL|
|S1683||Ipratropium Bromide||83 mg/mL||83 mg/mL||83 mg/mL|
|S2549||Trospium chloride||86 mg/mL||41 mg/mL||42 mg/mL|
|S2130||Atropine sulfate monohydrate||139 mg/mL||139 mg/mL||139 mg/mL|
|S4031||Aclidinium Bromide||<1 mg/mL||113 mg/mL||<1 mg/mL|
|S1397||Rocuronium Bromide||122 mg/mL||122 mg/mL||122 mg/mL|
|S1978||Methscopolamine||67 mg/mL||79 mg/mL||<1 mg/mL|
|S3047||Otilonium Bromide||113 mg/mL||113 mg/mL||113 mg/mL|
|S2508||Scopolamine HBr||76 mg/mL||76 mg/mL||<1 mg/mL|
|S2455||Bethanechol chloride||39 mg/mL||39 mg/mL||39 mg/mL|
|S2471||Gallamine Triethiodide||100 mg/mL||100 mg/mL||<1 mg/mL|
|S1608||Pyridostigmine Bromide||52 mg/mL||52 mg/mL||52 mg/mL|
|S2659||5-hydroxymethyl Tolterodine (PNU 200577, 5-HMT, 5-HM)||<1 mg/mL||68 mg/mL||68 mg/mL|
|S2614||Arecoline HBr||47 mg/mL||47 mg/mL||10 mg/mL|
|S4231||Pilocarpine HCl||48 mg/mL||48 mg/mL||48 mg/mL|
|S2087||Rivastigmine Tartrate||80 mg/mL||42 mg/mL||80 mg/mL|
|S1929||Irsogladine||<1 mg/mL||2 mg/mL||<1 mg/mL|
|S2490||Neostigmine Bromide||60 mg/mL||<1 mg/mL||<1 mg/mL|
|S3144||Darifenacin HBr||<1 mg/mL||100 mg/mL||<1 mg/mL|
|S3202||Catharanthine||<1 mg/mL||67 mg/mL||3 mg/mL|
|S4575||Pralidoxime (chloride)||34 mg/mL||<1 mg/mL||1 mg/mL|
|S4014||Hyoscyamine||<1 mg/mL||58 mg/mL||58 mg/mL|
|S4023||Procaine HCl||55 mg/mL||55 mg/mL||<1 mg/mL|
|S4024||Homatropine Methylbromide||74 mg/mL||74 mg/mL||10 mg/mL|
|S4025||Homatropine Bromide||71 mg/mL||71 mg/mL||<1 mg/mL|
|S4027||Flavoxate HCl||10 mg/mL||3 mg/mL||<1 mg/mL|
|S4121||Succinylcholine Chloride Dihydrate||79 mg/mL||1 mg/mL||<1 mg/mL|
|S2054||Orphenadrine Citrate||<1 mg/mL||92 mg/mL||<1 mg/mL|
|S4034||Diphemanil Methylsulfate||28 mg/mL||25 mg/mL||<1 mg/mL|
|S4617||Dextromethorphan (hydrobromide hydrate)||<1 mg/mL||74 mg/mL||74 mg/mL|
|S1832||Atracurium Besylate||33 mg/mL||100 mg/mL||100 mg/mL|
|S4143||Pentoxyverine Citrate||100 mg/mL||100 mg/mL||8 mg/mL|
|S4619||Itopride hydrochloride||78 mg/mL||78 mg/mL||38 mg/mL|
|S4422||Nitenpyram||54 mg/mL||54 mg/mL||54 mg/mL|
|S7366||LY2119620||<1 mg/mL||87 mg/mL||10 mg/mL|
|S4162||Benzethonium Chloride||90 mg/mL||90 mg/mL||90 mg/mL|
|S2287||Cytisine||38 mg/mL||38 mg/mL||38 mg/mL|
|S4171||Choline Chloride||28 mg/mL||28 mg/mL||28 mg/mL|
|S4069||Hexamethonium Dibromide||73 mg/mL||<1 mg/mL||<1 mg/mL|
|S4660||Glycopyrrolate||79 mg/mL||65 mg/mL||59 mg/mL|
|S4072||Decamethonium Bromide||84 mg/mL||34 mg/mL||25 mg/mL|
|S4505||Vinblastine sulfate||<1 mg/mL||100 mg/mL||<1 mg/mL|
|S3117||Oxybutynin chloride||4 mg/mL||79 mg/mL||79 mg/mL|
|S4542||Trihexyphenidyl hydrochloride||<1 mg/mL||7 mg/mL||24 mg/mL|
|S2082||Adiphenine HCl||70 mg/mL||30 mg/mL||18 mg/mL|
|S4718||Acetylcholine iodide||54 mg/mL||54 mg/mL||54 mg/mL|
|S4292||Diphenidol HCl||13 mg/mL||69 mg/mL||36 mg/mL|
|S1913||Tropicamide||<1 mg/mL||57 mg/mL||57 mg/mL|
Donepezil is a specific and potent AChE inhibitor for bAChE and hAChE with IC50 of 8.12 nM and 11.6 nM , respectively.
Donepezil-mediated eACh activity in vitro. After being cultured in serum-free EBM-2, HUVECs were treated with donepezil at a concentration of 10 umol/L for 24 hours. E and F: Representative images (x 400 magnification) of anti-ChAT and -VAChT immunofluorescence. Scale bar: 50 um. ChAT indicates choline acetyltransferase; eACh, endothelium-derived acetylcholine; EBM-2, endothelial basal medium 2; HUVECs, human umbilical vein endothelial cells; PCR, polymerase chain reaction; VAChT, vesicular acetylcholine transporter.
Tiotropium Bromide hydrate is a monohydrate of tiotropium bromide (Spiriva; Tiova; BA 679BR; tiopropium) that is an anticholinergic and bronchodilator and a muscarinic receptor antagonist.
(-)-Huperzine A is a potent, highly specific and reversible inhibitor of acetylcholinesterase (AChE) with Ki of 7 nM, exhibiting 200-fold more selectivity for G4 AChE over G1 AChE. Also acts as an NMDA receptor antagonist. Phase 4.
Pancuronium dibromide is a competitive nicotinic acetylcholine receptor antagonist, used as a muscle relaxant.
Tolterodine tartrate is a tartrate salt of tolterodine that is a competitive muscarinic receptor antagonist.
Acotiamide Hydrochloride is the hydrochloride salt form of acotiamide, a prokinetic agent with gastrointestinal (GI) motility-enhancing activity. It is a new orally active selective acetylcholinesterase inhibitor.
Harmaline, a natural occurrence β-carboline alkaloid, is a central nervous system stimulant and an acetylcholinesterase (AChR) inhibitor; also inhibits histamine N-methyltransferase.
Galantamine is a phenanthrene alkaloid and a reversible, competitive acetylcholinesterase inhibitor with IC50 of 0.35 μM, exhibits 50-fold selectivity against butyryl-cholinesterase. It is studied as a treatment for Alzheimer's disease and other central nervous system disorders.
Lycorine is a toxic crystalline alkaloid found in various Amaryllidaceae species that weakly inhibits acetylcholinesterase (AChE) and ascorbic acid biosynthesis.
Jatrorrhizine, one of the active constituents of Coptis chinensis Franch, has multiple bioactivities, such as hypoglycemic, antimicrobial, and antioxidant activities. It is an inhibitor of AChE with IC50 of 872 nM and demonstrates >115-fold selectivity for AChE over BuChE.
Palmatine, an isoquinoline alkaloid, has sedative, antidepressant, antioxidative, anti-ulcerative, antacid, anticancer, and anti-metastatic activities.
Dehydroevodiamine (DHE), a major phytochemical in fruits of Evodia rutaecarpa, can inhibit AChE. It has hypotensive and neuroprotective effects and modulates nitric oxide production.
Loganin is an iridoid glycoside first isolated from the seeds of Strychnos nux-vomica, a member of the Loganiaceae family. It is a non-competitive inhibitor of BACE1 with IC50 of 47.97 μM an also inhibits AChE and BChE with IC50 values of 3.95 μM and 33.02 μM, respectively.
Tacrine is a centerally active cholinesterase inhibitor that has been used to counter the effects of muscle relaxants, as a respiratory stimulant, and in the treatment of Alzheimer's disease and other central nervous system disorders. It also acts as a histamine N-methyltransferase inhibitor.
Umeclidinium bromide is a long-acting muscarinic antagonist approved for the maintenance treatment of chronic obstructive pulmonary disease (COPD).
Pirenzepine is an antimuscarinic agent which inhibits gastric acid secretion at lower doses than are required to affect gastrointestinal motility, salivary, central nervous system, cardiovascular, ocular and urinary functions.
Methacholine is a synthetic choline ester that acts as a non-selective muscarinic receptor agonist in the parasympathetic nervous system but has little effects on the nicotinic receptors.
Benactyzine hydrochloride is a centrally acting muscarinic antagonist. It is used as an antidepressant in the treatment of depression and associated anxiety.
Fesoterodine Fumarate is a prodrug of 5-hydroxymethyl tolterodine that is a muscarinic AChR receptor antagonist, used to treat overactive bladder syndrome.
Paroxetine HCl is an antidepressant drug of the SSRI type.
PNU-120596 is a positive allosteric modulator of α7 nAChR with EC50 of 216 nM.
C) A summary: MCAO-induced infarct volumes were significantly smaller in treated vs. untreated animals: p=0.0147 (n=10; two-tailed, the Mann–Whitney U-test). The results are presented as mean+S.E.M.
Oxybutynin is a competitive antagonist of the M1, M2, and M3 subtypes of the muscarinic acetylcholine receptor, used to relieve urinary and bladder difficulties.
Amfebutamone (Bupropion) HCl is a selective norepinephrine-dopamine reuptake inhibitor with IC50 of 6.5 and 3.4 μM for the reuptake of dopamine and norepinephrine, respectively.
Solifenacin succinate is a urinary antispasmodic of the antimuscarinic class.
Varenicline Tartrate is a nicotinic AChR partial agonist, used to treat nicotine addiction.
Galanthamine is an AChE inhibitor with IC50 of 0.35 μM, exhibits 50-fold selectivity against butyryl-cholinesterase.
Vecuronium is a non-depolarizing neuromuscular blocking agent, used for skeletal muscle relaxation during surgery.
Ipratropium Bromide is an antagonist of M3 type muscarinic acetylcholine receptors, used for the treatment of chronic obstructive pulmonary disease (COPD).
Trospium chloride is a competitive muscarinic cholinergic receptor antagonist.
Atropine sulfate monohydrate is a competitive antagonist for the muscarinic acetylcholine receptor, used to decrease the production of saliva and secretions of the airway prior to surgery.
Aclidinium Bromide inhibits human muscarinic AChR M1, M2, M3, M4 and M5 with Ki of 0.1 nM, 0.14 nM, 0.14 nM, 0.21 nM and 0.16 nM, respectively.
Rocuronium Bromide is a competitive AchR antagonist, used in modern anaesthesia.
Methscopolamine is a muscarinic acetylcholine receptor blocker.
Otilonium bromide is an antimuscarinic.
Scopolamine HBr is a competitive muscarinic acetylcholine receptor with an IC50 of 55.3 nM.
Bethanechol chloride is a selective muscarinic receptor agonist without any effect on nicotinic receptors.
Gallamine Triethiodide is a cholinergic receptor blocker with an IC50 of 68.0 ± 8.4 μM.
Pyridostigmine Bromide is a parasympathomimetic and a reversible cholinesterase inhibitor.
Acetylcholine (ACh)-related protein expression in vivo. Choline acetyltransferase (ChAT) in the ischemic area were determined among 3 experimental groups. Data of Western blotting are represented as fold of control.
5-hydroxymethyl tolterodine (PNU 200577) is a new muscarinic receptor antagonist with Kb of 0.84 nM.
Arecoline is a muscarinic acetylcholine receptor agonist.
Arecoline affects expression of epithelial-mesenchymal transition-related genes in a dose-dependent manner. Expression of epithelial-mesenchymal transition-related genes (CK19, E-cadherin, N-cadherin and vimentin) in HaCaT cells was determined by western blotting and the results were quantified. Data shown are means ± SD, *P<0.05, **P<0.01, ***P<0.001. CK19, cytokeratin 19.
Pilocarpine HCl is a nonselective muscarinic acetylcholine receptor agonist used to produce an experimental model of epilepsy.
Rivastigmine Tartrate is a cholinesterase inhibitor with IC50 of 5.5 μM, and used as a parasympathomimetic or cholinergic agent for the treatment of mild to moderate Alzheimer disease.
Irsogladine is an anti-gastric ulcer agent that facilitates gap-junctional intercellular communication through M1 muscarininc acetylcholine receptor binding.
Neostigmine Bromide is a reversible acetylcholinesterase inhibitor.
Darifenacin is a selective M3 muscarinic receptor antagonist with pKi of 8.9.
Catharanthine inhibits nicotinic receptor mediated diaphragm contractions with IC50 of 59.6 μM.
Pralidoxime is an antidote to organophosphate pesticides and chemicals; An acetylcholinesterase (AChE) reactivator.
Hyoscyamine is an AChR inhibitor with IC50 of 7.5 nM.
Procaine is an inhibitor of sodium channel, NMDA receptor and nAChR with IC50 of 60 μM, 0.296 mM and 45.5 μM, which is also an inhibitor of 5-HT3 with KD of 1.7 μM.
Procaine pretreatment inhibits JAK2 and STAT3 expression. (A) Relative Jak2 mRNA level detected by qRT-PCR. (B) Relative Stat3 mRNA level detected by qRT-PCR. (C) JAK2 and STAT3 protein expression detected by western blot. (D) Relative protein levels of JAK2 and STAT3 based on Western blot results. sham, rats undergone sham surgery. CCI, rats undergone sciatic nerve chronic compression injury (CCI) as the neuropathic pain (NPP) model. CCI+procaine, NPP model rats pretreated with procaine. The detection is performed on the 20th day post surgery (n=3). GAPDH is used as an internal reference. *p<0.05, **p<0.01. JAK2, Janus kinase 2. STAT3, signal transducer and activator of transcription 3.
Homatropine Methylbromide is muscarinic AChR antagonist, inhibits endothelial and smooth muscle muscarinic receptors of WKY-E and SHR-E with IC50 of 162.5 nM and 170.3 nM, respectively.
Homatropine Bromide is an muscarinic AChR antagonist, inhibits endothelial and smooth muscle muscarinic receptors of WKY-E and SHR-E with IC50 of 162.5 nM and 170.3 nM, respectively.
Flavoxate is a muscarinic AChR antagonist with IC50 of 12.2 μM.
Succinylcholine Chloride Dihydrate is a nicotinic AChR agonist and also acts as a depolarizing neuromuscular blocker.
Orphenadrine Citrate is a skeletal muscle relaxant, it acts in the central nervous system to produce its muscle relaxant effects.
Diphemanil Methylsulfate is a quaternary ammonium anticholinergic, it binds muscarinic acetycholine receptors (mAchR).
Dextromethorphan is an antitussive (cough suppressant) drug of the morphinan class with sedative, dissociative, and stimulant properties (at higher doses).
Atracurium Besylate is a neuromuscular blocking agent with ED95 of 0.2 mg/kg.
Pentoxyverine Citrate is an antitussive (cough suppressant) commonly used for cough associated with illnesses like common cold.
Itopride hydrochloride is an AChE inhibitor. The IC50 of itopride with AChE is 2.04 +/- 0.27 μM.
Nitenpyram is a nicotinic acetylcholine receptor (AchR) agonist, used as veterinary medicine to treat parasites of livestock and pets.
LY2119620 is a specific, and allosteric agonist of human M2 and M4 muscarinic acetylcholine receptors.
Benzethonium chloride is a potent inhibitor of nAChRs, it inhibits α4β2 nAChRs and α7 nAChRs with IC50 of 49 nM and 122 nM, respectively.
Cytisine is a nicotinic acetylcholine receptor agonist.
Choline chloride is a quaternary ammonium salt used as an additive for animal feed. It is important as a precursor of acetylcholine, as a methyl donor in various metabolic processes, and in lipid metabolism.
Hexamethonium Dibromide is a selective antagonist of neuronal-type nicotinic AChR in ganglia.
Glycopyrrolate is a muscarinic antagonist used as an antispasmodic, in some disorders of the gastrointestinal tract, and to reduce salivation with some anesthetics.
Decamethonium Bromide is a nicotinic AChR partial agonist and neuromuscular blocking agent.
Vinblastine sulfate inhibits microtubule formation and suppresses nAChR activity with IC50 of 8.9 μM in a cell-free assay, used to treat certain kinds of cancer.
Rivastigmine is a cholinesterase inhibitor with IC50 of 5.5 μM. It inhibits acetylcholinesterase (IC50 = 4.15 µM) and butyrylcholinesterase (IC50 = 37 nM).
Oxybutynin is an anticholinergic medication used to relieve urinary and bladder difficulties.
Trihexyphenidyl hydrochloride is an antiparkinsonian agent of the antimuscarinic class.
Adiphenine HCl is a nicotinic receptor inhibitor with IC50 of 15 μM, used as an antispasmodic drug.
Acetylcholine iodide is a neurotransmitter found at neuromuscular junctions, autonomic ganglia, parasympathetic effector junctions, a subset of sympathetic effector junctions, and at many sites in the central nervous system.
Diphenidol HCl is a potent antagonist of muscarinic M2 and M3 receptor with pKb of 6.72 and 7.02, respectively, used in the treatment of vomiting and vertigo.
Tropicamide is an anticholinergic and a muscarinic receptor subtype M4-preferring antagonist with IC50 of 8.0 nM.