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AChR

AChR

货号 产品名 CAS号 信息
CSN19999 Vu0476406 1451993-12-6 VU0476406 is an important in vivo tool compound to enable translation of pharmacodynamics from rodent to non-human primates (NHP).
CSN21180 VU0467154 1451993-15-9 VU0467154 is a positive allosteric modulator of the M4 muscarinic acetylcholine receptor (mAChR), potentiating the response to ACh with pEC50s of 7.75, 6.2 and 6 for rat, human and cynomolgus monkey M4 receptor, respectively.
CSN27595 VU0238441   85511-68-8 VU0238441 is a potent agonist of muscarinic acetylcholine receptor M5 with EC50 of 2.1 μM.
CSN27586 VU0119498   79183-37-2 VU0119498 is a M1 muscarinic receptor agonist with EC50 of 3.1 μM, and pan mAChR M3, M5 positive allosteric modulator (PAM),and is a neuroprotective agent.
CSN23552 VU 0365114 1208222-39-2 VU 0365114 is a allosteric modulator of M5 with EC50 of 2.7 μM.
CSN21286 Varenicline 2HCl 866823-63-4 Varenicline HCl is a nicotinic receptor partial agonist and it stimulates nicotine receptors more weakly than nicotine itself does.
CSN23217 UB-165 fumarate 2454492-43-2 UB-165 is a potent nAChR ligand, which displays functional selectivity between nAChR subtypes. It is a full agonist at α3β2- and very weak partial agonist at α4β2- containing nAChRs with Ki values of 0.27, 20 (IC50), 2790 and 990 nM for α4β2, α3, α7 and α1β1δε respectively.
CSN23174 UB-165 200432-86-6 UB 165 is a full nAChR α3β2 agonist and a very weak partial nAChR α4β2 agonist with Ki value of 0.27nM and IC50 value of 20nM, respectively.
CSN21285 Revefenacin 864750-70-9 TD-4208 is a long-actingmuscarinic cholinergic receptor (mAChR) antagonist and may be potentially useful for the treatment of respiratory disease.
CSN21941 1,2,3,4-Tetrahydroacridin-9-amine xhydrochloride xhydrate 206658-92-6 Tacirne is an active cholinesterase inhibitor that blocks the degradation of cholinergic nerves in the cerebral cortex and hippocampus to increase cholinergic transmission. Tacrine induces hepatic damages in vitro. It can also induce oxidative stress and mitochondrial dysfunction. Tacrine treatment in HepG2 cells markedly inhibits the phosphorylation of GSK3β.
CSN21835 Solifenacin 242478-37-1 Solifenacin is a competitive antagonist of muscarinic receptors that potently blocks signaling through M1, M2, and M3 with Kis of 25, 125, and 10 nM, respectively.
CSN23115 SIB-1553A 191611-89-9 SIB-1553A is a nicotinic acetylcholine receptor agonist potentially for the treatment of Alzheimer’s disease (AD).
CSN24694 (R)-N-(Quinuclidin-3-yl)-2,3-dihydrobenzo[b][1,4]dioxine-6-carboxamide fumarate 527680-57-5 Selective α7 nAChR agonist
CSN23842 (αS)-7-((3-Hydroxy-2-phenylpropanoyl)oxy)-9-methyl-3-oxa-9-azatricyclo[3.3.1.02,4]nonane 9-oxide hydrobromide hydrate N/A Scopolamine N-oxide hydrobromide is an antagonist of the muscarinic acetylcholine.
CSN24865 6-Hydroxy-8-methyl-8-azabicyclo[3.2.1]octan-3-yl 3-hydroxy-2-phenylpropanoate 17659-49-3 Raceanisodamine is the active ingredient of Chinese herbal extracts that has vasoactive activity used to treat acute disseminated intravascular coagulation in patients in bacteremic shock.
CSN17113 Promethazine HCl 58-33-3 Promethazine HCl is the effective antagonist of the H1 receptor and moderate antagonist of mACh receptor.
CSN25236 Pirmenol 68252-19-7 Pirmenol inhibited the muscarinic acetylcholine receptor-operated K+ current (I[K.ACh]) in atrial cells and on experimental atrial fibrillation in isolated guinea-pig hearts.
CSN19465 Pirmenol HCl 61477-94-9 Pirmenol HCl inhibits IK.ACh by blocking muscarinic receptors. The IC50 of Pirmenol for inhibition of Carbachol-induced IK.ACh is 0.1 μM.
CSN20198 PHA-543613 hydrochloride 1586767-92-1 PHA-543613 HCl acts as a potent and selective agonist for the α7 subtype of neural nicotinic acetylcholine receptors, with a high level of brain penetration and good oral bioavailability.
CSN24691 PHA-543613 478149-53-0 PHA-543613 acts as a potent and selective agonist for the α7 subtype of neural nicotinic acetylcholine receptors, with a high level of brain penetration and good oral bioavailability. It is under development as a possible treatment for cognitive deficits in schizophrenia.
CSN20199 PHA-543613 2HCl 478148-58-2 PHA-543613 2HCl acts as a potent and selective agonist for the α7 subtype of neural nicotinic acetylcholine receptors, with a high level of brain penetration and good oral bioavailability.
CSN20484 PF-06827443 2115022-67-6 PF-06827443 is an otent, low clearance, orally bioavailable, and CNS penetrant muscarinic M1-selectivepositive allosteric modulator (PAM) with minimal agonist activity.
CSN24546 Oxotremorine M iodide 3854-04-4 Oxotremorine M iodide is a potent and selective muscarinic acetylcholine receptor (mAChR) agonist. Oxotremorine M iodide potentiates NMDA receptors by muscarinic receptor dependent and independent mechanisms[1].
CSN24692 NS3861 fumarate 216853-60-0 NS3861 is an α3β2 full agonist and an α3β4 partial agonist.
CSN23663 NS 1738 501684-93-1 NS 1738 is an allosteric modulator of α7 nicotinic acetylcholine receptor with cognitive-enhancing properties in vivo.
CSN26128 nAChR agonist 1 1394371-75-5 nAChR agonist 1 is a novel positive allosteric modulator of α7 nAChR. It has shown excellent safety profile in phase 1 clinical trials and is being evaluated for efficacy and safety as monotherapy in patients with mild to moderate Alzheimer’s disease.
CSN19962 N-Methylcytisine 486-86-2 N-Methylcytisine's nicotinic receptors have high affinity (KD = 50 nM)to nAChR from squid optical ganglia.
CSN23835 Mivacurium dichloride 106861-44-3 Mivacurium dichloride is a benzylisoquinoline derivative and is a short-acting non-depolarizing neuromuscular blocking agent and skeletal muscle relaxant. Mivacurium dichloride couples with the nAChR to reduce or inhibit the depolarizing effect of acetylcholine on the terminal disc of the muscle cell.
CSN21136 Methylbenactyzium Bromide 3166-62-9 Methylbenactyzium Bromide is a mAchR antagonist, used as a spasmolytic for the treatment of gastrointestinal ulcer and gastrointestinal spasms.
CSN24142 Mecamylamine HCl 826-39-1 Mecamylamine HCl is a non-competitive nicotinic acetylcholine receptor antagonist with antidepressant-like effects in mice.
CSN25425 LY2033298 886047-13-8 LY2033298 is a robust allosteric potentiator that is highly selective for the human M4 muscarinic acetylcholine receptor subtype. LY2033298 enhances inhibition by oxotremorine of light-induced phase shifts in hamster circadian activity rhythms.
CSN19428 Lobeline HCl 134-63-4 Lobeline HCl is a mixed agonist–antagonist of nAchR agonist and has multiple function such as VMAT2 ligand, inhibiting the reuptake of dopamine and serotonin, antagonist at μ-opioid receptors and P-glycoprotein inhibitor.
CSN24690 1,4-Diazabicyclo[3.2.2]nonan-4-yl(5-(3-(trifluoromethyl)phenyl)furan-2-yl)methanone hydrochloride 753499-14-8 High affinity α7 nAChR partial agonist; anti-inflammatory
CSN19397 (4aS,6R,8aS)-3-Methoxy-11-methyl-5,6,9,10,11,12-hexahydro-4aH-benzo[2,3]benzofuro[4,3-cd]azepin-6-ol 357-70-0 Galanthamine is a long-acting, centrally active acetylcholinesterase (AChE) inhibitor (IC50 = 410 nM) and allosteric potentiator at neuronal nicotinic ACh receptors.
CSN19398 Galanthamine HBr 1953-04-4 Galanthamine hydrobromide is a natural occuring AchE inhibitor with IC50 value of 410nM and allosteric potentiator at neuronal nAchRs, used for the treatment of cognitive decline in mild to moderate Alzheimer's disease and various other memory impairments.
CSN23811 Dicyclomine HCl 67-92-5 Dicyclomine is an anticholinergic that blocks muscarinic receptors. Dicyclomine is used to treat intestinal hypermotility and the symptoms of irritable bowel syndrome (also known as spastic colon). It relieves muscle spasms and cramping in the gastrointestinal tract by blocking the activity of acetylcholine on cholinergic (or muscarinic) receptors on the surface of muscle cells. It is a smooth muscle relaxant.
CSN22786 Dianicline 2HCl 292634-27-6 Dianicline is a selective α4β2 nAChR partial agonist with IC50 of 105 nM.
CSN25424 Cyclopentolate HCl 5870-29-1 Cyclopentolate (DL-Cyclopentolate) hydrochloride is an Atropine-like muscarinic receptors antagonist with a pKB value of 7.8 (on the circular ciliary muscle). Cyclopentolate hydrochloride is an anti-muscarinic agent commonly used in the ophthalmologic practice.
CSN24754 CCMI   917837-54-8 CCMI is a positive allosteric modulator of α7 nAChRs.
CSN20356 BQCA 338747-41-4 BQCA is a highly selective allosteric potentiator of the M1 mAChR and reduces the concentration of ACh required to activate M1 up to 129-fold with an inflection point value of 845 nM.
CSN19722 Bms-902483 1192810-88-0 BMS-902483 is a potent α7 nicotinic acetylcholine receptor partial agonist, which improved cognition in preclinical rodent models.
CSN22357 Beperidium iodide 86434-57-3 Beperidium iodide shows a competitive antagonistic effect against acetylcholine receptor with a pA2 of 7.93.
CSN20796 Benactyzine HCl 57-37-4 Benactyzine HCl is a centrally acting mAchR antagonist, used in the treatment of depression and in research to investigate the role of cholinergic systems on behavior.
CSN20387 TC-6683 1025007-04-8 AZD1446 is a highly selective α4β2 nicotinic acetylcholine receptor agonist for the treatment of cognitive disorders.
CSN19803 AF-DX 384 methanesulfonate 118290-27-0 AFDX384 is a bioactive chemical interacting with muscarinic acetylcholine receptor.
CSN20263 Nelonicline 1026134-63-3 ABT-126 is an alpha7 nicotinic acetylcholine receptor agonist and nicotinic acetylcholine receptor agonist. Nelonicline is potentially useful for the treatment of Alzheimer's diseases. ABT-126 may be useful to reduce dyskinesias in both early- and later-stage Parkinson's disease.
CSN25275 (S)-4-Chloro-N-(quinuclidin-3-yl)benzamide hydrochloride 128311-08-0 (S)-PNU-282987 is the an absolute stereochemistry form of PNU-282987.
CSN25570 (-)-(S)-B-973B 2244989-34-0 (-)-(S)-B-973B is positive allosteric modulator of α7 nAChRs with EC50 of ~0.3 μM.
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