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nAChR

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Cat. No. Product Name Field of Application Chemical Structure
DC73656 RGH-560
RGH-560 (RGH560) is a potent, selective α7 nAChR positive allosteric modulator (PAM) with EC50 of 190 nM (Ca2+-influx).
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DC73655 MK4334
MK4334 is a potent, selective positive allosteric modulator (PAM) of the α7 nAChR with potential for treatment of Alzheimer's disease.
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DC73654 JWX-A0108
JWX-A0108 is a novel selective type I α7 nAChR positive allosteric modulator (PAM) with EC50 of 4.35 uM, shows no potentiation effect on α3β4 nAChR, α4β2 nAChR, or 5-HT3AR.
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DC73653 DM506
DM506 is a novel ibogamine derivative and inhibitor of α7 and α9α10 nicotinic acetylcholine receptors (nAChRs) with IC50 of 5.1 uM, 5.6 uM and 6.4 uM for α9α10, α7β2 and α7nAChR, respectively.
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DC73652 CVN417
CVN417 (CVN-417) is a potent, selective and brain-penetrant α6-containing nicotinic acetylcholine receptor (α6 nAChR) antagonist with Ca2+ flux IC50 of 86 nM.
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DC73651 Cris-104
Cris-104 is a selective α4β2* neuronal nAChR agonist, demonstrates antinociceptive and antihypersensitivity in rodent acute/inflammatory and chronic pain models.
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DC73650 AT1001
AT1001 (AT-1001) is a high affinity and selective α3β4 nAChR antagonist with Ki value of 2.4 nM, >90-fold selectivity over the other major subtypes (α4β2 and α7 nAChR).
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DC73649 AN317
AN317 is a functionally selective, partial agonist of α6β2-containing nicotinic acetylcholine receptor (nAChR) with pEC50 of 7.17 (α6/α3β2β3V9'S receptor) in cell-based assays, inhibits the effect of nicotine with IC50 of 1.1 uM.
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DC73648 ABT-594 dihydrochloride
Tebanicline dihydrochloride (ABT-594) is a potent, orally active neuronal nicotinic acetylcholine receptor (alpha 4 beta 2 nAChR) agonist with Ki of 37 pM (rat brain) and 55 pM (transfected human receptor).
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DC73647 ABT-418 hydrochloride
ABT-418 hydrochloride (ABT418) is an analog of (-)-nicotine and cholinergic ligand (activator) of nAChRs, a potent inhibitor of [3H]-cytisine binding to nAChR in rat brain with Ki of 2 nM.
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DC11247 Nelonicline Featured
Nelonicline (ABT-126) is a potent, selective α7 nicotinic receptor (nAChR) partial agonist for the treatment of cognitive impairment with schizophrenia..
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DC41803 α-Conotoxin MII Featured
α-Conotoxin MII is a highly potent and selective competitive antagonist for α3β2 subunit-containing nicotinic receptors (IC50 = 0.5 - 3.5 nM at α3β2 expressed in Xenopus oocytes). Also potently blocks β3-containing neuronal nicotinic receptors. Displays > 200-fold selectivity for α3β2 over α2β2, α4β2 and α3β4.
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DC72654 UB-165
UB-165 is a nAChR agonist, being a full agonist of the α3β2 isoform and a partial agonist of the α4β2* isoform, with a Ki value of 0.27 nM for [3H]-nicotine binding in rat brain.
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DC7588 PNU120596 Featured
PNU-120596 is a positive allosteric modulator of α7 nAChR with EC50 of 216 nM.
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DC8303 GTS 21 2HCl(DMXBA) Featured
GTS 21 dihydrochloride is a partial agonist of α7 nicotinic acetylcholine receptors (nAChRs); also a weak α4β2 and 5-HT3 antagonist at micromolar concentrations.
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DC72359 PHA-543613 dihydrochloride
PHA-543613 dihydrochloride is a potent, orally active, brain-penetrant and selective α7 nAChR agonist with a Ki value of 8.8 nM. PHA-543613 dihydrochloride displays selectivity for α7-nAChR over α3β4, α1β1γδ, α4β2 and 5-HT3 receptors. PHA-543613 dihydrochloride can be used for the cognitive deficits of Alzheimer's disease and schizophrenia research.
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DC72214 Pyrantel
Pyrantel is an orally active anthelmintic and an agonist of the nicotinic acetylcholine receptor (nAChR). Pyrantel can cause spasmodic muscle paralysis in parasites. Pyrantel can be used in the study of parasitic infections such as ascariasis, hookworm infections, intestinal worms (pinworm infections), trichinosis and trichinosis.
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DC46413 DPNB-ABT594
DPNB-ABT594 is a nitrobenzyl-caged ABT594 and activates nAChRs containing the α4β2 subunits with good selectivity than the α7 subunit. DPNB-ABT594 can be used to map the distribution of nAChRs on neurons of the medial habenula (MHb) and helps to gain a deeper understanding of the nAChR‐mediated Ca2+ signalling in the MHb.
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DC71804 Zolunicant
Zolunicant (MM-110) is a potent inhibitor against nicotinic α3β4 receptors with an IC50 of 0.90 μM to combat addiction. Zolunicant can decrease the self-administration of several addictive agents including morphine, cocaine, methamphetamine, nicotine, and ethanol in rat model. Zolunicant can be studied as a potential treatment for multiple forms of drug abuse. Zolunicant also reveals a potent leishmanicide effect against Leishmania amazonensis.
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DC71803 Tribendimidine
Tribendimidine is an orally active, broad-spectrum anthelmintic agent, with particularly high activity against A. lumbricoides and N. americanus. Tribendimidine is also an L-type nicotinic acetylcholine receptor (nAChR) agonist.
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DC71366 T761-0184
T761-0184 is a potent α7 nicotinic receptor (nAChR) antagonist.
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DC71153 Chlorisondamine diiodide
Chlorisondamine (diiodide) is a potent nicotinic acetylcholine receptor (nAChR) antagonist and a ganglion blocker. Chlorisondamine antagonizes some of nicotine's central actions in a potent, long-lasting and pharmacologically selective way.
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DC71110 S 24795
S 24795 is a partial agonist of α7 nAChR and improves mnemonic function in aged mice for the treatment of aging-related memory disturbances.
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DC70830 TC-6683
TC-6683 (AZD1446) is a potent and highly selective α4β2 nAChR agonist with Ki of 30/34 nM against hα4β2/rα4β2, with little to no affinity against h α3β2 and h α7 (Ki>6.7 uM).TC-6683 (10 uM) produced <30% inhibition of specific binding or enzyme activity at all targets except the human (87%) and murine (97%) 5-HT3 receptors at a panel of 70 receptors, ion channels, and enzymes at NovaScreen/Caliper.TC-6683 (AZD1446) enhanced working memory in the object recognition paradigm in rats at every dose tested (0.1−3 mg/kg, po), exhibited favorable pharmaceutical properties and in vivo efficacy in animal models.
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DC70738 RJR-2403 hemioxalate
RJR-2403 (Rivanicline, Metanicotine) is a potent, selective neuronal nicotinic ACh (nAChR) agonist with high affinity to rat brain cortex (Ki=26 nM), does not significantly activate muscle type nAChRs or muscarinic receptors; RJR-2403 is comparable to nicotine in activating rat thalamic synaptosomes with EC50 of 732 nM; significantly improves passive avoidance retention after scopolamine-induced amnesia and enhanced both working and reference memory in rats, also demonstrates greatly reduced cardiovascular effects; exerts its antinociceptive effect via nicotinic rather than either opioid or muscarinic mechanisms.
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DC70735 RGM079
RGM079 (RGM-079) is a potent, selective α7 nAChR positive allosteric modulator (PAM) with EC50 of 8.3 uM.RGM079 exhibited a balanced pharmacokinetic profile and antioxidant properties comparable or even higher than well-known natural polyphenols.RGM079 shows neuroprotective properties in Alzheimer's disease (AD)-toxicity related models.RGM079 causes a concentration-dependent neuroprotective effect against the toxicity induced by okadaic acid (OA) in the human neuroblastoma cell line SH-SY5Y.RGM079 is able to restore the cellular viability after exposure to OA and amyloid peptide Aβ1–42, with cell death almost completely prevented at 10 and 30 μM, respectively, in primary cultures of rat cortical neurons;RGM079 shows in vivo analgesic activity in the complete CFA-induced paw inflammation model after intraperitoneal administration.
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DC70201 AP-202
AP-202 (AP202) is a highly potent and selective α4β2 nAChR antagonist with binding Ki of 18 nM, 57-fold selectivity over α3β4 receptor.AP-202 is agonist activity, also dispalys 40-fold, 10-fold and 90-fold selectivity over α4β4, α3β2, α3β4α5 receptors, does not activate α7 nAChR or block acetylcholine induced changes in membrane potential.AP-202 showed significant activity in blocking nicotine priming-induced as well as cue-induced reinstatement of nicotine seeking in vivo.
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DC8902 PNU282987 Featured
DC49704 nAChR modulator-1
nAChR modulator-1, a insecticide, is a insect nAChR orthosteric modulator.
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DC49703 nAChR modulator-2
nAChR modulator-2, a insecticide, is a insect nAChR orthosteric modulator.
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