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AChR Modulators

Cat.No. Product Name Information Product Use Citations Product Validations
S2629 PNU-120596 PNU-120596 (Nsc 216666) is a positive allosteric modulator of α7 nAChR with EC50 of 216 nM.
Front Med (Lausanne), 2021, 8:642960
J Leukoc Biol, 2020, 10.1002/JLB.6MA0720-344RRR
Pharmacol Biochem Behav, 2020, 10.1016/j.pbb.2020.172916
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S0518 NS 1738 NS 1738 (NSC 213859) is a novel positive allosteric modulator of the α7 nicotinic acetylcholine receptor (α7 nAChR), with respect to positive modulation of Xenopus laevis oocyte α7 nAChR with EC50 of 3.4 μM, as well as a comparable efficacy at the rat α7 nAChR with EC50 of 3.9 μM.
S0552 BNC210 BNC210 (H-Ile-Trp-OH, IW-2143) is a negative allosteric modulator of alpha-7 nicotinic acetylcholine receptor (α7 nAChR).
S0782 VU0238441 VU0238441 is a pan muscarinic acetylcholine receptor (mAChR) positive allosteric modulator (PAM) with EC50 of 2.1 μM, 2.2 μM, 2.8 μM, 3.2 μM and >10 μM for M5, M3, M2, M1 and M4, respectively.
S0783 VU0119498 VU0119498 is a pan Gq muscarinic acetylcholine receptor (mAChR) M1, M3, M5 positive allosteric modulator (PAM) with EC50 of 6.1 μM, 6.4 μM, 4.1 μM, respectively.
E0799 VU 0365114 VU 0365114 is a muscarinic acetylcholine receptor M5-preferring (mAChR M5-preferring) positive allosteric modulator (PAM) with an EC50 of 2.7 μM.
E0382 W-84 Dibromide W-84 dibromide (HDMPPA) is a potent allosteric modulator of M2-acetylcholine receptors, which retards 3HN-methylscopolamine dissociation.
E5792New BAY 2413555 BAY 2413555 is a first selective positive allosteric modulator of the muscarinic acetylcholine receptor (M2R) to restore cardiac autonomic balance. It also inhibits CYP2C8 and CYP2C9 with IC50 values of 17 µM and 13 µM, respectively.
S5931 BQCA BQCA (benzylquinolone carboxylic acid) is a highly selective positive allosteric modulator of the M1 muscarinic acetylcholine receptor (mAChR).
S5747 Morantel tartrate Morantel (CP-12009-18, UK 296418) is a positive allosteric modulator of neuronal nicotinic acetylcholine receptors (nAChRs).
S2646 VU0238429 VU0238429 (M5 PAM) is the first positive allosteric modulator of muscarinic acetylcholine receptor subtype 5 (mAChR5/M5) with EC50 of 1.16 μM at M5 and both > 30 μM at M1 and M3. This compound shows no potentiator activity at M2 or M4.
S1351 Ivermectin Ivermectin is a glutamate-gated chloride channel (GluCls) activator, used as a broad-spectrum antiparasitic drug. This compound is a specific positive allosteric effector of P2X4 and α7 nicotinic acetylcholine receptors (nAChRs). It is a specific inhibitor of Impα/β1-mediated nuclear import and has potent antiviral activity towards both HIV-1 and dengue virus. This chemical induces autophagy through the AKT/mTOR signaling pathway and mitophagy.
Nat Commun, 2025, 16(1):7156
J Adv Res, 2025, S2090-1232(25)00874-4
Biomed Pharmacother, 2025, 189:118248