α7nachr

PNU-120596 (NSC-216666) is a positive allosteric modulator of α7 nAChR with EC50 of 216 nM.

4BP-TQS is an allosteric agonist of α7 nAChRs.

Simufilam dihydrochloride (PTI-125 dihydrochloride) is a low toxicity, orally active filamin A (FLNA) activator, which can be used for the research of Alzheimer's disease. Simufilam dihydrochloride preferentially binds altered FLNA and restores its native conformation, restoring receptor and synaptic activities and reducing its α7nAChR/TLR4 associations and downstream pathologies.

Methyllycaconitine citrate (MLA) is an α7 neuronal nicotinic acetylcholine receptor (α7nAChR) antagonist that crosses the blood-brain barrier.

Pozanicline dihydrochloride (ABT-089 dihydrochloride) is an orally bioavailable agonist of the nicotinic acetylcholine receptor (nAChR) with a Ki of 16.7 nM.

α7nAChRModulator-3 (Compound 6p) is a positive allosteric modulator of α7nAChR, with an IC50 value of 1.3 μM. This compound is utilized in studies to inhibit auditory gating deficits in mouse models resembling schizophrenia.

α7nAChRModulator-2 (Compound 7b) is an α7nAChR positive allosteric modulator (PAM) with an EC50 of 2.1 μM. It is utilized in research focused on cognitive impairment.

GAT2711 is a full agonist of α9nAChR, with an EC50 of 230 nM. It exhibits 340 times greater selectivity for α9 over α7nAChR. In THP-1 cells, GAT2711 inhibits ATP-induced IL-1β release. Additionally, GAT2711 retains full analgesic activity in α7nAChR knockout mice.

RO5126946 is a Novel α7 nicotinic acetylcholine receptor-positive allosteric modulator. RO5126946 allosterically modulates α7nAChR activity. RO5126946 increased acetylcholine-evoked peak current and delayed current decay but did not affect the recovery of α7nAChRs from desensitization. In addition, RO5126946's effects were absent when nicotine-evoked currents were completely blocked by coapplication of the α7nAChR-selective antagonist methyl-lycaconitine.

R-(+)-Cotinine ((+)-Cotinine), a metabolite of Nicotine, demonstrates minimal activity across numerous pharmacological targets but enhances acetylcholine (Ach)-evoked current in human α7 nicotinic acetylcholine receptors (nAChRs) [1].

α-Conotoxin PnIA TFA, a potent and selective antagonist of the mammalian α7 nAChR, shows promise for neurological research, particularly in the study of neuropathic pain and Alzheimer's disease [1].

NS 1738 (NSC-213859) is a positive allosteric modulator of the α7-containing neuronal nicotinic acetylcholine receptors (nAChRs)

Azemiopsin, a potent inhibitor of the nicotinic acetylcholine receptor (nAChR), demonstrates half maximal inhibitory concentrations (IC50s) of 0.18 μM for T. californica nAChR and 22 μM for human α7 nAChR. Moreover, it effectively blocks acetylcholine-induced currents in Xenopus oocytes that heterologously express human muscle-type nAChR [1].

α-Conotoxin MrIC is a biased agonist selective for the α7 nicotinic acetylcholine receptor (nAChR), with activation contingent upon the presence of type II positive allosteric modulators, such as PNU120596. It is utilized to investigate neurological disorders and delineate the pharmacological characteristics of the α7nAChR [1].

RGH-560 (compound 53) exhibits highly advanced α7 nAChR positive modulation, favorable physicochemical properties, and robust in vivo procognitive potential. It is useful for studying Scopolamine-induced amnesia in mice [1].