α7nachr

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

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.

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

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

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].

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

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.

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].

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].

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