nachr agonist 2

Compound 8, identified as a selective alpha4beta2 (α4β2) neuronal acetylcholine receptor (nAChR) agonist, demonstrates a dissociation constant (Kd) of 26 nM, indicating high affinity for this receptor subtype.

Pozanicline hydrochloride is an orally bioavailable nicotinic acetylcholine receptor (nAChR) agonist with a Ki of 16.7 nM for binding to [3H]cytisine sites[1]. Pozanicline hydrochloride is an α4β2-selective nAChR agonist, which binds to rat brain α4β2 nAChR with a Ki of 17 nM while binding to α7 nAChR is insignificant[2].

5-AAM-2-CP is one of the major metabolites of Acetamiprid. Acetamiprid, a nAChR agonist, is a neonicotinoid insecticide used worldwide.

AR-R17779 hydrochloride is a potent, selective full agonist of the nAChR, demonstrating K i values of 92 nM for the α7 subtype and 16,000 nM for the α4β2 subtype. It is noted for its ability to enhance learning and memory in rats, suggesting potential therapeutic applications. Additionally, this compound exhibits anxiolytic properties and can mitigate inflammation by activating anti-inflammatory cholinergic (vagal) pathways [1] [2] [4].

CMPI hydrochloride, a potent and selective nAChR agonist, functions as a positive allosteric modulator (PAM) specifically targeting the α4:α4 subunit interface of the nAChR. It enhances the response of the (α4)3(β2)2 nAChR to acetylcholine (ACh) (10 μM) with an EC 50 of 0.26 μM. With its potential for researching nicotine dependence and various neuropsychiatric conditions linked to reduced brain cholinergic activity, CMPI hydrochloride stands as a significant compound in neurological research.

DPNB-ABT 594 is a nitrobenzyl-caged ABT 594, a selective α4β2 nAChR agonist. One-photon uncaging evokes large inward currents and Ca2+transients on cell bodies and dendrites of medial habenular neurons in mouse brain slices. Two-photon uncaging induces fast nAChR-mediated currents. Photolyzed with high quantum yield of 0.20. Effective photolysis occurs using one- or two-photon excitation; one-photon uncaging requires illumination at 410 nm for 1.5-3 ms; two-photon uncaging requires illumination with appropriate two photon pulse laser at 710 nm for ~2 ms.

Bradanicline is a potent and highly selective agonist of the α7 nicotinic acetylcholine receptor (nAChR) with an EC50 of 17 nM and a Ki of 1.4 nM for the human α7 nAChR. It is primarily employed in research pertaining to cognitive disorders [1] [2].

5-AMAM-2-CP, a significant metabolite of Acetamiprid, serves as a global insecticide within the neonicotinoid class and acts as an nAChR agonist [1] [2].

Anatoxin-a (ATX-a), a neurotoxic alkaloid, functions as an agonist for the nicotinic acetylcholine receptor (nAChR) and as an inhibitor of Acetylcholinesterase (AChE) [1] [2].