Insect neuronal nicotinic acetylcholine receptor (nAChR) (nAChR)

The insect nicotinic acetylcholine receptor (nAChR) is a member of the Cys-loop superfamily of pentameric ligand-gated ion channels and serves as the primary mediator of fast excitatory synaptic transmission in the insect central nervous system (CNS) [1.1.1, 1.1.2]. These receptors are composed of five subunits, typically including alpha and beta types, which assemble to form a cation-selective pore that opens upon the binding of acetylcholine [1.1.3, 1.4.3]. In insects, nAChRs are critical for various physiological processes, including sensory processing, motor coordination, and complex behaviors such as learning, memory, and sleep [1.2.3, 1.5.2]. Because of their vital role in the insect nervous system and their distinct pharmacological differences from vertebrate counterparts, nAChRs are the primary molecular targets for several major classes of insecticides, most notably the neonicotinoids [1.2.2, 1.3.4]. Drugs like imidacloprid and thiamethoxam act as agonists or modulators at these receptors, causing persistent activation that leads to hyperexcitability, paralysis, and eventual death of the insect [1.3.3, 1.5.1]. However, the widespread use of these compounds has raised significant safety concerns regarding their impact on non-target beneficial insects, such as pollinators, and the potential for developing insecticide resistance through target-site mutations [1.5.1, 1.5.2].

Other names

Insect nAChRNeuronal nicotinic acetylcholine receptorNicotinic acetylcholine receptornAChR

Agonist, Allosteric modulator, Competitive modulator, Antagonist