Acetamiprid, a Neonicotinoid Insecticide, is a nAChR Agonist

Nicotinic acetylcholine receptors (nAChRs) are receptor peptides that respond to the neurotransmitter acetylcholine. Specifically, nAChRs are typical cation-selective ligand-gated ion channels. Besides, it can mediate rapid neurotransmission in the central and peripheral nervous systems. In the immune system, nAChRs regulate the inflammatory process and signal through different intracellular pathways. Moreover, acetylcholine binding protein (AChBP) is a soluble homolog of the extracellular ligand-binding domain of nAChR.

Furthermore, nAChRs is a key participant in neuronal communication. It converts neurotransmitter binding into membrane electrical depolarization. Meanwhile, the ligand-binding pocket (LBP) of agonists or antagonists in nAChRs is located at the interface between two adjacent subunits. Therefore, many neuronal nAChR subtypes supported by different subunit combinations show different pharmacological and biophysical properties. Nonetheless, different subtypes of neuronal nAChR also show complex expression profiles in the nervous system. nAChRs help to control resting membrane potential, regulate synaptic transmission and mediate rapid excitatory transmission. Importantly, nAChRs involve a series of physiological and pathological functions, so they are important therapeutic targets. Here, we will introduce a nAChR agonist, Acetamiprid.

Acetamiprid, a Neonicotinoid Insecticide, is a nAChR Agonist.

Above all, Acetamiprid is a neonicotinoid insecticide used worldwide. Acetamiprid is a nAChR agonist, and is relevant to neuromuscular and reproductive disorders.

Next in importance, Acetamiprid decreases in body weight and mildly affected spermatogenesis. Particularly, Acetamiprid decreases the expression of testosterone-metabolism genes, nAChR subunit genes, and proliferation-associated genes in mice.

Once again, Acetamiprid disrupts subsequent testosterone biosynthesis by decreasing the rate of conversion of cholesterol to testosterone. At the same time, it also disrupts it by preventing cholesterol from entering the mitochondria within the Leydig cells. Obviously, these effects caused reproductive damage to the rats

All in all, Acetamiprid, a neonicotinoid insecticide, is a nAChR agonist.


Kong D, et al. Biol Reprod. 2017 Jan 1;96(1):254-265.