Nicotinic Acetylcholine Receptor Modulators and Antibodies

Nicotinic Acetylcholine Receptor Modulators and Antibodies

Nicotinic acetylcholine receptors (nACh receptors or nAChRs) possess a crucial function in neurotransmission and are implicated in addiction and several illnesses. nAChRs generally function as ligand-gated ion channels and are composed of five homologous subunits that combine to create a central cation channel.

This channel is regulated by the binding of the endogenous nAChR agonist, acetylcholine, at the interfaces of the extracellular subunits. The subunit composition of nicotinic receptors can vary from α7 homomers to α4β2α6β2β3 heteromers. These subtypes differ in their affinity for acetylcholine and other nAChR agonists, such as nicotine, as well as the efficiency with which their channels are opened and desensitized. Additionally, subtypes vary in their affinity for nAChR antagonists, as well as positive and negative allosteric modulators.


The use of electrophysiological and molecular genetic techniques has facilitated the characterization of the structures of ligand binding sites of nicotinic receptors, the cation channel, and the links between them. These approaches have furthered the understanding of the organization of nAChR subunits and their respective contributions to function. Crystallography and cryo-electron microscopy also provide valuable insights into the structures and functions of nACh receptors.


Postsynaptic nAChRs play a critical role in neuromuscular and autonomic neurotransmission in the peripheral nervous system. In the brain, pre- and peri-synaptic nAChRs modulate neurotransmission and are responsible for the addictive effects of nicotine. Moreover, subtypes of nACh receptors in lymphocytes and non-synaptic locations may regulate inflammation and other cellular functions.


nAChR agonists bind to and activate nAChRs, mimicking the action of acetylcholine. Agonists can enhance cholinergic neurotransmission by stimulating ACh receptors, leading to signaling cascades. nAChR agonists that selectively target specific nicotinic receptor subtypes may have therapeutic potential for various conditions, including cognitive disorders, neurodegenerative diseases, and psychiatric disorders.


nAChR antagonists bind to nAChRs and block their activation by acetylcholine or other nAChR agonists. nAChR antagonists can inhibit cholinergic neurotransmission by preventing the binding of acetylcholine, leading to the decreased release of neurotransmitters. nAChR antagonists may have therapeutic applications, such as in smoking cessation therapies, where they reduce the reinforcing effects of nicotine by blocking nAChRs.

Though the targeting of nAChRs for therapeutic purposes has garnered considerable attention, discerning subtypes remains a persistent obstacle due to structural similarity. Further research is required to shed light on the structure and function of nAChRs, as well as the development of improved pharmacological tools such as nAChR agonists and nAChR antagonists that target nAChRs in the treatment of addiction, pain, inflammation, and other medical conditions.


nAChR products are essential tools for research focused on understanding the role of nicotinic receptors in various biological processes. Alomone Labs offers a range of nAChR products, including nAChR agonists, nAChR antagonists, antibodies, fluorescent toxins, research packs, and more, providing everything you need for nAChR research.



How Rabies Modulates Macrophages

Rabies is infamous for its high mortality rate, with around 60,000 reported deaths each year. It’s usually contracted from infected dogs, but bats are also significant carriers in the Americas…

Making better pacemaker cells

How can differentiation into pacemaker cells be boosted?

2023 © Alomone Labs. All Rights Reserved.

Terms of ServicePrivacy Policy