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Nicotinic acetylcholine receptor (nAChR) agonists, antagonists and modulators act on ligand-gated cation channels. Each receptor is a pentamer of subunits arranged around a central pore that opens when acetylcholine binds. A refined structure of the Torpedo receptor at 4 Å resolution, published in 2005, resolved its ligand-binding, membrane and cytoplasmic regions. Muscle-type receptors mediate neuromuscular transmission, while neuronal subtypes such as α7 and α4β2 are studied in attention, memory and nicotine dependence. Agonists include PNU 282987, which is selective for α7, and the partial agonist varenicline. PNU-120596, described in 2005, is a positive allosteric modulator of α7 that enhances acetylcholine-evoked currents. Vecuronium bromide, a neuromuscular blocking agent, acts on the muscle-type receptor.
nAChR modulator-2 is an orthosteric modulator of insect nicotinic acetylcholine receptors (nAChRs). This compound functions as an effective insecticide by influencing neurotransmission in target insects, leading to neurotoxic effects. It is particularly useful in research applications aimed at understanding insect physiology and the development of novel pest control strategies.
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nAChR modulator-1 is an orthosteric modulator of insect nicotinic acetylcholine receptors (nAChR), functioning as a targeted insecticide agent. This compound demonstrates significant biological activity by disrupting neurotransmission in insects, leading to paralysis and death. It is widely utilized in research applications for studying pest control mechanisms and developing novel insecticide strategies.
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GAT107 is a potent positive allosteric modulator (PAM) of the α7 nicotinic acetylcholine receptor (nAChR). It enhances receptor activity, making it useful for research into neuropharmacology and potential treatments for cognitive disorders. Its mechanism allows for modulation of cholinergic signaling, which is crucial in areas such as memory and learning. GAT107 can aid in elucidating the functional properties of α7 nAChR in various biological contexts.
Synonyms: Bancol
Bensultap is a nicotinic acetylcholine receptor (nAChR) modulator known for its insecticidal properties against the Colorado beetle and other insect pests. This compound exhibits mild and temporary neuromodulatory effects on the rat nervous system, making it relevant for research into nAChR function and insect neurobiology. Its applications extend to studies in pest management and the exploration of neural signaling pathways impacted by nAChR modulation.
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JNJ-1930942 is a selective positive allosteric modulator of the α(7) nicotinic acetylcholine receptor (nAChR) that effectively crosses the blood-brain barrier. This compound facilitates heightened intracellular Ca2+ levels and promotes neurotransmission at synapses in the hippocampal dentate gyrus. Additionally, JNJ-1930942 has been shown to reverse sensory gating deficits in DBA/2 mouse models, making it a valuable tool for research in neuropsychiatric disorders and synaptic physiology.
