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nAChR

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.

Items 26-28 of 28

  • (R)-(+)-Anatabine
    Cat. No.
    A67722
    CAS No.
    126454-22-6

    (R)-(+)-Anatabine

    (R)-(+)-Anatabine is an NF-κB inhibitor that acts to lower amyloid-β (Aβ) production by preventing the β-cleavage of amyloid precursor protein (APP). As the less active R-enantiomer of Anatabine, it retains the ability to modulate α4β2 nAChR activity. This compound exhibits anti-inflammatory properties and is being investigated for its potential applications in the treatment of neurodegenerative disorders.

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    5 mg
    $405.00
    25 mg
    $1,275.00
    All 3 sizes
  • AChE/nAChR-IN-1
    Cat. No.
    A67753
    CAS No.
    59417-09-3

    AChE/nAChR-IN-1

    AChE/nAChR-IN-1 is a dual inhibitor targeting acetylcholinesterase (AChE) and nicotinic acetylcholine receptors (nAChR). This compound exhibits potent toxicity and larvicidal activity against Culex pipiens larvae, with an LC50 of 4 ng/mL. AChE/nAChR-IN-1 is utilized in research focused on controlling mosquito populations and studying mosquito-borne diseases.

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  • Adiphenine
    Cat. No.
    B21342
    CAS No.
    64-95-9

    Adiphenine

    Adiphenine is a non-competitive inhibitor of nicotinic acetylcholine receptors (nAChR), exhibiting IC50 values of 1.9 μM for α1, 1.8 μM for α3β4, 3.7 μM for α4β2, and 6.3 μM for α4β4. This compound demonstrates significant anticonvulsant properties, making it valuable for studies related to seizure disorders and neuropharmacology. Its selective action on various nAChR subtypes positions Adiphenine as a useful tool for exploring the role of these receptors in different biological contexts.

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    25 mg
    $1,275.00
    50 mg
    $1,625.00
    All 3 sizes

Items 26-28 of 28

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