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 26-41 of 41

  • BTMPS
    Cat. No.
    A67649

    BTMPS

    BTMPS is a selective antagonist of the nicotinic acetylcholine receptor (nAChR). It has been shown to mitigate the adverse effects of morphine in animal models, making it a valuable tool for research into addiction and pain management therapies. Its role in modulating neurotransmitter systems presents opportunities for further studies in neuropharmacology and the development of novel therapeutic strategies.

    1 mg
    $20.00
    10 g
    $25.00
    All 5 sizes
  • bPiDI
    Cat. No.
    A67654

    bPiDI

    bPiDI is a selective antagonist of the α6β2 nicotinic acetylcholine receptors (nAChRs). It effectively inhibits nicotine-evoked dopamine release in the striatum, making it a valuable tool for studying dopaminergic signaling pathways. This compound is particularly useful in research pertaining to nicotine addiction and dopamine-related disorders.

    5 mg
    $80.00
    10 mg
    $140.00
    All 5 sizes
  • Ropanicant
    Cat. No.
    A67656

    Ropanicant

    Synonyms: SUVN-911 free base

    Ropanicant is a potent and selective antagonist of the neuronal nicotinic acetylcholine α4β2 receptor. This compound exhibits oral bioavailability, making it a valuable tool for investigating the role of α4β2 receptor modulation in depression research. Its properties facilitate studies focused on neuropharmacology and the development of therapeutic strategies targeting mood disorders.

    Out of stock

    All 3 sizes
  • Lobelanidine
    Cat. No.
    A67670

    Lobelanidine

    Lobelanidine is a selective antagonist of nicotinic acetylcholine receptors (nAChR), effectively inhibiting the α7 nAChR response as well as the α3β2/α3β4 nAChR responses, with IC50 values of 2.8 μM and 8.2 μM, respectively. This compound serves as a valuable tool for investigating the role of nAChRs in neuronal signaling and various neurological disorders. Its pharmacological properties make it suitable for research applications in neurobiology, drug discovery, and toxicology studies.

    1 mg
    $280.00
    5 mg
    $680.00
    All 7 sizes
  • nAChR antagonist 1
    Cat. No.
    A67673

    nAChR antagonist 1

    nAChR antagonist 1 is a selective antagonist of the α7 nicotinic acetylcholine receptor, exhibiting an IC50 value of 3.3 μM. This compound is valuable for studying the role of α7 nAChR in various neurological conditions, including schizophrenia, Alzheimer's disease, and inflammatory disorders. Its modulatory effects on neurotransmission make it a relevant tool for exploring therapeutic strategies in these disease contexts.

    25 mg
    $1,275.00
    50 mg
    $1,625.00
    All 3 sizes
  • Methyllycaconitine
    Cat. No.
    A67679

    Methyllycaconitine

    Synonyms: MLA

    Methyllycaconitine is a selective competitive antagonist of the α7 nicotinic acetylcholine receptor (α7nAChR). It demonstrates significant neuroprotective effects by alleviating cytotoxicity induced by amyloid-β peptides in SH-SY5Y cells and mitigating methamphetamine-induced effects in the mouse striatum. Methyllycaconitine is a valuable tool for research into neurological disorders, including Alzheimer's disease.

    Out of stock

    All 3 sizes
  • T761-0184
    Cat. No.
    A67685

    T761-0184

    T761-0184 is a potent antagonist of the alpha-7 nicotinic acetylcholine receptor (nAChR). This compound effectively inhibits nAChR activity, making it a valuable tool for studying neurotransmission and synaptic plasticity. It holds potential for research applications in neurological disorders and offers insights into the mechanisms underlying cholinergic signaling.

    25 mg
    $1,275.00
    50 mg
    $1,625.00
    All 3 sizes
  • Chlorisondamine
    Cat. No.
    A67695

    Chlorisondamine

    Chlorisondamine is a nicotinic acetylcholine receptor antagonist that functions as a ganglionic blocker. It has been employed in studies to assess neurogenic factors influencing blood pressure and sympathetic vasomotor tone in animal models. Chlorisondamine exhibits antihypertensive properties, with significant effects on blood pressure, cardiac output, and heart rate, notably in murine experimental designs.

    25 mg
    $1,275.00
    50 mg
    $1,625.00
    All 3 sizes
  • (S)-UFR2709
    Cat. No.
    A67702

    (S)-UFR2709

    (S)-UFR2709 is a competitive antagonist of nicotinic acetylcholine receptors (nAChRs), with a notable preference for the α4β2 subtype over α7. This compound exhibits anxiolytic properties, effectively reducing anxiety and lowering ethanol consumption and preference in alcohol-preferring rat models. (S)-UFR2709 serves as a valuable reagent for research into nicotine addiction and related behavioral studies.

    5 mg
    $795.00
    All 1 sizes
  • nAChR antagonist 3
    Cat. No.
    A67707

    nAChR antagonist 3

    nAChR antagonist 3 is a selective antagonist of the α7 nicotinic acetylcholine receptor, demonstrating an IC50 of 0.86 μM. It exhibits protective effects against toxicity induced by paraoxon, making it a valuable tool for studying organophosphate poisoning. This compound is suitable for research applications focusing on neuroprotection and receptor modulation associated with cholinergic signaling pathways.

    Out of stock

    All 3 sizes
  • (rel)-Asperparaline A
    Cat. No.
    A67712

    (rel)-Asperparaline A

    Synonyms: (rel)-Aspergillimide; (rel)-VM55598

    (rel)-Asperparaline A is a potent antagonist of nicotinic acetylcholine receptors (nAChR), extracted from okara fermented with Aspergillus japonicas JV-23. This compound displays significant paralytic activity in silkworms, highlighting its potential as an anthelmintic agent. Its selectivity and effectiveness make it valuable for research applications focused on neurotransmission and parasitic control.

    1 mg
    $210.00
    5 mg
    $795.00
    All 2 sizes
  • Dihydro-β-erythroidine
    Cat. No.
    A67731

    Dihydro-β-erythroidine

    Dihydro-β-erythroidine is a competitive antagonist of nicotinic receptors, specifically targeting α4β2 subtypes. It effectively inhibits the discriminative stimulus properties associated with nicotine, as well as the anxiolytic effects induced by nicotine. This compound is widely utilized in neuropharmacological research to explore the role of nicotinic receptors in addiction, anxiety, and related behaviors.

    25 mg
    $2,285.00
    50 mg
    $2,935.00
    All 3 sizes
  • SR 16584
    Cat. No.
    A67736

    SR 16584

    SR 16584 is a selective antagonist of the α3β4 nicotinic acetylcholine receptor (nAChR), exhibiting an IC50 value of 10.2 μM. This compound is utilized in research investigating the role of nAChRs in neurological disorders and potential therapeutic applications. Its specific inhibition of α3β4 nAChR makes it valuable for studying the receptor's involvement in neurotransmission and related signaling pathways.

    1 mg
    $90.00
    5 mg
    $325.00
    All 3 sizes
  • ANQ9040
    Cat. No.
    A67744

    ANQ9040

    ANQ9040 is a steroidal relaxant that acts as a non-depolarizing nicotinic antagonist. It exhibits relatively low affinity for nicotinic receptors, making it suitable for investigating receptor function and characterizing neuromuscular mechanisms. This compound is primarily utilized in research applications related to muscle relaxation and neuromuscular transmission studies.

    Out of stock

    All 3 sizes
  • Microgrewiapine A
    Cat. No.
    A67752

    Microgrewiapine A

    Microgrewiapine A is a selective antagonist of nicotinic acetylcholine receptors (nAChR), specifically inhibiting human α4β2 and α3β4 subtypes with 60% and 70% efficacy, respectively. This compound demonstrates cytotoxic effects in HT-29 human colon cancer cells, exhibiting an IC50 value of 6.8 μM. Microgrewiapine A holds potential for research applications in cancer biology and neuropharmacology.

    5 mg
    $550.00
    All 1 sizes
  • Dexmecamylamine
    Cat. No.
    A67757

    Dexmecamylamine

    Synonyms: (+)-Mecamylamine; TC-5214

    Dexmecamylamine is a selective antagonist of the nicotinic acetylcholine receptors (nAChR), specifically targeting the α3β4, α4β2, α7, and α1β1γδ subtypes with IC50 values in the micromolar range. This compound demonstrates notable anxiolytic and antidepressant-like effects, making it a valuable tool in neurological research and the study of mood disorders. Its ability to modulate nAChR activity positions it as a potential lead for therapeutic development in psychiatric conditions.

    Out of stock

    All 3 sizes

Items 26-41 of 41

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