NS 9283-d4
NS 9283-d4 is the deuterated-labeled NS 9283 (HY-110168). NS 9283 (A-969933) is a α4β2 nicotinic acetylcholine receptor (α4β2 nAChR) positive allosteric modulator that preferentially targets the (α4)3 (β2)2 stoichiometric conformation. NS 9283 increases the potency of ACh-induced currents without enhancing the maximal effect of ACh. NS 9283 also enhances prefrontal glutamate release, modulates attention-related electrophysiological responses, and potentiates the antinociceptive effects associated with α4β2 nAChR agonists. NS 9283 can be used in research related to inflammatory pain, postoperative pain, osteoarthritis pain, and Parkinson's disease.
For research use only. We do not sell to patients.
- Formula: C14H4D4N4O
- Molecular Weight:252.26
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
IC50 & Target
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α4β2 nAChR |
Application
1. This compound can be used as a tracer
2. This compound can be used as an internal standard for quantitative analysis by NMR, GC-MS, or LC-MS.
Chemical Information
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Unlabeled CAS 913830-15-6
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Molecular Weight 252.26
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Formula C14H4D4N4O
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SMILES
N#CC1=CC=CC(C2=NC(C3=C([2H])N=C([2H])C([2H])=C3[2H])=NO2)=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Human pluripotent stem cell midbrain dopaminergic neuron differentiation
Human pluripotent stem cells are directed toward midbrain dopaminergic neurons by first inducing a neural floor-plate-like progenitor state, then patterning cells with ventralizing SHH signaling and midbrain/WNT-FGF cues, and finally maturing progenitors into neurons expressing dopaminergic markers such as TH, NURR1/NR4A2, PITX3, DAT/SLC6A3, VMAT2/SLC18A2, GIRK2/KCNJ6, FOXA2, LMX1A, and EN1. The main readouts are loss of pluripotency, acquisition of FOXA2+/LMX1A+ midbrain floor-plate progenitors, emergence of βIII-tubulin+/MAP2+ neurons, and production of TH+ dopaminergic neurons with molecular, dopamine-release, and electrophysiological features of midbrain dopaminergic identity.
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Formalin-Induced Paw Inflammation/Nociceptive Inflammation
The formalin-induced paw inflammation/nociceptive test is a chemical persistent pain model in rodents in which subcutaneous injection of formalin into the hind paw produces spontaneous nocifensive behaviors such as flinching and licking. The response is classically biphasic, consisting of an early acute phase (Phase I) reflecting direct activation of peripheral nociceptors (particularly C-fiber afferents), followed by a later prolonged phase (Phase II) associated with central sensitization in the spinal dorsal horn driven by sustained afferent input and inflammatory signaling. This model is widely used to evaluate analgesic and anti-inflammatory interventions because it captures both peripheral nociception and central sensitization processes within a single assay system.
Purity & Documentation
References
[3]. Rode F, et al. Positive allosteric modulation of α4β2 nAChR agonist induced behaviour. Brain research. 2012 Jun 06;1458:67-75. [Content Brief]
[4]. Grupe M, et al. Unravelling the mechanism of action of NS9283, a positive allosteric modulator of (α4)3(β2)2 nicotinic ACh receptors. British Journal of Pharmacology. 2013;168:2000-2010. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)