Product Name: 3-(2,4-Dimethoxybenzylidene)anabaseine (GTS-21, DMXB-A)
CAS Number: 156223-05-1
Appearance: White Powder
Purity: 99%
Product Description:
3-(2,4-Dimethoxybenzylidene)anabaseine, also known as GTS-21 (DMXB-A), is a selective α7 nicotinic acetylcholine receptor (α7-nAChR) agonist with additional antagonistic activity on α4β2 nAChR (Ki = 20 nM) and 5-HT3A receptors (IC50 = 3.1 μM). This compound has been widely studied for its anti-inflammatory and cognitive-enhancing properties, making it a valuable tool in neuroscience and therapeutic research.
Biological Activity:
- Target Affinity:
- α7-nAChR: Selective agonist.
- α4β2 nAChR: High-affinity antagonist (Ki = 20 nM).
- 5-HT3A Receptor: Antagonist (IC50 = 3.1 μM).
- Mechanism of Action:
- Activates α7-nAChR to promote anti-inflammatory responses and cognitive enhancement.
- Inhibits 5-HT3A receptor activity, potentially contributing to its neuroprotective effects.
In Vitro Studies:
- Binds to human α4β2 nAChR with 100-fold higher potency than to human α7-nAChR.
- Demonstrates differential potency compared to (-)-nicotine, with 18-fold and 2-fold reduced activity at α4β2 and α7 nAChRs, respectively.
In Vivo Studies:
- Animal Model: C57BL/6 mice irradiated with 12 Gy to induce radiation-induced lung injury (RILI).
- Dosage: 4 mg/kg administered intraperitoneally on days 1, 3, 7, 14, and 21.
- Results:
- Reduced pulmonary inflammatory infiltrate and fibrosis in radiation-treated mice.
- Demonstrated protective effects against radiation-induced lung injury.
Applications:
- Neuroscience Research: Investigated for its role in enhancing cognition and protecting against neuroinflammation.
- Therapeutic Development: Potential applications in treating cognitive deficits and inflammatory conditions.
- Radiation Injury Studies: Shown to mitigate radiation-induced tissue damage, making it a candidate for further studies in protective therapeutics.
Storage Information:
- Conditions: Store at 2-8°C in a tightly sealed container to ensure product stability.
Features:
- High Purity: Ensures reliability in experimental outcomes.
- Selective Activity: Effective for targeted research applications in neuroscience and inflammation.
- Versatile Research Tool: Applicable in cognitive, anti-inflammatory, and radioprotection studies.
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