152148-63-5
Chemical Structure
A 80426
- CAS No.: 152148-63-5
- Formula:C23H27NO2
- Molecular Weight:349.47
IUPAC Name: (R)-2-(benzofuran-6-yl)-N-((5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)methyl)-N-methylethan-1-amine
InChIKey: MHPMXTGKTXJIDI-IBGZPJMESA-N
SMILES: C(N(CCC=1C=C2C(=CC1)C=CO2)C)[C@H]3C=4C(=C(OC)C=CC4)CCC3
Biological Activity: A 80426 is an orally active serotonin (5-HT uptake) inhibitor (IC50 = 13 nM; Ki = 3.8 nM) and α2-Adrenoceptor receptor antagonist (Ki = 2 nM). A 80426 shows weak antagonistic effect to dopamine D1 receptor (Ki = 744 nM) and D2 receptor (Ki = 52 nM). A 80426 upregulates the expression and activity of TRPV1, activates the NF-κB and PI3K pathways, and reduces the levels of pro-inflammatory cytokines IL-1β, IL-6, and TNF-α. A 80426 can be used in research related to inflammatory pain and depression[1][2].
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A 80426 | A 80426 is an orally active serotonin (5-HT uptake) inhibitor (IC50 = 13 nM; Ki = 3.8 nM) and α2-Adrenoceptor receptor antagonist (Ki = 2 nM). A 80426 shows weak antagonistic effect to dopamine D1 receptor (Ki = 744 nM) and D2 receptor (Ki = 52 nM). A 80426 upregulates the expression and activity of TRPV1, activates the NF-κB and PI3K pathways, and reduces the levels of pro-inflammatory cytokines IL-1β, IL-6, and TNF-α. A 80426 can be used in research related to inflammatory pain and depression. | |||||||||||||||||||||
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References
- [1]. Ling X, et al. A-80426 suppresses CFA-induced inflammatory pain by suppressing TRPV1 activity via NFκB and PI3K pathways in mice. Clinics (Sao Paulo, Brazil). 2023;78:100213. [Content Brief]
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[2]. Giardina, W. J., et al. (1995). A‐80426, a potent and selective α2‐adrenoceptor antagonist with serotonin uptake‐blocking activity and putative antidepressant‐like effects: II. Pharmacology profile. Drug development research, 35(4), 246-260.
