LY 367265

Catalog No.: A29932
SERT Inhibitor/5-HT₂A receptor Antagonist
LY 367265 is a potent inhibitor of the serotonin transporter (SERT) with an IC₅₀ value of 3.1 nM and also serves as a selective antagonist for the 5-HT₂A receptor (Kᵢ = 0.81 nM). It displays minimal activity on the norepinephrine transporter (NET) and low affinity for other serotonin receptor subtypes, reinforcing its selectivity. LY 367265 enhances the efflux of [³H]5-HT in a concentration-dependent manner (EC₅₀ = 250 nM) and can counteract the contraction induced by Sumatriptan, indicating its antagonistic effects on 5-HT₁D-like receptors. This compound is valuable for research into neurological disorders, including anxiety and post-traumatic stress disorder.
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Research use only. We do not sell to patients.

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Adooq Products cited in reputable paper
Science VOLUME 380, ISSUE 6663 (2023)
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Cell Vol. 185 Issue 23 p4428-4447.e28
Cell Vol 177, Issue 7, p1933-1947.e25
Cell Vol 156, Issue 5, p857-1114
Nature Volume 622 Issue 7982 (2023)
Nature volume 620, pages890-897 (2023)
Nature volume 610, pages540-546 (2022)
Nature volume 588, pages83-88 (2020)
Nature volume 574, pages268-272 (2019)
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Nature volume 567, pages118-122 (2019)
Nature volume 551, pages639-643 (2017)
Nature volume 551, pages247-250 (2017)
Nature volume 548, pages356-360 (2017)
Nature volume 545, pages187-192 (2017)
Biological Activity
DescriptionLY 367265 is a potent inhibitor of the serotonin transporter (SERT) with an IC₅₀ value of 3.1 nM and also serves as a selective antagonist for the 5-HT₂A receptor (Kᵢ = 0.81 nM). It displays minimal activity on the norepinephrine transporter (NET) and low affinity for other serotonin receptor subtypes, reinforcing its selectivity. LY 367265 enhances the efflux of [³H]5-HT in a concentration-dependent manner (EC₅₀ = 250 nM) and can counteract the contraction induced by Sumatriptan, indicating its antagonistic effects on 5-HT₁D-like receptors. This compound is valuable for research into neurological disorders, including anxiety and post-traumatic stress disorder.
Product Information
Catalog NumA29932
FormulaC24H25FN4O2S
Molecular Weight452.54
CAS Number210751-39-6
SMILESO=S1(N(CCN2CC=C(CC2)C3=CNC4=C3C=CC(F)=C4)C5=CC=CC6=C5N1CCC6)=O
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