氟辛克生
中文名稱 | 氟辛克生 |
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中文同義詞 | N-(2-(4-((2R)-2,3-二氫-2-(羥甲基)-1,4-苯并二惡英-5-基)-1-哌嗪基)乙基)-4-氟苯甲酰胺;氟辛克生;化合物 T16711;化合物 FLESINOXAN |
英文名稱 | Flesinoxan |
英文同義詞 | N-[2-[4-[[(R)-2,3-Dihydro-2α-hydroxymethyl-1,4-benzodioxin]-5-yl]-1-piperazinyl]ethyl]-4-fluorobenzamide;N-[2-[4-[[(S)-2,3-Dihydro-2β-hydroxymethyl-1,4-benzodioxin]-5-yl]-1-piperazinyl]ethyl]-4-fluorobenzamide;FLESINOXAN;N-(2-(4-((2R)-2,3-Dihydro-2-(hydroxymethyl)-1,4-benzodioxin-5-yl)-1-piperazinyl)ethyl)-4-fluorobenzamide;Benzamide, N-[2-[4-[(2R)-2,3-dihydro-2-(hydroxymethyl)-1,4-benzodioxin-5-yl]-1-piperazinyl]ethyl]-4-fluoro- |
CAS號 | 98206-10-1 |
分子式 | C22H26FN3O4 |
分子量 | 415.46 |
EINECS號 | |
相關(guān)類別 | |
Mol文件 | 98206-10-1.mol |
結(jié)構(gòu)式 |
氟辛克生 性質(zhì)
比旋光度 | D +26° (c = 1 in methanol) |
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沸點 | 635.8±55.0 °C(Predicted) |
密度 | 1.271±0.06 g/cm3(Predicted) |
儲存條件 | Store at -20°C |
溶解度 | 二甲基亞砜:31.25 mg/mL(75.22 mM) |
酸度系數(shù)(pKa) | 14.09±0.10(Predicted) |
形態(tài) | 固體 |
顏色 | 米白色至淺黃色 |
5-HT 1A Receptor 24 nM (EC 50 ) |
Flesinoxan acts as a partial agonist at postsynaptic and as a full agonist at presynaptic 5-HT1A receptors. The capacity of Flesinoxan to antagonize the effect of 5-HT on CA3 pyramidal neurons was similar to that of 8-hydroxy-2-(di-n-propylamino)-tetralin (8-OH-DPAT).
The intravenous administration of Flesinoxan suppresses the firing activity of both CA3 pyramidal neurons and dorsal raphe 5-HT neurons. The acute brain penetration of [
3
H]Flesinoxan and [
3
H]8-OH-DPAT are determined. Nine minutes after intravenous administration, [
3
H]8-OH-DPAT reached significantly greater brain concentration than [
3
H]Flesinoxan.
Subcutaneous administration of Flesinoxan and 8-OH-DPAT produce a dose-dependent hypothermia. The Flesinoxan-induced hypothermia is significantly attenuated by prior administration of the non-selective 5-HT1A antagonist pindolol and the 5-HT1/2 antagonist methysergide. Similar degrees of hypothermia are achieved with 3 mg/kg of Flesinoxan and 0.5 mg/kg of 8-OH-DPAT. The maximal effect of Flesinoxan occurs 30 min later than that of 8-OH-DPAT and fades more slowly.
安全信息
更新日期 | 產(chǎn)品編號 | 產(chǎn)品名稱 | CAS號 | 包裝 | 價格 |
---|---|---|---|---|---|
2024/11/08 | HY-121653 | Flesinoxan | 1 mg | 2045元 | |
2024/11/08 | HY-121653 | 氟辛克生 Flesinoxan | 98206-10-1 | 5mg | 4500元 |