98206-10-1
基本信息
N-(2-(4-((2R)-2,3-二氢-2-(羟甲基)-1,4-苯并二恶英-5-基)-1-哌嗪基)乙基)-4-氟苯甲酰胺
N-[2-[4-[[(S)-2,3-Dihydro-2β-hydroxymethyl-1,4-benzodioxin]-5-yl]-1-piperazinyl]ethyl]-4-fluorobenzamide
N-[2-[4-[[(R)-2,3-Dihydro-2α-hydroxymethyl-1,4-benzodioxin]-5-yl]-1-piperazinyl]ethyl]-4-fluorobenzamide
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-
物理化学性质
| 比旋光度 | D +26° (c = 1 in methanol) |
| 沸点 | 635.8±55.0 °C(Predicted) |
| 密度 | 1.271±0.06 g/cm3(Predicted) |
| 储存条件 | -20°C储存 |
| 溶解度 | DMSO: 31.25 mg/mL (75.22 mM) |
| 酸度系数(pKa) | 14.09±0.10(Predicted) |
| 形态 | Solid |
| 颜色 | Off-white to light yellow |
常见问题列表
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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.