氟辛克生

• 常用名: 氟辛克生
• 英文名: (R)-Flesinoxan
• CAS号: 98206-10-1
• 分子量: 415.45800
• 密度: 1.271g/cm3
• 沸点: 635.8ºC at 760mmHg
• 分子式: C₂₂H₂₆FN₃O₄
• 熔点: N/A
• 闪点: 338.3ºC

氟辛克生用途

Flesinoxan 是一种降压剂,是一种有效的,高亲和力的选择性的 5-羟色胺 1A (5-HT1A) 受体激动剂,EC50 值为 24 nM。Flesinoxan 还具有有效的抗焦虑/抗抑郁作用。

氟辛克生名称

• 中文名: 氟辛克生
• 英文名: 4-fluoro-N-[2-[4-[(2S)-2-(hydroxymethyl)-2,3-dihydro-1,4-benzodioxin-5-yl]piperazin-1-yl]ethyl]benzamide
• 中文别名: 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

氟辛克生生物活性

• 描述: Flesinoxan 是一种降压剂,是一种有效的,高亲和力的选择性的 5-羟色胺 1A (5-HT1A) 受体激动剂,EC50 值为 24 nM。Flesinoxan 还具有有效的抗焦虑/抗抑郁作用。
• 靶点实验:

  5-HT1A Receptor:24 nM (EC50)

• 体内研究: Flesinoxan在突触后充当部分激动剂,在突触前5-HT1A受体充当完全激动剂。Flesinoxan拮抗5-HT对CA3锥体神经元作用的能力与8-羟基-2-(二正丙基氨基)-四氢萘(8-OH-DPAT)相似[1]。静脉注射Flesinoxan可抑制CA3锥体神经元和中缝背侧5-HT神经元的放电活动。测定[3H]Flesinoxan和[3H]8-OH-DPAT的急性脑渗透。静脉注射后9分钟,[3H]8-OH-DPAT的脑浓度显着高于[3H]Flesinoxan[1]。皮下施用Flesinoxan和8-OH-DPAT产生剂量依赖性低温。通过预先施用非选择性5-HT1A拮抗剂吲哚醇和5-HT1/2拮抗剂甲基麦角苷,显着减弱了Flesinoxan诱导的体温过低。用3mg/kg的Flesinoxan和0.5mg/kg的8-OH-DPAT实现相似程度的低温。Flesinoxan的最大作用比8-OH-DPAT晚30分钟发生,并且消退更慢[1]。
• 参考文献:

  [1]. Hadrava V, et al. Characterization of 5-hydroxytryptamine1A properties of flesinoxan: in vivo electrophysiology and hypothermia study. Neuropharmacology. 1995 Oct;34(10):1311-26.

  [2]. Schoeffter P, et al. Centrally acting hypotensive agents with affinity for 5-HT1A binding sites inhibit forskolin-stimulated adenylate cyclase activity in calf hippocampus. Br J Pharmacol. 1988 Nov;95(3):975-85.

  [3]. Rodgers RJ, et al. Antianxiety and behavioral suppressant actions of the novel 5-HT1A receptor agonist, flesinoxan. Pharmacol Biochem Behav. 1994 Aug;48(4):959-63.

氟辛克生物理化学性质

• 密度: 1.271g/cm3
• 沸点: 635.8ºC at 760mmHg
• 分子式: C₂₂H₂₆FN₃O₄
• 分子量: 415.45800
• 闪点: 338.3ºC
• 精确质量: 415.19100
• PSA: 74.27000
• LogP: 1.90360
• InChIKey: NYSDRDDQELAVKP-SFHVURJKSA-N
• SMILES: O=C(NCCN1CCN(c2cccc3c2OCC(CO)O3)CC1)c1ccc(F)cc1
• 折射率: 1.585

氟辛克生靶点实验

查看更多实验

实验名称：TP_TRANSPORTER: transepithelial transport (basal to apical) in MDR1-expressing LLC-PK... 来源：ChEMBL 靶标：ATP-dependent translocase ABCB1 External Id：CHEMBL2076692

实验名称：Agonistic efficacy was evaluated by adenylyl cyclase assay in CHO cells stably expres... 来源：ChEMBL 靶标：5-hydroxytryptamine receptor 1A External Id：CHEMBL615697

实验名称：Antagonistic efficacy was evaluated by adenylyl cyclase assay in CHO cells stably exp... 来源：ChEMBL 靶标：5-hydroxytryptamine receptor 1A External Id：CHEMBL835003

实验名称：Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum act... 来源：ChEMBL 靶标：NON-PROTEIN TARGET External Id：CHEMBL3137722

实验名称：Highest frequency of moderate liver toxicity observed during clinical trials, express... 来源：ChEMBL 靶标：NON-PROTEIN TARGET External Id：CHEMBL3137723

实验名称：Acute liver toxicity defined via clinical observations and clear clinical-chemistry r... 来源：ChEMBL 靶标：N/A External Id：CHEMBL3137724

实验名称：Highest frequency of acute liver toxicity observed during clinical trials, expressed ... 来源：ChEMBL 靶标：NON-PROTEIN TARGET External Id：CHEMBL3137725

实验名称：Cytolytic liver toxicity, either proven histopathologically or where the ratio of max... 来源：ChEMBL 靶标：N/A External Id：CHEMBL3137726

实验名称：Choleostatic liver toxicity, either proven histopathologically or where the ratio of ... 来源：ChEMBL 靶标：N/A External Id：CHEMBL3137727

实验名称：Severe hepatitis, defined as possibly life-threatening liver failure or through clini... 来源：ChEMBL 靶标：N/A External Id：CHEMBL3137728

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氟辛克生英文别名

• unii-8hv9s83fny