欧前胡素 T2845

Product Introduction
Bioactivity


英文名: Imperatorin

描述: Imperatorin (8-Isopentenyloxypsoralene) 是NO synthesis 和BChE 的抑制剂，IC50分别为 9.2 μmol 和 31.4 μmol。它也是TRPV1的微弱激动剂，EC50为 12.6±3.2 μM。

体外活性: Imperatorin是一种属于香豆素-特别是呋喃香豆素的植物次生代谢产物。通过α1β2γ2S受体，Imperatorin增强了GABA诱导的氯离子电流(IGABA)。在100 μmol时Imperatorin增强了IGABA 50.5±16.3%，而在300 μmol时增强了109.8±37.7%。在A. dahurica的根中发现的Imperatorin与Phellopterin共同抑制了大鼠大脑GABAA受体的苯二氮卓位点上的[3H]地西泮结合，其IC50分别为Imperatorin的12.3 μmol和Phellopterin的400 nmol。Imperatorin在3.5至14 mmol的浓度范围内，通过与GABA-T的活性位点不可逆地结合，以时间依赖性和浓度依赖性的方式显著且不可逆地抑制GABA-T。Imperatorin是可逆的乙酰胆碱酯酶(AChE)抑制剂，以剂量依赖的方式作用。通过分光光度法测试了Imperatorin和来自Angelica archangelica L.果实的粗提物的AChE和BChE抑制活性，浓度分别为12.5, 25, 50, 和100 μg/mL。Imperatorin对AChE的抑制较弱(13.75-46.11 %)，而对BChE的抑制作用显著(37.46-83.98 %)，对BChE而非AChE表现出选择性，BChE的IC50为31.4 μmol。Imperatorin与(+)-Byakangelicol是最有效的BACE-1抑制剂，IC50分别为91.8 μmol和104.9 μmol。作为一种NO合成抑制剂，Imperatorin (IC50=9.2 μmol)也显示出有效性。Imperatorin是TRPV1的弱激动剂，这是一个涉及检测多种有害刺激的通道，表现出12.6±3.2 μM的EC50。

体内活性: At doses of 10 and 20 mg/kg and 30 min after injection, Imperatorin shows an anxiolytic effect and improved different stages of memory and learning processes-both acquisition and consolidation. It is also shown that acute administration Imperatorin at doses of 10 and 20 mg/kg reduced the anxiogenic effect of nicotine (0.1 mg/kg, subcutaneous, s.c.). At 30 and 40 mg/kg, i.p. Imperatorin significantly enhanced the anticonvulsant activity of carbamazepine against maximal electroshock-induced seizures expressed by lowering the ED50 from 10.8 to 6.8 mg/kg (by 34 %) and 6 mg/kg (by 42 %), respectively. Furthermore, Imperatorin at 30 mg/kg and carbamazepine at 6.8 mg/kg exhibit an increase the total brain concentration of carbamazepine from 1.260 to 2.328 μg/mL (by 85%), which may be caused by modifying the blood-barrier permeability or acting like an inhibitor of multi-drug resistance proteins[1]. Imperatorin, a naturally occurring furanocoumarin, inactivates gamma-aminobutyric acid transaminase and inhibits acetylcholinesterase activity. Imperatorin administered acutely at the doses of 5 and 10 mg/kg prior to the injection of scopolamine (1 mg/kg) improves memory acquisition and consolidation impaired by scopolamine. Furthermore, repeatable (7 days, twice daily) administration of the highest dose of Imperatorin (10 mg/kg) significantly attenuates the effects of scopolamine on memory acquisition, whereas the doses of 5 and 10 mg/kg of this furanocoumarin are effective when memory consolidation is measured [3].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 55 mg/mL (203.49 mM)


关键字: TRP Channel | inhibit | Cholinesterase (ChE) | Inhibitor | Transient receptor potential channels | Imperatorin

相关产品: (Z)-Capsaicin | Methyl salicylate | ICILIN | ML204 | NMDAR/TRPM4-IN-2 | ML-SA1 | SAR7334 | Mesendogen | GSK1016790A | Pinokalant

相关库: Anti-Neurodegenerative Disease Compound Library | Drug Repurposing Compound Library | FDA-Approved & Pharmacopeia Drug Library | Anti-Cancer Drug Library | Membrane Protein-targeted Compound Library | Inhibitor Library | Anti-Cancer Approved Drug Library | Traditional Chinese Medicine Monomer Library | Antiparasitic Natural Product Library | RO5 Drug-like Natural Product Library

欧前胡素 T2845信息由TargetMol中国为您提供，如您想了解更多关于欧前胡素 T2845报价、型号、参数等信息，欢迎来电或留言咨询。

注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途