Imperatorin-Ammidin-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEImperatorinCat. No.: HY-N0285CAS No.: 482-44-0Synonyms: Ammidin分式: CHO分量: 270.28作靶点: AChE; TRP Channel作通路: Neuronal Signaling; Membrane Transporter/Ion Channel储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 mont

2、h溶解性数据体外实验 DMSO : 50 mg/mL (184.99 mM; Need ultrasonic)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (9.25 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (9.25 mM); Clear solution1/3 Master of Small Molecules 您边的抑制剂师www.MedChemEBIOLOGICAL ACTIVITY物活性 Imper

3、atorin种有效的 NO synthesis 抑制剂，IC50 为 9.2 mol，也BChE 抑制剂，IC50 为 31.4 mol。ImperatorinTRPV1 的微弱激动剂，EC50 为 12.63.2 M。IC50 & Target IC50: 9.2 mol (NO synthesis), 31.4 mol (BChE) 1EC50: 12.63.2 M (TRPV1) 2体外研究 Imperatorin is a plant secondary metabolite belonging to the coumarins-specifically the furanocouma

4、rins.Imperatorin enhances the GABA-induced chloride ion current (IGABA) through the 122S receptors.Imperatorin potentiates IGABA at 100 mol by 50.516.3 % and at 300 mol by 109.837.7 %, respectively.Imperatorin, together with Phellopterin, found in the roots of A. dahurica, inhibit 3Hdiazepam binding

5、 to thebenzodiazepine site of the rat brain GABAA receptor in vitro with an IC50 of 12.3 mol for Imperatorin and400 nmol for Phellopterin. Imperatorin, in a concentration ranging from 3.5 to 14 mmol, significantly andirreversibly inhibits GABA-T in a time-dependent and concentration-dependent manner

6、, by irreversiblybinding with the active site of GABA-T.Imperatorin is a reversible acetylcholinesterase (AChE) inhibitor, andacts in dose-dependent manner. The AChE and BChE inhibitory activities of Imperatorin and a crude extractfrom the fruits of Angelica archangelica L. is tested by the spectrop

7、hotometric method at concentrations of12.5, 25, 50, and 100 g/mL. Imperatorin displays low inhibition towards AChE (13.75-46.11 %), whereas ithas remarkable inhibitory effect against BChE (37.46-83.98 %). Imperatorin shows selectivity toward BChErather than AChE, with an IC50 for BChE of 31.4 mol. I

8、mperatorin, together with (+)-Byakangelicol, arefound to be the most effective BACE-1 inhibitors, with IC50s of 91.8 and 104.9 mol, respectively.Imperatorin (IC50=9.2 mol) is also effective as an inhibitor of NO synthesis 1. Imperatorin is a weakagonist of TRPV1, a channel implicated in detecting se

9、veral noxious stimuli, exhibiting EC50 of 12.63.2 M2.体内研究 At doses of 10 and 20 mg/kg and 30 min after injection, Imperatorin shows an anxiolytic effect and improveddifferent stages of memory and learning processes-both acquisition and consolidation. It is also shown thatacute administration Imperat

10、orin at doses of 10 and 20 mg/kg reduced the anxiogenic effect of nicotine (0.1mg/kg, subcutaneous, s.c.). At 30 and 40 mg/kg, i.p. Imperatorin significantly potentiates the anticonvulsantactivity of carbamazepine against maximal electroshock-induced seizures expressed by lowering the ED50from 10.8

11、to 6.8 mg/kg (by 34 %) and 6 mg/kg (by 42 %), respectively. Moreover, Imperatorin at 30 mg/kgand carbamazepine at 6.8 mg/kg shows increases the total brain concentration of carbamazepine from 1.260to 2.328 g/mL (by 85%), which may be caused by modifying the blood-barrier permeability or acting like

12、aninhibitor of multi-drug resistance proteins 1. Imperatorin, a naturally occurring furanocoumarin, inactivatesgamma-aminobutyric acid transaminase and inhibits acetylcholinesterase activity. Imperatorin administeredacutely at the doses of 5 and 10 mg/kg prior to the injection of scopolamine (1 mg/k

13、g) improves memoryacquisition 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 ofscopolamine on memory acquisition, whereas the doses of 5 and 10 mg/kg of this fur

14、anocoumarin areeffective when memory consolidation is measured 3.PROTOCOL2/3 Master of Small Molecules 您边的抑制剂师www.MedChemEAnimal Mice 3Administration 3 The experiments are carried out on naive male Swiss mice weighing 20-25 g. Drugs are administeredintraperitoneally (i.p.) at the volume of 10 mL/kg.

15、 Fresh drug solutions are prepared on each day ofexperimentation. Control groups receive saline injections of the same volume and via the same route ofadministration. During the acute treatment, the animals are allocated to the following drug groups: saline,rivastigmine (0.5 mg/kg, i.p.), scopolamin

16、e (1 mg/kg, i.p.), Imperatorin (1, 5, 10 mg/kg, i.p.), or Imperatorincoadministered with scopolamine. To measure the memory acquisition processes, scopolamine isadministered 20 min before the pretest, whereas Imperatorin and rivastigmine are administered 30 min beforethe pretest. To measure the memo

17、ry consolidation processes, rivastigmine or scopolamine (1 mg/kg) isadministered immediately after the pretest, whereas Imperatorin is administered 15 min after pretest or afterscopolamine injection. On the second day, the mice are retested. In the second set of the experiments,animals are randomly

18、allocated to receive 6 days of i.p. injections of Imperatorin (1, 5, and 10 mg/kg, i.p.) orsaline, twice daily (8:00 a.m. and 8:00 p.m.). On the seventh day, these animals are subjected to saline,scopolamine (1 mg/kg, i.p.), Imperatorin (1, 5, and 10 mg/kg, i.p.), or Imperatorin coadministered withs

19、copolamine. To measure the memory acquisition processes, scopolamine is administered 20 min before thepretest and Imperatorin 30 min before the pretest. To measure the memory consolidation processes,scopolamine (1 mg/kg) is administered immediately after the pretest, whereas Imperatorin is administered 15min after the pretest or after scopolamine injection. On the eighth day, the mice are retested.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Kozio E, et al. Imperatorin