plus-Borneol-d-Borneol-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemE(+)-BorneolCat. No.: HY-N1368ACAS No.: 464-43-7Synonyms: d-Borneol分式: CHO分量: 154.25作靶點: GABA Receptor作通路: Membrane Transporter/Ion Channel; Neuronal Signaling儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month

2、溶解性數(shù)據(jù)體外實驗 DMSO : 100 mg/mL (648.30 mM)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (16.21 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemESolubility: 2.5 mg/mL (16.21 mM); Clear solution3. 請依序添加每種溶劑： 10% DMSO 90% co

3、rn oilSolubility: 2.5 mg/mL (16.21 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 (+)-Borneol (d-Borneol)于中藥鎮(zhèn)痛和醉的天然雙環(huán)單萜，增強 GABA 受體活性的 EC50 值為248 M。IC50 & Target EC50: 248 M (GABA receptor) 1體外研究 (+)-Borneol is present in the essential oils of numerous medicinal plants, including valerian (Valerianaoffici

4、nalis), chamomile (Matricaria chamomilla) and lavender (Lavandula officinalis). Extracts of these plantsare used traditionally to relieve anxiety, restlessness and insomnia. (+)-Borneol is found to have a highlyefficacious positive modulating action at GABAA receptors. (+)-Borneol enhances the actio

5、n of lowconcentrations of GABA by more than 1000% (EC50=248 M) 1.體內(nèi)研究 (+)-Borneol has remarkable anti-hyperalgesic effects on neuropathic and inflammatory pain in animal models.Both oral administration (125, 250 or 500 mg/kg) and intrathecal injection (i.t.) (15, 30 and 60 g) of (+)-Borneol reduce m

6、echanical hypersensitivity dose-dependently in SNL and CFA models. The antihyperalgesiceffects of (+)-Borneol are abolished by a selective GABAA receptor (GABAAR) antagonist bicuculline. (+)-Borneol (500 mg/kg, p.o. or 60 g, i.t.) does not influence motor function 2. After per oral application, (+)-

7、Borneol is absorbed rapidly into the brain and could be determined 5 min after dosing. The maximal brainconcentration (86.52 g/g) is reached after 1 h post-dosing. (+)-Borneol could affect the contents of AAneurotransmitters in mice brain and the change in excitatory ratio leads to borneols double s

8、ide effects onthe central nervous system 3.PROTOCOLAnimal Mice: Inflammatory pain is induced by injection of Complete Freunds adjuvant (CFA, 1 mg/mL). Ten min laterAdministration 2 mice are treated with (+)-Borneol (125, 250, 500 mg/kg) or vehicle. Mechanical hypersensitivity is thenmeasured 2.MCE h

9、as not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Granger RE, et al. (+)- And (-)-borneol: efficacious positive modulators of GABA action at human recombinantalpha1beta2gamma2LGABA(A) receptors. Biochem Pharmacol. 2005 Apr 1;69(7):1101-11.2. Jiang J, et al. (+)-Borneol alleviates mechanical hyperalgesia in models of chronic inflammatory and neuropathic pain in mice. Eur JPharmacol. 2015 Jun 15;757:53-8.McePdfHeight2/2 Master of Small Molecules 您邊的抑制劑師www.MedChemECaution: Product has not been fully validate