Isocorynoxeine-7-Isocorynoxeine-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEIsocorynoxeineCat. No.: HY-N0775CAS No.: 51014-29-0Synonyms: 7-Isocorynoxeine分式: CHNO分量: 382.45作靶點(diǎn): 5-HT Receptor作通路: GPCR/G Protein; Neuronal Signaling儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體

2、外實(shí)驗(yàn) DMSO : 50 mg/mL (130.74 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 2.6147 mL 13.0736 mL 26.1472 mL5 mM 0.5229 mL 2.6147 mL 5.2294 mL10 mM 0.2615 mL 1.3074 mL 2.6147 mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。體內(nèi)實(shí)驗(yàn) 請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥式選擇適當(dāng)?shù)娜芙獍福渲魄罢?qǐng)先配制澄清的儲(chǔ)備液，再依次添加助溶劑(為保證實(shí)驗(yàn)結(jié)果

3、的可靠性，體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (6.54 mM); Clear solutionBIOLOGICAL ACTIVITY1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemE物活性 Isocorynoxeine，種與鉤藤堿有關(guān)的物堿，對(duì) 5-HT2A 受體介導(dǎo)的電流反應(yīng)呈劑量依賴(lài)性抑制，IC50 為72.4 M。IC50 & Ta

4、rget 5-HT2A Receptor72.4 M (IC50)體外研究 Isocorynoxeine inhibits 5-HT2A receptor-mediated 5-HT currents. Isocorynoxeine prefer to interact with 5-HT2A receptors rather than with 5-HT2C receptors in the brain.Isocorynoxeine exhibits less potent inhibitoryactivity (with IC50 values of 100 M) against the

5、5-HT2C receptor-mediated response than the 5-HT2Areceptor-mediated response in oocytes. Isocorynoxeine dose-dependently and competitively inhibits 5-HT-evoked currents in Xenopus oocytes expressing 5-HT2A receptors, but has less of a suppressive effect onthose in oocytes expressing 5-HT2C receptors

6、1.體內(nèi)研究 The effects of Rhynchophylline, Corynoxeine, and Isocorynoxeine, isorhynchophylline-related alkaloidspresent are tested in Uncaria species, on 5-MeO-DMT-induced head-twitch behaviour in reserpinized mice.Neither Rhynchophylline H=1.369, P=0.504 nor Corynoxeine H=0.242, P=0.886 affects the beh

7、aviour, whileIsocorynoxeine significantly attenuates it at 30 mg/kg (i.p.) H=7.582, P 1.PROTOCOLAnimal Mice 1Administration 1 Male ICR mice are pretreated with Reserpine (5 mg/kg, i.p.) 3 h before the start of the experiments.Rhynchophylline (RHY), Corynoxeine (COX), Isocorynoxeine (ICOX, 10 and 30

8、mg/kg) or vehicle is injectedi.p. 30 min before 5-MeO-DMT 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Matsumoto K, et al. Suppressive effects of isorhynchophylline on 5-HT2A receptor function in the brain: behavioural andelectrophysiological studies. Eur J Pharmacol. 2005 Jul 11;517(3):191-9.McePdfHeightCaution: Product has not been fully validated for medical applicati