8-OH-DPAT-8-Hydroxy-DPAT-DataSheet-生命科學試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemE8-OH-DPATCat. No.: HY-112061CAS No.: 78950-78-4Synonyms: 8-Hydroxy-DPAT分式: CHNO分量: 247.38作靶點: 5-HT Receptor作通路: GPCR/G Protein; Neuronal Signaling儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DM

2、SO : 155 mg/mL (626.57 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 4.0424 mL 20.2118 mL 40.4236 mL5 mM 0.8085 mL 4.0424 mL 8.0847 mL10 mM 0.4042 mL 2.0212 mL 4.0424 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。體內(nèi)實驗請根據(jù)您的實驗動物和給藥式選擇適當?shù)娜芙獍福渲魄罢埾扰渲瞥吻宓膬湟?/p>

3、，再依次添加助溶劑(為保證實驗結(jié)果的可靠性，體內(nèi)實驗的作液，建議您現(xiàn)現(xiàn)配，當天使；澄清的儲備液可以根據(jù)儲存條件，適當保存；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. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (10.11 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (10.11 mM); Clear solution1/2 Master

4、of Small Molecules 您邊的抑制劑師www.MedChemE3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (10.11 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 8-OH-DPAT種有效的，選擇性的 5-HT 激動劑，對 5-HT1A 的 pIC50 值為 8.19，對 5-HT7 的 Ki 值為 466nM，對 5-HT1B (pIC50, 5.42) 和 5-HT (pIC50 5) 的作很弱。IC50 & Target pIC50: 8.19 (5-HT1A) 1

5、Ki: 466 nM (5-HT7) 2體外研究 8-OH-DPAT is a potent and selective 5-HT agonist, with a pIC50 of 8.19 for 5-HT1A; weakly binds to 5-HT1B(pIC50, 5.42), 5-HT (pIC50 1. 8-OH-DPAT has high affinity at 5-HT7 with a Ki of 466 nM, and does not bindto 5-HT6 or 5-HT4 2.體內(nèi)研究 8-OH-DPAT (1 mg/kg) normalizes hypolocom

6、otion, significantly increases wakefulness and reduces theduration of REM sleep without effect on the duration of non-REM sleep in the dark period in orexin knockout(KO) mice. 8-OH-DPAT shows no obvious effect on wakefulness or the duration of either REM sleep or non-REM sleep in WT mice. 8-OH-DPAT

7、(1 mg/kg, s.c.) activates 5-HT1A receptor in orexin knockout mice 3.PROTOCOLAnimal Mice 3Administration 3 The locomotor activity of mice is measured by an infrared sensor placed in individual home cages. Tocompare the locomotor activity in the light and dark periods, locomotor activity is monitored

8、at 30-minintervals starting at 8:00 a.m. and 8:00 p.m., respectively. To measure the effects of psychostimulants (8-OH-DPAT, 1, 3 mg/kg, s.c; etc.) on locomotor activity in the dark period, all drugs are administered at 8:00 p.m.,and locomotor activity is then measured through 3 h 3.MCE has not inde

9、pendently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. DEREK N. MIDDLEMISS, et al. 8-HYDROXY-2-(DI-n-PROPYLAMINO)-TETRALIN DISCRIMINATES BETWEEN SUBTYPES OF2. Bard JA, et al. Cloning of a novel human serotonin receptor (5-HT7) positively linked to adenylate cyclase. J Biol Chem. 1993 Nov5;268(31):23422-6.3. Mori T, et al. Narcolepsy-like sleep disturbance in orexin knockout mice are normalized by the 5-HT1A receptor agonist 8-OH-DPAT.Psychopharmacology (Berl). 2016 Jun;233(12):2343-53.McePdfHeightCaution: Product has not been fully validate