JNJ-5207852 - Histamine Receptor Antagonist - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEJNJ-5207852Cat. No.: HY-12190CAS No.: 398473-34-2分式: CHNO分量: 316.48作靶点: Histamine Receptor作通路: GPCR/G Protein; Immunology/Inflammation; NeuronalSignaling储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据

2、体外实验 DMSO : 77.5 mg/mL (244.88 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 3.1598 mL 15.7988 mL 31.5976 mL5 mM 0.6320 mL 3.1598 mL 6.3195 mL10 mM 0.3160 mL 1.5799 mL 3.1598 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。体内实验请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实验

3、结果的可靠性，体内实验的作液，建议您现现配，当天使；澄清的储备液可以根据储存条件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.58 mg/mL (8.15 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.58 mg/mL (8.15 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90%

4、 corn oil1/2 Master of Small Molecules 您边的抑制剂师www.MedChemESolubility: 2.58 mg/mL (8.15 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 JNJ-5207852组胺 H3 受体有选择性的有效拮抗剂，其对和类 H3 受体的 pKi 值分别为 8.9，9.24。IC50 & Target H3 receptor H3 receptor8.9 (pKi, for rat) 9.24 (pKi, for human)体内研究 In mice and rats, JNJ-5207852

5、 (1-10mg/kg s.c.) increases time spent awake and decreases REM sleep andslow-wave sleep, but fails to have an effect on wakefulness or sleep in H3 receptor knockout mice. Norebound hypersomnolence, as measured by slow-wave delta power, is observed. The wake promotingeffects of this H3 receptor antag

6、onist are not associated with hypermotility. A 4-week daily treatment of micewith JNJ-5207852 (10 mg/kg i.p.) does not lead to a change in body weight, possibly due to the compoundbeing a neutral antagonist at the H3 receptor. JNJ-5207852 is extensively absorbed after oral administrationand reaches

7、high brain levels 1.PROTOCOLAnimal Rats 1Administration 1 Male, Sprague-Dawley rats weighing 282-334 g are used. The animals are individually housed with freeaccess to food and water. To assure that there are no pre-existing group differences in activity levels prior tothe initiation of treatment, L

8、MA is monitored and recorded during a 2 h habituation period. Following the 2 hhabituation period, testing is briefly interrupted and animals are s.c. injected with either saline (1 mL/kg; n=6),JNJ-5207852 (3, 10, 30 mg/kg; n=6-7 animals/group) or Damphetamine (0.75 mg/kg; n=6). Testing isimmediatel

9、y resumed following the compound injection 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Barbier AJ, et al. Acute wake-promoting actions of JNJ-5207852, a novel, diamine-based H3 antagonist. Br J Pharmacol. 2004Nov;143(5):649-61.2. Abuhamdah RM, et al. Effects of methimepip and JNJ-5207852 in Wistar rats exposed to an open-field with and without object and inBalb/c mice exposed to a radial-arm maze. Front Syst Neurosci. 2012 Jul 16;6:54.McePdfHeightCaution: Product has not been fully validated