產(chǎn)品目錄

規(guī)格	1mg 5mg 10mg 20mg
CAS	170568-47-5
別名	N/A
化學名	N/A
分子式	C23H27ClN4O3
分子量	442.94
溶解度	Soluble in DMSO
儲存條件	Store at -20°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request

產(chǎn)品描述：

U-101017 is a partial agonist of benzodiazepine receptor and GABAA receptor, with anxiolytic effects.

PNU-101017 potentiates GABA-stimulated Cl- currents at low concentrations (<1 μM)[1]. U-101017 concentration-dependently inhibits the binding of [3H]FNZ to the membrane preparation of rat cerebral cortex in vitro with Ki of 3.37±0.22 nM[2].

Pre-ischemic treatment with either PNU-101017 significantly protects the CA1 neuronal population, and PNU-101017 reduces the loss to 50%. Delaying PNU-101017 administration until immediately after reperfusion does not reduce the neuroprotective activity[1]. U-101017 (30 μmol/kg, p.o.) time-dependently blocks [3H]FNZ binding to the mouse cerebral cortex. U-101017 dose-dependently decreases the levels of cGMP with ED50s of 260.0 (163-425) and 0.37 (0.12-1.04) in nonstressed and foot shock-stressed mice, respectively. Flumazenil, an antagonist of GABAA receptors, has no significant effect on cGMP in nonstressed mice, but pretreatment with flumazenil significantly blocks U-101017 (10 μmol/kg, p.o.)-induced reductions in cGMP. In stressed mice, flumazenil is ineffective in altering cerebellar cGMP, but pretreatment with these doses of flumazenil significantly (p < 0.01) blocks U-101017-induced attenuation of stress-induced elevations in cGMP[2].

[1]. Hall ED, et al. Comparative neuroprotective properties of the benzodiazepine receptor full agonist diazepam and the partial agonist PNU-101017 in the gerbil forebrain ischemia model. Brain Res. 1998 Jul 6;798(1-2):325-9. [2]. Sethy VH, et al. The novel anxiolytic U-101017: in vitro and ex vivo binding profile and effect on cerebellar cGMP. Pharmacol Biochem Behav. 1997 Oct;58(2):609-13.

特別提醒：

1. 本產(chǎn)品僅供科研使用。請勿用于醫(yī)藥、臨床診斷或治療，食品及化妝品等用途。請勿存放于普通住宅區(qū)。

2. 為了您的安全和健康，請穿好實驗服并佩戴一次性手套和口罩操作。

原創(chuàng)作者：上海莼試生物技術(shù)有限公司

在線咨詢

留言注意事項：

1.遵守中華人民共和國有關(guān)法律、法規(guī)，尊重網(wǎng)上道德，承擔一切因您的行為而直接或間接引起的法律責任。

2.請您真實的反映產(chǎn)品的情況,不要捏造、誣蔑、造謠。如對產(chǎn)品有任何疑問,也可以留言咨詢。

3.未經(jīng)本站同意，任何人不得利用本留言簿發(fā)布個人或團體的具有廣告性質(zhì)的信息或類似言論。

您感興趣的產(chǎn)品*
您的單位*
聯(lián)系人*
聯(lián)系電話*
詳細地址*
常用郵箱*
請輸入您對我們的意見或建議*
驗證碼*