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1431641-29-0

中文名稱(chēng) ADX71743
CAS 1431641-29-0
1431641-29-0 結(jié)構(gòu)式 1431641-29-0 結(jié)構(gòu)式

基本信息

英文別名
ADX71743
ADX71743 >=98% (HPLC)

常見(jiàn)問(wèn)題列表

生物活性
ADX71743 是一種高度選擇性,非競(jìng)爭(zhēng)性且透過(guò)血腦屏障的代謝型谷氨酸受體 7 負(fù)變構(gòu)調(diào)節(jié)劑 (mGlu7 NAM)。ADX71743 具有抗焦慮活性。
靶點(diǎn)

mGlu7

體外研究

ADX71743 has an IC 50 of 300 nM in-house cell lines. Pretreatment of ADX71743 (3 μM; for 20 min) before high-frequency stimulation (HFS) results in an almost complete blockade of LTP induction.
ADX71743 (0.1, 10 μM) reverses L-AP4-induced depression of synaptic transmission and results in a concentration-dependent reversal of the L-AP4-induced depression. 0.1 μM ADX71743 reverses the effects of L-AP4 by 11% and 10 μM results in a 20% reversal.
ADX71743 can against an EC 80 of glutamate (IC 50 of 22 nM) as well as against an EC 80 of L-AP4 (IC 50 of 125 nM).

體內(nèi)研究

ADX71743 (50, 100, 150 mg/kg; SC) results in robust reductions in numbers of buried marbles to near maximal levels at lower doses (50 and 100 mg/kg).
ADX71743 (12.5, 100 mg/kg for mice and 100 mg/kg for rat; SC) has a T 1/2 of 0.68, 0.40 hours, a C max of 1380, 12766 ng/ml of 12.5 mg/kg and 100 mg/kg in mice.

Animal Model: Adult male C57Bl6/J mice (24-30 g)
Dosage: 50, 100, 150 mg/kg
Administration: SC
Result: Resulted in robust reductions in numbers of buried marbles to near maximal levels at lower doses (50 and 100 mg/kg).
Animal Model: Adult male C57Bl6/J mice (24-30 g) and Sprague-Dawley rats (250-350 g)
Dosage: 12.5, 100 mg/kg for mice and 100 mg/kg for rat (Pharmacokinetic Analysis)
Administration: SC
Result: Had a T 1/2 of 0.68, 0.40 hours, a C max of 1380, 12766 ng/ml of 12.5 mg/kg and 100 mg/kg in mice.
Had a T 1/2 of 1.5 hours, a C max of 16800 ng/ml of 100 mg/kg in rat.
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