ADX71743 是一种高度选择性，非竞争性且透过血脑屏障的代谢型谷氨酸受体 7 负变构调节剂 (mGlu7 NAM)。ADX71743 具有抗焦虑活性。
| 生物活性 | ADX71743 is a highly selective, noncompetitive and brain-penetrantmetabotropic glutamate receptor 7negative allosteric modulator (mGlu7 NAM). ADX71743 has anxiolytic-like activity[1][2]. |
| IC50& Target[1] | |
体外研究
(In Vitro) | ADX71743 has an IC50of 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[1].
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[2].
ADX71743 can against an EC80of glutamate (IC50of 22 nM) as well as against an EC80of L-AP4 (IC50of 125 nM)[2].
|
体内研究
(In Vivo) | 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)[2].
ADX71743 (12.5, 100 mg/kg for mice and 100 mg/kg for rat; SC) has a T1/2of 0.68, 0.40 hours, a Cmaxof 1380, 12766 ng/ml of 12.5 mg/kg and 100 mg/kg in mice[2].
| Animal Model: | Adult male C57Bl6/J mice (24-30 g)[2] | | 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)[2] | | Dosage: | 12.5, 100 mg/kg for mice and 100 mg/kg for rat (Pharmacokinetic Analysis) | | Administration: | SC | | Result: | Had a T1/2of 0.68, 0.40 hours, a Cmaxof 1380, 12766 ng/ml of 12.5 mg/kg and 100 mg/kg in mice.
Had a T1/2of 1.5 hours, a Cmaxof 16800 ng/ml of 100 mg/kg in rat. |
|
| 分子量 | |
| Formula | |
| CAS 号 | |
| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
