97075-46-2
中文名稱
化合物AMN 082 DIHYDROCHLORIDE
英文名稱
1,2-EthanediaMine, N,N'-bis(diphenylMethyl)-, dihydrochloride
CAS
97075-46-2
分子式
C28H29ClN2
分子量
429
MOL 文件
97075-46-2.mol
97075-46-2 結(jié)構(gòu)式
基本信息
中文別名
N1,N2-二苯甲基乙烷-1,2-二胺二鹽酸鹽化合物AMN 082 DIHYDROCHLORIDE
英文別名
N,N'-dibenzhydrylethane-1,2-diamineN1,N2-Dibenzhydrylethane-1,2-diamine dihydrochloride
1,2-EthanediaMine, N,N'-bis(diphenylMethyl)-, dihydrochloride
常見(jiàn)問(wèn)題列表
生物活性
AMN082 是一種選擇性，具有口服活性，可透過(guò)血腦屏障的 mGluR7 激動(dòng)劑，通過(guò)跨膜區(qū)的變構(gòu)位點(diǎn)直接激活受體信號(hào)。在表達(dá) mGluR7 的轉(zhuǎn)染哺乳動(dòng)物細(xì)胞上，AMN082 有效抑制 cAMP 積累并刺激 GTPγS 結(jié)合 (EC50, 64-290 nM)。AMN082 對(duì)其他 mGluR 亞型和選擇性離子型谷氨酸受體具有選擇性。具有抗抑郁作用。體外研究
Preincubation of the synaptosomes with AMN082 (1 μM) for 10 min before 4-aminopyridine treatment efficiently inhibits the 4-aminopyridine-evoked release of glutamate, without altering the basal release of glutamate.
體內(nèi)研究
AMN082 (6 mg/kg; p.o.) induces stress hormone increases in an mGluR7-dependent fashion in mGluR7
+/+
mice (C57BL/6 genetic background).
AMN082 (1.25-5.0 mg/kg, i.p.; 30 min before every Cocaine or Morphine injection during repeated drug administration or before Cocaine or Morphine challenge) dose-dependently attenuates the development, as well as the expression of Cocaine or Morphine locomotor sensitization.
| Animal Model: | Male Swiss mice (20-25g) |
| Dosage: | 1.25, 2.5, 5.0 mg/kg |
| Administration: | I.p.; given 30 min prior to Cocaine (10 mg/kg) or Morphine (10 mg/kg) challenge on day 17 or 20, respectively |
| Result: | Significantly attenuated the expression of Cocaine-induced locomotor sensitization; Attenuated the induction of Morphine-induced sensitization. |