JNJ-42153605 is a positive allosteric modulator of the metabotropic glutamate 2 (mGlu2) receptor with EC50 of 17 nM.
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描述 | Metabotropic glutamate receptors (mGlu) are a family of class C G-protein-coupled receptors responsible for the fine-tuning of synaptic efficacy. The mGlu2 receptor is a member of the group II subfamily that negatively regulates the release of glutamate and GABA. JNJ-42153605 is a potent and selective mGlu2 positive allosteric modulator with an EC50 value of 17nM and Emax of 285%. The IC50 value of JNJ-42153605 for mGlu2 PAM binding is 15nM. The lipophilic ligand efficiency and lipophilicity-corrected ligand efficiency values of JNJ-42153605 are 5.2 and 9.8, respectively. The oral administration of JNJ-42153605 (3mg/kg) suppressed rapid eye movement (REM) sleep in mice during the first 2 h after treatment when compared to vehicle controls. JNJ-42153605 also prolonged the onset latency of REM sleep onset in mice. In the mouse model of phencyclidine-induced hyperlocomotion, JNJ-42153605 significantly attenuated phencyclidine-induced locomotor activity in a dose-dependent manner with an ED50 of 5.4mg/kg[4]. In the 6 Hz (32 mA stimulus intensity) model, median effective dose (ED50) values for JNJ‐42153605 were 3.8 mg/kg[5]. |
Dose | Rat: 0.1 mg/kg[1] (i.v.); 3 mg/kg[2] (p.o.), 3 mg/kg- 30 mg/kg[3] (p.o.); 10 mg/kg[2] (s.c.) | ||||||||||||||||||||
Administration | i.v., p.o., s.c. | ||||||||||||||||||||
Pharmacokinetics |
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计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.50mL 0.50mL 0.25mL |
12.49mL 2.50mL 1.25mL |
24.97mL 4.99mL 2.50mL |
CAS号 | 1254977-87-1 |
分子式 | C22H23F3N4 |
分子量 | 400.44 |
别名 | |
运输 | 蓝冰 |
存储条件 |
粉末 Sealed in dry,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
溶解度 |
DMSO: 16 mg/mL(39.96 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |