1802326-66-4
1802326-66-4 結(jié)構(gòu)式
基本信息
3-氯-N-[2-氧代-2-[[(1S)-1-苯基乙基]氨基]乙基]苯甲酰胺
JNJ 63533054
JNJ-63533054 >=98% (HPLC)
JNJ-63533054 (JNJ63533054
3-Chloro-N-[2-oxo-2-[[(1S)-1-phenylethyl]amino]ethyl]benzamide
Benzamide, 3-chloro-N-[2-oxo-2-[[(1S)-1-phenylethyl]amino]ethyl]-
物理化學(xué)性質(zhì)
常見問題列表
| Target | Value |
|
human GPR139
(Cell-free assay) | 0.024 μM(Ki) |
|
mouse GPR139
(Cell-free assay) | 0.054 μM(Ki) |
|
rat GPR13
(Cell-free assay) | 0.075 μM(Ki) |
JNJ-63533054 specifically activates human GPR139 in the calcium mobilization (EC
50
of 16 nM) and GTPγS binding (EC
50
of 17 nM) assays. JNJ-63533054 also activates the rat and mouse GPR139 receptor with similar potency (rat EC
50
of 63 nM, mouse EC
50
of 28 nM).
In a saturation study for human GPR139, a single population of high-affinity binding sites for [3H] JNJ-63533054 is observed (K
d
of 10 nM). The B
max
value is 26 pmol/mg of protein. Saturation studies for the rat GPR139 and mouse GPR139 yielded K
d
values within the same range (32 nM and 23 nM, respectively; B
max
= 8.5 pmol/mg of protein and 6.2 pmol/mg of protein, respectively).
JNJ-63533054 (3-30 mg/kg; oral administration; once; SD rats) treatment induces a dose-dependent reduction in locomotor activity in the first hour.
The pharmacokinetics of JNJ-63533054 (Compound 7c; 1 mg/kg iv; 5 mg/kg po) in rat is examined. The IV clearance is 53 mL/min/kg, the C
max
is 317 ng/mL (~1 μM), the t
1/2
is 2.5 hours, and JNJ-63533054 is able to cross the blood-brain barrier (BBB) with a brain to plasma ratio (b/p) of 1.2.
| Animal Model: | Male Sprague-Dawley rats (350-450 g) |
| Dosage: | 3 mg/kg, 10 mg/kg, and 30 mg/kg |
| Administration: | Oral administration; once |
| Result: | Induced a dose-dependent reduction in locomotor activity in the first hour. |