162042-44-6
162042-44-6 結(jié)構(gòu)式
基本信息
中文別名
化合物 T15682 英文別名
L371,2571-[1-[4-(1-acetylpiperidin-4-yl)oxy-2-methoxybenzoyl]piperidin-4-yl]-4H-3,1-benzoxazin-2-one
1-[4-[(1-Acetyl-4-piperidinyl)oxy]-2-methoxybenzoyl]-4-(2-oxo-2H-3,1-benzoxazin-1(4H)-yl)piperidine
2H-3,1-Benzoxazin-2-one, 1-[1-[4-[(1-acetyl-4-piperidinyl)oxy]-2-methoxybenzoyl]-4-piperidinyl]-1,4-dihydro-
物理化學(xué)性質(zhì)
沸點(diǎn)728.9±60.0 °C(Predicted)
密度1.282±0.06 g/cm3(Predicted)
儲(chǔ)存條件Store at RT
溶解度Soluble to 10 mM in DMSO with gentle warming
酸度系數(shù)(pKa)0.73±0.20(Predicted)
形態(tài)粉末
顏色White to off-white
常見問題列表
生物活性
L-371,257 是一種口服生物有效的，不能透過血腦屏障的，競爭性的，選擇性催產(chǎn)素受體 (oxytocin receptor) 拮抗劑 (pA2=8.4)，對(duì)催產(chǎn)素受體 (Ki=19 nM) 和血管加壓素 V1a 受體 (vasopressin V1a receptor，Ki=3.7 nM) 具有高親和力。靶點(diǎn)
Ki: 19 nM (oxytocin receptor), 3.7 nM (vasopressin V1a receptor)
體內(nèi)研究
Systemic administration of nonpenetrant oxytocin receptor antagonist L-371,257 (0.5 and 1.0 mg/kg; i.p. injection) stimulates weight gain in rats.
| Animal Model: | Six-hour fasted rats |
| Dosage: | 0.5 and 1.0 mg/kg |
| Administration: | Intraperitoneal injection (a single) 30-45 minutes prior to the start of the dark cycle and access to food; Intraperitoneal injection (given repeatedly) over 6 days. |
| Result: |
A single injection significantly stimulated weight gain at 0.5 and 1.0 mg/kg relative to vehicle treatment.
When given repeatedly over 6 days, 0.5 mg/kg significantly stimulated body weight gain (10.5±2.2 g) relative to vehicle treatment (4.7±2.7 g). |