N5-[亚氨基(甲硫基)甲基]-L-鸟氨酸
- CAS号:156719-41-4
- 英文名:S-METHYL-L-THIOCITRULLINE
- 中文名:N5-[亚氨基(甲硫基)甲基]-L-鸟氨酸
- CBNumber:CB0670742
- 分子式:C7H15N3O2S
- 分子量:205.28
- MOL File:156719-41-4.mol
- 沸点 :369.4±52.0 °C(Predicted)
- 密度 :1.35±0.1 g/cm3(Predicted)
- 储存条件 :Store at 0°C
- 溶解度 :Soluble in DMSO
- 酸度系数(pKa) :2.48±0.24(Predicted)
N5-[亚氨基(甲硫基)甲基]-L-鸟氨酸性质、用途与生产工艺
- 生物活性 S-MTC 是一种选择性的 I 型一氧化氮合酶 (NOS) 抑制剂。
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靶点
NOS
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体外研究
S-MTC (10 or 100 μM) reduces cellular NO release in the absence of Aβ 1-42 . At 100 μM, S-MTC decreases cell viability. S-MTC (100 μM) significantly lowers nitrite production (11.2±1.1 μM) when compared to control (no NOS inhibitor exposure; 19.6±1.2 μM). Nitrite productions after Aβ 1-42 and L-NOARG (100 μM) or Aβ 1-42 and S-MTC (100 μM) treatments are significantly lower than Aβ 1-42 alone (33.5±2.0 and 34.5±1.6 μM, respectively). S-MTC (100 μM) is able to significantly reduce nitrite production (25.2±1.1 μM) as compared to Aβ 1-42 treatment alone (38.3±2.7 μM), when administered after Aβ 1-42 at the 1 h time point. S-MTC (100 μM) concentration decreases both MTT (87±1% of control) and NR (80±1% of control, respectively) levels. The co-administration of S-MTC (100 μM) and Aβ 1-42 significantly reverses the effects of Aβ 1-42 alone (72±2% vs 61±2% of control).
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体内研究
S-MTC (S-methyl-L-thiocitrulline) is a selective neuronal NOS-inhibitor. Following pretreatment with S-MTC (i.c.v.), the HBO 2 -induced antinociception is significantly antagonized. In Experiment #2, different groups of mice are pretreated with naltrexone hydrochloride (NTX) (3.0 mg/kg, i.p.), L-NAME (1.0 μg/mouse, i.c.v.), S-MTC (1.0 μg/mouse, i.c.v.) or N 5 -(1-iminoethyl)-L-ornithine (L-NIO) (3.0 mg/kg, s.c.) 15-30 min prior to HBO 2 treatment. The antinociceptive effect assessed 90 min after HBO 2 treatment is completely abolished by NTX and L-NAME, antagonized by two-thirds by S-MTC and largely unaffected by L-NIO (F=25.57, p<0.0001). At a dose of 0.3 mg/kg, S-MTC (SMTC) causes a rise in mean blood pressure (BP). At doses of 1.0, 3.0 and 10 mg/kg, S-MTC causes falls in heart rate, rises in BP and vasoconstriction in all three vascular beds.
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