L-Methionine-(S,R)-sulfoximine is an inhibitor of glutamine synthetase and a sulfoximine derivative of L-methionine. It inhibits pea glutamine synthetase by 31 to 64% when used at concentrations ranging from 5 to 25 µM following preincubation with L-glutamine, an effect that is absent without L-glutamine preincubation. It also inhibits glutamine synthetase in isolated chick embryo retinas.
L-Methionine-(S,R)-Sulfoximine (MSX; MSO), a highly specific and irreversible inhibitor of Glutamine synthetase (GS), is also a potent convulsant which metabolically and morphologically primarily affects astroglia. L-Methionine-(S,R)-Sulfoximine has been employed to inhibit the Gln-dependent ammonia-stimulated neuronal toxicity in vitro, potentiating Gln deficit-dependent depression. L-Methionine-(S,R)-Sulfoximine tremendously increases the rate of release of fixed nitrogen in cyanobacteria. L-Methionine-(S,R)-Sulfoximine is a promising candidate for research in biofertilizers and convulsive seizures (CS).
体内研究
L-Methionine - (S, R) - Sulfoximine (75 mg/kg, intraperitoneal injection, 210 minutes) had no effect on hippocampal glutamine synthetase (GS) activity and GS protein expression in rats during the first 150 minutes, but significantly reduced GS activity during the last 165-210 minutes. In addition, L-Methionine - (S, R) - Sulfoximine also reduced the intensity of seizures (CS) and epileptic seizures induced by administration of pilo in rats.
L-Methionine - (S, R) - Sulfoximine (75 mg/kg, intraperitoneal injection) reduced K+- induced depolarization induced D-Asp release and maintained unchanged glutamate uptake in the hippocampus and endometrial cortex of rats with temporal lobe epilepsy (TLE) model.
Animal Model:
Male rats (24 days old, Sprague Dawley)
Dosage:
75 mg/kg
Administration:
210 min, i.p., measurements were taken at MSO “0”, after 15 min (referred to as MSO “15”, Pilo “15” and MSO + Pilo “15”) and after 60 min (MSO “60”, Pilo “60” and MSO + Pilo “60”, respectively
Result:
Did not affect the hippocampal GS activity and the expression of GS protein for the first 150 min, but significantly decreased the activity during 165-210 min after MSO administration in rats. Additionally, MSO reduced the intensity of CS caused by Pilo administration.
Animal Model:
Hippocampus and enthorhinal cortex of TLE model rats
Dosage:
75 mg/kg
Administration:
i.p., Administration 150 minutes before decapitation
Result:
Markedly reduced D-Asp release evoked by K+-induced depolarization and slightly decreased [3H]D-Asp uptake at higher concentrations of [3H]D-Asp in TLE model rats.
分子式
C5H12N2O3S
分子量
180.23
CAS号
15985-39-4
中文名称
L-蛋氨酸磺酸盐
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder
-20°C
3 years
4°C
2 years
In solvent
-80°C
6 months
-20°C
1 month
溶解性数据
In Vitro:
H2O : 50 mg/mL (277.42 mM; Need ultrasonic)
DMSO : < 1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble or slightly soluble)