Sarcosine, a glycine transporter type 1 inhibitor and an N-methyl-D-aspartate (NMDA) receptor co-agonist at the glycine binding site, potentiates NMDA receptor function[3]. Sarcosine, similar to other NMDA receptor-activating agents, is an effective adjuvant in the treatment of schizophrenia. Because sarcosine facilitates NMDA receptor function, it may affect the seizure threshold. In the iv PTZ test, sarcosine did not exert a significant effect on the seizure threshold at any of the doses tested (100, 200, 400 and 800 mg/kg, ip). However, at doses of 400 and 800 mg/kg, sarcosine significantly raised the threshold for electroconvulsions[4]. Using whole-cell recordings from cultured embryonic mouse hippocampal neurons found that sarcosine evoked a dose-dependent, strychnine sensitive, Cl(-) current that cross-inhibited glycine currents. Sarcosine evoked this current with Li(+) in the extracellular solution to block GlyT1, in neurons treated with the essentially irreversible GlyT1 inhibitor N[3-(4'-fluorophenyl)-3-(4'-phenylphenoxy)propyl]sarcosine (NFPS), and in neurons plated in the absence of glia[5].
Sarcosine/肌氨酸 细胞实验
Cell Line
Concentration
Treated Time
Description
References
NIH 3T3 mouse fibroblasts
500 µM
16 hours
To evaluate the effect of sarcosine on autophagy. Results showed that sarcosine stimulated basal macroautophagy in a dose-dependent manner and partially enhanced autophagy under serum removal and oxidative stress conditions.
Cell Rep. 2018 Oct 16;25(3):663-676. e6
LNCaP cells
1 µM
24 hours
Sarcosine stimulated the expression of SARDH and PIPOX in LNCaP cells, increased SAMe production and DNA methylation.
Mol Oncol. 2019 May;13(5):1002-1017
22Rv1 cells
1 µM
24 hours
Sarcosine stimulated the expression of SARDH and PIPOX in 22Rv1 cells, increased SAMe production and DNA methylation.
Mol Oncol. 2019 May;13(5):1002-1017
PNT1A cells
1 µM
24 hours
Sarcosine stimulated the expression of SARDH and PIPOX in PNT1A cells, increased SAMe production and DNA methylation.
Mol Oncol. 2019 May;13(5):1002-1017
PC9
0.5 mM
24 hours
To evaluate the effect of Sarcosine on ferroptosis, results showed that Sarcosine significantly enhanced RSL3 and IKE-induced ferroptosis.
Exp Hematol Oncol. 2025 Apr 24;14(1):60
A549
0.5 mM
24 hours
To evaluate the effect of Sarcosine on ferroptosis, results showed that Sarcosine significantly enhanced RSL3 and IKE-induced ferroptosis.
Exp Hematol Oncol. 2025 Apr 24;14(1):60
Murine bone marrow-derived dendritic cells
20 mM
24 hours
To evaluate the effect of sarcosine on dendritic cell migration, results showed that sarcosine significantly increased dendritic cell migration
J Immunother Cancer. 2019 Nov 21;7(1):321
Sarcosine/肌氨酸 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Fischer 344 × Brown Norway (FBN) hybrid male rats
Aged rats
Dietary supplementation
1,250 mg/kg
8 weeks
To evaluate the effect of sarcosine supplementation on the metabolome and autophagy in aged rats. Results showed that sarcosine supplementation increased plasma sarcosine levels, altered the metabolome, and enhanced autophagic flux in the liver.
Cell Rep. 2018 Oct 16;25(3):663-676. e6
Mice
Toluene-induced motor incoordination, memory impairment, and hypothermia model
Intraperitoneal injection
100 and 300 mg/kg
Single dose, 30 min pretreatment
Sarcosine pretreatment reversed toluene-induced motor incoordination, memory impairment, and hypothermia but did not affect toluene-induced enhancement of brain stimulation reward
Toxicol Appl Pharmacol. 2012 Dec 1;265(2):158-65
BALB/c nude mice
Xenograft model
Oral
2 mM
Every three days for a total of six treatments
To validate the effect of Sarcosine on ferroptosis and chemosensitivity in vivo, results showed that Sarcosine enhanced the efficacy of cisplatin.
Exp Hematol Oncol. 2025 Apr 24;14(1):60
Rats
Rapid kindling model of epileptogenesis
Intraperitoneal injection
3 g/kg
Once daily for 5 days
To evaluate the antiepileptogenic effect of sarcosine and its effects on hippocampal DNA methylation. Results showed that sarcosine significantly suppressed epileptogenesis in rats, accompanied by suppressed hippocampal GlyT1 expression, reduced 5mC levels, and increased 5hmC levels.
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