Glycine transporter type 1 (GlyT1) inhibitor; Positive allosteric modulator of NMDA receptors [1][2]

Sarcosine enhanced NMDA receptor-mediated excitatory postsynaptic field potentials (fEPSPs) in rat hippocampal slices. This potentiation was blocked by the NMDA antagonist AP5, confirming NMDA receptor dependence [2]

Sarcosine (100–300 μM) increased the amplitude and slope of fEPSPs in a concentration-dependent manner without affecting non-NMDA receptor-mediated responses [2]

In the pentylenetetrazol (PTZ)-induced seizure model, intraperitoneal Sarcosine (600 mg/kg) significantly delayed seizure onset latency (by 48%) and reduced mortality rate (from 100% to 30%) compared to controls [1]

In maximal electroshock (MES) tests, Sarcosine (600 mg/kg i.p.) decreased seizure duration by 35% and protected 40% of mice from tonic hindlimb extension [1]
The electroconvulsive threshold is markedly elevated by Sarcosine (400–800 mg/kg; ip) [2].

Animal/Disease Models: Albino Swiss mouse body weight (25-30 g)[2]
Doses: 100 mg/kg, 200 mg/kg, 400 mg/kg, 800 mg/kg
Route of Administration: intraperitoneal (ip) injection
Experimental Results: in mice MEST In trials, epilepsy thresholds were elevated at doses of 400 mg/kg and 800 mg/kg.

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For PTZ seizures: Mice received PTZ (85 mg/kg, s.c.) 30 min after Sarcosine (300 or 600 mg/kg, i.p.) dissolved in saline. Seizure latency and mortality were monitored for 30 min [1]

For MES seizures: Mice were pretreated with Sarcosine (600 mg/kg i.p.) 30 min before electrical stimulation (50 mA, 0.2 sec). Tonic extension duration and protection rates were recorded [1]

For hippocampal slice studies: Rats were sacrificed, and brain slices (400 μm) were perfused with artificial CSF. fEPSPs were evoked by Schaffer collateral stimulation [2]

Metabolism / Metabolites
Sarcosine is metabolized to glycine by sarcosine dehydrogenase, while glycine-N-methyltransferase converts glycine into sarcosine.

Toxicity Summary
Creatine is an oncogenic metabolite. Exogenous creatine appears to upregulate the expression of human epidermal growth factor receptor 2 (HER2/neu), a potent oncoprotein, in androgen-dependent prostate cancer cells. Therefore, creatine may induce prostate cancer progression by increasing HER2/neu expression. Toxicity Data
Not Applicable In mice, no death or behavioral toxicity (e.g., ataxia, sedation) was observed at anticonvulsant doses (≤600 mg/kg) [1]

[1]. Effects of sarcosine, a glycine transporter type 1 inhibitor, in two mouse seizure models. Pharmacol Rep. Mar-Apr 2010;62(2):392-7.

[2]. Effects of sarcosine and N, N-dimethylglycine on NMDA receptor-mediated excitatory field potentials. J Biomed Sci. 2017; 24: 18.

Deliquescent crystals or powder. Slightly sweet taste. (NTP, 1992)
sarcosine is an N-methyl derivative of glycine, belonging to the N-alkylglycine family. It is an intermediate in the glycine metabolic pathway. It can act as an inhibitor of glycine transporter 1, a glycine receptor agonist, a human metabolite, an E. coli metabolite, and a mouse metabolite. It is an N-alkylglycine, N-methyl amino acid, belonging to the N-methylglycine family. It is the conjugate base of sarcosine salts and the conjugate acid of sarcosine acids. It is a zwitterion of sarcosine.
sarcosine has been studied for the treatment of schizophrenia.
sarcosine is present in or produced by E. coli (K12 strain, MG1655 strain).
sarcosine has been reported to exist in lancelet worms, fruit flies, and other organisms with relevant data.
sarcosine is an amino acid, an intermediate and byproduct of glycine synthesis and degradation, with potential antidepressant and antischizophrenic activity. Sarcosine is a product of dietary choline and creatine and is rapidly converted into glycine. Oral administration of sarcosine in combination with certain antipsychotic drugs can increase glycine concentration in the brain, thereby enhancing NMDA receptor activation and alleviating symptoms. Sarcosine is an N-methyl derivative of glycine. Sarcosine is metabolized to glycine by sarcosine dehydrogenase, while glycine-N-methyltransferase converts glycine back to sarcosine. Sarcosine is a natural amino acid found in muscles and other body tissues. In the laboratory, it can be synthesized from chloroacetic acid and methylamine. Sarcosine is naturally present in the process of choline metabolism to glycine. Sarcosine has a sweet taste and is readily soluble in water. It is used in the manufacture of biodegradable surfactants and toothpaste, among other applications. Sarcosine is widely found in organisms, including egg yolks, turkey, ham, vegetables, and legumes. Sarcosine is produced from dietary choline and methionine and is rapidly degraded into glycine. Creatine itself is non-toxic, as evidenced by the deficiency phenotype of sarcinemia (a congenital abnormality in sarcin metabolism). Sarcinemia can be caused by severe folate deficiency, as folate is required for the conversion of sarcin to glycine (Wikipedia). Sarcin has recently been identified as a biomarker for invasive prostate cancer. Studies have found that sarcin levels are significantly elevated during the progression of prostate cancer to metastasis and can be detected in urine. Sarcin levels are also elevated in invasive prostate cancer cell lines compared to benign prostatic epithelial cells (A3519). Sarcin is an amino acid intermediate in choline metabolism.

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sarcosine (N-methylglycine) is an endogenous glycine derivative that inhibits GlyT1, thereby increasing glycine levels in the synaptic cleft and enhancing NMDA receptor function [1][2]
It has shown anticonvulsant effects in pentylenetetrazol (PTZ) and maximal electroshock (MES) models, supporting its potential application in the treatment of epilepsy [1]
NMDA receptor enhancement suggests its potential application in neurological disorders involving NMDA dysfunction (e.g., schizophrenia) [2]

C3H7NO2

89.09

89.047

107-97-1

637-96-7 (HCl); Sarcosine-15N; Sarcosine-d3;118685-91-9

1088

White to off-white solid powder

1.1±0.1 g/cm3

195.1±23.0 °C at 760 mmHg

208-212 °C (dec.)(lit.)

71.8±22.6 °C

0.2±0.8 mmHg at 25°C

1.431

-0.79

2

3

2

6

52.8

0

CNCC(=O)O

FSYKKLYZXJSNPZ-UHFFFAOYSA-N

InChI=1S/C3H7NO2/c1-4-2-3(5)6/h4H,2H2,1H3,(H,5,6)

2-(methylamino)acetic acid

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Solubility in Formulation 1: 100 mg/mL (1122.46 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.

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 (Please use freshly prepared in vivo formulations for optimal results.)