Sarcosine
N-methylglycine, a GlyT-1-inhibiting NMDA modulator studied as a schizophrenia and depression add-on in humans.
Pharmacology
Contents
WHAT IS SARCOSINE?
Detailed overview
Sarcosine (N-methylglycine) is a naturally occurring amino acid derivative formed from glycine and methionine that inhibits the GlyT-1 glycine transporter, raising synaptic glycine levels and thereby potentiating NMDA-receptor signaling at the glycine (co-agonist) site. This targets the glutamatergic NMDA hypofunction thought to underlie schizophrenia and some mood disorders. In human randomized trials used as an add-on (typically 1-2 g per day) it reduced schizophrenia symptoms and improved cognitive measures, and a 2013 trial showed an antidepressant effect in major depression. Combined with clozapine it reportedly added no benefit. It is sold as a dietary supplement and is not an approved medicine.
Mechanism
GlyT-1 inhibitor, potentiates NMDA glycine site
Evidence
Several human RCTs and meta-analyses (add-on)
Legal status
Dietary supplement, not a medicine
Receptor profile
- GlyT-1 glycine transporter (type 1)Strong
- NMDA receptor glycine (co-agonist) siteModerate
- Prefrontal glutamatergic circuitsModerate
Safety
Side effects, stop signs, contraindications
Side effects · 4
- Mild stomach upset, nausea, occasionally loose stool
- Possible overstimulation, restlessness or disturbed sleep if taken late in the day
- Headache or dizziness in some users
- Long-term safety in healthy users is understudied
Contraindications · 4
- Pregnancy and breastfeeding: insufficient safety data, avoid
- With clozapine it reportedly adds no benefit, and the combination should be considered carefully
- In kidney disease or reduced renal function, medical supervision is advised
- Not a substitute for psychiatric treatment; even as an add-on it should be discussed with a physician
Related Nootropics
Same therapeutic category
Studies
Related research and clinical findings
Glycine transporter I inhibitor, N-methylglycine (sarcosine), added to antipsychotics for the treatment of schizophrenia
Tsai G, Lane HY, Yang P, Chong MY, Lange N
Glycine transporter I inhibitor, N-methylglycine (sarcosine), added to clozapine for the treatment of schizophrenia
Lane HY, Huang CL, Wu PL, Liu YC, Chang YC, Lin PY, Chen PW, Tsai G
Sarcosine (N-methylglycine) treatment for acute schizophrenia: a randomized, double-blind study
Lane HY, Liu YC, Huang CL, Chang YC, Liau CH, Perng CH, Tsai GE
Inhibition of glycine transporter-I as a novel mechanism for the treatment of depression
Huang CC, Wei IH, Huang CL, Chen KT, Tsai MH, Tsai P, Tun R, Huang KH, Chang YC, Lane HY, Tsai GE
Adjunctive sarcosine plus benzoate improved cognitive function in chronic schizophrenia patients with constant clinical symptoms: A randomised, double-blind, placebo-controlled trial
Lin CY, Liang SY, Chang YC, Ting SY, Kao CL, Wu YH, Tsai GE, Lane HY
Efficacy and cognitive effect of sarcosine (N-methylglycine) in patients with schizophrenia: A systematic review and meta-analysis of double-blind randomised controlled trials
Chang CH, Lin CH, Liu CY, Chen SJ, Lane HY
FAQ
FAQ
N-methylglycine, a GlyT-1-inhibiting NMDA modulator studied as a schizophrenia and depression add-on in humans.
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Structure & chemistry
The information here is strictly for educational and scientific purposes. It does not replace medical advice or clinical consultation, and it does not encourage illegal substance or pharmaceutical use. Data is sourced. When in doubt, consult your doctor.