SSR103800
SSR103800 is an orally active and selective glycine transporter-1 (GlyT1) inhibitor with an IC50 of 2 nM for hGlyT1. SSR103800 elevates synaptic glycine levels by blocking GlyT1, thereby indirectly enhancing glutamate-NMDA receptor function. SSR103800 can be used for research on schizophrenia and depression.
For research use only. We do not sell to patients.
- CAS No.: 1508339-76-1
- Formula: C22H21Cl2F3N2O
- Molecular Weight:457.32
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
hGlyT1 2.0 nM (IC50) |
rGlyT1 5.3 nM (IC50) |
mGlytT1 6.8 nM (IC50) |
In Vitro
SSR103800 (10 min) selectively inhibits glycine uptake in human neuroblastoma SK-N-MC cells, rat astrocytoma C6 cells, and mouse brain cortex homogenates, with IC50 values of 2.0 nM, 5.3 nM, and 6.8 nM, respectively[1].
SSR103800 (0.01-1 µM) significantly enhances evoked NMDA-mediated EPSCs in rat hippocampal CA1 pyramidal cells, with a maximal enhancement of 328% at 1 µM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
SSR103800 (3-30 mg/kg; p.o.; single administration; microdialysis sampling for 180 min) increases extracellular levels of glycine in the prefrontal cortex in freely moving Sprague-Dawley rats[1].
SSR103800 (3-30 mg/kg; p.o.; single administration; 60 min before testing) blocks hyperactivity in the MK-801 (HY-15084B)-induced Swiss mouse model[1].
SSR103800 (10-30 mg/kg; p.o.; single administration; 60 min before testing) reduces hyperlocomotion in the PCP-induced OFA rat model[1].
SSR103800 (3 mg/kg; p.o.; single administration; 90 min before testing) reverses low-dose PCP-induced short-term episodic-like visual memory deficits in the object recognition test in chronic PCP-sensitized rats[1].
SSR103800 (0.1-10 mg/kg; p.o.; single administration; 60 min before testing) ameliorates social cognitive deficits in a neonatal PCP-treated adult Wistar Han rat model[1].
SSR103800 (3-30 mg/kg; i.p.; single administration; 30 min before testing) enhances prepulse inhibition of the startle reflex in the DBA/1J mouse model[1].
SSR103800 (0.3-3 mg/kg; p.o.; administered twice; 15 min after the first phase and 60 min before the second phase) reduces immobility time in the Wistar rat forced swim test[1].
SSR103800 (1-30 mg/kg; p.o.; single administration; 60 min before testing) blocks tonic immobility in the Mongolian gerbil neck pinch-induced model[1].
SSR103800 (10-30 mg/kg; p.o.; single administration; 60 min before testing) partially reverses spontaneous locomotor hyperactivity in NMDA transgenic mouse model with a B6xD2.F1 genetic background[2].
SSR103800 (10-30 mg/kg; p.o.; single administration; 60 min before testing) fails to block amphetamine-induced hyperactivity in Swiss mice[2].
SSR103800 (10-30 mg/kg; p.o.; single administration; 60 min before testing) fails to block spontaneous locomotor hyperactivity in dopamine transporter knockout mouse models with a B6xD2.F1 genetic background[2].
SSR103800 (30 mg/kg; p.o.; single administration; measured at 1-2 h) does not induce catalepsy in the bar test model in C57BL/6J mice[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Swiss mice (male, 18-21 g)[1]
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Dosage:3, 10, 15, 20, 30 mg/kg
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Administration:p.o.; single administration; 60 min before testing
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Result:Antagonized MK-801-induced hyperactivity with a minimal effective dose of 15 mg/kg.
Decreased significantly MK-801-induced hypermotility at 20 mg/kg.
Completely reversed MK-801-induced hyperactivity at 30 mg/kg.
Induced a significant hypo-locomotor effect on its own at 30 mg/kg.
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Animal Model:OFA rats (male juveniles, 220-270 g)[1]
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Dosage:1, 3, 10 mg/kg
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Administration:p.o.; single administration; 60 min before testing
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Result:Significantly decreased locomotor hyperactivity in PCP treated rats at 1, 3 and 10 mg/kg.
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Animal Model:Sprague-Dawley rats (male, 320-350 g)[1]
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Dosage:3, 10, 30 mg/kg
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Administration:p.o.; single administration; microdialysis sampling for 180 min
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Result:Produced a rapid and sustained increase in PFC extracellular levels of glycine, with a maximal increase observed at 30 mg/kg.
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Animal Model:DBA/1J mice (male, 20-22 g)[1]
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Dosage:3, 10, 30 mg/kg
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Administration:i.p.; single administration; 30 min before testing
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Result:Significantly enhanced PPI at the 78 dB and 86 dB intensity levels at 30 mg/kg.
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Animal Model:Gerbils (6-9 per group)[1]
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Dosage:1, 3, 10, 30 mg/kg
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Administration:p.o.; single administration; 60 min before testing
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Result:Significantly decreased the duration of tonic immobility at 10 and 30 mg/kg.
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Animal Model:NMDA Nr1neo-/- transgenic mice (B6xD2.F1 hybrid background) and wild-type littermates[2]
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Dosage:10, 30 mg/kg
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Administration:p.o.; single administration; 60 min before testing
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Result:Significantly attenuated hyperactivity in NMDA Nr1neo-/- mice at 10 and 30 mg/kg.
Did not produce motor effects in wild-type animals.
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Animal Model:DAT-/- knockout mice (B6xD2.F1 hybrid background, Slc6a3tm1Mca) and wild-type littermates[2]
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Dosage:10, 20, 30 mg/kg
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Administration:p.o.; single administration; 60 min before testing
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Result:Did not significantly attenuate hyperactivity in DAT-/- mice.
Did not produce motor effects in wild-type animals.
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Animal Model:C57BL/6J mice (Male)[2]
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Dosage:30 mg/kg
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Administration:p.o.; single administration; measured at 1-2 h
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Result:Completely devoid of cataleptic effect.
Chemical Information
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CAS No. 1508339-76-1
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Molecular Weight 457.32
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Formula C22H21Cl2F3N2O
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SMILES
O=C(C1=C(C(C(F)(F)F)=CC=C1Cl)Cl)N[C@H](C2=CC=CC=C2)[C@@]3([H])C4CCN(CC4)C3
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
SSR103800 Related Classifications
HY-189045 Related Classifications
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