| Identification | Back Directory | [Name]
rel-N-Methyl-N-[[(1R,2S)-1,2,3,4-tetrahydro-6-methoxy-1-phenyl-2-naphthalenyl]methyl]glycine hydrochloride | [CAS]
949588-40-3 | [Synonyms]
Org 25935
SCH 900435
SCH-900435
ORG25935-SCH900435
ORG 25935 hydrochloride
2-[[(1R,2S)-6-methoxy-1-phenyl-1,2,3,4-tetrahydronaphthalen-2-yl]methyl-methylamino]acetic acid
rel-N-Methyl-N-[[(1R,2S)-1,2,3,4-tetrahydro-6-methoxy-1-phenyl-2-naphthalenyl]methyl]glycine hydrochloride | [Molecular Formula]
C21H26ClNO3 | [MDL Number]
MFCD19708017 | [MOL File]
949588-40-3.mol | [Molecular Weight]
375.89 |
| Hazard Information | Back Directory | [Uses]
Org 25935 is a potent and selective glycine transporter 1 protein (GlyT1) inhibitor with an IC50 value of 100 nM. Org 25935 can decrease ethanol (EtOH) intake and EtOH preference in rats, whereas water intake is unaffected. Org 25935 can be used for researching alcohol dependence or abuse[1]. | [Enzyme inhibitor]
This synthetic drug (FW = 339.43 g/mol; CAS 949588-40-3), known systematically as 2-([(1R,2S)-6-methoxy-1-phenyl-1,2,3,4-tetrahydronaphthalen- 2-yl]methylmethylamino)acetate, is a selective inhibitor of the sodium/chloride-dependent glycine transporter GlyT1, counteracting the effects of the dissociative drug ketamine. Rationale: Elevation of extracellular synaptic concentration of glycine by blockade of GlyT1 is believed to potentiate NMDA receptor function in vivo, thereby suggesting a rational approach for the treatment of schizophrenia and cognitive disorders. Moreover, accumbal glycine receptors (GlyRs) are involved in mediating the dopamine activating effects of ethanol, and that administration of glycine locally into the nucleus accumbens (nAc) reduces ethanol consumption in ethanol high-preferring rats. Org-25935 decreased ethanol intake and ethanol preference, as compared with vehicle, whereas water intake was unaffected. This effect was dose-dependent, developed gradually and was sustained for up to 40 days Note: Other GlyT1 inhibitors include GSK931145, Lu AA21279, NFPS, Org 25935, SB-710622, SSR 504734, whereas D-serine is an agonist. All GlyT1 inhibitors increased seizure thresholds dose-dependently, indicative of anticonvulsant activity. | [IC 50]
GlyT1: 100 nM (IC50) | [References]
[1] Molander A, et al. The glycine reuptake inhibitor Org 25935 decreases ethanol intake and preference in male wistar rats. Alcohol Alcohol. 2007;42(1):11-18. DOI:10.1093/alcalc/agl085 |
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