758698-37-2

Upstream product

• 530-62-1 1,1'-carbonyldiimidazole 
• 139-59-3 4-phenoxyanilin 
• 92-95-5 4-biphenyl isocyanate 
• 851967-60-7 [(S)-2-phenyl-1-(2-pyrrolidin-1-yl-ethylcarbamoyl)-ethyl]-carbamic acid tert-butyl ester 
• 13734-34-4 N-tert-butoxycarbonyl-L-phenylalanine 
• 7154-73-6 1-(2-aminoethyl)pyrrolidine 

Relevant academic research and scientific papers

GLYT2 MODULATORS

α-, β-, and γ-amino acid derivatives of formula I are disclosed as selective GlyT2 inhibitors for the treatment of central nervous system (CNS) conditions such as muscle spasticity, tinnitus, epilepsy and neuropathic pain. Formula I

Novel glycine transporter type-2 reuptake inhibitors. Part 1: α-amino acid derivatives

A variety of α-amino acid derivatives were prepared as glycine transport inhibitors and their ability to block the uptake of [ 14C]-glycine in COS7 cells transfected with human glycine transporter-2 (hGlyT-2) was evaluated. An array of substituents at the chiral center was studied and overall, L-phenylalanine was identified as the preferred amino acid residue. Compounds prepared from L-amino acids were more potent GlyT-2 inhibitors than analogs derived from the corresponding D-amino acids. Introducing an achiral amino acid such as glycine, or incorporating geminal substitution in the α-position, led to a significant reduction in GlyT-2 inhibitory properties.