Synthesis, characterization and in vitro pharmacology of novel pregabalin derivatives.
A series of novel pregabalin derivatives were synthesized starting from N-protected pregabalin, different amino sugars, adamantylamine, serotonin and tryptamine. New compounds were spectroscopically characterized and in vitro tested on gabapentin receptor binding assay. The serotonin-pregabalin adduct showed significant binding effect and its IC50 value was determined.
Horvat
Stefica
S
Department of Organic Chemistry and Biochemistry, Rudjer Bosković Institute, P.O. Box 180, 10002 Zagreb, Croatia.
Hamersak
Zdenko
Z
Stipetić
Irena
I
Jolas
Thierry
T
D000818:Animals; D002540:Cerebral Cortex / Q000187:drug effects; D066298:In Vitro Techniques; D020128:Inhibitory Concentration 50; D009682:Magnetic Resonance Spectroscopy; D000069583:Pregabalin; D051381:Rats; D013055:Spectrophotometry, Infrared; D005680:gamma-Aminobutyric Acid / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology
D000069583:Pregabalin; D005680:gamma-Aminobutyric Acid