Design, synthesis and evaluation of substituted triarylnipecotic acid derivatives as GABA uptake inhibitors: identification of a ligand with moderate affinity and …
Conformationally restrained GABA analogs such as nipecotic acid and guvacine are known to be potent GABA uptake inhibitors.ll However, determining the efficacy of such compounds in vivo has been hampered by their poor penetration of the blood-brain barrier, a property attributable to their high degree of hydrophil- icity. In an effort to overcome this problem, Ali et aZ.12 examined the effect of adding lipophilic side chains to the nitrogen atom of various GABA transport ...
