155201-30-2Relevant academic research and scientific papers
Potential anxiolytic agents. Part 4: Novel orally-active N5-substituted pyrido[1,2-a]benzimidazoles with high GABA-A receptor affinity
Jordan, Alfonzo D,Vaidya, Anil H,Rosenthal, Daniel I,Dubinsky, Barry,Kordik, Cheryl P,Sanfilippo, Pauline J,Wu, Wu-Nan,Reitz, Allen B
, p. 2381 - 2386 (2007/10/03)
A series of pyrido[1,2-a]benzimidazoles (PBIs) with substitution on the N5-nitrogen has been synthesized and found to possess high affinity for the benzodiazepine (BZD) site on the GABA-A receptor. The compounds evaluated include those bearing a heteroalkyl group and heterocyclic rings. The most promising of these compounds is ethoxymethyl analogue 24, which has an IC50 of 0.1 nM for the BZD site on the GABA-A receptor and has been advanced to human clinical trials.
