The nature of 1,4-benzodiazepines/receptor interactions.
A general survey of receptor binding affinity data for 1,4-benzodiazepines, associated with the results of crystal structure determinations, quantum-mechanical calculations, structure-activity relationships and pharmacokinetic data, leads the authors to propose a new scheme for benzodiazepine-receptor interactions. 1,4-Benzodiazepines would interact with positively charged receptor sites by means of two hydrogen bonds accepted respectively by the carbonyl oxygen at position 2 and by the N4 atom of the diazepine ring. A third point of interaction would be given by the phenyl ring at C5 which would fit almost exactly in a hydrophobic pocket of the receptor.
D000818:Animals; D001569:Benzodiazepines / Q000378:metabolism*; D066298:In Vitro Techniques; D007700:Kinetics; D008958:Models, Molecular; D051381:Rats; D011963:Receptors, GABA-A / Q000378:metabolism*; D013329:Structure-Activity Relationship
D011963:Receptors, GABA-A; D001569:Benzodiazepines