Selective affinity of one enantiomer of suriclone demonstrated by a binding assay with benzodiazepine receptors.
The binding of racemic 3H-suriclone on the BZD receptor was performed in special conditions in order to discriminate between the affinity of the two enantiomers: a rebinding method was used. In the first incubation 40% of 3H-suriclone was specifically bound to the BZD receptor. In the second incubation performed with the supernatant coming from the first incubation, less than 1% of the radiolabelled suriclone was specifically bound to the BZD receptor. These results suggest that most probably only one of the two enantiomers of suriclone may bind the BZD receptor. It appears that this enantiomer has the greatest affinity constant ever found for a BZD receptor agonist (Kd = 20 pM at 37 degrees C in presence of GABA and 70 pM in absence of GABA).
D000818:Animals; D005260:Female; D066298:In Vitro Techniques; D007700:Kinetics; D009287:Naphthyridines; D009419:Nerve Tissue Proteins / Q000378:metabolism; D010879:Piperazines / Q000378:metabolism*; D051381:Rats; D011919:Rats, Inbred Strains; D011963:Receptors, GABA-A / Q000378:metabolism*; D013237:Stereoisomerism; D013457:Sulfur Compounds; D013570:Synaptic Membranes / Q000378:metabolism
D009287:Naphthyridines; D009419:Nerve Tissue Proteins; D010879:Piperazines; D011963:Receptors, GABA-A; D013457:Sulfur Compounds; C037283:suriclone