Enhancement of 3H-diazepam binding by SQ 65,396: a novel anti-anxiety agent.
SQ 65,396, a clinically active anti-anxiety agent, enhanced the binding of 3H-diazepam at 1.5 nM. This effect was due to an increase in the affinity for the ligand, without a change in the number of 3H-diazepam binding sites. This action of SQ 65,396 may mediate its anti-anxiety effects by affecting the action of an endogenous modulator of the "benzodiazepine receptor." Several other substances and treatments increase the affinity of 3H-diazepam for its receptors by mechanisms which may be related to the effect produced by SQ 65,396.
D000818:Animals; D014151:Anti-Anxiety Agents / Q000494:pharmacology*; D001921:Brain / Q000187:drug effects / Q000378:metabolism; D003975:Diazepam / Q000378:metabolism*; D066298:In Vitro Techniques; D007700:Kinetics; D008297:Male; D011720:Pyrazoles / Q000494:pharmacology*; D011725:Pyridines / Q000494:pharmacology*; D051381:Rats; D011955:Receptors, Drug / Q000187:drug effects / Q000378:metabolism
D014151:Anti-Anxiety Agents; D011720:Pyrazoles; D011725:Pyridines; D011955:Receptors, Drug; C006315:cartazolate; D003975:Diazepam