[Solubilization of the central benzodiazepine receptor and study of its interaction with nicotinamide].
It was shown that nicotinamide and NAD inhibit the specific binding of [3H]flunitrazepam to benzdiazepine receptors without causing a direct influence of gamma-aminobutyric acid (GABA) receptors. The GABA-benzdiazepine complex was separated by solubilization with 0.5% lubrol PX. The solubilized preparations contain the binding sites for [3H]flunitrazepam alone (Kd = 5.9 nm). The Kd value for the membrane-bound benzdiazepine receptor is 2.9 nM. NAD inhibited the specific binding of [3H]flunitrazepam to the solubilized membrane preparation when used at concentrations by several orders of magnitude lower than that of nicotinamide. Using gel filtration on Sepharose 6B-CL, the molecular mass of the soluble benzdiazepine receptor protein was determined.
Fomenko
A I
AI
Stepanenko
S P
SP
Donchenko
G V
GV
Khalmuradov
A G
AG
D000818:Animals; D001667:Binding, Competitive; D001921:Brain / Q000378:metabolism; D005445:Flunitrazepam / Q000378:metabolism; D008297:Male; D009536:Niacinamide / Q000378:metabolism* / Q000494:pharmacology; D051381:Rats; D011963:Receptors, GABA-A / Q000187:drug effects / Q000378:metabolism*; D012995:Solubility
D011963:Receptors, GABA-A; D009536:Niacinamide; D005445:Flunitrazepam
Soliubilizatsiia tsentral'nogo retseptora benzodiazepinov i izuchenie ego vzaimodeĭstviia s nikotinamidom.