Specific binding of [3H]diazepam in mouse glioblastoma: the influence of clonazepam and Ro 5-4864 on [3H]diazepam binding.
The reversible specific binding of [3H]diazepam was observed by a radioligand method in homogenates of cultured cells of mouse glioblastoma. It was characterized by an equilibrium dissociation constant Kd = 91 +/- 5 nM and the number of maximal binding sites (Bmax) of 1006 +/- 100 fmol/mg protein. The half-saturation and half-degradation periods for the ligand-receptor complex were 15 and 10 s, respectively. The specific binding sites from glioblastoma are similar to the peripheral-type receptors as their inhibition constant for Ro 5-4864 Ki = 16 nM and that for clonazepam Ki = 30 microM.
D000818:Animals; D001570:Benzodiazepinones / Q000494:pharmacology*; D001665:Binding Sites; D002460:Cell Line; D002998:Clonazepam / Q000494:pharmacology*; D003975:Diazepam / Q000378:metabolism*; D005910:Glioma; D051379:Mice; D009457:Neuroglia / Q000378:metabolism*
D001570:Benzodiazepinones; C028513:4'-chlorodiazepam; D002998:Clonazepam; D003975:Diazepam