Specific binding of [3H]diazepam in mouse glioblastoma: the influence of clonazepam and Ro 5-4864 on [3H]diazepam binding

• Published in: Neuroscience letters Vol. 52; no. 3; p. 259
• Main Authors: Zlobina, G P, Kondakova, L I, Khalansky, A S
• Format: Journal Article
• Language: English
• Published: Ireland 21-12-1984
• Subjects: Animals; Benzodiazepinones - pharmacology; Binding Sites; Cell Line; Clonazepam - pharmacology; Diazepam - metabolism; Glioma; Mice; Neuroglia - metabolism
• ISSN: 0304-3940
• DOI: 10.1016/0304-3940(84)90171-X

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.