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- W1974536241 abstract "1 A high density of [3H]-PK 11195 binding sites was present in gerbil cortical membranes (Bmax [3H]-PK 11195 1360 ± 71 fmol mg−1 protein) in comparison to rat cortical membranes (254 ± 21 fmol mg−1 protein). This effect was species-specific as similar findings were obtained with hippocampal membranes (Bmax 1430 ± 111 fmol mg−1 protein in gerbil, compared to 196 ± 31 in rat). 2 RO 5–4864, also a peripheral type benzodiazepine compound, displayed low affinity for the [3H]-PK 11195 site in the gerbil (pKi 6.57 ± 0.02 and 6.70 ± 0.12 in hippocampus and cortex respectively) compared to rat (pKi 8.16 ± 0.07 and 8.48 ± 0.02). Central benzodiazepine compounds, diazepam and flunitrazepam, also displayed this trend. 3 RO 5–4864 displaced [3H]-PK 11195 binding from gerbil and rat cortical membranes through a competitive interaction with Hill slopes close to unity. In both tissues, saturation isotherms of [3H]-PK 11195 binding indicated that the presence of RO 5–4864 caused changes in Kd without any effect on Bmax. In kinetic experiments, the presence of RO 5–4864 failed to modify the rate of dissociation of [3H]-PK 11195 from equilibrium in both rat and gerbil cortical membranes. 4 Forebrain ischaemia in the Mongolian gerbil (5 min bilateral carotid artery occlusion) with 7 days recovery caused a significant (P < 0.05) decrease in the density of hippocampal 5-HT1A binding sites labelled by [3H]-8-OH-DPAT (Bmax control, 393 ± 33 fmol mg−1 protein; ischaemic, 289 ± 21 fmol mg−1 protein) and an increase (P < 0.01) in [3H]-PK 11195 binding sites (Bmax control, 1430 ± 111 fmol mg−1 protein; ischaemic, 2160 ± 170 fmol mg−1 protein). Ischaemia and recovery had no effect on the affinity of either ligand. 5 Autoradiography experiments in gerbil brain sections revealed that the ischaemia-induced increase in [3H]-PK 11195 binding was consistent and significant in the CA1 subfield on the hippocampus (control, 152 ± 42 fmol mg−1 tissue; ischaemic; 314 ±; 43 fmol mg−1 tissue)." @default.
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- W1974536241 date "1993-06-01" @default.
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- W1974536241 title "Changes in [3H]-PK 11195 and [3H]-8-OH-DPAT binding following forebrain ischaemia in the gerbil" @default.
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- W1974536241 doi "https://doi.org/10.1111/j.1476-5381.1993.tb13588.x" @default.
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