3 of 11 Complete Record Tagged AN- 89344355| TI- Binding sites for [3H]2-oxo-quazepam in the brain of the cat: evidence

for heterogeneity of benzodiazepine recognition sites.| AU- Giorgi O^Corda MG^Gritti I^Mariotti M^Ongini E^Biggio G| CS- Department of Experimental Biology, University of Cagliari, Italy.| JN- Neuropharmacology| CP- (ENGLAND)| PY- Jul 18 1989| VO- 28 (7) p715-8| SN- 0028-3908| LA- ENGLISH| JA- 8911| SF- INDEX MEDICUS| AB- In the present study, the distribution of benzodiazepine recognition site subtypes in the brain of the cat was investigated.^To this aim, the binding properties of [3H]2-oxo-quazepam ([3H]2OXOQ) and [3H]beta-CCE, two ligands with preferential affinity for Type I benzodiazepine recognition sites, were compared to binding parameters for [3H]flunitrazepam ([3H]FNT) in different areas of the cat brain.^The ratio of [3H]2OXOQ to [3H]FNT binding sites indicated that, in the cerebellum, Type I sites accounted for 90% of the total number of benzodiazepine recognition sites.^The cerebral cortex, thalamus and mesencephalic reticular formation had also a high proportion of Type I sites (73-78%), whilst the two subtypes were almost equally distributed in the hippocampus, amygdala and bulbar reticular formation.^A similar distribution of subtypes of benzodiazepine recognition sites was indicated by the ratio of [3H]beta CCE to [3H]FNT binding sites for different areas of the brain.^These results demonstrate the existence of heterogeneity of recognition sites for benzodiazepines in the brain of the cat and support the view that [3H]2OXOQ preferentially labels Type I sites.| GS- Animal^Male| DE- *Benzodiazepine Tranquilizers_Metabolism_ME^ *Benzodiazepinones_Metabolism_ME^*Brain Chemistry_Drug Effects_DE^ *Receptors, GABA-Benzodiazepine_Metabolism_ME^Carbolines_Metabolism_ME^Cats^ Flunitrazepam_Metabolism_ME| RN- 0 (Receptors, GABA-Benzodiazepine)^1622-62-4 (Flunitrazepam)^49606-44-2 (Sch 15725)^74214-62-3 (beta-carboline-3-carboxylic acid ethyl ester)|| 5 of 11 Complete Record Tagged AN- 89262554| TI- gamma-Aminobutyric acid receptors at the ventral surface of the medulla inhibit respiratory motor outflow to the laryngeal musculature.| AU- King KA^Holtman JR Jr| CS- Department of Pharmacology, College of Medicine, University of Kentucky, Lexington 40536.| JN- Neuropharmacology| CP- (ENGLAND)| PY- Mar 19 1989| VO- 28 (3) p255-62| SN- 0028-3908| CN- HL 36050^HL 39146| LA- ENGLISH| JA- 8909| SF- INDEX MEDICUS| AB- The effect of activating gamma-aminobutyric acid (GABA) receptors at the ventral surface of the medulla on the activity of the recurrent laryngeal nerve and phrenic nerve was assessed in the cat.^Characteristics of the effects of GABA on the activity of the recurrent laryngeal nerve were compared with those on that of the phrenic nerve which has previously been shown to be inhibited by the application of GABA to the ventral surface of

the medulla.^Application of GABA (0.017-4.05 mg) to the intermediate area produced a dose-related inhibition of respiratory activity in the recurrent laryngeal nerve, as well as the phrenic nerve, that culminated in apnea.^ The inhibition in each nerve was seen as a decrease in amplitude of nerve activity with no change in respiratory rate.^The onset time, peak time and recovery time from GABA-induced inhibition of activity in the recurrent laryngeal and phrenic nerves were not significantly different.^The ED50 value for GABA and its 95% confidence interval for inhibition of the activities of the recurrent laryngeal and phrenic nerves were 0.26 mg (0.190.36 mg) and 0.27 mg (0.20-0.37 mg), respectively.^Therefore, the potency of GABA for the inhibition of the activity of these nerves was not significantly different.^The GABA receptor antagonist, bicuculline (10 micrograms), reversed the inhibition of the activities of both the recurrent laryngeal and the phrenic nerves.^The time for return of phasic activity in each nerve after bicuculline was not significantly different.(ABSTRACT TRUNCATED AT 250 WORDS)| GS- Animal^Support, Non-U.S. Gov't^Support, U.S. Gov't, P.H.S.| DE- *Larynx_Physiology_PH^*Medulla Oblongata_Physiology_PH^*Receptors, GABABenzodiazepine_Physiology_PH^*Respiratory Muscles_Physiology_PH^ Bicuculline_Pharmacology_PD^Cats^Neurons_Drug Effects_DE^Phrenic Nerve_Drug Effects_DE^Recurrent Laryngeal Nerve_Physiology_PH^Respiration_Drug Effects_DE^Respiratory Muscles_Innervation_IR| RN- 0 (Receptors, GABA-Benzodiazepine)^485-49-4 (Bicuculline)|| 7 of 11 Complete Record Tagged AN- 89257366| TI- Solubilization of peripheral-type benzodiazepine binding sites from cat cerebral cortex.| AU- Awad M^Gavish M| CS- Rappaport Family Institute for Research in the Medical Sciences, Faculty of Medicine, Technion-Israel Institute of Technology, Haifa.| JN- J Neurochem| CP- (UNITED STATES)| PY- Jun 1989| VO- 52 (6) p1880-5| SN- 0022-3042| LA- ENGLISH| JA- 8909| SF- INDEX MEDICUS| AB- The present study demonstrates for the first time the solubilization of peripheral-type benzodiazepine binding sites (PBS) from cat cerebral cortex. ^ Of all detergents tested [digitonin, 3-[(3-cholamidopropyl)dimethylammonio]1-propane sulfonate (CHAPS), Tween 20, deoxycholate, and Triton X-100] in the presence of NaCl, the best solubilization (15% of initial activity) was obtained using 0.5% of the zwitterionic detergent CHAPS plus 2 M NaCl.^ Specific binding of [3H]PK 11195 to membrane-bound and solubilized PBS was saturable, yielding equilibrium dissociation constants (KD) of 1.3 +/- 0.2 and 1.9 +/- 0.3 nM, respectively, and maximal numbers of binding sites of 1,435 +/- 150 and 980 +/- 126 fmol/mg protein, respectively.^The KD value of PK 11195 binding to solubilized PBS obtained from experimental kinetic analysis was 0.95 +/- 0.09 nM.^The relative potencies of various compounds (PK 11195, Ro 5-4864, diazepam, flunitrazepam, clonazepam, methyl-betacarboline-3-carboxylate, and Ro 15-1788) in displacing [3H]PK 11195 specific binding from membrane-bound and solubilized PBS were similar.^Most of the solubilized binding activity was destroyed by heating at 60 degrees C for 30 min or by treatment with 2 M guanidinium chloride, which indicates the presence of a protein-binding site in the solubilized preparation.^Over 85% of the solubilized binding activity was retained after 1 week at 4 degrees C, which will enable future application of purification procedures

without major concern for stability of the material.| GS- Animal^Female^Male^Support, Non-U.S. Gov't| DE- *Benzodiazepines_Metabolism_ME^*Cerebral Cortex_Metabolism_ME^Binding Sites^ Binding, Competitive^Cats^Cholic Acids_Pharmacology_PD^ Detergents_Pharmacology_PD^Isoquinolines_Pharmacology_PD^ Membranes_Metabolism_ME^Solubility| RN- 75621-03-3 (3-((3-cholamidopropyl)dimethylammonium)-1-propanesulfonate)^ 85340-56-3 (PK 11195)||