Benzodiazepine binding sites in human pineal gland
The high affinity binding of [3H]flunitrazepam (FNZP) to crude membrane preparations was examined in human pineal glands. Scatchard analysis of the data at equilibrium revealed a single population of binding sites with dissociation constant = 2.36-2.53 nM and binding site concentration = 59-108 fmol...
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todo:paper_00142999_v106_n2_p399_Lowenstein2023-10-03T14:12:02Z Benzodiazepine binding sites in human pineal gland Lowenstein, P.R. Rosenstein, R. Caputti, E. Cardinali, D.P. Benzodiazepine receptors Cerebral cortex GABA Human Pineal gland 4 aminobutyric acid 4' chlorodiazepam benzodiazepine derivative benzodiazepine receptor bicuculline clonazepam diazepam flumazenil flunitrazepam radioisotope brain cortex central nervous system drug binding drug receptor binding flunitrazepam h 3 human human cell normal human pharmacokinetics pineal body priority journal Adolescent Adult Aged Animal Benzodiazepinones Binding, Competitive Cerebral Cortex Child Child, Preschool Clonazepam Diazepam Flumazenil Flunitrazepam gamma-Aminobutyric Acid Human In Vitro Infant Kinetics Male Middle Age Pineal Gland Rats Rats, Inbred Strains Receptors, GABA-A Support, Non-U.S. Gov't The high affinity binding of [3H]flunitrazepam (FNZP) to crude membrane preparations was examined in human pineal glands. Scatchard analysis of the data at equilibrium revealed a single population of binding sites with dissociation constant = 2.36-2.53 nM and binding site concentration = 59-108 fmol/mg protein. When various benzodiazepine (BZP) analogues were tested for their ability to inhibit [3H]FNZP binding the following Ki (nM) were found: clonazepam (0.13), RO 15-1788 (0.60), FNZP (2.14), diazepam (13.5), Ro 5-4864 (>10000). In both human pineal gland and cerebral cortex 10-100 μM γ-aminobutyric acid (GABA) increased BZP binding by about 30%, an effect inhibited by the GABA receptor blocker bicuculline. The stimulatory effect of GABA on [3H]FNZP binding in rat cerebral cortex (about 60%) decreased as a function of time elapsed postmortem at room temperature to reach values similar to those observed in human brains. These results suggest the existence of central type BZP receptors in the human pineal glands. © 1984. JOUR info:eu-repo/semantics/openAccess http://creativecommons.org/licenses/by/2.5/ar http://hdl.handle.net/20.500.12110/paper_00142999_v106_n2_p399_Lowenstein |
| institution |
Universidad de Buenos Aires |
| institution_str |
I-28 |
| repository_str |
R-134 |
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Biblioteca Digital - Facultad de Ciencias Exactas y Naturales (UBA) |
| topic |
Benzodiazepine receptors Cerebral cortex GABA Human Pineal gland 4 aminobutyric acid 4' chlorodiazepam benzodiazepine derivative benzodiazepine receptor bicuculline clonazepam diazepam flumazenil flunitrazepam radioisotope brain cortex central nervous system drug binding drug receptor binding flunitrazepam h 3 human human cell normal human pharmacokinetics pineal body priority journal Adolescent Adult Aged Animal Benzodiazepinones Binding, Competitive Cerebral Cortex Child Child, Preschool Clonazepam Diazepam Flumazenil Flunitrazepam gamma-Aminobutyric Acid Human In Vitro Infant Kinetics Male Middle Age Pineal Gland Rats Rats, Inbred Strains Receptors, GABA-A Support, Non-U.S. Gov't |
| spellingShingle |
Benzodiazepine receptors Cerebral cortex GABA Human Pineal gland 4 aminobutyric acid 4' chlorodiazepam benzodiazepine derivative benzodiazepine receptor bicuculline clonazepam diazepam flumazenil flunitrazepam radioisotope brain cortex central nervous system drug binding drug receptor binding flunitrazepam h 3 human human cell normal human pharmacokinetics pineal body priority journal Adolescent Adult Aged Animal Benzodiazepinones Binding, Competitive Cerebral Cortex Child Child, Preschool Clonazepam Diazepam Flumazenil Flunitrazepam gamma-Aminobutyric Acid Human In Vitro Infant Kinetics Male Middle Age Pineal Gland Rats Rats, Inbred Strains Receptors, GABA-A Support, Non-U.S. Gov't Lowenstein, P.R. Rosenstein, R. Caputti, E. Cardinali, D.P. Benzodiazepine binding sites in human pineal gland |
| topic_facet |
Benzodiazepine receptors Cerebral cortex GABA Human Pineal gland 4 aminobutyric acid 4' chlorodiazepam benzodiazepine derivative benzodiazepine receptor bicuculline clonazepam diazepam flumazenil flunitrazepam radioisotope brain cortex central nervous system drug binding drug receptor binding flunitrazepam h 3 human human cell normal human pharmacokinetics pineal body priority journal Adolescent Adult Aged Animal Benzodiazepinones Binding, Competitive Cerebral Cortex Child Child, Preschool Clonazepam Diazepam Flumazenil Flunitrazepam gamma-Aminobutyric Acid Human In Vitro Infant Kinetics Male Middle Age Pineal Gland Rats Rats, Inbred Strains Receptors, GABA-A Support, Non-U.S. Gov't |
| description |
The high affinity binding of [3H]flunitrazepam (FNZP) to crude membrane preparations was examined in human pineal glands. Scatchard analysis of the data at equilibrium revealed a single population of binding sites with dissociation constant = 2.36-2.53 nM and binding site concentration = 59-108 fmol/mg protein. When various benzodiazepine (BZP) analogues were tested for their ability to inhibit [3H]FNZP binding the following Ki (nM) were found: clonazepam (0.13), RO 15-1788 (0.60), FNZP (2.14), diazepam (13.5), Ro 5-4864 (>10000). In both human pineal gland and cerebral cortex 10-100 μM γ-aminobutyric acid (GABA) increased BZP binding by about 30%, an effect inhibited by the GABA receptor blocker bicuculline. The stimulatory effect of GABA on [3H]FNZP binding in rat cerebral cortex (about 60%) decreased as a function of time elapsed postmortem at room temperature to reach values similar to those observed in human brains. These results suggest the existence of central type BZP receptors in the human pineal glands. © 1984. |
| format |
JOUR |
| author |
Lowenstein, P.R. Rosenstein, R. Caputti, E. Cardinali, D.P. |
| author_facet |
Lowenstein, P.R. Rosenstein, R. Caputti, E. Cardinali, D.P. |
| author_sort |
Lowenstein, P.R. |
| title |
Benzodiazepine binding sites in human pineal gland |
| title_short |
Benzodiazepine binding sites in human pineal gland |
| title_full |
Benzodiazepine binding sites in human pineal gland |
| title_fullStr |
Benzodiazepine binding sites in human pineal gland |
| title_full_unstemmed |
Benzodiazepine binding sites in human pineal gland |
| title_sort |
benzodiazepine binding sites in human pineal gland |
| url |
http://hdl.handle.net/20.500.12110/paper_00142999_v106_n2_p399_Lowenstein |
| work_keys_str_mv |
AT lowensteinpr benzodiazepinebindingsitesinhumanpinealgland AT rosensteinr benzodiazepinebindingsitesinhumanpinealgland AT caputtie benzodiazepinebindingsitesinhumanpinealgland AT cardinalidp benzodiazepinebindingsitesinhumanpinealgland |
| _version_ |
1782029829670961152 |