Dihydroergocryptine binding sites in bovine and rat pineal glands
High affinity binding of [3H]dihydroergocryptine (DHE) to crude membrane preparations of bovine and rat pineal glands was examined by a rapid filtration procedure through Whatman GFB paper. Scatchard analysis of bovine pineal membranes revealed a single population of binding sites with Kd = (4.8 ± 1...
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todo:paper_01651838_v2_n4_p305_Vacas2023-10-03T15:02:50Z Dihydroergocryptine binding sites in bovine and rat pineal glands Vacas, M.I. Lowenstein, P.R. Cardinali, D.P. alpha-adrenoceptors pineal gland superior cervical ganglion [3H]dihydroergocryptine binding adrenalin alpha adrenergic receptor dihydroergocryptine h 3 drug receptor isoprenaline methysergide noradrenalin octopamine oxidopamine phenoxybenzamine phentolamine postsynaptic receptor propranolol radioisotope serotonin unclassified drug animal experiment article autonomic nervous system cattle endocrine system in vitro study pharmacokinetics pineal body rat Scatchard plot superior cervical ganglion High affinity binding of [3H]dihydroergocryptine (DHE) to crude membrane preparations of bovine and rat pineal glands was examined by a rapid filtration procedure through Whatman GFB paper. Scatchard analysis of bovine pineal membranes revealed a single population of binding sites with Kd = (4.8 ± 1.9) × 10−8M (mean±S.E.M., n= 3 and binding site concentration= 834 ± 103 fmol/mg of protein. When various α- and β-adrenergic agonists or antagonists were tested for their ability to inhibit [3H]DHE binding the following Ki values (μM) were obtained: DHE (0.039), phentolamine (0.102), phenoxybenzomine (0.262), methysergide (0.670), l-epinephrine (2.27), serotonin (3.09), l-norepinephrine (3.20), octopamine (30.3), l-propranolol (1710), l-isoproterenol (〉2000). In order to obtain information on the pre- or postsynaptic location of pineal DHE binding sites, pineal 900 g supernatants were prepared from rats subjected to bilateral superior cervical ganglionectomy or sham-operation 7 days earlier. Ganglionectomy caused a 53% increase in the number of binding sites without changing significantly their Kd (5.2 × 10−8 M and 5.5 × 10−8 M in ganglionectomized and control rats, respectively). These results are compatible with the view that postsynaptic α-adrenoceptors are present in the pineal gland. © 1980, Elsevier/North-Holland Biomedical Press. All rights reserved. JOUR info:eu-repo/semantics/openAccess http://creativecommons.org/licenses/by/2.5/ar http://hdl.handle.net/20.500.12110/paper_01651838_v2_n4_p305_Vacas |
| 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 |
alpha-adrenoceptors pineal gland superior cervical ganglion [3H]dihydroergocryptine binding adrenalin alpha adrenergic receptor dihydroergocryptine h 3 drug receptor isoprenaline methysergide noradrenalin octopamine oxidopamine phenoxybenzamine phentolamine postsynaptic receptor propranolol radioisotope serotonin unclassified drug animal experiment article autonomic nervous system cattle endocrine system in vitro study pharmacokinetics pineal body rat Scatchard plot superior cervical ganglion |
| spellingShingle |
alpha-adrenoceptors pineal gland superior cervical ganglion [3H]dihydroergocryptine binding adrenalin alpha adrenergic receptor dihydroergocryptine h 3 drug receptor isoprenaline methysergide noradrenalin octopamine oxidopamine phenoxybenzamine phentolamine postsynaptic receptor propranolol radioisotope serotonin unclassified drug animal experiment article autonomic nervous system cattle endocrine system in vitro study pharmacokinetics pineal body rat Scatchard plot superior cervical ganglion Vacas, M.I. Lowenstein, P.R. Cardinali, D.P. Dihydroergocryptine binding sites in bovine and rat pineal glands |
| topic_facet |
alpha-adrenoceptors pineal gland superior cervical ganglion [3H]dihydroergocryptine binding adrenalin alpha adrenergic receptor dihydroergocryptine h 3 drug receptor isoprenaline methysergide noradrenalin octopamine oxidopamine phenoxybenzamine phentolamine postsynaptic receptor propranolol radioisotope serotonin unclassified drug animal experiment article autonomic nervous system cattle endocrine system in vitro study pharmacokinetics pineal body rat Scatchard plot superior cervical ganglion |
| description |
High affinity binding of [3H]dihydroergocryptine (DHE) to crude membrane preparations of bovine and rat pineal glands was examined by a rapid filtration procedure through Whatman GFB paper. Scatchard analysis of bovine pineal membranes revealed a single population of binding sites with Kd = (4.8 ± 1.9) × 10−8M (mean±S.E.M., n= 3 and binding site concentration= 834 ± 103 fmol/mg of protein. When various α- and β-adrenergic agonists or antagonists were tested for their ability to inhibit [3H]DHE binding the following Ki values (μM) were obtained: DHE (0.039), phentolamine (0.102), phenoxybenzomine (0.262), methysergide (0.670), l-epinephrine (2.27), serotonin (3.09), l-norepinephrine (3.20), octopamine (30.3), l-propranolol (1710), l-isoproterenol (〉2000). In order to obtain information on the pre- or postsynaptic location of pineal DHE binding sites, pineal 900 g supernatants were prepared from rats subjected to bilateral superior cervical ganglionectomy or sham-operation 7 days earlier. Ganglionectomy caused a 53% increase in the number of binding sites without changing significantly their Kd (5.2 × 10−8 M and 5.5 × 10−8 M in ganglionectomized and control rats, respectively). These results are compatible with the view that postsynaptic α-adrenoceptors are present in the pineal gland. © 1980, Elsevier/North-Holland Biomedical Press. All rights reserved. |
| format |
JOUR |
| author |
Vacas, M.I. Lowenstein, P.R. Cardinali, D.P. |
| author_facet |
Vacas, M.I. Lowenstein, P.R. Cardinali, D.P. |
| author_sort |
Vacas, M.I. |
| title |
Dihydroergocryptine binding sites in bovine and rat pineal glands |
| title_short |
Dihydroergocryptine binding sites in bovine and rat pineal glands |
| title_full |
Dihydroergocryptine binding sites in bovine and rat pineal glands |
| title_fullStr |
Dihydroergocryptine binding sites in bovine and rat pineal glands |
| title_full_unstemmed |
Dihydroergocryptine binding sites in bovine and rat pineal glands |
| title_sort |
dihydroergocryptine binding sites in bovine and rat pineal glands |
| url |
http://hdl.handle.net/20.500.12110/paper_01651838_v2_n4_p305_Vacas |
| work_keys_str_mv |
AT vacasmi dihydroergocryptinebindingsitesinbovineandratpinealglands AT lowensteinpr dihydroergocryptinebindingsitesinbovineandratpinealglands AT cardinalidp dihydroergocryptinebindingsitesinbovineandratpinealglands |
| _version_ |
1807321283501752320 |