دورية أكاديمية
Adrenergic receptors in human liver plasma membranes: predominance of beta 2- and alpha 1-receptor subtypes.
| العنوان: | Adrenergic receptors in human liver plasma membranes: predominance of beta 2- and alpha 1-receptor subtypes. |
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| المؤلفون: | Kawai Y, Powell A, Arinze IJ |
| المصدر: | The Journal of clinical endocrinology and metabolism [J Clin Endocrinol Metab] 1986 May; Vol. 62 (5), pp. 827-32. |
| نوع المنشور: | Journal Article; Research Support, Non-U.S. Gov't; Research Support, U.S. Gov't, P.H.S. |
| اللغة: | English |
| بيانات الدورية: | Publisher: Oxford University Press Country of Publication: United States NLM ID: 0375362 Publication Model: Print Cited Medium: Print ISSN: 0021-972X (Print) Linking ISSN: 0021972X NLM ISO Abbreviation: J Clin Endocrinol Metab Subsets: MEDLINE |
| أسماء مطبوعة: | Publication: 2017- : New York : Oxford University Press Original Publication: Springfield, Ill. : Charles C. Thomas |
| مواضيع طبية MeSH: | Liver/*metabolism , Receptors, Adrenergic, alpha/*metabolism , Receptors, Adrenergic, beta/*metabolism, Aged ; Binding, Competitive ; Cell Membrane/metabolism ; Dihydroalprenolol/metabolism ; Dihydroergotoxine/metabolism ; Female ; Guanylyl Imidodiphosphate/pharmacology ; Humans ; Iodocyanopindolol ; Kinetics ; Male ; Middle Aged ; Pindolol/analogs & derivatives ; Pindolol/metabolism ; Prazosin/metabolism ; Radioligand Assay ; Sympatholytics/metabolism ; Sympathomimetics/metabolism ; Yohimbine/metabolism |
| مستخلص: | Adrenergic receptors in human liver plasma membranes were characterized by radioligand binding assays. The binding of [3H]dihydroalprenolol [( 3H]DHA) to partially purified membranes was rapid, of high affinity, saturable, and stereospecific. The binding of [125I]iodocyanopindolol to the same membranes was also saturable and stereospecific, but extremely slow, and at 37 C required about 6 h for equilibration. The maximum number of binding sites from six livers determined with these two beta-receptor ligands was 36-83 fmol/mg protein. Catecholaminergic agonists competed for these binding sites in the order typical for beta 2-adrenergic receptors. IPS 339 [(tertiarybutylamino-3-ol-2-propyl)oximino-9-fluorene hydrochloride], a beta 2-selective antagonist, was at least 3 orders of magnitude more potent in inhibiting the binding of [3H]DHA than the beta 1-antagonist, atenolol. Computer-aided analysis of the competition curves as well as Hofstee transformations of the binding data indicated the predominance of the beta 2-subtype. The GTP analog guanyl-5'-yl-imidodiphosphate, decreased the binding affinity of the agonist, l-isoproterenol, indicating the modulation of agonist-promoted coupling of the receptors to guanine nucleotide regulatory proteins. The maximum number of binding sites for the binding of [3H]prazosin and [3H]dihydroergocryptine were the same (60-70 fmol/mg protein), indicating that the majority of the alpha-receptors are of the alpha 1-subtype. Competition experiments with prazosin and yohimbine confirmed the predominance of the alpha 1-receptor subtype, although the presence of alpha 2-receptors cannot be completely ruled out. These results indicate that adrenergic receptors in human liver plasma membranes are predominantly of the beta 2- and alpha 1-subtypes. |
| معلومات مُعتمدة: | HD-08792 United States HD NICHD NIH HHS |
| المشرفين على المادة: | 0 (Receptors, Adrenergic, alpha) 0 (Receptors, Adrenergic, beta) 0 (Sympatholytics) 0 (Sympathomimetics) 11032-41-0 (Dihydroergotoxine) 2Y49VWD90Q (Yohimbine) 34273-04-6 (Guanylyl Imidodiphosphate) 60106-89-0 (Dihydroalprenolol) 83498-72-0 (Iodocyanopindolol) BJ4HF6IU1D (Pindolol) XM03YJ541D (Prazosin) |
| تواريخ الأحداث: | Date Created: 19860501 Date Completed: 19860515 Latest Revision: 20131121 |
| رمز التحديث: | 20221213 |
| DOI: | 10.1210/jcem-62-5-827 |
| PMID: | 3007555 |
| قاعدة البيانات: | MEDLINE |
| تدمد: | 0021-972X |
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| DOI: | 10.1210/jcem-62-5-827 |