دورية أكاديمية
Identification and characterisation of beta-adrenoceptors on intact equine peripheral blood lymphocytes with the radioligand (-)-[125I]-iodocyanopindolol.
العنوان: | Identification and characterisation of beta-adrenoceptors on intact equine peripheral blood lymphocytes with the radioligand (-)-[125I]-iodocyanopindolol. |
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المؤلفون: | Abraham G; Institute of Pharmacology, Pharmacy and Toxicology, Faculty of Veterinary Medicine, University of Leipzig, Germany., Broddet OE, Ungemach FR |
المصدر: | Equine veterinary journal [Equine Vet J] 2001 Sep; Vol. 33 (5), pp. 487-93. |
نوع المنشور: | Journal Article; Research Support, Non-U.S. Gov't |
اللغة: | English |
بيانات الدورية: | Publisher: Wiley Country of Publication: United States NLM ID: 0173320 Publication Model: Print Cited Medium: Print ISSN: 0425-1644 (Print) Linking ISSN: 04251644 NLM ISO Abbreviation: Equine Vet J Subsets: MEDLINE |
أسماء مطبوعة: | Publication: <2009- > : Hobokken, NJ : Wiley Original Publication: Newmarket, Suffolk : Equine Veterinary Journal, Ltd |
مواضيع طبية MeSH: | Adrenergic beta-Antagonists* , Iodocyanopindolol*, Horses/*physiology , Lymphocytes/*metabolism , Receptors, Adrenergic, beta/*classification , Receptors, Adrenergic, beta/*isolation & purification, Animals ; Binding Sites/physiology ; Cyclic AMP/metabolism ; Iodine Radioisotopes ; Kinetics ; Ligands ; Stereoisomerism |
مستخلص: | In this study, beta-adrenoceptors of intact equine lymphocytes were identified and subclassified by (-)-[125I]-iodocyanopindolol (ICYP) binding. ICYP binding to intact equine lymphocytes was rapid, saturable (maximal number of binding sites 320 +/- 20 ICYP binding sites/cell, n = 12) and of high affinity (KD value for ICYP 14.4 +/- 1.7 pmol/l, n = 12). Binding was stereospecific as shown by the 10 times greater potency of (-)-propranolol to inhibit binding than its (+)-isomer. Beta-adrenoceptor agonists inhibited ICYP binding with an order of potency: (-)-isoprenaline >(-)-adrenaline >(-)-noradrenaline; the same order of potency was obtained for agonist-induced stimulation of lymphocyte cyclic AMP content. The selective beta2-adrenoceptor antagonist ICI 118,551 was about 1000 times more potent in inhibiting ICYP binding than was the beta1-selective adrenoceptor antagonist CGP 20712A. It is, therefore, concluded that in intact equine lymphocytes, ICYP labels a class of functional beta-adrenoceptors that belong predominantly (>90%) to the beta2-adrenoceptor subtype; a small (<10%) beta1-adrenoceptor component, however, cannot be ruled out completely. ICYP binding to equine lymphocytes might be a suitable model to study function and regulation of the beta-adrenoceptor system in the horse in vivo. The aim of this study was to characterise the beta-adrenoreceptor subtypes present on equine lymphocytes. |
المشرفين على المادة: | 0 (Adrenergic beta-Antagonists) 0 (Iodine Radioisotopes) 0 (Ligands) 0 (Receptors, Adrenergic, beta) 83498-72-0 (Iodocyanopindolol) E0399OZS9N (Cyclic AMP) |
تواريخ الأحداث: | Date Created: 20010918 Date Completed: 20020212 Latest Revision: 20190901 |
رمز التحديث: | 20231215 |
DOI: | 10.2746/042516401776254862 |
PMID: | 11558744 |
قاعدة البيانات: | MEDLINE |
تدمد: | 0425-1644 |
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DOI: | 10.2746/042516401776254862 |