دورية أكاديمية

Identification and characterisation of beta-adrenoceptors on intact equine peripheral blood lymphocytes with the radioligand (-)-[125I]-iodocyanopindolol.

التفاصيل البيبلوغرافية
العنوان: Identification and characterisation of beta-adrenoceptors on intact equine peripheral blood lymphocytes with the radioligand (-)-[125I]-iodocyanopindolol.
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
الوصف
تدمد:0425-1644
DOI:10.2746/042516401776254862