دورية أكاديمية
أعرض في EDS

Myocardial beta-adrenoceptor down-regulation by norepinephrine is linked to reduced norepinephrine uptake activity.

التفاصيل البيبلوغرافية
العنوان: Myocardial beta-adrenoceptor down-regulation by norepinephrine is linked to reduced norepinephrine uptake activity.
المؤلفون: Dong E; Cardiology Unit, Box 679, Cardiology Research Laboratories, Department of Medicine, University of Rochester Medical Center, 601 Elmwood Avenue, Rochester NY, USA., Yatani A, Mohan A, Liang CS
المصدر: European journal of pharmacology [Eur J Pharmacol] 1999 Nov 12; Vol. 384 (1), pp. 17-24.
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: Elsevier Science Country of Publication: Netherlands NLM ID: 1254354 Publication Model: Print Cited Medium: Print ISSN: 0014-2999 (Print) Linking ISSN: 00142999 NLM ISO Abbreviation: Eur J Pharmacol Subsets: MEDLINE
أسماء مطبوعة: Publication: 2005- : Amsterdam : Elsevier Science
Original Publication: Amsterdam, North Holland Pub. Co.
مواضيع طبية MeSH: Heart Ventricles/*drug effects , Norepinephrine/*pharmacokinetics , Norepinephrine/*pharmacology , Receptors, Adrenergic, beta/*metabolism, Adenylyl Cyclases/metabolism ; Adrenergic beta-Agonists/pharmacology ; Adrenergic beta-Antagonists/metabolism ; Adrenergic beta-Antagonists/pharmacology ; Animals ; Binding, Competitive/drug effects ; Colforsin/pharmacology ; Dobutamine/pharmacology ; Dogs ; Down-Regulation/drug effects ; Enzyme Activation/drug effects ; Guanylyl Imidodiphosphate/pharmacology ; Heart Ventricles/metabolism ; Hemodynamics/drug effects ; Imidazoles/pharmacology ; In Vitro Techniques ; Iodine Radioisotopes ; Iodocyanopindolol/metabolism ; Iodocyanopindolol/pharmacology ; Isoproterenol/pharmacology ; Myocardial Contraction/drug effects ; Receptors, Adrenergic, beta/drug effects ; Receptors, Adrenergic, beta-1/metabolism ; Receptors, Adrenergic, beta-2/metabolism ; Ventricular Function
مستخلص: Chronic administration of norepinephrine for 8 weeks has been shown to reduce neuronal norepinephrine uptake activity and increase interstitial norepinephrine concentration in the heart. To determine whether the changes could lead to myocardial beta-adrenoceptor down-regulation or beta-adrenergic subsensitivity, we measured left ventricular contractile responses to dobutamine, myocardial beta-adrenoceptor density, beta subtype distribution, competitive inhibition agonist binding, and adenylyl cyclase activity activation by isoproterenol, 5'-guanylylimidodiphosphate, and forskolin in dogs after a norepinephrine or saline infusion for 8 weeks. We found that norepinephrine infusion reduced myocardial beta-adrenoceptor density, beta(1)-adrenoceptor subtype density, and high-affinity site for isoproterenol. Left ventricular contractile responses to dobutamine were reduced in the norepinephrine-infused animals. In addition, norepinephrine infusion decreased the basal adenylyl cyclase activity and the adenylyl cyclase responses to isoproterenol, 5'-guanylylimidodiphosphate, and forskolin. The findings indicate that a decrease in cardiac norepinephrine uptake predisposes the heart to norepinephrine-induced myocardial beta-adrenoceptor down-regulation, and that norepinephrine, when present in a sufficient amount over a long period as it is in chronic heart failure, can reduce myocardial beta-adrenergic responsiveness by both homologous and heterologous desensitization.
معلومات مُعتمدة: HL-39260 United States HL NHLBI NIH HHS
المشرفين على المادة: 0 (Adrenergic beta-Agonists)
0 (Adrenergic beta-Antagonists)
0 (Imidazoles)
0 (Iodine Radioisotopes)
0 (Receptors, Adrenergic, beta)
0 (Receptors, Adrenergic, beta-1)
0 (Receptors, Adrenergic, beta-2)
1F7A44V6OU (Colforsin)
34273-04-6 (Guanylyl Imidodiphosphate)
3S12J47372 (Dobutamine)
83498-72-0 (Iodocyanopindolol)
CNU8DA2K9J (CGP 20712A)
EC 4.6.1.1 (Adenylyl Cyclases)
L628TT009W (Isoproterenol)
X4W3ENH1CV (Norepinephrine)
تواريخ الأحداث: Date Created: 19991228 Date Completed: 20000118 Latest Revision: 20190624
رمز التحديث: 20231215
DOI: 10.1016/s0014-2999(99)00652-4
PMID: 10611414
قاعدة البيانات: MEDLINE
الوصف
تدمد:0014-2999
DOI:10.1016/s0014-2999(99)00652-4