Characterization of agonist-induced internalization and down-regulation of beta-adrenergic receptors in isolated rat lung and heart preparations. 1993

J F Liao, and H T Change, and C F Chen
Department & Institute of Pharmacology, National Yang-Ming Medical College, Taipei, Taiwan, Republic of China.

Using isolated lung and heart preparations from male Sprague-Dawley rats, this study characterizes whether the beta-adrenergic receptor (BAR) agonist isoproterenol (ISO) can induce internalization and down-regulation of BAR in these tissues. The results showed that ISO-induced BAR internalization was time- and concentration-dependent in the lung preparations. When the lung and heart preparations were compared, however, the same ISO (10 microM, 30 min) treatment only induced BAR internalization in the lung but not in the heart preparations. Pretreatment of hypertonic sucrose medium (0.45-0.6 M) for 30 min inhibited about 50% of ISO-induced BAR internalization in the lung preparations. Treatment of either ISO (10 microM) or terbutaline (10 microM) for 3 hr or 12 hr did not significantly decrease the number of BAR in both tissue preparations. However, ISO (10 microM, 12 hr) increased the KD value of the radioligand [125I]-iodocyanopindolol for BAR in the heart homogenates. This ISO-induced KD change was not observed in the presence of cycloheximide (20 micrograms/ml), a protein synthesis inhibitor. In the presence of cycloheximide (20 micrograms/ml), ISO also did not decrease the BAR number in either tissue preparation.

UI MeSH Term Description Entries
D006982 Hypertonic Solutions Solutions that have a greater osmotic pressure than a reference solution such as blood, plasma, or interstitial fluid. Hypertonic Solution,Solution, Hypertonic,Solutions, Hypertonic
D007545 Isoproterenol Isopropyl analog of EPINEPHRINE; beta-sympathomimetic that acts on the heart, bronchi, skeletal muscle, alimentary tract, etc. It is used mainly as bronchodilator and heart stimulant. Isoprenaline,Isopropylarterenol,4-(1-Hydroxy-2-((1-methylethyl)amino)ethyl)-1,2-benzenediol,Euspiran,Isadrin,Isadrine,Isopropyl Noradrenaline,Isopropylnoradrenaline,Isopropylnorepinephrine,Isoproterenol Hydrochloride,Isoproterenol Sulfate,Isuprel,Izadrin,Norisodrine,Novodrin,Hydrochloride, Isoproterenol,Noradrenaline, Isopropyl,Sulfate, Isoproterenol
D008168 Lung Either of the pair of organs occupying the cavity of the thorax that effect the aeration of the blood. Lungs
D008297 Male Males
D009206 Myocardium The muscle tissue of the HEART. It is composed of striated, involuntary muscle cells (MYOCYTES, CARDIAC) connected to form the contractile pump to generate blood flow. Muscle, Cardiac,Muscle, Heart,Cardiac Muscle,Myocardia,Cardiac Muscles,Heart Muscle,Heart Muscles,Muscles, Cardiac,Muscles, Heart
D009928 Organ Specificity Characteristic restricted to a particular organ of the body, such as a cell type, metabolic response or expression of a particular protein or antigen. Tissue Specificity,Organ Specificities,Specificities, Organ,Specificities, Tissue,Specificity, Organ,Specificity, Tissue,Tissue Specificities
D010869 Pindolol A moderately lipophilic beta blocker (ADRENERGIC BETA-ANTAGONISTS). It is non-cardioselective and has intrinsic sympathomimetic actions, but little membrane-stabilizing activity. (From Martindale, The Extra Pharmocopoeia, 30th ed, p638) Prindolol,LB-46,Visken,LB 46,LB46
D011412 Propanolamines AMINO ALCOHOLS containing the propanolamine (NH2CH2CHOHCH2) group and its derivatives. Aminopropanols
D011433 Propranolol A widely used non-cardioselective beta-adrenergic antagonist. Propranolol has been used for MYOCARDIAL INFARCTION; ARRHYTHMIA; ANGINA PECTORIS; HYPERTENSION; HYPERTHYROIDISM; MIGRAINE; PHEOCHROMOCYTOMA; and ANXIETY but adverse effects instigate replacement by newer drugs. Dexpropranolol,AY-20694,Anaprilin,Anapriline,Avlocardyl,Betadren,Dociton,Inderal,Obsidan,Obzidan,Propanolol,Propranolol Hydrochloride,Rexigen,AY 20694,AY20694,Hydrochloride, Propranolol
D011943 Receptors, Adrenergic, beta One of two major pharmacologically defined classes of adrenergic receptors. The beta adrenergic receptors play an important role in regulating CARDIAC MUSCLE contraction, SMOOTH MUSCLE relaxation, and GLYCOGENOLYSIS. Adrenergic beta-Receptor,Adrenergic beta-Receptors,Receptors, beta-Adrenergic,beta Adrenergic Receptor,beta-Adrenergic Receptor,beta-Adrenergic Receptors,Receptor, Adrenergic, beta,Adrenergic Receptor, beta,Adrenergic beta Receptor,Adrenergic beta Receptors,Receptor, beta Adrenergic,Receptor, beta-Adrenergic,Receptors, beta Adrenergic,beta Adrenergic Receptors,beta-Receptor, Adrenergic,beta-Receptors, Adrenergic

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