AGONIST-INDUCED DESENSITIZATION OF BETA-ADRENOCEPTOR FUNCTION IN HUMANS - SUBTYPE-SELECTIVE REDUCTION IN BETA-1-ADRENOCEPTOR OR BETA-2-ADRENOCEPTOR MEDIATED PHYSIOLOGICAL-EFFECTS BY XAMOTEROL OR PROCATEROL

被引:47
作者
BRODDE, OE
DAUL, A
MICHELREHER, M
BOOMSMA, F
VELD, AJMI
SCHLIEPER, P
MICHEL, MC
机构
[1] ERASMUS UNIV,HOSP DIJKZIGT,DEPT INTERNAL MED 1,ROTTERDAM,NETHERLANDS
[2] ICI PHARMA DEUTSCHLAND,PLANKSTADT,GERMANY
关键词
Lymphocytes; β[!sub]1[!/sub]-adrenoceptors; β[!sub]2[!/sub]-adrenoceptors;
D O I
10.1161/01.CIR.81.3.914
中图分类号
R5 [内科学];
学科分类号
1002 ; 100201 ;
摘要
We investigated the effects of β2- (procaterol 2x50 μg/day for 9 days) and β1- (xamoterol 2x200 mg/day for 14 days) adrenoceptor agonists on lymphocyte β2-adrenoceptor density and β1- and β2-adrenoceptor in vivo function (assessed as isoprenaline-infusion-evoked hemodynamic effects and exercise-induced tachycardia) in healthy volunteers. Procaterol decreased lymphocyte β2-adrenoceptor density and all β2-adrenoceptor-mediated in vivo effects but did not affect β1-adrenoceptor-mediated in vivo effects. In contrast, xamoterol neither affected lymphocyte β2-adrenoceptors nor β2-adrenoceptor-mediated in vivo effects but decreased β1-adrenoceptor-mediated in vivo effects. It is concluded that in humans, generally long-term application of β1- or β2-adrenoceptor agonists causes desensitization of β-adrenoceptor function but in a β-adrenoceptor subtype-selective fashion.
引用
收藏
页码:914 / 921
页数:8
相关论文
共 34 条
[1]   VAGAL ACTIVITY IS INCREASED DURING INTRAVENOUS ISOPRENALINE INFUSION IN MAN [J].
ARNOLD, JMO ;
MCDEVITT, DG .
BRITISH JOURNAL OF CLINICAL PHARMACOLOGY, 1984, 18 (03) :311-316
[2]   EFFECTS OF THE BETA-2-ADRENOCEPTOR ANTAGONIST ICI-118,551 ON EXERCISE TACHYCARDIA AND ISOPRENALINE-INDUCED BETA-ADRENOCEPTOR RESPONSES IN MAN [J].
ARNOLD, JMO ;
OCONNOR, PC ;
RIDDELL, JG ;
HARRON, DWG ;
SHANKS, RG ;
MCDEVITT, DG .
BRITISH JOURNAL OF CLINICAL PHARMACOLOGY, 1985, 19 (05) :619-630
[3]  
BRODDE OE, 1988, ANN CLIN RES, V20, P311
[4]   HUMAN-HEART BETA-ADRENOCEPTORS - A FAIR COMPARISON WITH LYMPHOCYTE BETA-ADRENOCEPTORS [J].
BRODDE, OE ;
BECKERINGH, JJ ;
MICHEL, MC .
TRENDS IN PHARMACOLOGICAL SCIENCES, 1987, 8 (10) :403-407
[5]   SUBTYPE-SELECTIVE UP-REGULATION OF HUMAN SAPHENOUS-VEIN BETA-2-ADRENOCEPTORS BY CHRONIC BETA-ADRENOCEPTOR ANTAGONIST TREATMENT [J].
BRODDE, OE ;
ZERKOWSKI, HR ;
DOETSCH, N ;
KHAMSSI, M .
NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY, 1989, 339 (04) :479-482
[6]   DIFFERENTIATION OF BETA-1-ADRENOCEPTOR AND BETA-2-ADRENOCEPTOR-MEDIATED EFFECTS IN HUMANS [J].
BRODDE, OE ;
DAUL, A ;
WELLSTEIN, A ;
PALM, D ;
MICHEL, MC ;
BECKERINGH, JJ .
AMERICAN JOURNAL OF PHYSIOLOGY, 1988, 254 (02) :H199-H206
[7]   TERBUTALINE-INDUCED DESENSITIZATION OF HUMAN-LYMPHOCYTE BETA-2-ADRENOCEPTORS - ACCELERATED RESTORATION OF BETA-ADRENOCEPTOR RESPONSIVENESS BY PREDNISONE AND KETOTIFEN [J].
BRODDE, OE ;
BRINKMANN, M ;
SCHEMUTH, R ;
OHARA, N ;
DAUL, A .
JOURNAL OF CLINICAL INVESTIGATION, 1985, 76 (03) :1096-1101
[8]   IN SUPPORT OF CARDIAC CHRONOTROPIC BETA-2 ADRENOCEPTORS [J].
BROWN, JE ;
MCLEOD, AA ;
SHAND, DG .
AMERICAN JOURNAL OF CARDIOLOGY, 1986, 57 (12) :F11-F16
[9]   NEW POSITIVE INOTROPIC AGENTS IN THE TREATMENT OF CONGESTIVE-HEART-FAILURE - MECHANISMS OF ACTION AND RECENT CLINICAL DEVELOPMENTS .1. [J].
COLUCCI, WS ;
WRIGHT, RF ;
BRAUNWALD, E .
NEW ENGLAND JOURNAL OF MEDICINE, 1986, 314 (05) :290-299
[10]   COMPARISON OF THE BETA-1-SELECTIVE AFFINITY OF PRENALTEROL AND CORWIN DEMONSTRATED BY RADIOLIGAND BINDING [J].
COOK, N ;
RICHARDSON, A ;
BARNETT, DB .
EUROPEAN JOURNAL OF PHARMACOLOGY, 1984, 98 (3-4) :407-412