THE DOPAMINE-D(1) RECEPTOR AGONISTS, A68930 AND SKF-38393, INDUCE AROUSAL AND SUPPRESS REM-SLEEP IN THE RAT

被引:62
作者
TRAMPUS, M [1 ]
FERRI, N [1 ]
ADAMI, M [1 ]
ONGINI, E [1 ]
机构
[1] SCHERING PLOUGH SPA, RES LABS, I-20060 COMAZZO, ITALY
关键词
DOPAMINE-D(1) RECEPTOR AGONISTS; A68930; SK-AND-F-38393; GROOMING BEHAVIOR; REM (RAPID EYE MOVEMENT) SLEEP; (RAT);
D O I
10.1016/0014-2999(93)90823-Z
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
The effects of the dopamine D1 receptor full agonist, A68930, on sleep-wake patterns an grooming behavior were studied in the rat. The partial dopamine D1 receptor agonist, SKF 38393, was used for comparison. A68930 (0.003-0.3 mg/kg s.c.) increased waking time, reduced the amount of rapid eye movement (REM) sleep and enhanced spontaneous grooming dose dependently. The ED50 were 0.06, 0.02 and 0.05 mg/kg, respectively. The D1 antagonist, SCH 23390 (0.003 mg/kg s.c.), blocked the effects of A68930 on wakefulness and grooming but not those on REM sleep. SKF 38393 (0.1-10 mg/kg s.c.) increased grooming with an ED50 of 1.4 mg/kg and a dose-response relationship similar to that of A68930 (potency ratio 28). Conversely, the increase of wakefulness and reduction of REM sleep caused by SKF 38393 had dose-response curves different from those of A68930. The results support the view that D1 receptors may have a physiological function in producing arousal.
引用
收藏
页码:83 / 87
页数:5
相关论文
共 23 条
[1]   DOPAMINE RECEPTOR AGONISTS - SELECTIVITY AND DOPAMINE-D1 RECEPTOR EFFICACY [J].
ANDERSEN, PH ;
JANSEN, JA .
EUROPEAN JOURNAL OF PHARMACOLOGY-MOLECULAR PHARMACOLOGY SECTION, 1990, 188 (06) :335-347
[2]   PARTIAL AND FULL DOPAMINE D1-RECEPTOR AGONISTS IN MICE AND RATS - RELATION BETWEEN BEHAVIORAL-EFFECTS AND STIMULATION OF ADENYLATE-CYCLASE ACTIVITY INVITRO [J].
ARNT, J ;
HYTTEL, J ;
SANCHEZ, C .
EUROPEAN JOURNAL OF PHARMACOLOGY, 1992, 213 (02) :259-267
[3]   OPERATIONAL MODELS OF PHARMACOLOGICAL AGONISM [J].
BLACK, JW ;
LEFF, P .
PROCEEDINGS OF THE ROYAL SOCIETY SERIES B-BIOLOGICAL SCIENCES, 1983, 220 (1219) :141-162
[4]   MOLECULAR-BIOLOGY OF THE DOPAMINE-RECEPTORS [J].
CIVELLI, O ;
BUNZOW, JR ;
GRANDY, DK ;
ZHOU, QY ;
VANTOL, HHM .
EUROPEAN JOURNAL OF PHARMACOLOGY-MOLECULAR PHARMACOLOGY SECTION, 1991, 207 (04) :277-286
[5]  
DALY S A, 1991, British Journal of Pharmacology, V104, p60P
[6]   D-1-DOPAMINE RECEPTORS AND THE TOPOGRAPHY OF UNCONDITIONED MOTOR BEHAVIOR - STUDIES WITH THE SELECTIVE, FULL EFFICACY BENZAZEPINE D-1-AGONIST SKF-83189 [J].
DALY, SA ;
WADDINGTON, JL .
JOURNAL OF PSYCHOPHARMACOLOGY, 1992, 6 (01) :50-60
[7]   A68930 - A POTENT AGONIST SELECTIVE FOR THE DOPAMINE-D1 RECEPTOR [J].
DENINNO, MP ;
SCHOENLEBER, R ;
MACKENZIE, R ;
BRITTON, DR ;
ASIN, KE ;
BRIGGS, C ;
TRUGMAN, JM ;
ACKERMAN, M ;
ARTMAN, L ;
BEDNARZ, L ;
BHATT, R ;
CURZON, P ;
GOMEZ, E ;
KANG, CH ;
STITTSWORTH, J ;
KEBABIAN, JW .
EUROPEAN JOURNAL OF PHARMACOLOGY, 1991, 199 (02) :209-219
[8]  
Finny D.J., 1971, PROBIT ANAL, P8
[9]  
IORIO LC, 1983, J PHARMACOL EXP THER, V226, P462
[10]  
JOHNSON KB, 1992, J PHARMACOL EXP THER, V262, P855