Relaxant effect of levcromakalim in isolated human small subcutaneous arteries

被引:6
作者
Husken, BCP
Vroom, MB
Timmenga, EJF
Pfaffendorf, M
VanZwieten, PA
机构
[1] UNIV AMSTERDAM,ACAD MED CTR,DEPT ANAESTHESIOL,1105 AZ AMSTERDAM,NETHERLANDS
[2] UNIV AMSTERDAM,ACAD MED CTR,DEPT PLAST RECONSTRUCT SURG,1105 AZ AMSTERDAM,NETHERLANDS
关键词
levcromakalim; glibenclamide; artery; subcutaneous; (human);
D O I
10.1016/0014-2999(95)00714-8
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
The effect of levcromakalim, an ATP-sensitive K+ channel opener, on isolated subcutaneous arteries from mammary tissues obtained from female patients undergoing reconstructive breast surgery was investigated. The small arteries were preserved in the University of Wisconsin (UW) solution. The contractile responses to K+ and 9,11-dideoxy-11 alpha,9 alpha-epoxy-methano-prostaglandin F-2 alpha (U46619) and the relaxant responses to levcromakalim and to the endothelium-dependent vasodilator, methacholine, in these arteries remained fully intact after preservation in UW solution for at least 5 days. The pD(2) value and maximal relaxation obtained from the concentration-response curve of levcromakalim (n = 7) were 5.78 +/- 0.23 and 81 +/- 6%, respectively. The vasodilator effect of levcromakalim was significantly antagonised by the ATP-sensitive K+ channel blocker, glibenclamide (1 and 3 mu M). In conclusion, isolated human arteries contain ATP-sensitive K+ channels, which can be modulated by K+ channel openers and blockers. Subcutaneous small arteries, as used in our experiments, appear to be very suitable for pharmacological experiments.
引用
收藏
页码:313 / 316
页数:4
相关论文
共 15 条
[1]   EVIDENCE FOR INCREASED MEDIA THICKNESS, INCREASED NEURONAL AMINE UPTAKE, AND DEPRESSED EXCITATION CONTRACTION COUPLING IN ISOLATED RESISTANCE VESSELS FROM ESSENTIAL HYPERTENSIVES [J].
AALKJAER, C ;
HEAGERTY, AM ;
PETERSEN, KK ;
SWALES, JD ;
MULVANY, MJ .
CIRCULATION RESEARCH, 1987, 61 (02) :181-186
[2]   POTASSIUM CHANNEL OPENERS AND OTHER REGULATORS OF K-ATP CHANNELS [J].
CHALLINORROGERS, JL ;
MCPHERSON, GA .
CLINICAL AND EXPERIMENTAL PHARMACOLOGY AND PHYSIOLOGY, 1994, 21 (08) :583-597
[3]   INTRACELLULAR ATP DIRECTLY BLOCKS K+ CHANNELS IN PANCREATIC B-CELLS [J].
COOK, DL ;
HALES, CN .
NATURE, 1984, 311 (5983) :271-273
[4]   CLINICAL-STUDIES WITH THE POTASSIUM CHANNEL ACTIVATOR CROMAKALIM IN NORMOTENSIVE AND HYPERTENSIVE SUBJECTS [J].
DONNELLY, R ;
ELLIOTT, HL ;
MEREDITH, PA ;
REID, JL .
JOURNAL OF CARDIOVASCULAR PHARMACOLOGY, 1990, 16 (05) :790-795
[5]  
EKIN ST, 1993, J HEART LUNG TRANSPL, V12, P624
[6]  
HUSKEN BCP, 1995, BRIT J PHARMACOL, V114, pP35
[7]   CONTRACTILE PROPERTIES OF SMALL ARTERIAL RESISTANCE VESSELS IN SPONTANEOUSLY HYPERTENSIVE AND NORMOTENSIVE RATS [J].
MULVANY, MJ ;
HALPERN, W .
CIRCULATION RESEARCH, 1977, 41 (01) :19-26
[8]   ATP-REGULATED K+ CHANNELS IN CARDIAC-MUSCLE [J].
NOMA, A .
NATURE, 1983, 305 (5930) :147-148
[9]   EFFECT OF PRESERVATION SOLUTION ON RESULTS OF CADAVERIC KIDNEY-TRANSPLANTATION [J].
PLOEG, RJ ;
VANBOCKEL, JH ;
LANGENDIJK, PTH ;
GROENEWEGEN, M ;
VANDERWOUDE, FJ ;
PERSIJN, GG ;
THOROGOOD, J ;
HERMANS, J .
LANCET, 1992, 340 (8812) :129-137
[10]   MOVING TOGETHER - K+ CHANNEL OPENERS AND ATP-SENSITIVE K+ CHANNELS [J].
QUAST, U ;
COOK, NS .
TRENDS IN PHARMACOLOGICAL SCIENCES, 1989, 10 (11) :431-435