THE STEREOSPECIFIC EFFECTS OF ISOFLURANE ISOMERS IN-VIVO

被引:79
作者
LYSKO, GS
ROBINSON, JL
CASTO, R
FERRONE, RA
机构
[1] Ohmeda, Pharmaceutical Products Division, Murray Hill, NJ 07974
关键词
ANESTHETIC; RECEPTOR; STEREOISOMER; ISOFLURANE; (RAT);
D O I
10.1016/0014-2999(94)90519-3
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
The anesthetic potency of racemic isoflurane and the optically pure stereoisomers was examined in rats. The (+) isomer was 53% more potent than the (-) isomer (minimum alveolar concentration (MAC) = 1.06 +/- 0.07% vs. 1.62 +/- 0.02%, P < 0.05). MAC for racemic isoflurane was 1.32 +/- 0.03%. Both stereoisomers and the racemic isoflurane produced similar depression of arterial pressure. However, the (+) isomer blunted the cardiovascular response to a painful stimulus to a greater extent than did an equi-MAC dose of the (-) isomer. These are the first data to describe pharmacological differences between stereoisomers of a volatile anesthetic administered in vivo by the conventional route (inhaled) and measuring the clinically relevant index of anesthesia, MAC. These data are consistent with a receptor-mediated anesthetic mechanism by volatile anesthetics.
引用
收藏
页码:25 / 29
页数:5
相关论文
共 16 条
[1]  
BOSNJAK ZJ, 1993, FASEB J, V7, pA707
[2]  
BURT DR, 1985, RECEPTOR BINDING, P53
[3]   VOLATILE ANESTHETICS DEPRESS CALCIUM-CHANNEL BLOCKER BINDING TO BOVINE CARDIAC SARCOLEMMA [J].
DRENGER, B ;
QUIGG, M ;
BLANCK, TJJ .
ANESTHESIOLOGY, 1991, 74 (01) :155-165
[4]   STEREOSPECIFIC EFFECTS OF INHALATIONAL GENERAL ANESTHETIC OPTICAL ISOMERS ON NERVE ION CHANNELS [J].
FRANKS, NP ;
LIEB, WR .
SCIENCE, 1991, 254 (5030) :427-430
[5]   ISOFLURANE ANESTHESIA IS STEREOSELECTIVE [J].
HARRIS, B ;
MOODY, E ;
SKOLNICK, P .
EUROPEAN JOURNAL OF PHARMACOLOGY, 1992, 217 (2-3) :215-216
[6]  
HARRIS B, 1993, J PHARMACOL EXP THER, V265, P1392
[7]   HALOTHANE DEPRESSES D600-BINDING TO BOVINE HEART SARCOLEMMA [J].
HOEHNER, PJ ;
QUIGG, MC ;
BLANCK, TJJ .
ANESTHESIOLOGY, 1991, 75 (06) :1019-1024
[8]   PREPARATION OF THE ISOFLURANE ENANTIOMERS [J].
HUANG, CG ;
ROZOV, LA ;
HALPERN, DF ;
VERNICE, GG .
JOURNAL OF ORGANIC CHEMISTRY, 1993, 58 (26) :7382-7387
[9]  
HUIDOBROTORO JP, 1987, J PHARMACOL EXP THER, V242, P963
[10]  
KOBLIN DD, 1986, ANESTHESIA, P597