Stereoselective modification of circular dichroism spectra of rat lung beta-adrenoceptor protein preparation by enantiomers of epinephrine

被引:0
作者
Patil, PN [1 ]
Fraundorfer, P [1 ]
Dutta, PK [1 ]
机构
[1] OHIO STATE UNIV,DEPT CHEM,COLUMBUS,OH 43210
关键词
chirality of agonist-efficacy; beta-adrenoceptor; stereoselective change of receptor; epinephrine enantiomers;
D O I
10.1002/(SICI)1520-636X(1996)8:7<463::AID-CHIR1>3.0.CO;2-C
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The presence of beta-adrenoceptor in a rat lung membrane preparation was confirmed by stereoselective competition of enantiomers of epinephrine with labeled iodocyanopindolol. The receptor-rich protein fraction, when combined with the pharmacologically active (-)-epinephrine, exhibited specific changes in the 205-220 nm region of circular dichroism spectra, indicating that the receptor helices may be perturbed. The (+)-epinephrine combined with the lung protein produced little or no change of the spectra. Bovine serum albumin, when combined with either enantiomer of epinephrine, produced nonstereoselective alterations of the spectra. Thus, the data provide important evidence for the higher intrinsic pharmacologic activity of the natural (-)-epinephrine over the unnatural (+)-enantiomer. (C) 1996 Wiley-Liss, Inc.
引用
收藏
页码:463 / 465
页数:3
相关论文
共 14 条
[1]  
ARIENS EJ, 1954, ARCH INT PHARMACOD T, V99, P32
[2]   OPERATIONAL MODELS OF PHARMACOLOGICAL AGONISM [J].
BLACK, JW ;
LEFF, P .
PROCEEDINGS OF THE ROYAL SOCIETY SERIES B-BIOLOGICAL SCIENCES, 1983, 220 (1219) :141-162
[3]  
CUSHNY AR, 1926, BIOL RELATIONS OPTIC, P46
[4]  
DANON A, 1972, J PHARMACOL EXP THER, V182, P295
[5]  
FRAUNDORFER PF, 1994, J PHARMACOL EXP THER, V270, P665
[6]  
FREIFELDER D, 1982, PHYSICAL BIOCH
[7]   COMPARISON OF DISSOCIATION CONSTANTS AND OF RELATIVE EFFICACIES OF SELECTED AGONISTS ACTING ON PARASYMPATHETIC RECEPTORS [J].
FURCHGOTT, RF ;
BURSZTYN, P .
ANNALS OF THE NEW YORK ACADEMY OF SCIENCES, 1967, 144 (A2) :882-+
[8]   EVIDENCE FOR AN ALPHA-II-TYPE HELICAL CONFORMATION FOR BACTERIORHODOPSIN IN THE PURPLE MEMBRANE [J].
GIBSON, NJ ;
CASSIM, JY .
BIOCHEMISTRY, 1989, 28 (05) :2134-2139
[9]  
JOHNSON WC, 1974, ANNU REV PHYS CHEM, V29, P93
[10]  
PATIL PN, 1974, PHARMACOL REV, V26, P323