C-10-O-EQ-N-(4-AZIDO-5-(125)IODO SALICYLOYL)-BETA-ALANYL-BETA ALANYL RYANODINE (AZ-BETA-AR), A NOVEL PHOTO-AFFINITY LIGAND FOR THE RYANODINE BINDING-SITE

被引：9
作者：
BIDASEE, KR
BESCH, HR
KWON, S
EMMICK, JT
BESCH, KT
GERZON, K
HUMERICKHOUSE, RA
机构：
[1] Department of Pharmacology and Toxicology, Indiana University School of Medicine, Indianapolis, Indiana, 46202-5120
来源：
JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS | 1994年 / 34卷 / 01期
关键词：
SARCOPLASMIC RETICULUM CALCIUM-RELEASE CHANNEL RYANODINE RECEPTOR; C(10)-O(EQ)-N-(4-AZIDO-5-(125)IODO SALICYLOYL)-BETA-ALANYL RYANODINE (AZ-BETA-AR);
D O I：
10.1002/jlcr.2580340106
中图分类号：
Q5 [生物化学];
学科分类号：
071010 ; 081704 ;
摘要：
A high affinity, photoactivatable, radio-iodinated ligand for the ryanodine binding site(s) of the sarcoplasmic reticulum calcium-release channel, C-10-O(e)-N-(4-azido-5-iodo-125 salicyloyl)-beta-alanyl-beta-alanyl ryanodine (Az-betaAR), was synthesized at a specific activity of 1400mCi/mmol. Prepared by condensing the versatile synthon, N-(4-azido-5-iodo-125 salicyloyl)-beta-alanine with C-10-O(eq)-beta-alanyl ryanodine, Az-betaAR, like [H-3] ryanodine, does not demonstrate saturation binding kinetics. 127Az-betaAR exhibits an IC50 of 27.2 +/- 2 x 10(-9) M (mean +/- SD) compared to ryanodine's 6.2 +/- 0.4 x 10(-9) M for the ryanodine receptor/calcium release channel of sarcoplasmic reticulum vesicles isolated from rabbit skeletal muscle.
引用
收藏
页码：33 / 47
页数：15
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