THE ACE INHIBITOR [H-3] SQ29,852 IDENTIFIES A HIGH-AFFINITY RECOGNITION SITE LOCATED IN THE HUMAN TEMPORAL CORTEX

被引:7
作者
BARNES, NM
COSTALL, B
EGLI, P
HOROVITZ, ZP
IRONSIDE, JW
NAYLOR, RJ
WILLIAMS, TJ
机构
[1] SQUIBB INST MED RES,PRINCETON,NJ 08540
[2] UNIV LEEDS,DEPT PATHOL,LEEDS LS2 9JT,W YORKSHIRE,ENGLAND
关键词
Angiotensin coverting enzyme; Human temporal cortex; [!sup]3[!/sup]H]SQ29,852;
D O I
10.1016/0361-9230(90)90273-3
中图分类号
Q189 [神经科学];
学科分类号
071006 ;
摘要
The angiotensin coverting enzyme (ACE) inhibitor [3H]SQ29,852 identified a single high affinity recognition site (defined by 10.0 μM captopril) in the human temporal cortex (pKD 8.62 ± 0.03; Bmax 248 ± 24 fmol mg-1 protein, mean±S.E.M., n = 4). ACE inhibitors and thiorphan competed to a similar level for the [3H]SQ29,852 binding site in the human temporal cortex with a rank order of affinity (pKi values mean ± S.E.M., n = 3), lisinopril (9.49 +- 0.02), captopril (9.16 ±0.08), SQ29.852 (8.58 ± 0.04), epicaptopril (7.09 ± 0.08), fosinopril (7.08 ± 0.05) and thiorphan (6.40 ± 0.04). Since this rank order of affinity is similar to the affinity of these compounds to inhibit brain ACE activity it is concluded that [3H]SQ29,852 selectively labels the inhibitor recognition site of ACE in the human temporal cortex. © 1990.
引用
收藏
页码:183 / 185
页数:3
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