The ACE inhibitor [3H]SQ29,852 identifies a high affinity recognition site located in the human temporal cortex

N. M. Barnes; B. Costall; P. Egli; Z. P. Horovitz; J. W. Ironside; R. J. Naylor; T. J. Williams

doi:10.1016/0361-9230(90)90273-3

The ACE inhibitor [³H]SQ29,852 identifies a high affinity recognition site located in the human temporal cortex

N. M. Barnes^*
, B. Costall
, P. Egli
, Z. P. Horovitz
, J. W. Ironside
, R. J. Naylor
, T. J. Williams

^*Corresponding author for this work

Pharmacy

Research output: Contribution to journal › Article › peer-review

Abstract

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 (pK_D 8.62 ± 0.03; B_max 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.

Original language	English
Pages (from-to)	183-185
Number of pages	3
Journal	Brain Research Bulletin
Volume	25
Issue number	1
DOIs	https://doi.org/10.1016/0361-9230(90)90273-3
Publication status	Published - Jul 1990

Keywords

Angiotensin coverting enzyme
Human temporal cortex
[H]SQ29,852

ASJC Scopus subject areas

General Neuroscience

Access to Document

10.1016/0361-9230(90)90273-3

Cite this

@article{f072d62771f7434b9c4ff933c55cb0df,

title = "The ACE inhibitor [3H]SQ29,852 identifies a high affinity recognition site located in the human temporal cortex",

abstract = "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.",

keywords = "Angiotensin coverting enzyme, Human temporal cortex, [H]SQ29,852",

author = "Barnes, \{N. M.\} and B. Costall and P. Egli and Horovitz, \{Z. P.\} and Ironside, \{J. W.\} and Naylor, \{R. J.\} and Williams, \{T. J.\}",

year = "1990",

month = jul,

doi = "10.1016/0361-9230(90)90273-3",

language = "English",

volume = "25",

pages = "183--185",

journal = "Brain Research Bulletin",

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AU - Barnes, N. M.

AU - Costall, B.

AU - Egli, P.

AU - Horovitz, Z. P.

AU - Ironside, J. W.

AU - Naylor, R. J.

AU - Williams, T. J.

PY - 1990/7

Y1 - 1990/7

N2 - 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.

AB - 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.

KW - Angiotensin coverting enzyme

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KW - [H]SQ29,852

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