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

Journal Article · Sun Jul 01 00:00:00 EDT 1990 · Brain Research Bulletin; (USA)

DOI:https://doi.org/10.1016/0361-9230(90)90273-3· OSTI ID:6143111

Barnes, N M; Costall, B; Egli, P; Horovitz, Z P; Ironside, J W; Naylor, R J; Williams, T J ^[1]

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1. Univ. of Bradford, West Yorkshire (England)

The angiotensin converting enzyme (ACE) inhibitor ({sup 3}H)SQ29,852 identified a single high affinity recognition site (defined by 10.0 microM 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 ({sup 3}H)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 ({sup 3}H)SQ29,852 selectively labels the inhibitor recognition site of ACE in the human temporal cortex.

• OSTI ID: 6143111
• Journal Information: Brain Research Bulletin; (USA), Vol. 25:1; ISSN 0361-9230
• Country of Publication: United States
• Language: English

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550201* - Biochemistry- Tracer Techniques