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

Research output: Contribution to journalArticlepeer-review

Abstract

The angiotensin converting enzyme (ACE) inhibitor [3H]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 [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 languageEnglish
Pages (from-to)183-5
Number of pages3
JournalBrain Research Bulletin
Volume25
Issue number1
Publication statusPublished - Jul 1990

Keywords

  • Adult
  • Aged
  • Angiotensin-Converting Enzyme Inhibitors
  • Binding Sites
  • Cerebral Cortex
  • Humans
  • In Vitro Techniques
  • Iodine Radioisotopes
  • Kinetics
  • Male
  • Middle Aged
  • Organophosphorus Compounds
  • Proline
  • Temporal Lobe

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