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 language | English |
|---|---|
| Pages (from-to) | 183-5 |
| Number of pages | 3 |
| Journal | Brain Research Bulletin |
| Volume | 25 |
| Issue number | 1 |
| Publication status | Published - Jul 1990 |
Keywords / Materials (for Non-textual outputs)
- 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