| 靶点: |
NEP |
| 体内研究: |
In conscious deoxycorticosterone acetate (DOCA)/salt hypertensive rats, 300 μmol/kg, i.v., of SQ28603 significantly lowers mean arterial pressure (MAP) from 177±12 to 154±8 mm Hg and increases urinary cyclic guanosine monophosphate (GMP) excretion from 204±70 to 1,068±326 pmol/kg/min within 2 h. SQ28603 also significantly reduces NEP activity by 95% in the kidneys (1.28±0.08 vs. 18.35±0.61 μmol/min after SQ28603 and vehicle respectively) and by 77% in the lungs (0.29±0.03 vs. 0.92±0.14 μmol/kg after SQ28603 and vehicle, respectively). In conclusion, inhibition of NEP activity by SQ28603 significantly decreases MAP and increases plasma ANP concentrations and urinary excretion of cyclic GMP in conscious DOCA/salt hypertensive rats. The potent neutral endopeptidase inhibitor SQ28603 significantly increases excretion of sodium from 4.9±2.3 to 14.3±2.1 muequiv./min and cyclic 3',5'-guanosine monophosphate from 118±13 to 179±18 pmol/min after intravenous administration of 300 μmol/kg (approximately 80 mg/kg) in conscious female cynomolgus monkeys. |
| 参考文献: |
1. Seymour AA, et al. Antihypertensive and renal activity of SQ 28,603, an inhibitor of neutral endopeptidase. J Cardiovasc Pharmacol. 1991 Feb;17(2):296-304. 2. Seymour AA, et al. Evaluation of SQ 28,603, an inhibitor of neutral endopeptidase, in conscious monkeys. Can J Physiol Pharmacol. 1991 Oct;69(10):1609-17. |
| 保存条件: |
-20℃ |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
3.74 ml |
18.702 ml |
37.405 ml |
| 5 mM |
0.748 ml |
3.74 ml |
7.481 ml |
| 10 mM |
0.374 ml |
1.87 ml |
3.74 ml |
| 50 mM |
0.075 ml |
0.374 ml |
0.748 ml |
|
| 注意: |
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