Pub. Date : 1993 Oct
PMID : 8242249
9 Functional Relationships(s)Download |
Sentence | Compound Name | Protein Name | Organism |
| 1 | Pharmacological profile of valsartan: a potent, orally active, nonpeptide antagonist of the angiotensin II AT1-receptor subtype. | Valsartan | angiotensinogen | Rattus norvegicus |
| 2 | The pharmacological profile of valsartan, (S)-N-valeryl-N-([2"-(1H-tetrazol-5-yl)biphenyl-4-yl]-methyl)-vali ne, a potent, highly selective, and orally active antagonist at the angiotensin II (AII) AT1-receptor, was studied in vitro and in vivo. | Valsartan | angiotensinogen | Rattus norvegicus |
| 3 | The pharmacological profile of valsartan, (S)-N-valeryl-N-([2"-(1H-tetrazol-5-yl)biphenyl-4-yl]-methyl)-vali ne, a potent, highly selective, and orally active antagonist at the angiotensin II (AII) AT1-receptor, was studied in vitro and in vivo. | Valsartan | angiotensinogen | Rattus norvegicus |
| 4 | Valsartan competed with [125I]-AII at its specific binding sites in rat aortic smooth muscle cell membranes (AT1-receptor subtype) with a Ki of 2.38 nM, but was about 30,000 times less active in human myometrial membranes (AT2-receptor subtype). | Valsartan | angiotensinogen | Rattus norvegicus |
| 5 | In rabbit aortic rings incubated for 5 min with valsartan, at concentrations of 2, 20 and 200 nM, the concentration-response curve of AII was displaced to the right and the maximum response was reduced by 33%, 36% and 40%, respectively. | Valsartan | angiotensinogen | Rattus norvegicus |
| 6 | In bovine adrenal glomerulosa, valsartan inhibited AII-stimulated aldosterone release without affecting the maximum response (pA2 8.4). | Valsartan | angiotensinogen | Rattus norvegicus |
| 7 | In the pithed rat, oral administration of valsartan (10 mg kg-1) shifted the AII-induced pressor response curves to the right, without affecting responses induced by the electrical stimulation of the sympathetic outflow or by noradrenaline. | Valsartan | angiotensinogen | Rattus norvegicus |
| 8 | Animals treated with valsartan 24 h before pithing also showed significant inhibition of the response to AII. | Valsartan | angiotensinogen | Rattus norvegicus |
| 9 | These results demonstrate that valsartan is a potent, specific, highly selective antagonist of AII at theAT1-receptor subtype and does not possess agonistic activity. | Valsartan | angiotensinogen | Rattus norvegicus |