Drugs online research references
Biochem Biophys Res Commun. 1990 Feb 28;167(1):310-6.
A deeply recessed active site in angiotensin-converting enzyme is indicated from the binding characteristics of biotin-spacer-inhibitor reagents.
Bernstein KE, Welsh SL, Inman JK.
Department of Pathology, Emory University, Atlanta, GA 30322.
Two biotinylated derivatives of the angiotensin-converting enzyme (ACE) inhibitor, lisinopril, were synthesized. Compounds BL11 (epsilon-biotinamidocaproyl-lisinopril) and BL19 (epsilon-biotinamidocaproyl-beta-alanyl-beta-alanyl-lisinopril) have, respectively, 11 and 19 atoms of spacing structure between the biotin and the inhibitor moieties. Both compounds were found to be potent inhibitors of mouse kidney ACE, but they lost this ability in the presence of streptavidin in free solution. However, BL19 (but not BL11), when complexed to ACE, retained enough residual binding strength for streptavidin to allow the complex to be specifically removed from solution by streptavidin-agarose beads. It was thus possible to employ BL19 for the affinity isolation of ACE from crude mixtures. These results indicate that the bound determinant of lisinopril must lie at least 11 A below the outer surface of the ACE molecule.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=2155615&dopt=Abstract
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Eur J Pharmacol. 1990 Mar 13;178(1):79-83.
Converting enzyme inhibition and vascular prostacyclin synthesis: effect of kinin receptor antagonism.
Hoffmann G, Pietsch R, Gobel BO, Weisser B, Bonner G, Vetter H, Dusing R.
Medizinische Universitats-Poliklinik, Bonn, F.R.G.
The effects of angiotensin I-converting enzyme (ACE) inhibitors and bradykinin (BK) on prostacyclin (PGI2) production in isolated arterial tissue were investigated. Rings of rat abdominal aorta were incubated in Krebs-Ringer bicarbonate buffer and PGI2 generation was assessed by the determination of its stable hydrolysis product; 6-keto-PGF1 alpha. The addition of both ACE inhibitors, captopril and lisinopril, and bradykinin resulted in dose-dependent stimulation of PGI2 biosynthesis when the individual substance was added into the incubation buffer at final concentrations between 10(-8) and 10(-5) M. The bradykinin-induced stimulation of PGI2 synthesis was dose dependently inhibited by the BK receptor antagonist, D-Arg[Hyp3, Thi5,8, D-Phe7]BK. The captopril- and lisinopril-induced stimulation of vascular 6-keto-PGF1 alpha production was also significantly decreased when the BK antagonist was added to the incubation medium together with the ACE inhibitors. Our results show that both captopril and lisinopril stimulate PGI2 synthesis in arterial tissue and that this effect may be secondary to changes in the activity of the kinin system.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=2158900&dopt=Abstract
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Nephron. 1990;55 Suppl 1:43-8.
Lisinopril in hypertensive patients with renal function impairment.
de Jong PE, Apperloo AJ, Heeg JE, de Zeeuw D.
Department of Medicine, State University Hospital, Groningen, The Netherlands.
The antihypertensive and renal effects of the angiotensin-converting enzyme inhibitor lisinopril were studied in a group of patients with moderate-to-severe hypertension and impaired renal function. After 12 weeks of treatment, most patients had good blood pressure response to lisinopril monotherapy. During this period, correlations between antihypertensive effect, drug dose, and serum drug level were observed. These correlations were no longer evident after prolonged treatment. During a 1-year follow-up period, the drug dose was lowered gradually without losing antihypertensive effect. Hyperkalemia occurred in one third of the patients. During the 1-year follow-up, the glomerular filtration rate (GFR) decreased in two thirds of the patients and remained stable in the other third. In this latter group, the pretreatment GFR was higher, and the effective renal plasma flow had increased, whereas in the patients with a decreased GFR no renal vasodilation had occurred during lisinopril therapy. Thus, lisinopril is an effective antihypertensive drug for patients with impaired renal function. The dose should be adjusted to the pretreatment GFR, and a decrease in dosage should be considered with prolonged treatment.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=2161083&dopt=Abstract
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