Drugs online research references
Nucl Med Commun. 2000 Apr;21(4):325-31.
Aspirin renography in the diagnosis of renovascular hypertension: a comparative study with captopril renography.
Maini A, Gambhir S, Singhal M, Kher V.
Department of Nuclear Medicine, Sanjay Gandhi Postgraduate Institute of Medical Sciences, Lucknow, India. amaini
J Med Chem. 1988 Jan;31(1):204-12.
(Phosphinyloxy)acyl amino acid inhibitors of angiotensin converting enzyme (ACE). 1. Discovery of (S)-1-[6-amino-2-[[hydroxy(4-phenylbutyl)phosphinyl]oxy]-1-oxohexyl]-L -proline a novel orally active inhibitor of ACE.
Karanewsky DS, Badia MC, Cushman DW, DeForrest JM, Dejneka T, Loots MJ, Perri MG, Petrillo EW Jr, Powell JR.
Squibb Institute for Medical Research, Princeton, New Jersey 08543-4000.
The synthesis of a series of orally active, phosphinyloxyacyl proline inhibitors of angiotensin converting enzyme (ACE) is described. The in vitro and in vivo ACE inhibitory activities are reported for each compound. The structure-activity relationship for this series of compounds in relation to the carboxyalkyl dipeptide ACE inhibitors as well as other types of hydroxyphosphinyl-containing ACE inhibitors (e.g., the corresponding nitrogen and carbon isosteres) is discussed. Within an isosteric series of phosphorus-containing inhibitors based on the lysylproline terminal dipeptide sequence, only the phosphonates (oxygen isosteres) show a high level of oral activity. Optimum potency and oral activity in the phosphonate series occurs with the (phenylbutyl)- and n-hexylphosphonate side chains. An aminobutyl side chain in the P1' residue is an absolute requirement for full expression of oral activity. The most potent of these compounds, 8b (SQ 29,852), has intravenous and oral activities superior in potency to those of captopril in the normotensive rat.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=3336020&dopt=Abstract
Circ Shock. 1987;23(1):1-5.
Acute hemorrhage reduces angiotensin converting enzyme activity in conscious sheep.
Cameron V, Espiner EA, Nicholls MG, Sinclair LM.
Department of Endocrinology, Princess Margaret Hospital, Christchurch, New Zealand.
When levels of plasma angiotensin converting activity (ACE) were measured in 11 sheep undergoing a 15 ml/kg hemorrhage, levels before hemorrhage (5.7 +/- 0.5 nmol/min/ml) fell significantly at 120 min (3.7 +/- 0.6 nmol/min/ml) and 150 min (3.4 +/- 0.5 nmol/min/ml) after hemorrhage (P less than 0.01). Plasma ACE activity remained constant in ten control sheep studied under the same conditions but not hemorrhaged. The time course of the fall in plasma ACE activity was then studied in an additional four sheep undergoing 15 ml/kg hemorrhage, which reduced mean arterial pressure by 25% at 10 min after hemorrhage. Plasma ACE activity was variable for 60 min post-hemorrhage, but then fell to levels significantly lower than baseline values at 150 min (P less than 0.05). The decrease in plasma ACE activity associated with hemorrhage was small when compared to the effect of an IV infusion of the ACE inhibitor, Captopril (SQ14225, 28 micrograms/min for 3 hr), which reduced plasma ACE activity in the same sheep to almost undetectable levels. These results show that hemorrhage significantly reduces plasma ACE activity in sheep. However, this effect is small and is unlikely to affect the production of plasma AII following acute hemorrhage.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=2826037&dopt=Abstract
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