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Otorhinolaryngologic Diseases

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Small molecule drug

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PBPs(Bacterial penicillin-binding protein)	1

SCH 34826, i.e., (S)-N-(N-(2,2[(2,2-dimethyl-1,3-dioxolan-4- yl)methoxy]-2-oxo-1-(phenyl-methyl)ethyl)-phenylalanyl)-beta-alanine, is a potent and selective inhibitor of neutral endopeptidase 24.11 (NEP), an enzyme that degrades the atrial natriuretic peptide (ANP). The effects of SCH 34826 on hypertension and left ventricular hypertrophy (LVH) in spontaneously hypertensive rats (SHRs) were evaluated following 1 month of treatment by measuring the blood pressure, cardiac weight, and left ventricular fibrosis. Adult SHRs were treated with SCH 34826 at 10, 30, or 100 mg/kg given orally twice daily or with vehicle. The systolic blood pressure (SBP) and heart rate (HR) were recorded weekly by the tail-cuff method. Cardiac structural damage was determined by morphometric analysis. Over the dose range examined, the drug produced no significant changes in either blood pressure or heart rate. Despite the lack of antihypertensive activity, SCH 34826 at 100 mg/kg reduced both the cardiac mass (-10%) and the amount of fibrotic tissue present in the left ventricle (-42%). These data indicate that chronic inhibition of NEP by SCH 34826 interacts with mechanisms underlying myocardial hypertrophy and cardiac remodeling.

01 Dec 1991·Journal of Hypertension

Chronic inhibition of neutral endopeptidase reduces left ventricular hypertrophy without changing blood pressure in spontaneously hypertensive rats

Article

Author: Forlani, Angelo ; Monopoli, Angela ; Ongini, Ennio

The orally active neutral endopeptidase inhibitors SCH 34826 and SCH 42495 reduced left ventricular hypertrophy without changing the blood pressure of spontaneously hypertensive rats.The relevance of these results are discussed with regard to the role of (1) nonhemodynamic factors in the pathogenesis of the hypertrophy and (2) atrial natriuretic peptide in controlling the hypertrophy.

01 Jan 1991·Therapeutic Drug MonitoringQ3 · MEDICINE

Simple Measurement of Isepamicin, a New Aminoglycoside Antibiotic, in Guinea Pig and Human Plasma, Using High-Performance Liquid Chromatography with Ultraviolet Detection

Q3 · MEDICINE

Article

Author: Dionisotti, Silvio ; Scaglione, Franco ; Ongini, Ennio ; Bamonte, Francesco

Isepamicin, the 1-N-(S-alpha-hydroxy-beta-aminopropionyl) derivative of gentamicin B, is a new aminoglycoside antibiotic, which not only has most of the properties of amikacin but also is effective against several amikacin-resistant strains of bacteria. The drug was assayed in guinea-pig and human plasma with a high-performance liquid chromatographic procedure using precolumn derivatization with 1-fluoro-2,4-dinitrobenzene and ultraviolet detection. Linearity was established over the range 0.5-40 micrograms/ml using 50 microliters of plasma. Accuracy has a mean relative error of less than 3% and precision a mean coefficient of variation of 5%. Isepamicin was determined without interference from plasma constituents or other drugs commonly prescribed during aminoglycoside therapy. This procedure correlates well with radioimmunoassay and can be used either in experimental studies or therapeutic monitoring of plasma levels.

100 Deals associated with Schering-Plough SpA

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100 Translational Medicine associated with Schering-Plough SpA

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Pipeline

Pipeline Snapshot as of 17 Nov 2024

The statistics for drugs in the Pipeline is the current organization and its subsidiaries are counted as organizations,Early Phase 1 is incorporated into Phase 1, Phase 1/2 is incorporated into phase 2, and phase 2/3 is incorporated into phase 3

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