| Description |
SCH 42495 is an orally active neutral metalloendopeptidase (NEP) inhibitor with antihypertensive effect. SCH 42495 is the orally active ethylester prodrug of SCH 42354[1].
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| Related Catalog |
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| Target |
NEP[1]
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| In Vitro |
SCH 42354 selectively inhibits hydrolysis of leu-enkephalin and ANF (IC50 of 8.3 and 10.0 nM, respectively) in vitro[1].
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| In Vivo |
SCH 42495 (30 mg/kg; oral gavage; twice daily) causes a significant reduction in the pulmonary vascular remodelling and ventricular hypertrophy in hypoxic rats after 10 days[2]. Treatment with SCH 42495 (30 mg/kg; oral gavage; twice daily) leads to a decrease in cardiovascular remodelling secondary to chronic hypoxia in rats[2]. SCH 42495 (oral doses of 1, 3, or 10 mg/kg) produces significant reductions in blood pressure in DOCA-N a hypertensive rats of 22±6, 43±7, and 62±12 mm Hg, respectively[1]. Animal Model: Hypoxic rats[2] Dosage: 30 mg/kg Administration: Oral gavage; twice daily for 10 days Result: Caused a significant reduction in the pulmonary vascular remodelling and ventricular hypertrophy. Led to a decrease in cardiovascular remodelling secondary to chronic hypoxia.
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| References |
[1]. Watkins RW, et al. Atrial natriuretic factor potentiating and hemodynamic effects of SCH 42495, a new, neutral metalloendopeptidase inhibitor. Am J Hypertens. 1993 May;6(5 Pt 1):357-68. [2]. Thompson JS, et al. Effects of the neutral endopeptidase inhibitor, SCH 42495, on the cardiovascular remodelling secondary to chronic hypoxia in rats. Clin Sci (Lond). 1994 Jul;87(1):109-14.
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