PMID: 2483426Jan 1, 1989Paper

Inhibition of converting enzyme in brain tissue and cerebrospinal fluid of rats following chronic oral treatment with the converting enzyme inhibitors ramipril and Hoe 288.

Journal of Cardiovascular Pharmacology
P GohlkeT Unger

Abstract

A direct central nervous system (CNS)-related component of the cardiovascular actions of converting enzyme (CE) inhibitors will be governed by the ability of these drugs to gain access to the brain. We investigated the inhibitory effect of the two CE inhibitors ramipril and Hoe 288 on CE activity in different brain regions and in the cerebrospinal fluid of rats. One-week oral gavage treatment with ramipril (10 mg/kg/day) and Hoe 288 (10 mg/kg/day) resulted in a marked inhibition of CE activity in the brain cortex (90 and 91%, respectively), the hypothalamus (78 and 82%, respectively), and in the brainstem (67 and 66%, respectively). The complete blockade of plasma CE activity was paralleled by a 84% inhibition of CE activity in cerebrospinal fluid. Both CE inhibitors failed significantly to inhibit CE activity in the striatum. Our results demonstrate that the CE inhibitors Hoe 288 and ramipril were able to pass the blood-brain barrier (BBB) to inhibit central CE activity. The penetration of CE inhibitors into the CNS appears to depend on the lipophilicity of the drugs and on the mode of drug application. The possibility that an inhibition of CE activity in circumventricular organs outside the BBB such as the subfornical organ a...Continue Reading

Citations

Aug 1, 1997·Pharmacology, Biochemistry, and Behavior·N E Rowland, M J Fregly
Dec 29, 2011·Age·Vincenzo SolfrizziUNKNOWN Italian Longitudinal Study on Aging Working Group
Oct 1, 1994·Hypertension·D R AllanN K Hollenberg
Apr 15, 2004·Hypertension Research : Official Journal of the Japanese Society of Hypertension·Shinji TakaiMizuo Miyazaki
Aug 18, 2020·Neurotherapeutics : the Journal of the American Society for Experimental NeuroTherapeutics·Nora HegazyAhmed Fahmy

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