Abstract
Angiotensin converting enzyme (ACE) inhibitors now have an important place in the treatment of hypertension and congestive cardiac failure1-3. After the introduction of the first angiotensin converting enzyme inhibitor Captopril there has been a profusion of new second and third generation ACE inhibitors4 which is analogous to the multiplicity of beta-blockers. These compounds all act by binding to and inhibiting the active site of the enzyme. However, whether inhibition of plasma ACE is the only determinant of the hypotensive effect of these agents or whether inhibition of tissue ACE is also essential has yet to be determined5. ACE occurs in a great variety of tissues, including the endothelium of blood vessels, the brain, kidney, reproductive organs, gastrointestinal tract, adrenal and lung. It is possible that different ACE inhibitors may have variable bioavailability in different tissues or may have differential effects on individual tissue ACE.
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References
Johnston CI, Arnoida K, Hiwatari M. Angiotensin converting enzyme inhibitors in the treatment of hypertension. Drugs 27: 271 (1984).
Edwards CRW, Padfield PL. Angiotesin converting enzyme inhibitors: past, present and bright future. Lancet 1: 30 (1985).
Brunner HR, Nussberger J, Wacker B. The present molecules of converting enzyme inhibitors. J. ardiovasc Pharmacol 7: 82 (1985).
Wyvratt MJ, Patchett AA. Recent developments in designing angiotensin converting enzyme inhibitors. Medicinal es Rev 5: 483 (1985).
Johnston CI, Jackson B, Cubela R, Arnoida L. Mechanisms for hypotensive action of angiotensin converting enzyme inhibitors. Clin xp Hypertension A6: 551 (1984).
Ondetti MA, Cushman DW. Enzymes of the renin angiotensin system and their inhibitors. Ann ev Biochem 51: 238 (1982).
Fyhrquist F, Tikkanen I, Gronhagen-Riska C, Hurtling L, Hichens M. Inhibititor binding assay for angiotensin converting enzyme. Clin hem 30: 696 (1984).
Jackson B, Cubela R, Johnston CI. Angiotensin converting enzyme (ACE) characterization by 125I-MK351A binding studies of plasma and tissue ACE during variation of salt status in the rat. J. Hypertension 4: 759 (1986).
Johnston CI, Jackson B, Cubela R, Larmour I, Arnoida L. Evaluation of angiotensin converting enzyme (ACE) in the pharmacokinetics and pharmacodynamics of ACE inhibitors. J. Cardiovasc harmacol 9(suppl 1):S9 (1986).
Jackson B, Cubela R, Johnston CI. Angiotensin converting enzyme measurement in human serum using radioinhibitor ligand binding. Aust Expt Biol & Med Sci 64: 149 (1986b).
Jackson B, Cubela R, Johnston CI. Angiotensin converting enzyme inhibitors: measurement of relative inhibitory potency and serum drug levels by radioinhibitor binding displacement assay. J. ardiovasc Pharmacol 9: 699 (1987).
Jackson B, Cubela R, Johnston CI. Measurement of angiotensin converting enzyme inhibitors in serum by radioinhibitor binding displacement assay. Biochem harmacol 36: 1357 (1987).
Gronhagen-Riska C, Tikkanen I, Fyhrquist F. Competitive inhibitor binding assay (CIBA) of Captopril and other ACE inhibitors. Clin hemica Acta 162: 53 (1987).
Chai SY, Mendelsohn FAO, Paxinos G. Angiotensin converting enzyme in rat brain visualized by quantitative in vitro autoradiography. Neuroscience 20: 615 (1987).
Johnston CI, Cubela R, Sakaguchi K, Jackson B. Angiotensin converting enzyme inhibition in plasma and tissues. Clin xpt Hypertension A9: 307 (1987).
Jackson B, Cubela R, Sakaguchi S, Johnston CI. Pharmacokinetics of angiotensin converting enzyme inhibitor in tissue following oral lisinopril: Studies in the rat using quantitative radioinhibitor binding. Clin amp; Exp Pharmac & Physiol 14: 343 (1987).
Johnston CI, Cubela R, Jackson B. Inhibitory potency and plasma drug levels of angiotensin converting enzyme inhibitors in the rat. Clin & Exp harmac & Physiol 1988 (in press).
Cushman DW, Cheung HS. Spectrophotometry assay and properties of the angiotensin converting enzyme of rabbit lung. Biochem harmacol 20: 1637 (1971).
Unger T, Kaufmann-Buhler I, Scholkens B, Ganten D. Brain converting enzyme inhibition: a possible mechanism for the antihypertensive action of Captopril in spontaneously hypertensive rats. Eur Pharmacol 70: 467 (1981).
Cohen ML, Jurz KD. Angiotensin converting enzyme inhibition in tissues from spontaneously hypertensive rats after treatment with Captopril or MK421. J. harmacol Exp Ther 220: 63 (1982).
Jackson B, Cubela R, Johnston CI. Inhibiton of tissue angiotensin converting enzyme by Perindopril: invivo assessment in the rat using radioinhibitor binding displacement. J. harmac & Exp Therap 1988 (in press).
Sakaguchi K, Chai SY, Jackson B, Johnston CI, Mendelsohn FAO. Blockade of angiotensin converting enzyme inhibitor in circumventricular organs of the brain after oral lisinopril administration demonstrated by quantitative in vitro autoradiography. Clin amp; Exp Pharm & Physiol 14: 155 (1982).
Sakaguchi K, Chai SY, Jackson B, Johnston CI, Mendelsohn FAO. Inhibition of tissue angiotensin converting enzyme: Quantitation by autoradiography. Hypertension 1988 (in press).
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© 1989 Plenum Press, New York
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Johnston, C.I., Jackson, B., Cubela, R., Sivell, D., Kozhuki, M. (1989). Pharmacokinetics of Angiotensin Converting Enzyme Inhibitors in Plasma and Tissue Using Radioinhibitor Binding and Displacement Assays. In: Abe, K., Moriya, H., Fujii, S. (eds) Kinins V. Advances in Experimental Medicine and Biology, vol 247 A. Springer, Boston, MA. https://doi.org/10.1007/978-1-4615-9543-4_5
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DOI: https://doi.org/10.1007/978-1-4615-9543-4_5
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