A comparison of some extra-renal effects of spironolactone and canrenone. 1979

G J Huston, and E A Al-Dujaili

1 Measurement of changes in trans-mural rectal potential difference (t.m.r.p.d.) and plasma aldosterone levels have been used in a comparison of the extra-renal activities of spironolactone and its major metabolite canrenone. 2 A characteristic pressure artifact was observed during measurement of t.m.r.p.d. When pressure artifacts were eliminated, there was a log-linear relationship between increasing doses of intravenous aldosterone and maximum increase in t.m.r.p.d. 3 Pre-treatment for 5 days with spironolactone or canrenone produced a similar attenuation of the increase in t.m.r.p.d. produced by infused aldosterone, suggesting that canrenone is the active metabolite of spironolactone in the rectum. This is in contrast to the significantly greater renal activity of spironolactone that has been demonstrated after a similar treatment period. Neither antagonist treatment produced significant changes in pre-infusion plasma aldosterone concentrations. 4 The need for assay of the extra-renal activities of aldosterone antagonists in the assessment of their therapeutic potential is discussed.

UI MeSH Term Description Entries
D008297 Male Males
D008564 Membrane Potentials The voltage differences across a membrane. For cellular membranes they are computed by subtracting the voltage measured outside the membrane from the voltage measured inside the membrane. They result from differences of inside versus outside concentration of potassium, sodium, chloride, and other ions across cells' or ORGANELLES membranes. For excitable cells, the resting membrane potentials range between -30 and -100 millivolts. Physical, chemical, or electrical stimuli can make a membrane potential more negative (hyperpolarization), or less negative (depolarization). Resting Potentials,Transmembrane Potentials,Delta Psi,Resting Membrane Potential,Transmembrane Electrical Potential Difference,Transmembrane Potential Difference,Difference, Transmembrane Potential,Differences, Transmembrane Potential,Membrane Potential,Membrane Potential, Resting,Membrane Potentials, Resting,Potential Difference, Transmembrane,Potential Differences, Transmembrane,Potential, Membrane,Potential, Resting,Potential, Transmembrane,Potentials, Membrane,Potentials, Resting,Potentials, Transmembrane,Resting Membrane Potentials,Resting Potential,Transmembrane Potential,Transmembrane Potential Differences
D008875 Middle Aged An adult aged 45 - 64 years. Middle Age
D011245 Pregnadienes Pregnane derivatives containing two double bonds anywhere within the ring structures.
D011312 Pressure A type of stress exerted uniformly in all directions. Its measure is the force exerted per unit area. (McGraw-Hill Dictionary of Scientific and Technical Terms, 6th ed) Pressures
D012007 Rectum The distal segment of the LARGE INTESTINE, between the SIGMOID COLON and the ANAL CANAL. Rectums
D002192 Canrenone A synthetic pregnadiene compound with anti-aldosterone activity. 11614 R.P.,Aldadiene,Phanurane,SC-9376,R.P., 11614,SC 9376,SC9376
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000450 Aldosterone A hormone secreted by the ADRENAL CORTEX that regulates electrolyte and water balance by increasing the renal retention of sodium and the excretion of potassium. Aldosterone, (+-)-Isomer,Aldosterone, (11 beta,17 alpha)-Isomer
D000451 Mineralocorticoid Receptor Antagonists Drugs that bind to and block the activation of MINERALOCORTICOID RECEPTORS by MINERALOCORTICOIDS such as ALDOSTERONE. Aldosterone Antagonist,Aldosterone Antagonists,Aldosterone Receptor Antagonist,Mineralocorticoid Antagonist,Mineralocorticoid Receptor Antagonist,Aldosterone Receptor Antagonists,Mineralocorticoid Antagonists,Antagonist, Aldosterone,Antagonist, Aldosterone Receptor,Antagonist, Mineralocorticoid,Antagonist, Mineralocorticoid Receptor,Antagonists, Aldosterone,Antagonists, Aldosterone Receptor,Antagonists, Mineralocorticoid,Antagonists, Mineralocorticoid Receptor,Receptor Antagonist, Aldosterone,Receptor Antagonist, Mineralocorticoid,Receptor Antagonists, Aldosterone,Receptor Antagonists, Mineralocorticoid

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