Mexrenone

Mexrenone

Mexrenone

Chemical compound


Mexrenone (code names ZK-32055, SC-25152) is a steroidal antimineralocorticoid of the spirolactone group related to spironolactone that was never marketed.[1][2] It is the lactonic form of mexrenoic acid (mexrenoate), and mexrenoate potassium (SC-26714), the potassium salt of mexrenoic acid, also exists.[3] In addition to the mineralocorticoid receptor, mexrenone also binds to the glucocorticoid, androgen, and progesterone receptors.[4] Relative to spironolactone, it has markedly reduced antiandrogen activity (approximately one-tenth of the antimineralocorticoid dosage equivalent antiandrogen activity of spironolactone).[2] Eplerenone is the 9-11α-epoxy analogue of mexrenone.[5]

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References

  1. Cutler GB, Pita JC, Rifka SM, Menard RH, Sauer MA, Loriaux DL (July 1978). "SC 25152: A potent mineralocorticoid antagonist with reduced affinity for the 5 alpha-dihydrotestosterone receptor of human and rat prostate". The Journal of Clinical Endocrinology and Metabolism. 47 (1): 171–175. doi:10.1210/jcem-47-1-171. PMID 263288.
  2. Cutler GB, Sauer MA, Loriaux DL (April 1979). "SC 25152: a potent mineralocorticoid antagonist with decreased antiandrogenic activity relative to spironolactone". The Journal of Pharmacology and Experimental Therapeutics. 209 (1): 144–146. PMID 430374.
  3. Hofmann LM, Weier RM, Suleymanov OD, Pedrera HA (June 1977). "Mexrenoate potassium: a steroidal aldosterone antagonist and antihypertensive". The Journal of Pharmacology and Experimental Therapeutics. 201 (3): 762–768. PMID 864608.
  4. Szasz G, Budvari-Barany Z (19 December 1990). Pharmaceutical Chemistry of Antihypertensive Agents. CRC Press. pp. 87–. ISBN 978-0-8493-4724-5.
  5. Ménard J (March 2004). "The 45-year story of the development of an anti-aldosterone more specific than spironolactone". Molecular and Cellular Endocrinology. 217 (1–2): 45–52. doi:10.1016/j.mce.2003.10.008. PMID 15134800. S2CID 19701784.

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