SC-8109 explained

SC-8109 is a steroidal antimineralocorticoid of the spirolactone group which was never marketed.[1] [2] It is a potent antagonist of the mineralocorticoid receptor and is more potent than the related drug SC-5233 (of which SC-8109 is the 19-nor analogue).[3] However, SC-8109 was found to have relatively low oral bioavailability and potency,[4] though it nonetheless produced a mild diuretic effect in patients with congestive heart failure. Spironolactone (SC-9420; Aldactone), another spirolactone, followed and had both good oral bioavailability and potency, and was the first antimineralocorticoid to be marketed.[5]

In addition to its antimineralocorticoid activity, SC-8109 shows potent progestogenic activity, with similar potency relative to that of progesterone.[6] Its analogue, SC-5233, possesses similar but less potent progestogenic activity. In addition, SC-5233 has been assessed and found to possess some antiandrogenic activity, antagonizing the effects of testosterone in animals, and SC-8109 may as well.[7]

Relative affinities (%) of SC-8109 and related steroids[8]
Compound
100 3–10 <1 <1 3–10 ? ?
SC-8109 191 25–50 <1 <1 15–25 ? ?
Values are percentages (%). Reference ligands (100%) were progesterone for the, testosterone for the, estradiol for the, for the, and aldosterone for the .

See also

Notes and References

  1. Book: Bentley PJ . The Adrenal Gland . Endocrine Pharmacology: Physiological Basis and Therapeutic Applications. https://books.google.com/books?id=W6M9AAAAIAAJ&pg=PA160. 1980. CUP Archive. 978-0-521-22673-8. 160–.
  2. Book: Buchborn E, Bock KD . Diuresis and Diuretics / Diurese und Diuretica: An International Symposium Herrenchiemsee, June 17th–20th, 1959 Sponsored by CIBA / Ein Internationales Symposium Herrenchiemsee, 17.–20. Juni 1959 Veranstaltet mit Unterstützung der CIBA. 14 December 2013. Springer-Verlag. 978-3-642-49716-2. 224,261.
  3. Book: Ussing HH, Kruhoffer P, Thaysen HJ, Thorn NH . The Alkali Metal Ions in Biology: I. The Alkali Metal Ions in Isolated Systems and Tissues. II. The Alkali Metal Ions in the Organism. 8 March 2013. Springer Science & Business Media. 978-3-642-49246-4. 418–.
  4. Book: Brandon ML . Corticosteroids in medical practice. 1 January 1962. Thomas. 9780398002152.
  5. Book: Cokkinos DV . Introduction to Translational Cardiovascular Research. 6 November 2014. Springer. 978-3-319-08798-6. 61–.
  6. Book: Dorfman RI . Steroidal Activity in Experimental Animals and Man. 5 December 2016. Elsevier Science. 978-1-4832-7299-3. 371–.
  7. Kagawa CM, Sturtevant FM, Van Arman CG . Pharmacology of a new steroid that blocks salt activity of aldosterone and desoxycorticosterone . The Journal of Pharmacology and Experimental Therapeutics . 126 . 2 . 123–130 . June 1959 . 13665517 . [SC-5233] (total dose of 5 mg/rat) partially blocked the effects of testosterone propionate on the seminal vesicles and prostate in similar animals. .
  8. Book: Raynaud JP, Ojasoo T, Bouton MM, Philibert D . Drug Design. Receptor Binding as a Tool in the Development of New Bioactive Steroids. Medicinal Chemistry: A Series of Monographs . 1979. 11 . 169–214. Academic Press . 10.1016/B978-0-12-060308-4.50010-X. 9780120603084. https://books.google.com/books?id=bhAlBQAAQBAJ&pg=PA169.

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