Английская Википедия:7α-Thiospironolactone

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Версия от 13:53, 26 декабря 2023; EducationBot (обсуждение | вклад) (Новая страница: «{{Английская Википедия/Панель перехода}} {{short description|Chemical compound}} {{Drugbox | Verifiedfields = | Watchedfields = | verifiedrevid = | IUPAC_name = (7''R'',8''R'',9''S'',10''R'',13''S'',14''S'',17''R'')-10,13-Dimethyl-7-sulfanylspiro[2,6,7,8,9,11,12,14,15,16-decahydro-1''H''-cyclopenta[''a'']phenanthrene-17,5'-oxolane]-2',3-dione | image = 7α-Thiospironolactone.svg | width = 225px <!--Clinical data--> | trad...»)
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Шаблон:Short description Шаблон:Drugbox

7α-Thiospironolactone (7α-TS; developmental code name SC-24813; also known as deacetylspironolactone) is a steroidal antimineralocorticoid and antiandrogen of the spirolactone group and a minor active metabolite of spironolactone.[1][2] Other important metabolites of spironolactone include 7α-thiomethylspironolactone (7α-TMS; SC-26519), 6β-hydroxy-7α-thiomethylspironolactone (6β-OH-7α-TMS), and canrenone (SC-9376).[1][2][3][4]

Spironolactone is a prodrug with a short terminal half-life of 1.4 hours.[5][6][7] The active metabolites of spironolactone have extended terminal half-lives of 13.8 hours for 7α-TMS, 15.0 hours for 6β-OH-7α-TMS, and 16.5 hours for canrenone, and accordingly, these metabolites are responsible for the therapeutic effects of the drug.[5][6]

7α-TS and 7α-TMS have been found to possess approximately equivalent affinity for the rat ventral prostate androgen receptor (AR) relative to that of spironolactone.[8] The affinity of 7α-TS, 7α-TMS, and spironolactone for the rat prostate AR is about 3.0 to 8.5% of that of dihydrotestosterone (DHT).[8]

7α-TS, via a reactive metabolite formed by 17α-hydroxylase, is a suicide inhibitor of 17α-hydroxylase, and is thought to be involved in the inhibition of 17α-hydroxylase by spironolactone.[9][10][11]

Pharmacokinetics of spironolactone and metabolites[12]
Compound Cmax (ng/mL)
(day 1)		 Cmax (ng/mL)
(day 15)		 AUC (ng•hr/ml)
(day 15)		 t1/2 (hr)
Spironolactone 72 80 231 1.4
Canrenone 155 181 2173 16.5
Шаблон:Abbrlink 359 391 2804 13.8
Шаблон:Abbrlink 101 125 1727 15.0

A study assessed the interaction of spironolactone and 7α-TS with sex hormone-binding globulin and found that they had very low affinity for this carrier protein.[13]

See also

References

Шаблон:Reflist

Further reading

Шаблон:Spironolactone Шаблон:Androgen receptor modulators Шаблон:Mineralocorticoid receptor modulators


Шаблон:Steroid-stub Шаблон:Genito-urinary-drug-stub

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  1. ↑ 1,0 1,1 Шаблон:Cite journal
  2. ↑ 2,0 2,1 Шаблон:Cite journal
  3. ↑ Шаблон:Cite journal
  4. ↑ Шаблон:Cite journal
  5. ↑ 5,0 5,1 Шаблон:Cite journal
  6. ↑ 6,0 6,1 Шаблон:Cite journal
  7. ↑ Шаблон:Cite book
  8. ↑ 8,0 8,1 Шаблон:Cite journal
  9. ↑ Шаблон:Cite journal
  10. ↑ Шаблон:Cite journal
  11. ↑ Шаблон:Cite journal
  12. ↑ Шаблон:Cite journal
  13. ↑ Шаблон:Cite journal
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