Gestonorone acetate explained

Gestonorone acetate, or gestronol acetate, also known as norhydroxyprogesterone acetate, is a progestin of the 19-norprogesterone and 17α-hydroxyprogesterone groups which was developed in the early 1960s but was never marketed.[1] [2] [3] [4] [5] [6] [7] [8] [9] [10] [11] [12] [13] [14] It is the C17α acetate ester of gestronol (17α-hydroxy-19-norprogesterone).

Gestonorone acetate has been found to consistently inhibit ovulation at an oral dosage of 10 mg/day in combination with 50 μg/day oral ethinylestradiol.[15] Weak or no endometrial effects were observed at an oral dosage of 100 mg/day, basal vacuoles appeared at 130 to 140 mg/day, and full endometrial secretory transformation occurred at 220 mg/day.[16]

See also

Notes and References

  1. Noguchi S . Steroids. XX. Hydrolysis of steroidal esters by malt enzyme. 1. Selective hydrolysis of steroidal acetates. Yakugaku Zasshi. 81. 3. 1961. 369–373. 0031-6903. 10.1248/yakushi1947.81.3_369. free.
  2. Noguchi S . Steroids. XXIII Hydrolysis of steroidal esters by malt enzyme. 4. Synthesis of 17α,19-dihydroxyprogesterone and 17α-hydroxy-19-norprogesterone. Yakugaku Zasshi. 81. 3. 1961. 381–384. 0031-6903. 10.1248/yakushi1947.81.3_381. free.
  3. Dorfman RI, Kincl FA . Steroid anti-estrogens. Steroids. 1. 2. 1963. 185–209. 0039-128X. 10.1016/S0039-128X(63)80136-1.
  4. Suchowsky GK . Pregnancy-maintaining effect of synthetic progestogens in the rat . Acta Endocrinologica . 42 . 4 . 533–536 . April 1963 . 13979052 . 10.1530/acta.0.0420533 .
  5. Kalvoda J, Heusler K, Anner G, Wettstein A . Steroids. CXCVI. 19-Norsteroids. III. Synthesis of 19-norprogesterones . Helvetica Chimica Acta . 46 . 1963 . 1017–1029 . 0018-019X . 10.1002/hlca.19630460332.
  6. Junkmann K . [Experimental viewpoints in the testing of synthetic gestagens] . Deutsche Medizinische Wochenschrift . 88 . 13 . 629–638 . March 1963 . 13958089 . 10.1055/s-0028-1111990 . 260098023 .
  7. Kincl FA, Dorfman RI . Orally active steroidal ovulation inhibitors in the adult estrus rabbit. Steroids. 2. 5. 1963. 521–525. 0039-128X. 10.1016/0039-128X(63)90029-1.
  8. Suchowsky GK . Inhibition of ovulation by steroids . Journal of the Egyptian Medical Association . 1962-1963 . 1963 . 67–73 . 0013-2411 .
  9. Junkmann . The pharmacology of new gestational and anabolic steroids . Deutsch-Englische Medizinische Rundschau . 1 . 4 . 1962 . 385–399 . 0003-3332 .
  10. Suchowsky GK, Baldratti G . Relationship Between Progestational Activity and Chemical Structure of Synthetic Steroids . The Journal of Endocrinology . 30 . 2 . 159–170 . September 1964 . 14207040 . 10.1677/joe.0.0300159 .
  11. Nevinny-Stickel J . Inhibition of ovulation determined by estimation of pregnanediol excretion . International Journal of Fertility . 9 . 57–67 . 1964 . 14106269 .
  12. Jung H, Peters A . [The effect of various gestagens on the development of the fetus and rate of mortality in animal experiments] . Archiv Fur Gynakologie . 204 . 1 . 68–77 . 1967 . 5630697 . 10.1007/BF00668265 . 22416963 .
  13. Gilbert HG, Phillipps GH, English AF, Stephenson L, Woollett EA, Newall CE, Child KJ . The progestational and anti-estrogenic activities of some novel 11beta-substituted steroids . Steroids . 23 . 4 . 585–602 . April 1974 . 4829347 . 10.1016/0039-128X(74)90010-5 .
  14. Tang RR, Guo CC, Fan BL . Stereoselective asymmetric synthesis and characterization of 17α-acetyoxy-19-nor-progesterone. Journal of Central South University of Technology. 11. 3. 2004. 300–303. 1005-9784. 10.1007/s11771-004-0061-y. 195244927.
  15. Book: Pincus G . The Control of Fertility . 3 September 2013. Elsevier. 978-1-4832-7088-3. 222–.
  16. Book: Nevinny-Stickel J . Gewebs- und Neurohormone. Die gestagene Wirkung von Hydroxy-nor-Progesteronestern bei der Frau. Symposion der Deutschen Gesellschaft für Endokrinologie . The progestational effects of hydroxy-nor-progesterone esters in women. 1962. 248–255. Springer . 10.1007/978-3-642-86860-3_27. Nach oraler Verabreichung von 100 mg des Hydroxy-nor-ProgesteronAcetats sah man nur schwache oder noch keine gestagene Wirkung am Endometrium (Abb. 3). Nach der oralen Dosis von 130- 140 mg traten basale Vacuolen auf, nach 220 mg war - außer bei einer Patientin mit individuell geringerer Ansprechbarkeit des Endometriums (2) - eine volle sekretorische Umwandlung erreicht: [...]. 978-3-540-02909-0.

This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "Gestonorone acetate".

Except where otherwise indicated, Everything.Explained.Today is © Copyright 2009-2024, A B Cryer, All Rights Reserved. Cookie policy.