(1) The conceptual framework provides for both the variation in estr ogenic responses in various target organs.
(2) The in vitro metabolism of 7 alpha-methyl-19-nortestosterone (7 alpha-methyl-3-oxo-estr-4-ene-17 beta-ol) was investigated in male rat liver, ventral prostate, and epididymis.
(3) Fifty patients responded to treatment or had stable disease, and 28 did not respond (12 in the ORX and 16 in the ESTR group).
(4) This model of peripheral aromatization was utilized to evaluate in vivo pharmacological parameters of MDL 18,962 (10-(2-propynyl)estr-4-ene-3,17-dione) such as bioavailability of several formulations, time course and dose responses following different routes of drug administration, pharmacokinetics and tissue distribution of [14C]MDL 18,962.
(5) Both 10-[(1R)-1-hydroxyethyl]- and 10-[(1S)-1-hydroxyethyl]estr-4-ene-3,17-dione were oxygenated to 10-(1,1-dihydroxyethyl)estr-4-ene-3,17-dione and isolated following in situ dehydration as 10-acetylestr-4-ene-3,17-dione.
(6) Tissues were homogenized and incubated in vitro with labeled progesterone and 2 different antiovulatories, lynestrenol (17alpha-ethin yl-17beta-hydroxy-estr-4-one) and MK 665 (17alpha-chloroethinyl-19-nor-4 ,9(10)-androstadiene-17beta-ol-3-one).
(7) In contrast, both analogues of 19-hydroxyandrostenedione [10-[(1S)-1-hydroxyethyl]estr-4-ene-3,17-dione (2c) and 10-[(1R)-1-hydroxyethyl]estr-4-ene-3,17-dione (2e)] were converted to the intermediate analogue 3c in a process requiring O2 and either NADH or NADPH.
(8) 32 patients with high-risk pregnancies were treated with 3 X 5 mg of 17alpha-ally1-17beta-hydroxy-estr-4-ene (allylestrenol, Gestanon) daily.
(9) The key reaction in the synthesis of the hapten was the cuprate-mediated 1,4-conjugate addition on 3,3,17,17-bis-ethylenedioxy-5 alpha,10 alpha-oxido-estr-9(11)-ene by the Grignard reagent derived from trimethyl 4-bromoorthobutyrate; this regiospecifically introduces the 11 beta-butanoate function.
(10) All oxidative functions of aromatase, i.e., estrogen production, 19-oxygenated androgen production and 7-ethoxycoumarin deethylation, were inhibited in parallel in placental microsomes from non-smokers by the mechanism-based, time-dependent inactivators (suicide substrates) 10 beta-(2-propynyl)estr-4-ene-3,17-dione and 4-hydroxyandrost-4-ene-3,17-dione.
(11) The peripheral aromatization ([rho]BM) of androstenedione (A) and testosterone (T) was measured before and after administration of the aromatase inhibitor 10-(2 propynyl)estr-4-ene-3,17-dione (MDL-18,962) to five mature female baboons, Papio annubis.
(12) When microsomes were preincubated with the suicide substrates 10 beta-mercapto-estr-4-ene-3,17-dione (10 beta-SHnorA), or 17 beta-hydroxy-10 beta-mercaptoestr-4-ene-3-one (10 beta-SHnorT), it was found that 19-hydroxy-, 19-oxo- and aromatase activities were inhibited in parallel.
(13) The sulfate and phosphate conjugates of 19-nortestosterone (17beta-hydroxy-estr-4-ene-3-one) and ent-19-nortestosterone (ent-17beta-hydroxy-estr-4-ene-3-one) have been synthesized.
(14) Bioassays were conducted to determine various endocrinological properties of two spirolactone derivatives, 4',5'-dihydrospiro-[estr-4-ene-17,2'(3'H)-furan]-3-one (Compound I) and dispiro[cyclopropane-1,6'-estr-4'-ene-17',2"(3"h)-furan]-3'-one (Compound II).
(15) A convenient synthesis of both 5 beta,17 alpha-19-norpregn-20-yne-3 beta,17-diol (1) and 5 beta,17 alpha-19-norpregn-20-yne-3 alpha,17-diol (2) in multigram quantities from estr-4-ene-3,17-dione is reported.
(16) The compound 10-(2-propynyl)-estr-4-ene-3,17-dione is an effective inhibitor of the peripheral aromatization of both androstenedione and testosterone.
(17) The reversal potential of Str-induced current (EStr) was -75 mV, which was close to the K+ equilibrium potential (EK = -76.3 mV).
(18) The change in EStr for a ten fold change in extracellular K+ concentration was 58 mV, indicating that the membrane behaves like a K+ electrode in the presence of Str.
(19) The change of EStr for a ten fold change in extracellular K+ concentration was 58 mV, indicating that the membrane behaves like a K+ electrode in the presence of Str.
(20) The effect of silastic implants containing 0-5000 mcg of 17beta-estr adiol on serum concentrations of luteinizing hormone (LH), follicle stimulating hormone (FSH), prolactin and their relationship to social cues was studied in adult, ovariectomized mice.