Synthesis And Physicochemical Properties Of [19,20-13 C]-17alfa-ethinylestradiol

13C2-17a-ethinylestradiol (13C2-EE2) was synthesized from estrone and 13C2- C2H2-gas to measure the metabolic clearance rate and the plasma concentration of 17a-ethinylestradiol (EE2) in tall girls, who are treated with high dosages of this estrogen. Interesting characteristics determined by (i) MS: the molecular ion m/z 298.183 is the only labelled ion in the spectrum, and by (ii)1H-NMR d(ppm) 2.96 (dd, 1J(13C-H)=249 Hz, 2J(13C-H)=49.6 Hz; 1H; H20) and (iii) 13C-NMR d 88.8(dd, 1J(13C-13C)=166 Hz, 2J(13C-H20)=49.8 Hz; C19); 80.2 (dd, 1J(13C17-13C19)= 73 Hz, 2J(13C17-13C20)=12.3 Hz; C17) and 74.6 (dd, 1J(13C-13C)=166 Hz, 1J(13C-H)= 249 Hz; C20) confirm the synthesis and structure of 13C2-EE2.

Kinetics of cortisol metabolism and excretion: A hypothetic model based on the cumulative urinary radioactivity in eight multiple pituitary deficient patients

A new model is proposed to study the kinetics of [H-3]cortisol metabolism by using urinary data only. The model consists of 5 pools, in which changes of the fractions of dose are given by a system of 5 ordinary differential equations. After i.v. administration of [H-3]cortisol to 8 multiple pituitary deficient (MPD) patients (group I) the urines from each patient were collected in 9-15 portions during the following 3 days. From the urinary data the rate constants of cortisol metabolism were calculated. A published set of urinary data from patients with a normal cortisol metabolism (group II) was used for comparison. The overall half-life of the label in the circulation was 30 min for both groups; the half-life of the label excretion by both groups was 6 h and the time of maximal activity in the main metabolizing pool was 1.8 h in group I and 1.5 h in group II. The 20% of normal cortisol production rate (CPR) in the 8 MPD patients amounted to 7.2 +/- 1.9-mu-mol/(m2*d). Therefore, the low CPR but normal rate constants, i.e. a normal metabolic clearance rate of cortisol, in the MPD patients suggest a sensitive adjustment of the cortisol response in the target organs

Synthesis and Physicochemical Properties of [19,20-13C]-17α-Ethinylestradiol

13C2-17α-ethinylestradiol (13C2-EE2) was synthesized from estrone and 13C2-C2H2-gas to measure the metabolic clearance rate and the plasma concentration of 17α-ethinylestradiol (EE2) in tall girls, who are treated with high dosages of this estrogen. Interesting characteristics determined by (i) MS: the molecular ion m/z 298.183 is the only labelled ion in the spectrum, and by (ii)1H-NMR δ(ppm) 2.96 (dd, 1J(13C-H)=249 Hz, 2J(13C-H)=49.6 Hz; 1H; H20) and (iii) 13C-NMR δ 88.8(dd, 1J(13C-13C)=166 Hz, 2J(13C-H20)=49.8 Hz; C19); 80.2 (dd, 1J(13C17-13C19)= 73 Hz, 2J(13C17-13C20)=12.3 Hz; C17) and 74.6 (dd, 1J(13C-13C)=166 Hz, 1J(13C-H)= 249 Hz; C20) confirm the synthesis and structure of 13C2-EE2.