1045-29-0Relevant articles and documents
Pharmacokinetics and pharmacodynamics of anordrin (2α,17α-diethynyl-A-nor-5α-androstane-2β,17β-diol diproprionate)
Chatterton, Robert T.,Kowalski, Wlodzimierz,Lu, Yu-cai,Peters, Albert J.
, p. 217 - 223 (1994)
In order to determine the pharmacokinetics of anordrin a dose of 0.2 mg/kg of anordrin was administered i.v. to 5-cynomolgus monkeys; the same monkeys received the same dose i.m. at a later date.An additional 3 monkeys received 1.0 mg/kg of anordrin i.m.After administration of the compound, the dipropionate esters of anordrin were rapidly hydrolyzed to the dihydroxy parent compound, anordiol.After i.v. administration, anordin had a mean residence time (MRT) of 5.0 +/- (SE) min. Anordiol formed from anordrin had an MRT of 139 +/- 27 (SE) min.The metabolic clearance rates (MCR) of anordin and anordiol were 55 and 34 mL/min*kg, respectively.The apparent volume of distribution at steady state (Vss) for anordrin was 276 mL/kg, 7.5percent of body weight of the animals; anordrin had a much larger Vss of 4460 mL/kg.The MRT of anordiol after i.m. administration of 1.0 mg/kg of anordrin was 26.3 days.An average of 44percent of the dose appeared in urine regardless of the route of administration or dose.The MRT values of total radioactivity were the same when calculated from serum or urine after an i.v. dose, but after i.m. administration, values from urine were approximately 60percent of that calculated from serum, indicating that products appearing in urine had a shorter MRT than products appearing primarily in feces.A separate group of monkeys was given anordrin i.m. in doses ranging from 0.1 to 0.4 mg/kg on the first day of menses.The regression of length of menstrual cycle on dose was significant (P=0.004).Control cycle length was 30 days and the response was linear to 76 days with the maximum dose given. Keywords: anordrin, contraceptive; pharmacokinetics; pharmacodynamics; monkey
ASYMMETRIC SYNTHESIS AND USES OF COMPOUNDS IN DISEASE TREATMENTS
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, (2019/03/17)
The present application discloses, among other things, asymmetric synthesis a diastereomeric compound of formula (I) (e.g., α-anordrin) or salt thereof. Also provided are methods and compositions for treatment of estrogen deficiency as well as preventing or reducing an estrogen deficiency symptom using a diastereomeric compound of formula (I) (e.g., α-anordrin) or salt thereof alone or in combination with at least one additional agent. Further provided are methods and compositions for reducing a side effect of an additional agent in the context of combination therapy with a diastereomeric compound of formula (I) (e.g., α-anordrin) or salt thereof.
