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- W2034227949 abstract "Dihydrotestosterone heptanoate (DHT-hp), a seven-carbon fatty acid ester of DHT, was synthesized, and its pharmacokinetics and effects on hypothalamic-pituitary-testicular function were determined in men and pubertal boys. Plasma DHT levels markedly increased 24 h after im injection of DHThp, reached their peak during the first week, and fell to baseline levels after 4–6 weeks. An estimated 43–55% of DHT-hp was converted to DHT 4–6 weeks after injection. Plasma testosterone, estradiol, LH, and FSH levels decreased by 4 days after DHT-hp injection, were lowest during the second week, and returned to baseline values after 4–6 weeks. The LH and FSH responses to GnRH were diminished by chronic administration of DHT-hp to pubertal boys at 3-week intervals for 15 weeks. The affinity of DHT-hp was 100 times less than the affinity of DHT for the human androgen receptor, and no affinity for the estrogen receptor in breast tissue could be demonstrated. Since DHT is a nonaromatizable androgen, and neither DHT nor DHT-hp binds readily to the estrogen receptor, suppression of LH and FSH secretion by this drug probably occurs via an androgen-dependent mechanism. Receptor binding and pharmacokinetic data indicate that unesterified DHT is the active principle. DHT-hp is a useful derivative of DHT, since prompt, predictable, and sustained rises in DHT occur after its administration." @default.
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- W2034227949 date "1987-03-01" @default.
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- W2034227949 title "Dihydrotestosterone Heptanoate: Synthesis, Pharmacokinetics, and Effects on Hypothalamic-Pituitary-Testicular Function*" @default.
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- W2034227949 doi "https://doi.org/10.1210/jcem-64-3-557" @default.
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