Switch to
Predicate | Object |
---|---|
rdf:type | |
lifeskim:mentions | |
pubmed:issue |
3
|
pubmed:dateCreated |
1987-3-31
|
pubmed:abstractText |
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 DHT-hp, 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.
|
pubmed:grant | |
pubmed:language |
eng
|
pubmed:journal | |
pubmed:citationSubset |
AIM
|
pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Dihydrotestosterone,
http://linkedlifedata.com/resource/pubmed/chemical/Estradiol,
http://linkedlifedata.com/resource/pubmed/chemical/Gonadotropins, Pituitary,
http://linkedlifedata.com/resource/pubmed/chemical/Pituitary Hormone-Releasing Hormones,
http://linkedlifedata.com/resource/pubmed/chemical/Testosterone,
http://linkedlifedata.com/resource/pubmed/chemical/dihydrotestosterone heptanoate
|
pubmed:status |
MEDLINE
|
pubmed:month |
Mar
|
pubmed:issn |
0021-972X
|
pubmed:author | |
pubmed:issnType |
Print
|
pubmed:volume |
64
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
|
pubmed:pagination |
557-62
|
pubmed:dateRevised |
2007-11-14
|
pubmed:meshHeading |
pubmed-meshheading:3546348-Adult,
pubmed-meshheading:3546348-Dihydrotestosterone,
pubmed-meshheading:3546348-Estradiol,
pubmed-meshheading:3546348-Gonadotropins, Pituitary,
pubmed-meshheading:3546348-Humans,
pubmed-meshheading:3546348-Hypothalamo-Hypophyseal System,
pubmed-meshheading:3546348-Kinetics,
pubmed-meshheading:3546348-Male,
pubmed-meshheading:3546348-Middle Aged,
pubmed-meshheading:3546348-Pituitary Hormone-Releasing Hormones,
pubmed-meshheading:3546348-Testis,
pubmed-meshheading:3546348-Testosterone
|
pubmed:year |
1987
|
pubmed:articleTitle |
Dihydrotestosterone heptanoate: synthesis, pharmacokinetics, and effects on hypothalamic-pituitary-testicular function.
|
pubmed:publicationType |
Journal Article,
Research Support, U.S. Gov't, P.H.S.
|