2009
DOI: 10.1074/jbc.m109.049734
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Identification of Anabolic Selective Androgen Receptor Modulators with Reduced Activities in Reproductive Tissues and Sebaceous Glands

Abstract: Androgen replacement therapy is a promising strategy for the treatment of frailty; however, androgens pose risks for unwanted effects including virilization and hypertrophy of reproductive organs. Selective Androgen Receptor Modulators (SARMs) retain the anabolic properties of androgens in bone and muscle while having reduced effects in other tissues. We describe two structurally similar 4-aza-steroidal androgen receptor (AR) ligands, Cl-4AS-1, a full agonist, and TFM-4AS-1, which is a SARM. TFM-4AS-1 is a pot… Show more

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Cited by 37 publications
(34 citation statements)
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“…Female rats were ovariectomized (OVX) at 12 weeks, and test compound administration began at least 8 weeks post-surgery for 24 days (20). Animals were randomized into groups (n ϭ 10 -16), and compounds dissolved in propylene glycol were administered by subcutaneous injection.…”
Section: Methodsmentioning
confidence: 99%
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“…Female rats were ovariectomized (OVX) at 12 weeks, and test compound administration began at least 8 weeks post-surgery for 24 days (20). Animals were randomized into groups (n ϭ 10 -16), and compounds dissolved in propylene glycol were administered by subcutaneous injection.…”
Section: Methodsmentioning
confidence: 99%
“…Measurements of sebaceous gland size were assessed by using a Nikon Eclipse E1000M microscope/digital camera system and BioQuant software. Tibiae were collected for RNA processing and histological studies (20). Data were analyzed by one way analysis of variance, Fisher's protected least significant difference (Statview, Version 5.0).…”
Section: Methodsmentioning
confidence: 99%
See 3 more Smart Citations