A selective androgen receptor modulator with minimal prostate hypertrophic activity restores lean body mass in aged orchidectomized male rats

2008 ◽  
Vol 110 (3-5) ◽  
pp. 207-213 ◽  
Author(s):  
George Allan ◽  
Tifanie Sbriscia ◽  
Olivia Linton ◽  
Muh-Tsann Lai ◽  
Donna Haynes-Johnson ◽  
...  
Keyword(s):  
Androgen Receptor ◽  
Lean Body Mass ◽  
Body Mass ◽  
Male Rats ◽  
Selective Androgen Receptor Modulator ◽  
Receptor Modulator

A selective androgen receptor modulator with minimal prostate hypertrophic activity enhances lean body mass in male rats and stimulates sexual behavior in female rats

Endocrine ◽  
2007 ◽  
Vol 32 (1) ◽  
pp. 41-51 ◽  
Author(s):  
George F. Allan ◽  
Pamela Tannenbaum ◽  
Tifanie Sbriscia ◽  
Olivia Linton ◽  
Muh-Tsann Lai ◽  
...  
Keyword(s):  
Sexual Behavior ◽  
Androgen Receptor ◽  
Lean Body Mass ◽  
Body Mass ◽  
Female Rats ◽  
Male Rats ◽  
Selective Androgen Receptor Modulator ◽  
Receptor Modulator

Computed tomographic assessment of lean body mass in patients on selective androgen receptor modulator

2020 ◽  
Vol 59 (2) ◽  
pp. 100-103
Author(s):  
Richard Thomas ◽  
Atul B. Shinagare ◽  
Michael H. Rosenthal ◽  
Brandon Lee ◽  
Heather A. Jacene ◽  
...  
Keyword(s):  
Androgen Receptor ◽  
Lean Body Mass ◽  
Body Mass ◽  
Selective Androgen Receptor Modulator ◽  
Computed Tomographic ◽  
Receptor Modulator

scholarly journals Selective Androgen Receptor Modulator Treatment Improves Muscle Strength and Body Composition and Prevents Bone Loss in Orchidectomized Rats

Endocrinology ◽  
2005 ◽  
Vol 146 (11) ◽  
pp. 4887-4897 ◽  
Author(s):  
Wenqing Gao ◽  
Peter J. Reiser ◽  
Christopher C. Coss ◽  
Mitch A. Phelps ◽  
Jeffrey D. Kearbey ◽  
...  
Keyword(s):  
Skeletal Muscle ◽  
Androgen Receptor ◽  
Muscle Mass ◽  
Male Rats ◽  
Levator Ani Muscle ◽  
Dependent Manner ◽  
Agonist Activity ◽  
Mineral Density ◽  
Selective Androgen Receptor Modulator ◽  
Receptor Modulator

The partial agonist activity of a selective androgen receptor modulator (SARM) in the prostate was demonstrated in orchidectomized rats. In the current study, we characterized the full agonist activity of S-3-(4-acetylamino-phenoxy)-2-hydroxy-2-methyl-N-(4-nitro-3-trifluoromethyl-phenyl)-propionamide (a structurally related SARM referred to in other publications and hereafter as S-4) in skeletal muscle, bone, and pituitary of castrated male rats. Twelve weeks after castration, animals were treated with S-4 (3 or 10 mg/kg), dihydrotestosterone (DHT) (3 mg/kg), or vehicle for 8 wk. S-4 (3 and 10 mg/kg) restored soleus muscle mass and strength and levator ani muscle mass to that seen in intact animals. Similar changes were also observed in DHT-treated (3 mg/kg) animals. Compared with the anabolic effects observed in muscle, DHT (3 mg/kg) stimulated prostate and seminal vesicle weights moire than 2-fold greater than that observed in intact controls, whereas S-4 (3 mg/kg) returned these androgenic organs to only 16 and 17%, respectively, of the control levels. S-4 (3 and 10 mg/kg) and DHT (3 mg/kg) restored castration-induced loss in lean body mass. Furthermore, S-4 treatment caused a significantly larger increase in total body bone mineral density than DHT. S-4 (3 and 10 mg/kg) also demonstrated agonist activity in the pituitary and significantly decreased plasma LH and FSH levels in castrated animals in a dose-dependent manner. In summary, the strong anabolic effects of S-4 in skeletal muscle, bone, and pituitary were achieved with minimal pharmacologic effect in the prostate. The tissue-selective pharmacologic activity of SARMs provides obvious advantages over steroidal androgen therapy and demonstrates the promising therapeutic utility that this new class of drugs may hold.

scholarly journals Preclinical Characterization of a (S)-N-(4-Cyano-3-Trifluoromethyl-Phenyl)-3-(3-Fluoro, 4-Chlorophenoxy)-2-Hydroxy-2-Methyl-Propanamide: A Selective Androgen Receptor Modulator for Hormonal Male Contraception

Endocrinology ◽  
2008 ◽  
Vol 150 (1) ◽  
pp. 385-395 ◽  
Author(s):  
Amanda Jones ◽  
Jiyun Chen ◽  
Dong Jin Hwang ◽  
Duane D. Miller ◽  
James T. Dalton
Keyword(s):  
Androgen Receptor ◽  
Levator Ani ◽  
Male Rats ◽  
Male Contraception ◽  
Levator Ani Muscle ◽  
Dependent Manner ◽  
Mineral Density ◽  
Intact Male ◽  
Selective Androgen Receptor Modulator ◽  
Receptor Modulator

The pharmacologic effects of (S)-N-(4-cyano-3-trifluoromethyl-phenyl)-3-(3-fluoro, 4-chlorophenoxy)-2-hydroxy-2-methyl-propanamide (S-23) were characterized in male rats as an animal model of hormonal male contraception. S-23 showed high binding affinity (inhibitory constant = 1.7 ± 0.2 nm) and was identified as a full agonist in vitro. In castrated male rats, the ED50 of S-23 in the prostate and levator ani muscle was 0.43 and 0.079 mg/d, respectively. In intact male rats treated for 14 d, S-23 alone suppressed LH levels by greater than 50% at doses greater than 0.1 mg/d, with corresponding decreases in the size of the prostate but increases in the size of levator ani muscle. In intact male rats treated for up to 10 wk with S-23 and estradiol benzoate (EB; necessary to maintain sexual behavior in rats), S-23 showed biphasic effects on androgenic tissues and spermatogenesis by suppressing serum concentrations of LH and FSH. EB alone showed no effect on spermatogenesis. In the EB + S-23 (0.1 mg/d) group, four of six animals showed no sperm in the testis and zero pregnancies (none of six) in mating trials. After termination of treatment, infertility was fully reversible, with a 100% pregnancy rate observed after 100 d of recovery. S-23 increased bone mineral density and lean mass but reduced fat mass in a dose-dependent manner. This is the first study to show that a selective androgen receptor modulator combined with EB is an effective and reversible regimen for hormonal male contraception in rats. The beneficial effects of S-23 on the muscle, tissue selectivity, and favorable pharmacokinetic properties make it a strong candidate for use in oral male contraception. An aryl-propionamide selective androgen receptor modulator (S-23) is an effective and reversible agent for hormonal male contraception in rats.

Safety and Tolerability of LGD-4033, a Novel Non-Steroidal Oral Selective Androgen Receptor Modulator (SARM), in Healthy Men

2011 ◽  
pp. P3-207-P3-207
Author(s):  
Shehzad Basaria ◽  
Lauren Collins ◽  
Melinda Sheffield-Moore ◽  
Edgar L Dillon ◽  
Katie Orwoll ◽  
...  
Keyword(s):  
Androgen Receptor ◽  
Selective Androgen Receptor Modulator ◽  
Healthy Men ◽  
Receptor Modulator

scholarly journals Equine metabolism of the selective androgen receptor modulator AC‐262536 in vitro and in urine, plasma and hair following oral administration

2020 ◽  
Author(s):  
Charlotte Cutler ◽  
Marjaana Viljanto ◽  
Polly Taylor ◽  
Jocelyn Habershon‐Butcher ◽  
Tessa Muir ◽  
...  
Keyword(s):  
Androgen Receptor ◽  
Oral Administration ◽  
Selective Androgen Receptor Modulator ◽  
Receptor Modulator

scholarly journals Selective Androgen Receptor Modulator S42 Suppresses Prostate Cancer Cell Proliferation

Endocrinology ◽  
2018 ◽  
Vol 159 (4) ◽  
pp. 1774-1792 ◽  
Author(s):  
Takako Kawanami ◽  
Tomoko Tanaka ◽  
Yuriko Hamaguchi ◽  
Takashi Nomiyama ◽  
Hajime Nawata ◽  
...  
Keyword(s):  
Prostate Cancer ◽  
Cell Proliferation ◽  
Androgen Receptor ◽  
Cancer Cell ◽  
Prostate Cancer Cell ◽  
Cancer Cell Proliferation ◽  
Selective Androgen Receptor Modulator ◽  
Receptor Modulator
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