Pharmacological characterization of AC-262536, a novel selective androgen receptor modulator.
Because of the limitations and liabilities of current testosterone therapies, non-steroidal tissue-selective androgen receptor modulators may provide a clinically meaningful advance in therapy. Using a functional cell-based assay AC-262536 was identified as a potent and selective AR ligand, with partial agonist activity relative to the natural androgen testosterone. A 2-week chronic study in castrated male rats indicated that AC-262536 significantly improves anabolic parameters in these animals, especially in stimulating the growth of the levator ani and in suppressing elevated LH levels. In sharp contrast to testosterone, AC-262536 has weak androgenic effects, as measured by prostate and seminal vesicle weights. Thus, AC-262536 represents a novel class of selective androgen receptor modulators (SARMs) with beneficial anabolic effects.
Piu
Fabrice
F
ACADIA Pharmaceuticals Inc., 3911 Sorrento Valley Boulevard, San Diego, CA 92121, USA. fpiu@acadia-pharm.com
Gardell
Luis R
LR
Son
Thomas
T
Schlienger
Nathalie
N
Lund
Birgitte W
BW
Schiffer
Hans H
HH
Vanover
Kim E
KE
Davis
Robert E
RE
Olsson
Roger
R
Bradley
Stefania Risso
SR
D045930:Anabolic Agents / Q000494:pharmacology; D000728:Androgens; D000818:Animals; D053961:Azabicyclo Compounds / Q000494:pharmacology*; D001483:Base Sequence; D002460:Cell Line; D017931:DNA Primers / Q000235:genetics; D017930:Genes, Reporter; D006801:Humans; D008024:Ligands; D008297:Male; D009132:Muscles / Q000033:anatomy & histology / Q000187:drug effects; D009281:Naphthalenes / Q000494:pharmacology*; D009919:Orchiectomy; D009928:Organ Specificity; D010902:Pituitary Gland / Q000187:drug effects / Q000502:physiology; D011467:Prostate / Q000033:anatomy & histology / Q000187:drug effects; D051381:Rats; D017207:Rats, Sprague-Dawley; D011944:Receptors, Androgen / Q000235:genetics / Q000378:metabolism; D012669:Seminal Vesicles / Q000033:anatomy & histology / Q000187:drug effects; D013739:Testosterone / Q000494:pharmacology
C529258:AC-262536; D045930:Anabolic Agents; D000728:Androgens; D053961:Azabicyclo Compounds; D017931:DNA Primers; D008024:Ligands; D009281:Naphthalenes; D011944:Receptors, Androgen; D013739:Testosterone