title: Pharmacological characterization of AC-262536, a novel selective androgen receptor modulator.
abstract: 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.
authors.affiliation: ACADIA Pharmaceuticals Inc., 3911 Sorrento Valley Boulevard, San Diego, CA 92121, USA. fpiu@acadia-pharm.com
authors.forename: Fabrice
authors.initials: F
authors.lastname: Piu
authors.forename: Luis R
authors.initials: LR
authors.lastname: Gardell
authors.forename: Thomas
authors.initials: T
authors.lastname: Son
authors.forename: Nathalie
authors.initials: N
authors.lastname: Schlienger
authors.forename: Birgitte W
authors.initials: BW
authors.lastname: Lund
authors.forename: Hans H
authors.initials: HH
authors.lastname: Schiffer
authors.forename: Kim E
authors.initials: KE
authors.lastname: Vanover
authors.forename: Robert E
authors.initials: RE
authors.lastname: Davis
authors.forename: Roger
authors.initials: R
authors.lastname: Olsson
authors.forename: Stefania Risso
authors.initials: SR
authors.lastname: Bradley
mesh_terms: 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
chemical_list: C529258:AC-262536; D045930:Anabolic Agents; D000728:Androgens; D053961:Azabicyclo Compounds; D017931:DNA Primers; D008024:Ligands; D009281:Naphthalenes; D011944:Receptors, Androgen; D013739:Testosterone