220996-36-1Relevant articles and documents
Synthesis and evaluation of C-11, F-18 and I-125 small molecule radioligands for detecting oxytocin receptors
Smith, Aaron L.,Freeman, Sara M.,Stehouwer, Jeffery S.,Inoue, Kiyoshi,Voll, Ronald J.,Young, Larry J.,Goodman, Mark M.
experimental part, p. 2721 - 2738 (2012/05/20)
Compounds 1-4 were synthesized and investigated for selectivity and potency for the oxytocin receptor (OTR) to determine their viability as radioactive ligands. Binding assays determined 1-4 to have high binding affinity for both the human and rodent OTR
Nonpeptide oxytocin antagonists: Analogs of L-371,257 with improved potency
Williams, Peter D.,Bock, Mark G.,Evans, Ben E.,Freidinger, Roger M.,Gallicchio, Steven N.,Guidotti, Maribeth T.,Jacobson, Marlene A.,Michelle S, Kuo,Levy, Michelle R.,Edward V, Lis,Michelson, Stuart R.,Pawluczyk, Joseph M.,Perlow, Debra S.,Pettibone, Douglas J.,Quigley, Amy G.,Reiss, Duane R.,Salvatore, Christopher,Stauffer, Kenneth J.,Woyden, Carla J.
, p. 1311 - 1316 (2007/10/03)
Structure-activity studies on the oxytocin antagonist 1 (L-371,257; K(i) = 9.3 nM) have led to the identification of a related series of compounds containing an ortho-trifluoroethoxyphenylacetyl core which are orally bioavailable and have significantly improved potency in vitro and in vivo, e.g., compound 8 (L-374,943; K(i) = 1.4 nM).