The stereochemical requirements of the novel δ-opioid selective dipeptide antagonist TMT-Tic
Five conformationally constrained dipeptide TMT-L-Tic analogues have been synthesized and evaluated for their bioactivity using in vitro bioassays. The most potent and selective analogue (2S,3R)-TMT-L-Tic showed 9 nM binding affinity and 4000-fold selectivity for the δ vs μ opioid receptor. The lowest-energy conformation of (2S,3R)-TMT-L-Tic is suggested to be bioactive one in which the X, torsional angle is trans for TMT and gauche (+) for Tic.
Liao, Subo,Lin, Jun,Shenderovich, Mark D.,Han, Yinglin,Hasohata, Keiko,Davis, Peg,Qiu, Wei,Porreca, Frank,Yamamura, Henry I.,Hruby, Victor J.
p. 3049 - 3052
(2007/10/03)
More Articles about upstream products of 103733-30-8