New series of potent delta-opioid antagonists containing the H-Dmt-Tic-NH-hexyl-NH-R motif.
Li T, Shiotani K, Miyazaki A, Fujita Y, Tsuda Y, Ambo A, Sasaki Y, Jinsmaa Y, Marczak E, Bryant SD, Lazarus LH, Okada Y.
Li T, et al. Among authors: ambo a.
Bioorg Med Chem Lett. 2005 Dec 15;15(24):5517-20. doi: 10.1016/j.bmcl.2005.08.073. Epub 2005 Sep 23.
Bioorg Med Chem Lett. 2005.
PMID: 16183273
Heterodimeric compounds H-Dmt-Tic-NH-hexyl-NH-R (R=Dmt, Tic, and Phe) exhibited high affinity to delta- (K(i)delta=0.13-0.89nM) and mu-opioid receptors (K(i)mu=0.38-2.81nM) with extraordinary potent delta antagonism (pA(2)=10.2-10.4). These compounds represent the prototype for …
Heterodimeric compounds H-Dmt-Tic-NH-hexyl-NH-R (R=Dmt, Tic, and Phe) exhibited high affinity to delta- (K(i)delta=0.13-0.89nM) and mu-opioi …