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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 …
Potent Dmt-Tic pharmacophoric delta- and mu-opioid receptor antagonists.
Li T, Fujita Y, Shiotani K, Miyazaki A, Tsuda Y, Ambo A, Sasaki Y, Jinsmaa Y, Marczak E, Bryant SD, Salvadori S, Lazarus LH, Okada Y. Li T, et al. Among authors: ambo a. J Med Chem. 2005 Dec 15;48(25):8035-44. doi: 10.1021/jm050377l. J Med Chem. 2005. PMID: 16335927
53 results