872172-28-6Relevant articles and documents
New series of potent δ-opioid antagonists containing the H-Dmt-Tic-NH-hexyl-NH-R motif
Li, Tingyou,Shiotani, Kimitaka,Miyazaki, Anna,Fujita, Yoshio,Tsuda, Yuko,Ambo, Akihiro,Sasaki, Yusuke,Jinsmaa, Yunden,Marczak, Ewa,Bryant, Sharon D.,Lazarus, Lawrence H.,Okada, Yoshio
, p. 5517 - 5520 (2007/10/03)
Heterodimeric compounds H-Dmt-Tic-NH-hexyl-NH-R (R = Dmt, Tic, and Phe) exhibited high affinity to δ- (Kiδ = 0.13-0.89 nM) and μ-opioid receptors (Kiμ = 0.38-2.81 nM) with extraordinary potent δ antagonism (pA2 = 10.2-10.4). These compounds represent the prototype for a new class of structural homologues lacking μ-opioid receptor-associated agonism (IC50 = 1.6-5.8 μM) based on the framework of bis-[H-Dmt-NH]-alkyl (Okada, Y.; Tsuda, Y.; Fujita, Y.; Yokoi, T.; Sasaki, Y.; Ambo, A.; Konishi, R.; Nagata, M.; Salvadori, S.; Jinsmaa, Y.; Bryant, S. D.; Lazarus, L. H. J. Med. Chem. 2003, 46, 3201), which exhibited both high μ affinity and bioactivity.