480446-87-5Relevant academic research and scientific papers
Conversion of the potent δ-opioid agonist H-Dmt-Tic-NH-CH 2-Bid into δ-opioid antagonists by N1-benzimidazole alkylation
Balboni, Gianfranco,Guerrini, Remo,Salvadori, Severo,Negri, Lucia,Giannini, Elisa,Bryant, Sharon D.,Jinsmaa, Yunden,Lazarus, Lawrence H.
, p. 8112 - 8114 (2007/10/03)
N1-Alkylation of 1H-benzimidizole of the δ agonist H-Dmt-Tic-NH-CH2-Bid with hydrophobic, aromatic, olefinic, acid, ethyl ester, or amide (1-6) became δ antagonists (pA2 = 8.52-10.14). δ- and μ-Opioid receptor affinities w
Potent δ-opioid receptor agonists containing the Dmt-Tic pharmacophore
Balboni, Gianfranco,Salvadori, Severo,Guerrini, Remo,Negri, Lucia,Giannini, Elisa,Jinsmaa, Yunden,Bryant, Sharon D.,Lazarus, Lawrence H.
, p. 5556 - 5563 (2007/10/03)
Conversion of δ-opioid receptor antagonists containing the 2′,6′-dimethyl-L-tyrosine (Dmt)-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid (Tic) pharmacophore into potent δ-agonists required a third heteroaromatic nucleus, such as 1H-benzimidazole-2-yl (
