Author/Authors :
Severo Salvadori، نويسنده , , Stella Fiorini، نويسنده , , Claudio Trapella، نويسنده , , Frank Porreca، نويسنده , , Peg Davis، نويسنده , , Yusuke Sasaki، نويسنده , , Akihiro Ambo، نويسنده , , Ewa D. Marczak، نويسنده , , Lawrence H. Lazarus، نويسنده , , Gianfranco Balboni، نويسنده ,
Abstract :
H-Dmt-Tic-NH-CH2-Bid (UFP-502) was the first δ-opioid agonist prepared from the Dmt-Tic pharmacophore. It showed interesting pharmacological properties, such as stimulation of mRNA BDNF expression and antidepression. To evaluate the importance of 1H-benzimidazol-2-yl (Bid) in the induction of δ-agonism, it was substituted by similar heterocycles: The substitution of NH(1) by O or S transforms the reference δ-agonist into δ-antagonists. Phenyl ring of benzimidazole is not important for δ-agonism; in fact 1H-imidazole-2-yl retains δ-agonist activity.
Keywords :
Dmt-Tic pharmacophore , ?-Opioid receptors , UFP-502 , Opioid peptides
