Abstract—H-Dmt-Tic-NH-CH2-Bid (UFP-502) was the first d-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 d-agonism, it was substituted by similar heterocycles: The substitution of NH(1) by O or S transforms the reference d-agonist into d-antagonists. Phenyl ring of benzimidazole is not important for d-agonism; in fact 1H-imidazole-2-yl retains d-agonist activity.
Role of benzimidazole (Bid) in the d-opioid agonist pseudopeptide H-Dmt-Tic-NH-CH2-Bid (UFP-502)
SALVADORI, Severo;TRAPELLA, Claudio;
2008
Abstract
Abstract—H-Dmt-Tic-NH-CH2-Bid (UFP-502) was the first d-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 d-agonism, it was substituted by similar heterocycles: The substitution of NH(1) by O or S transforms the reference d-agonist into d-antagonists. Phenyl ring of benzimidazole is not important for d-agonism; in fact 1H-imidazole-2-yl retains d-agonist activity.File in questo prodotto:
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