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.
2008
Salvadori, Severo; Fiorini, S.; Trapella, Claudio; Porreca, F.; Davis, P.; Sasaki, Y.; Ambo, A.; Marczak, E. D.; Lazarus, L. H.; Balboni, G.
File in questo prodotto:
Non ci sono file associati a questo prodotto.

I documenti in SFERA sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.

Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11392/1512322
 Attenzione

Attenzione! I dati visualizzati non sono stati sottoposti a validazione da parte dell'ateneo

Citazioni
  • ???jsp.display-item.citation.pmc??? ND
  • Scopus 11
  • ???jsp.display-item.citation.isi??? 10
social impact