On the inhibition of capsaicin response in dorsal root ganglion neurons by nobilamide B and analogues: a structure-activity relationship study.
Medchemcomm
; 9(10): 1673-1678, 2018 Oct 01.
Article
em En
| MEDLINE
| ID: mdl-30429972
ABSTRACT
Nobilamide B, a TRPV1 antagonist, and a series of Ala-substituted analogues were synthesized and their neuroactivity was assessed in a primary culture of dorsal root ganglion (DRG) neurons. Analogues 4, 6, and 7 showed comparable activity, affecting capsaicin response in neurons, in contrast to 2, 3, and 5 which showed minimal blocking. Compounds 2, 3, and 5 correspond to analogues in which d-Phe, d-Leu and d-allo-Thr have been substituted with Ala, respectively. The observed loss of bioactivity in these three analogues highlights the importance of d amino acids in the primary structure of nobilamide B.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Idioma:
En
Revista:
Medchemcomm
Ano de publicação:
2018
Tipo de documento:
Article