On resin click-chemistry-mediated synthesis of novel enkephalin analogues with potent anti-nociceptive activity.
Sci Rep
; 9(1): 5771, 2019 04 08.
Article
em En
| MEDLINE
| ID: mdl-30962495
ABSTRACT
Here, we report the chemical synthesis of two DPDPE analogues 7a (NOVA1) and 7b (NOVA2). This entailed the solid-phase synthesis of two enkephalin precursor chains followed by a CuI-catalyzed azide-alkyne cycloaddition, with the aim of improving in vivo analgesic efficacy versus DPDPE. NOVA2 showed good affinity and selectivity for the µ-opioid receptor (KI of 59.2 nM, EC50 of 12.9 nM, EMax of 87.3%), and long lasting anti-nociceptive effects in mice when compared to DPDPE.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
D-Penicilina (2,5)-Encefalina
/
Química Click
/
Analgésicos
Limite:
Animals
/
Humans
/
Male
Idioma:
En
Revista:
Sci Rep
Ano de publicação:
2019
Tipo de documento:
Article
País de afiliação:
Itália