Antinociceptive effects of 1-acyl-4-dialkylaminopiperidine and 1-alkyl-4-dialkylaminopiperidine in mice: structure-activity relation study of matrine-type alkaloids.
Biol Pharm Bull
; 25(8): 1030-4, 2002 Aug.
Article
en En
| MEDLINE
| ID: mdl-12186404
ABSTRACT
We previously reported that (+)-matrine and (+)-allomatrine have antinociceptive properties mediated mainly through the activation of kappa-opioid receptors. 1-Acyl-4-dialkylaminopiperidines were synthesized as the simplest derivatives of matrine, and the structure-activity relations were examined by the acetic acid-induced abdominal contraction test. The antinociceptive potencies of 1-alkyl-4-dialkylaminopiperidines were significantly lower than those of the corresponding 1-acyl-4-dialkylaminopiperidines. These findings suggest that the amide group of (+)-matrine is an essential functional group that influences antinociceptive potency.
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Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Piperidinas
/
Alcaloides
/
Analgésicos
Límite:
Animals
Idioma:
En
Revista:
Biol Pharm Bull
Asunto de la revista:
BIOQUIMICA
/
FARMACOLOGIA
Año:
2002
Tipo del documento:
Article
País de afiliación:
Japón