ß2 -Adrenoceptor agonist activity of higenamine.
Drug Test Anal
; 13(2): 261-267, 2021 Feb.
Article
en En
| MEDLINE
| ID: mdl-33369180
ABSTRACT
Higenamine was included in the World Anti-Doping Agency (WADA) Prohibited Substances and Methods List as a ß2 -adrenoceptor agonist in 2017, thereby resulting in its prohibition both in and out of competition. The present mini review describes the physiology and pharmacology of adrenoceptors, summarizes the literature addressing the mechanism of action of higenamine and extends these findings with previously unpublished in silico and in vitro work. Studies conducted in isolated in vitro systems, whole-animal preparations and a small number of clinical studies suggest that higenamine acts in part as a ß2 -adrenoceptor agonist. In silico predictive tools indicated that higenamine and possibly a metabolite have a high probability of interacting with the ß2 -receptor as an agonist. Stable expression of human ß2 -receptors in Chinese hamster ovary (CHO) cells to measure agonist activity not only confirmed the activity of higenamine at ß2 but also closely agreed with the in silico prediction of potency for this compound. These data confirm and extend literature findings supporting the inclusion of higenamine in the Prohibited List.
Palabras clave
Texto completo:
1
Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Receptores Adrenérgicos beta 2
/
Agonistas Adrenérgicos beta
/
Tetrahidroisoquinolinas
/
Alcaloides
/
Sustancias para Mejorar el Rendimiento
Tipo de estudio:
Prognostic_studies
Límite:
Animals
/
Humans
Idioma:
En
Revista:
Drug Test Anal
Asunto de la revista:
FARMACOLOGIA
Año:
2021
Tipo del documento:
Article
País de afiliación:
Estados Unidos