The rat SSTR2 somatostatin receptor subtype is coupled to inhibition of cyclic AMP accumulation.
Biochem Biophys Res Commun
; 191(3): 968-76, 1993 Mar 31.
Article
en En
| MEDLINE
| ID: mdl-8096694
The rat somatostatin receptor SSTR2 subtype has been cloned and expressed in Chinese Hamster Ovary (CHO) cells. Four different radioligands were used to determine the pharmacological properties of this somatostatin receptor subtype. [125ITyr11]S-14, [125ITyr25]S-28, and cyclo (D-Trp-Lys-Abu-Phe-MeAla-[125ITyr]) displayed comparable affinities for the SSTR2 subtype (approximately 100 pM). The affinity of a fourth radioligand, D-beta Nal-cyclo (Cys-[125ITyr]-DTrp-Lys-Val-Cys)-Thr-H2N, was approximately 10-fold lower (approximately 1000 pM) than the three other radioligands. Competition of [125I]S-14 with either S-14 or S-28 also revealed comparable IC50 values (250 pM). In CHO cells transfected with the SSTR2 cDNA, S-14 inhibited forskolin-stimulated cAMP accumulation by 75% in a dose-dependent fashion (EC50 = 350 pM).
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Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Receptores de Somatostatina
/
AMP Cíclico
Límite:
Animals
Idioma:
En
Revista:
Biochem Biophys Res Commun
Año:
1993
Tipo del documento:
Article
Pais de publicación:
Estados Unidos