An immortalized myocyte cell line, HL-1, expresses a functional delta -opioid receptor.
J Mol Cell Cardiol
; 32(12): 2187-93, 2000 Dec.
Article
en En
| MEDLINE
| ID: mdl-11112994
ABSTRACT
The present study characterizes opioid receptors in an immortalized myocyte cell line, HL-1. Displacement of [(3)H]bremazocine by selective ligands for the mu (mu), delta (delta), and kappa (kappa) receptors revealed that only the delta -selective ligands could fully displace specific [(3)H]bremazocine binding, indicating the presence of only the delta -receptor in these cells. Saturation binding studies with the delta -antagonist naltrindole afforded a B(max)of 32 fmols/mg protein and a K(D)value for [(3)H]naltrindole of 0.46 n M. The binding affinities of various delta ligands for the receptor in HL-1 cell membranes obtained from competition binding assays were similar to those obtained using membranes from a neuroblastomaxglioma cell line, NG108-15. Finally, various delta -agonists were found to stimulate the binding of [(35)S]GTP gamma S, confirming coupling of the cardiac delta -receptor to G-protein. DADLE (D-Ala-D-Leu-enkephalin) was found to be the most efficacious in this assay, stimulating the binding of [(35)S]GTP gamma S to 27% above basal level. The above results indicate that the HL-1 cell line contains a functionally coupled delta -opioid receptor and therefore provides an in vitro model by which to study the direct effects of opioids on cardiac opioid receptors.
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Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Línea Celular
/
Receptores Opioides delta
/
Miocardio
/
Naltrexona
Tipo de estudio:
Prognostic_studies
Idioma:
En
Revista:
J Mol Cell Cardiol
Año:
2000
Tipo del documento:
Article
País de afiliación:
Estados Unidos