Endogenous opioid receptor-like receptor in human neuroblastoma SK-N-SH cells: activation of inhibitory G protein and homologous desensitization.
Neuroreport
; 8(8): 1913-8, 1997 May 27.
Article
em En
| MEDLINE
| ID: mdl-9223076
ABSTRACT
Endogenous expression of opioid receptor-like receptor (ORL1), in human neuroblastoma SK-N-SH cells was demonstrated by binding with nociceptin/ orphanin FQ (N/OFQ). Scatchard analysis of [3H]N/ OFQ saturation binding data gave Kd = 1.3 +/- 0.1 nM and Bmax = 1.58 +/- 2.5 fmol/mg protein. N/OFQ stimulation increased [35S]GTP gamma S binding to cell membranes and attenuated forskolin-induced cAMP accumulation in a concentration-dependent manner. The effects of N/OFQ were eliminated by the pretreatment of pertussis toxin (PTX) but not by the antagonists of opioid receptors, revealing mediation of N/OFQ signal transduction by ORL1 receptor and PTX sensitive G protein(s). The ability of N/OFQ to inhibit cAMP production was greatly reduced after prechallenging with N/OFQ, indicating that ORL1 undergoes homologous desensitization in neuronal cells.
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Base de dados:
MEDLINE
Assunto principal:
Neoplasias Encefálicas
/
Receptores Opioides
/
Proteínas de Ligação ao GTP
/
Neuroblastoma
Idioma:
En
Ano de publicação:
1997
Tipo de documento:
Article