Agonistic effect of buprenorphine in a nociceptin/OFQ receptor-triggered reporter gene assay.
Mol Pharmacol
; 56(2): 334-8, 1999 Aug.
Article
en En
| MEDLINE
| ID: mdl-10419552
ABSTRACT
The role of the opioid-like receptor 1 (ORL1) and its endogenous ligand, nociceptin/orphanin FQ (N/OFQ), in nociception, anxiety, and learning remains to be defined. To allow the rapid identification of agonists and antagonists, a reporter gene assay has been established in which the ORL1 receptor is functionally linked to the cyclic AMP-dependent expression of luciferase. N/OFQ and N/OFQ(1-13)NH(2) inhibited the forskolin-induced luciferase gene expression with IC(50) values of 0.81 +/- 0.5 and 0.87 +/- 0.16 nM, respectively. Buprenorphine was identified as a full agonist at the ORL1 receptor with an IC(50) value of 8.4 +/- 2.8 nM. Fentanyl and 7-benzylidenenaltrexone displayed a weak agonistic activity. The ORL1 antagonist [Phe(1)Psi(CH(2)-NH)Gly(2)]N/OFQ((1-13))NH(2) clearly behaved as an agonist in this assay with an IC(50) value of 85 +/- 47 nM. Thus, there is still a need for antagonistic tool compounds that might help to elucidate the neurophysiological role of N/OFQ.
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Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Buprenorfina
/
Receptores Opioides
/
Narcóticos
Límite:
Animals
/
Humans
Idioma:
En
Revista:
Mol Pharmacol
Año:
1999
Tipo del documento:
Article
País de afiliación:
Alemania