REGULAR ARTICLES
Cell Research (1997)7:69-77
© 1997 SIBS, CAS All rights reserved 1001-0602/97
Molecular characterization and functional expression of opioid
receptor-like1 receptor.
Wu YL, Pu L, Ling K, Zhao J, Cheng ZJ, Ma L, Pei G.
Shanghai Institute of Cell Biology, Chinese Academy of Sciences,
China.
Correspondence:
Pei G |
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Pei G
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The opioid receptor-like1 receptor (ORL1), an orphan receptor whose human
and murine complementary DNAs, has been characterized recently. ORL1 transcripts
are particularly abundant in the central nervous system. We demonstrated
that ORL1 expressed in human neuroblastoma SK-N-SH and SH-SY5Y cell lines
by radioligand binding assay, reverse transcription polymerase chain reaction
(RT-PCR) and Northern analysis in the present study. Stimulation with ORL1
specific agonist, nociceptin/orphanin FQ, increased [35S]GTP gamma S binding
to SK-N-SH cell membranes (EC50 = 14 +/- 0.45 nM), and attenuated forskolin-stimulated
accumulation of cellular cAMP (EC50 = 0.80 +/- 0.45 nM), indicative that
activation of ORL1 activates G proteins and inhibits adenylyl cyclase. Activation
of ORL1 receptor was also accessed using CHO:hORL1 cell line by microphysiometer.
Treatment of nociceptin/orphanin FQ increased extracellular acidification
rate significantly.
Keywords : Opioid
receptor-like1 receptor (OLR1), nociceptin/orphanin FQ(N/OFQ), SK-N-SH cells,
extracellular acidification, functional expression. |
