TY - JOUR
T1 - Nociceptin/orphanin FQ stimulates extracellular acidification and desensitization of the response involves protein kinase C
AU - Pei, Gang
AU - Ling, Kun
AU - Pu, Lu
AU - Cunningham, Martin D.
AU - Ma, Lan
N1 - Funding Information:
This research was supported by grants from the Shanghai Educational Development Foundation, the Natural Science Foundation of China (39630130 and 39625010), the Chinese Academy of Sciences (KY951-A1-301-01-05), and the German Max-Planck Society.
PY - 1997/7/21
Y1 - 1997/7/21
N2 - A Chinese hamster ovary (CHO) cell line, CHO-ORL1, stably expressing human opioid receptor-like receptor 1 (ORL1) has been used to determine ORL1-mediated signaling events using microphysiometry. Nociceptin/orphanin FQ (N/OFQ), a specific endogenous agonist of ORL1, induced an increase in extracellular acidification rate (ECAR) in CHO-ORL1 cells. The ECAR response stimulated by N/OFQ was concentration-dependent and pertussis toxin-sensitive. Repeated exposures of the cells to N/OFQ caused desensitization of ORL1. The ECAR response was recovered at the half-life of approximately 12 min after the initial challenge. Pretreatment with inhibitor of cAMP-dependent kinase did not affect desensitization of ORL1. However, specific inhibitors for protein kinase C almost abolished N/OFQ-induced desensitization of extracellular acidification responsiveness, indicating the involvement of protein kinase C in the process.
AB - A Chinese hamster ovary (CHO) cell line, CHO-ORL1, stably expressing human opioid receptor-like receptor 1 (ORL1) has been used to determine ORL1-mediated signaling events using microphysiometry. Nociceptin/orphanin FQ (N/OFQ), a specific endogenous agonist of ORL1, induced an increase in extracellular acidification rate (ECAR) in CHO-ORL1 cells. The ECAR response stimulated by N/OFQ was concentration-dependent and pertussis toxin-sensitive. Repeated exposures of the cells to N/OFQ caused desensitization of ORL1. The ECAR response was recovered at the half-life of approximately 12 min after the initial challenge. Pretreatment with inhibitor of cAMP-dependent kinase did not affect desensitization of ORL1. However, specific inhibitors for protein kinase C almost abolished N/OFQ-induced desensitization of extracellular acidification responsiveness, indicating the involvement of protein kinase C in the process.
KW - Extracellular acidification
KW - Nociceptin/orphanin FQ
KW - Opioid receptor
KW - Opioid receptor-like receptor 1 (ORL)
KW - Protein kinase C
KW - Receptor desensitization
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U2 - 10.1016/S0014-5793(97)00790-4
DO - 10.1016/S0014-5793(97)00790-4
M3 - Article
C2 - 9257731
AN - SCOPUS:0030843706
SN - 0014-5793
VL - 412
SP - 253
EP - 256
JO - FEBS Letters
JF - FEBS Letters
IS - 1
ER -