TY - JOUR
T1 - Rat NPFF1 receptor-mediated signaling
T2 - functional comparison of neuropeptide FF (NPFF), FMRFamide and PFR(Tic)amide
AU - Chen, Jin Chung
AU - Lee, Wei Hsin
AU - Chen, Pei Chun
AU - Tseng, Ching Ping
AU - Huang, Eagle Yi Kung
N1 - Funding Information:
This study was supported by the grants from the National Health Research Institutes (NHRI-EX93-8909BP), the National Science Council (NSC 92-2320-B-016-016), and C.Y. Foundation for Advancement of Education, Sciences and Medicine, Taipei, Taiwan, R.O.C.
PY - 2006/5
Y1 - 2006/5
N2 - Neuropeptide FF (NPFF) participates in many physiological functions associated with opioids in the mammalian CNS. We established a pheochromocytoma PC-12 cell line clone stably expressing rat NPFF1 receptors. Both NPFF and FMRFamide activated NPFF1 receptors to couple with Gi/o protein and inhibited adenylyl cyclase activity in PC-12/rNPFF1 cells, but there were no effects on MAPKs (ERK1/2 and p38 MAPK) or PI3K/Akt pathway. FMRFamide also inhibited DARPP-32/Thr34 phosphorylation in the presence of forskolin. Similarly, PFR(Tic)amide, a 'super-agonist' of NPFF receptors, inhibited the production of cAMP and slightly decreased DARPP-32/Thr34 phosphorylation in PC-12/rNPFF1 cells. Intracerebroventricular injections of PFR(Tic)amide blocked behavioral sensitization of locomotor activity to amphetamine, and intrathecal injection of PFR(Tic)amide caused a dose-dependent antinociception in vivo in rats. Thus, "over-activation" of NPFF receptors by PFR(Tic)amide induced different bio-effects from those induced by NPFF in vivo.
AB - Neuropeptide FF (NPFF) participates in many physiological functions associated with opioids in the mammalian CNS. We established a pheochromocytoma PC-12 cell line clone stably expressing rat NPFF1 receptors. Both NPFF and FMRFamide activated NPFF1 receptors to couple with Gi/o protein and inhibited adenylyl cyclase activity in PC-12/rNPFF1 cells, but there were no effects on MAPKs (ERK1/2 and p38 MAPK) or PI3K/Akt pathway. FMRFamide also inhibited DARPP-32/Thr34 phosphorylation in the presence of forskolin. Similarly, PFR(Tic)amide, a 'super-agonist' of NPFF receptors, inhibited the production of cAMP and slightly decreased DARPP-32/Thr34 phosphorylation in PC-12/rNPFF1 cells. Intracerebroventricular injections of PFR(Tic)amide blocked behavioral sensitization of locomotor activity to amphetamine, and intrathecal injection of PFR(Tic)amide caused a dose-dependent antinociception in vivo in rats. Thus, "over-activation" of NPFF receptors by PFR(Tic)amide induced different bio-effects from those induced by NPFF in vivo.
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U2 - 10.1016/j.peptides.2005.09.018
DO - 10.1016/j.peptides.2005.09.018
M3 - Article
C2 - 16490283
AN - SCOPUS:33646470290
SN - 0196-9781
VL - 27
SP - 1005
EP - 1014
JO - Peptides
JF - Peptides
IS - 5
ER -