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RF9, a potent and selective neuropeptide FF receptor antagonist, prevents opioid-induced tolerance associated with hyperalgesia.
The discovery of a potent and selective NPFF receptor antagonist, RF9, that can be administered systemically and indicate that NPFF receptors are part of a bona fide antiopioid system and that selective antagonists of these receptors could represent useful therapeutic agents for improving the efficacy of opioids in chronic pain treatment. Expand
A specific gamma-hydroxybutyrate receptor ligand possesses both antagonistic and anticonvulsant properties.
The results suggest that NCS-382 may represent a harbinger for a new class of anticonvulsant drugs that most probably act by modifying the endogenous GHB system. Expand
Endogenous mammalian RF-amide peptides, including PrRP, kisspeptin and 26RFa, modulate nociception and morphine analgesia via NPFF receptors
Results show that all endogenous RF-amide peptides display pain-modulating properties and point to NPFF receptors as essential players for these effects. Expand
gamma-Hydroxybutyrate ligands possess antidopaminergic and neuroleptic-like activities.
It is suggested that GHB agonists possessing antidopaminergic activities, may represent potential drugs endowed with neuroleptic properties. Expand
Anti-sedative and anti-cataleptic properties of NCS-382, a γ-hydroxybutyrate receptor antagonist
NCS-382 possesses antagonistic properties at gamma-hydroxybutyrate receptor sites. Its effect on the sedative/cataleptic behaviour observed in rats after gamma-hydroxybutyrate administration wasExpand
The flavonoid dioclein is a selective inhibitor of cyclic nucleotide phosphodiesterase type 1 (PDE1) and a cGMP-dependent protein kinase (PKG) vasorelaxant in human vascular tissue.
The data show that dioclein is a potent calmodulin-independent selective inhibitor of PDE1 and that inhibition of Pde1 is involved in the PKG-mediated vasorelaxant effect of dioc Klein in human saphenous vein and may represent a new archetype to develop more specific PDE 1 inhibitors. Expand
Xanthurenic Acid Binds to Neuronal G-Protein-Coupled Receptors That Secondarily Activate Cationic Channels in the Cell Line NCB-20
The results suggest that XA, acting through a GPCR-induced cationic channel modulatory mechanism, may exert excitatory functions in various brain neuronal pathways. Expand
Inhibition of neuronal FLT3 receptor tyrosine kinase alleviates peripheral neuropathic pain in mice
It is demonstrated that hematopoietic cells present at the nerve injury site express the cytokine FL, the ligand of fms-like tyrosine kinase 3 receptor (FLT3), and a novel FLT3 inhibitor is identified that attenuates neuropathic pain in mice. Expand
Involvement of neuropeptide FF receptors in neuroadaptive responses to acute and chronic opiate treatments
RF9, a potent and selective antagonist of NPFF receptors that can be administered systemically, is used by this study to investigate the consequences ofNPFF receptor blockade on acute and chronic stimulation of opioid receptors in mice. Expand
Effect of gamma-hydroxybutyrate and its antagonist NCS-382 on spontaneous cell firing in the prefrontal cortex of the rat
Gamma-hydroxybutyrate at low doses increased and at high doses decreased the spontaneous firing rate of prefrontal cortex (PFC) neurons recorded in urethane-anesthetized rats, suggesting that the excitatory effect of low doses of GHB is mediated by a GHB receptor whereas the inhibitory effect of high doses ofGHB involves a more complex mechanism. Expand