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Promotion of sleep by targeting the orexin system in rats, dogs and humans
TLDR
In rats, dogs and humans, somnolence is induced by pharmacological blockade of both orexin OX1 and OX2 receptors, and this results open new perspectives for investigating the role of endogenous orexins in sleep-wake regulation.
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5-HT2C receptor agonists: pharmacological characteristics and therapeutic potential.
TLDR
The results suggest that 5-HT2C receptor agonism is associated with therapeutic potential in obsessive compulsive disorder and depression.
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A synthetic agonist at the orphanin FQ/nociceptin receptor ORL1: anxiolytic profile in the rat.
TLDR
These data confirm the notable anxiolytic-like effects observed at low doses with the orphanin FQ/nociceptin neuropeptide given locally into the brain and support a role for orphan in F Q/nOCiceptin in adaptive behavioral fear responses to stress.
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Orphanin FQ acts as an anxiolytic to attenuate behavioral responses to stress.
TLDR
It is shown that OFQ plays an important role in higher brain functions because it can act as an anxiolytic to attenuate the behavioral inhibition of animals acutely exposed to stressful/anxiogenic environmental conditions.
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Targeted disruption of the orphanin FQ/nociceptin gene increases stress susceptibility and impairs stress adaptation in mice.
TLDR
OfQ/N appears to be crucially involved in the neurobiological regulation of stress-coping behavior and fear.
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Pharmacological characterization of the novel nonpeptide orphanin FQ/nociceptin receptor agonist Ro 64-6198: rapid and reversible desensitization of the ORL1 receptor in vitro and lack of tolerance…
TLDR
Data show that nonpeptide agonists at the ORL1 receptor have a good clinical potential as anxiolytics without causing tolerance, and Ro 64-6198 was able to reduce brain OrL1 binding sites in both acutely and chronically treated rats.
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Synthesis of (1S,3aS)-8-(2,3,3a,4,5, 6-hexahydro-1H-phenalen-1-yl)-1-phenyl-1,3,8-triaza-spiro[4. 5]decan-4-one, a potent and selective orphanin FQ (OFQ) receptor agonist with anxiolytic-like…
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Functional Consequences of Reduction in NMDA Receptor Glycine Affinity in Mice Carrying Targeted Point Mutations in the Glycine Binding Site
TLDR
A milder reduction in receptor glycine affinity results in an impairment of LTP and spatial learning and alterations in anxiety-related behavior, providing further evidence for the role of NMDA receptor activation in these processes.
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Dorsal periaqueductal gray-induced aversion as a simulation of panic anxiety: Elements of face and predictive validity
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A combined pharmacological and genetic approach to investigate the role of orphanin FQ in learning and memory
TLDR
A bi‐directional effect of OFQ/N containing systems on aspects of cognitive behaviour, particularly those elements associated with hippocampal function are suggested, consistent with a likely modulatory role of OFZ/N on hippocampal and associated cortical circuitry.
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