Structure–Activity Relationships of 1‐Benzoylazulenes at the OX1 and OX2 Orexin Receptors
Sign Up to like & getrecommendations! Published in 2019 at "ChemMedChem"
DOI: 10.1002/cmdc.201900074
Abstract: We previously demonstrated the potential of di‐ or trisubstituted azulenes as ligands (potentiators, weak agonists, and antagonists) of the orexin receptors. In this study we investigated 27 1‐benzoylazulene derivatives, uncovering seven potentiators of the orexin… read more here.
Keywords: orexin receptors; activity relationships; relationships benzoylazulenes; structure activity ... See more keywords
Spinal Orexin-2 Receptors are Involved in Modulation of the Lateral Hypothalamic Stimulation-Induced Analgesia
Sign Up to like & getrecommendations! Published in 2019 at "Neurochemical Research"
DOI: 10.1007/s11064-019-02749-w
Abstract: Role of the orexinergic system in pain modulation is well studied and involvement of the spinal orexin-1 receptors is well documented. In this study, we examined role of the spinal orexin-2 receptors in modulation of… read more here.
Keywords: orexin receptors; orexin; spinal orexin; stimulation ... See more keywords
Azulene-based compounds for targeting orexin receptors.
Sign Up to like & getrecommendations! Published in 2018 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2018.07.040
Abstract: A library of 70 000 synthetically accessible azulene-based compounds was virtually screened at the OX2 receptor. Based on the results, a series of azulene derivatives was synthesized and the binding to and activation of both orexin… read more here.
Keywords: targeting orexin; orexin; orexin receptors; azulene based ... See more keywords
Activation orexin 1 receptors in the ventrolateral periaqueductal gray matter attenuate nitroglycerin-induced migraine attacks and calcitonin gene related peptide up-regulation in trigeminal nucleus caudalis of rats
Sign Up to like & getrecommendations! Published in 2020 at "Neuropharmacology"
DOI: 10.1016/j.neuropharm.2020.107981
Abstract: This study aims to explore whether orexin 1 receptors (Orx1R) in the ventrolateral periaqueductal gray matter (vlPAG) play a role in the modulation of migraine headaches in adult male Wistar rats. To model chronic migraine-associated… read more here.
Keywords: orexin receptors; ventrolateral periaqueductal; gray matter; periaqueductal gray ... See more keywords
Blockade of the orexin receptors in the CA1 region of hippocampus decreased the lateral hypothalamic-induced antinociceptive responses in the model of orofacial formalin test in the rats
Sign Up to like & getrecommendations! Published in 2018 at "Peptides"
DOI: 10.1016/j.peptides.2017.10.006
Abstract: HighlightsA pathway from the lateral hypothalamus to CA1 modulates early (0–3 min) and late phases (15–33 min) of formalin‐induced orofacial nociception.Blockade of CA1 orexin receptors (OXRs) reduced LH‐induced antinociception during the early and late phases… read more here.
Keywords: orexin receptors; orofacial formalin; ca1; late phases ... See more keywords
The orexin receptors in the ventral tegmental area are involved in the development of sensitization to expression of morphine-induced preference in rats
Sign Up to like & getrecommendations! Published in 2020 at "Behavioural Pharmacology"
DOI: 10.1097/fbp.0000000000000587
Abstract: Recent studies have shown that orexin neurons in the lateral hypothalamus send a compelling project to the ventral tegmental area (VTA). Besides, orexin-1 (OX1) and orexin-2 (OX2) in the VTA are necessary for the development… read more here.
Keywords: orexin receptors; morphine induced; development; morphine ... See more keywords
The Orexin receptors: Structural and anti-tumoral properties
Sign Up to like & getrecommendations! Published in 2022 at "Frontiers in Endocrinology"
DOI: 10.3389/fendo.2022.931970
Abstract: At the end of the 20th century, two new neuropeptides (Orexin-A/hypocretin-1 and Orexin-B/hypocretins-2) expressed in hypothalamus as a prepro-orexins precursor, were discovered. These two neuropeptides interacted with two G protein-coupled receptor isoforms named OX1R and… read more here.
Keywords: anti tumoral; orexins receptors; tumoral properties; receptors structural ... See more keywords
A New Positron Emission Tomography Probe for Orexin Receptors Neuroimaging
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DOI: 10.3390/molecules25051018
Abstract: The orexin receptor (OX) is critically involved in motivation and sleep−wake regulation and holds promising therapeutic potential in various mood disorders. To further investigate the role of orexin receptors (OXRs) in the living human brain… read more here.
Keywords: orexin receptors; orexin; probe; positron emission ... See more keywords
Discovery of Small-Molecule Antagonists of Orexin 1/2 Receptors from Traditional Chinese Medicinal Plants with a Hypnotic Effect
Sign Up to like & getrecommendations! Published in 2023 at "Pharmaceuticals"
DOI: 10.3390/ph16040542
Abstract: Insomnia is an important public health problem. The currently available treatments for insomnia can cause some adverse effects. Orexin receptors 1 (OX1R) and 2 (OX2R) are burgeoning targets for insomnia treatment. It is an effective… read more here.
Keywords: small molecule; medicinal plants; hypnotic effect; traditional chinese ... See more keywords