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δ‐, but not µ‐, opioid receptor stabilizes K+ homeostasis by reducing Ca2+ influx in the cortex during acute hypoxia
Past work has shown that δ‐opioid receptor (DOR) activation by [D‐Ala2,D‐Leu5]‐enkephalin (DADLE) attenuated the disruption of K+ homeostasis induced by hypoxia or oxygen‐glucose deprivation (OGD) inExpand
Conformational Dynamics of Kir3.1/Kir3.2 Channel Activation Via δ-Opioid Receptors
TLDR
The fact that BRET changes at the Gβγ-Kir3 interface are predictive of a ligand’s ability to induce channel currents points to these conformational biosensors as screening tools for identifying GPCR ligands that induce Kir3 channel activation. Expand
Potent delta-opioid receptor agonists containing the Dmt-Tic pharmacophore.
TLDR
The data demonstrate that a linker separating the Dmt-Tic pharmacophore and Bid, regardless of the presence of a negative charge, is important in the acquisition of opioids exhibiting potent delta agonism and weak mu agonism from a parent delta antagonist. Expand
Anxiolytic- and antidepressant-like activities of H-Dmt-Tic-NH-CH(CH2-COOH)-Bid (UFP-512), a novel selective delta opioid receptor agonist
TLDR
The present findings demonstrate that UFP-512 behaves as a highly potent and selective agonist at Dop receptors and corroborate the proposal that the selective activation of DOP receptors elicits robust anxiolytic- and antidepressant-like effects in rodents. Expand
The chemokine Bv8/prokineticin 2 is up-regulated in inflammatory granulocytes and modulates inflammatory pain
TLDR
The fundamental role of granulocyte-derived PK2 (GrPK2) in initiating inflammatory pain and driving peripheral sensitization is demonstrated and inhibitors of PK2 formation or antagonizing PKRs may represent another therapeutic approach for controlling inflammatory pain. Expand
Antidepressant-like and anxiolytic-like effects following activation of the μ-δ opioid receptor heteromer in the nucleus accumbens
TLDR
Overall, these findings demonstrate that the μ-δ heteromer may be a potential suitable therapeutic target for treatment-resistant depression and anxiety disorders. Expand
Evaluation of the Dmt-Tic pharmacophore: Conversion of a potent δ-opioid receptor antagonist into a potent δ agonist and ligands with mixed properties
Analogues of the 2‘,6‘-dimethyl-l-tyrosine (Dmt)−1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid (Tic) pharmacophore were prepared to test the hypothesis that a “spacer” and a third aromatic centerExpand
Potent δ-Opioid Receptor Agonists Containing the Dmt−Tic Pharmacophore
Conversion of delta-opioid receptor antagonists containing the 2',6'-dimethyl-L-tyrosine (Dmt)-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid (Tic) pharmacophore into potent delta-agonists requiredExpand
Agonists at the δ‐opioid receptor modify the binding of µ‐receptor agonists to the µ–δ receptor hetero‐oligomer
TLDR
This data indicates that the mechanism of action of agonists and their regulation of the µ–δ receptor heteromer are not well understood and should be investigated further. Expand
Triazine compounds as antagonists at Bv8-prokineticin receptors.
TLDR
A new synthesis of some 1,3,5-triazin-4,6-diones as potential non peptidic prokineticin receptor antagonists are approached, containing the following substitutions: N(1), N(5), and C(2) can link an amino-ethyl-guanidine or an ethylendiamine or a 4-ethylbenzyl. Expand
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