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Differential targeting of Gbetagamma-subunit signaling with small molecules.
Virtual docking of a small-molecule library to a site on Gbetagamma subunits that mediates protein interactions demonstrates an approach for modulation of G protein-coupled receptor signaling that may represent an important therapeutic strategy.
Differential Targeting of Gßγ-Subunit Signaling with Small Molecules
Virtual docking of a small-molecule library to a site on Gβγ subunits that mediates protein interactions is performed to demonstrate an approach for modulation of G protein–coupled receptor signaling that may represent an important therapeutic strategy.
Nalmefene Induced Elevation in Serum Prolactin in Normal Human Volunteers: Partial Kappa Opioid Agonist Activity?
- G. Bart, J. Schluger, L. Borg, A. Ho, J. Bidlack, M. Kreek
- Biology, MedicineNeuropsychopharmacology
- 1 December 2005
Elevations in serum prolactin following nalmefene are consistent with this partial agonist effect at kappa-opioid receptors, and may enhance its therapeutic efficacy in selected addictive diseases.
Noradrenergic signaling the wakeful state inhibits microglial surveillance and synaptic plasticity in the mouse visual cortex.
The results indicate that microglial roles in surveillance and synaptic plasticity in the mouse brain are modulated by noradrenergic tone fluctuations between arousal states and emphasize the need to understand the effect of disruptions of adrenergic signaling in neurodevelopment and neuropathology.
Genetic alteration of phospholipase C beta3 expression modulates behavioral and cellular responses to mu opioids.
Data demonstrate that PLC beta3 constitutes a significant pathway involved in negative modulation of mu opioid responses, perhaps via protein kinase C, and suggests the possibility that differences in opioid sensitivity among individuals could be, in part, because of genetic factors.
Genetic alteration of phospholipase C β3 expression modulates behavioral and cellular responses to μ opioids
Data demonstrate that PLC β3 constitutes a significant pathway involved in negative modulation of μ opioid responses, perhaps via protein kinase C, and suggests the possibility that differences in opioid sensitivity among individuals could be, in part, because of genetic factors.
The kappa opioid receptor expressed on the mouse R1.1 thymoma cell line is coupled to adenylyl cyclase through a pertussis toxin-sensitive guanine nucleotide-binding regulatory protein.
- D. M. Lawrence, J. Bidlack
- Biology, ChemistryThe Journal of pharmacology and experimental…
- 1 September 1993
Evidence is presented that the kappa opioid binding site on R1.1 cell membranes is negatively coupled to adenylyl cyclase, and results suggest that a PTX-sensitive inhibitory guanine nucleotide-binding protein mediates the link between the thymoma kappa opioids receptor and adenyll cyclase.
Evidence for opioid receptors on cells involved in host defense and the immune system
Syntheses of novel high affinity ligands for opioid receptors.
Opioids Activate Brain Analgesic Circuits Through Cytochrome P450/Epoxygenase Signaling
These findings indicate that a neuronal P450 epoxygenase mediates the pain-relieving properties of morphine.