Fluorescence Fluctuation Spectroscopy of Dopaminergic Signaling in Pancreatic Beta Cells

Foust, Daniel J.; Ustione, Alessandro; Piston, David W.

doi:10.1016/j.bpj.2016.11.525

Cited by 2 publications

(1 citation statement)

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“…We and our colleagues previously showed that human and rodent insulin-secreting pancreatic bcells expressed D2-like receptors including D2R and D3R, and that agonist stimulation of these receptors by (-)-quinpirole and bromocriptine decreased glucose-stimulated insulin secretion (GSIS) 9,12,13,[27][28][29][56][57][58] . Therefore, we further functionally tested the ability of several of the MeI analogues to directly signal through b-cell D2-like receptors by examining their impact on GSIS in INS-1E cells, an insulin-secreting rat pancreatic b-cell line 59 .…”

Section: Mei Analogues Modify Glucose-stimulated Insulin Secretionmentioning

confidence: 99%

Development of novel tools for dissection of central versus peripheral dopamine D₂-like receptor signaling in dysglycemia

Bonifazi,

Ellenberger,

Farino

et al. 2024

Preprint

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Dopamine (DA) D2-like receptors in both the central nervous system (CNS) and the periphery are key modulators of metabolism. Moreover, disruption of D2-like receptor signaling is implicated in dysglycemia. Yet, the respective metabolic contributions of CNS versus peripheral D2-like receptors including D2(D2R) and D3(D3R) receptors remain poorly understood. To address this, we developed new pharmacological tools, D2-like receptor agonists with diminished and delayed blood-brain barrier capability, to selectively manipulate D2R/D3R signaling in the periphery. We designated bromocriptine methiodide (BrMeI), a quaternary methiodide analogue of D2/3R agonist and diabetes drug bromocriptine, as our lead compound based on preservation of D2R/D3R binding and functional efficacy. We then used BrMeI and unmodified bromocriptine to dissect relative contributions of CNS versus peripheral D2R/D3R signaling in treating dysglycemia. Systemic administration of bromocriptine, with unrestricted access to CNS and peripheral targets, significantly improved both insulin sensitivity and glucose tolerance in obese, dysglycemic micein vivo. In contrast, metabolic improvements were attenuated when access to bromocriptine was restricted either to the CNS through intracerebroventricular administration or delayed access to the CNS via BrMeI. Our findings demonstrate that the coordinated actions of both CNS and peripheral D2-like receptors are required for correcting dysglycemia. Ultimately, the development of a first-generation of drugs designed to selectively target the periphery provides a blueprint for dissecting mechanisms of central versus peripheral DA signaling and paves the way for novel strategies to treat dysglycemia.

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Section: Mei Analogues Modify Glucose-stimulated Insulin Secretionmentioning

confidence: 99%

Development of novel tools for dissection of central versus peripheral dopamine D₂-like receptor signaling in dysglycemia

Bonifazi,

Ellenberger,

Farino

et al. 2024

Preprint

View full text Add to dashboard Cite

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An electrochemical dopamine aptasensor using the modified Au electrode with spindle-shaped gold nanostructure

Taheri

Eskandari

Negahdary

2018

Microchemical Journal

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Fluorescence Fluctuation Spectroscopy of Dopaminergic Signaling in Pancreatic Beta Cells

Cited by 2 publications

References 0 publications

Development of novel tools for dissection of central versus peripheral dopamine D₂-like receptor signaling in dysglycemia

Development of novel tools for dissection of central versus peripheral dopamine D₂-like receptor signaling in dysglycemia

An electrochemical dopamine aptasensor using the modified Au electrode with spindle-shaped gold nanostructure

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Fluorescence Fluctuation Spectroscopy of Dopaminergic Signaling in Pancreatic Beta Cells

Cited by 2 publications

References 0 publications

Development of novel tools for dissection of central versus peripheral dopamine D2-like receptor signaling in dysglycemia

Development of novel tools for dissection of central versus peripheral dopamine D2-like receptor signaling in dysglycemia

An electrochemical dopamine aptasensor using the modified Au electrode with spindle-shaped gold nanostructure

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Product

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Development of novel tools for dissection of central versus peripheral dopamine D₂-like receptor signaling in dysglycemia

Development of novel tools for dissection of central versus peripheral dopamine D₂-like receptor signaling in dysglycemia