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Decrease of prostaglandin E2 receptor binding is accompanied by reduced antilipolytic effects of prostaglandin E2 in

B Richelsen, H Beck-Nielsen

Journal of Lipid Research

|January 1, 1985

Summary

Prostaglandin E2 (PGE2) treatment of rat adipocytes reduces PGE2 binding, decreasing its antilipolytic effect. This suggests receptor occupancy rather than receptor loss may explain the reduced biological response to PGE2.

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Area of Science:

Endocrinology
Cell Biology
Lipid Metabolism

Background:

Prostaglandin E2 (PGE2) plays a role in regulating adipocyte function.
Understanding receptor dynamics is crucial for elucidating cellular responses to hormones.

Purpose of the Study:

To investigate the effect of PGE2 treatment on PGE2 receptor binding in isolated rat adipocytes.
To examine the antilipolytic effects of PGE2, adenosine, and insulin following PGE2 treatment.

Main Methods:

Isolated rat adipocytes were treated with prostaglandin E2 (PGE2).
Subsequent [3H]PGE2 binding assays were performed.
Scatchard analysis was used to evaluate receptor binding kinetics.
Antilipolytic effects were assessed in control and PGE2-treated adipocytes.

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Main Results:

PGE2 treatment significantly decreased [3H]PGE2 binding by 61%, attributed to a reduced number of PGE2 receptors.
The antilipolytic effect of PGE2 was significantly reduced by 45% in PGE2-treated adipocytes.
The antilipolytic effects of adenosine were partially reduced, while insulin's effect remained unchanged.

Conclusions:

PGE2-induced reduction in receptor binding may result from tight receptor coupling and occupancy, not necessarily receptor loss.
Desensitization of PGE2's antilipolytic effect is specific but not absolute.
Insulin's antilipolytic action is independent of PGE2-induced receptor changes.