Activation of the G-protein-coupled receptor GPR30 induces anxiogenic effects in mice, similar to oestradiol

蛋白偶联受体 GPR30 的激活会在小鼠中引起与雌二醇类似的焦虑效应

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作者:Iris Kastenberger, Christian Lutsch, Christoph Schwarzer

Conclusions

Our data suggest that GPR30 induces acute anxiogenic effects of oestrogen in rodents. It is tempting to speculate that a potential imbalance in the expression of the anxiolytic beta oestrogen receptor and the anxiogenic GPR30 may also be involved in the negative symptoms of oestrogen replacement therapy in humans.

Results

We provide evidence from mouse behavioural tests that oestrogen-induced anxiogenic-like effects might be mediated, at least in part, by the G protein-coupled receptor GPR30. The short-term application of specific agonists against the alpha and beta oestrogen receptors did not result in marked behavioural changes. In contrast, the specific stimulation of GPR30 in male and ovariectomized female mice induced anxiogenic effects. The anxiogenic effects induced by the specific GPR30 agonist G-1 were comparable (and non-accumulative) to those observed after low doses of the general oestrogen receptor agonist 17b-oestradiol in male mice, thereby reflecting the behavioural changes observed in intact female mice during early pro-oestrus. Conclusions: Our data suggest that GPR30 induces acute anxiogenic effects of oestrogen in rodents. It is tempting to speculate that a potential imbalance in the expression of the anxiolytic beta oestrogen receptor and the anxiogenic GPR30 may also be involved in the negative symptoms of oestrogen replacement therapy in humans.

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