Niacin Activates The G Protein Estrogen Receptor (GPER)-mediated Signalling

Kingpinguin

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Niacin - Wikipedia

”Both niacin and nicotinamide activate the G protein-coupled estrogen receptor(GPER) in vitro.”

Source:
https://www.sciencedirect.com/science/article/abs/pii/S0898656814001041?via=ihub




G protein coupled estrogen receptor:

”G protein-coupled estrogen receptor 1(GPER), also known as G protein-coupled receptor 30 (GPR30), is a protein that in humans is encoded by the GPER gene.[5] GPER binds to and is activated by the female sex hormone estradiol and is responsible for some of the rapid effects that estradiol has on cells.”

GPER - Wikipedia



So is niacin/nicotinamide estrogenic and bad or is the activation of estrogen receptors a good thing?
Likely none of those or maybe estrogen is good to a certain degree.

”Although GPER signaling was originally thought to be tumor-promoting in breast cancer,[40]subsequent reports suggest that nonclassical estrogen signaling is tumor suppressive in breast cancer.[41][42][43] Consistent with this, recent studies showed that the presence of GPER protein in human breast cancer biopsies correlates with longer survival, suggesting a tumor suppressive role.[44] In line with findings in breast cancer, GPER signaling has also been shown to be tumor suppressive in adrenocortical carcinoma,[45] colorectal cancer,[46] endometrial cancer,[47] Leydig cell tumors,[48] non-small cell lung cancer,[49]gastric cancer,[50] liver cancer,[51]melanoma,[52] osteosarcoma,[53] ovarian cancer,[54] and prostate cancer.[55] Together, these reports suggest that GPER is a tumor suppressor in a wide range of cancer types, and activation of GPER may represent a new therapeutic strategy to treat cancer.”


”It is speculated that activation of GPER may be the mechanism by which estradiol mediates rapid effects on the oxytocin system,[31][33] for instance, rapidly increasing oxytocin receptor expression.[34]Estradiol has also been found to increase oxytocin levels and release in the medial preoptic area.”




Normal male sexual function: emphasis on orgasm and ejaculation

”The main cerebral structures involved in erection are contained within the medial preoptic area (MPOA) and paraventricular nucleus (PVN) in the hypothalamus (6). Dopamine is the most important brain neurotransmitter for erection, likely through its stimulation of oxytocin release (7)”

So estrogen can increase oxytocin in the MPOA just like dopamine can and cause libido and erections.

Preoptic area - Wikipedia

”In male rats, the mPOA affects the consummatory phase of sexual behavior, and possibly motivation, with lesions causing a complete loss of copulatory behaviors.[9]Conversely, electrical stimulation of this area triggers male copulatory behavior, as measured by decreases in the latency to ejaculate.[10] Furthermore, testosteroneimplanted into the mPOA of castrated males completely restores mating, as long as aromatase is not inhibited.[11]






So this all means that estrogen is indeed necessary for libido and erections quality with adequate testosterone. And studies show that having good testosterone but low estrogen causes impotence in males. Studies also show that estrogen is needed for dopamine release in the MPOA which is the area of the brain responsible for sexual desire. Also estrogen is needed for proper cGMP which is needed for eNos and erections in general. Thus this all shows estrogen likely has some anti tumor properties to a certain degree and is needed for normal sexual function.

Altough my belief is not that one should strive to alter or boost their own estrogen as a man or even woman. My approach is that if you’re healthy and not overweight or showing symptoms of over expression of aromatase or estrogen in general I would not fiddle with AIs or supplements known to lower estrogen. Your body knows what it is doing if your in a healthy state and I would let it convert the estrogen from my testosterone as needed.
 
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