Metergoline - Serotonin Antagonist & Dopamine Agonist For R&D

Discussion in 'IdeaLabs' started by haidut, Oct 7, 2016.

  1. haidut

    haidut Member

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    Yes, you want 5-HT1 and 5-HT2B antagonism. So, combining metergoline or cyproheptadine with lisuride or cabergoline should help neutralize some of those side effects. I even posted a study showing cypro fully prevented the fibrotic effects of 5-HT2B agonists like cabergoline. And yes, if metergoline half life is shorter it will have to be used more often to balance the effects of cabergoline. Or you can use cypro as it has a half life of up to 12 hours in most people.
     
  2. Chris1122

    Chris1122 Member

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    Great, thanks. I'll give it a try. Do you think NAC (N-Acetyl Cysteine) could help regulate excessive dopamine as well?
     
  3. haidut

    haidut Member

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    Have not look into this, but I would not use NAC as you usually have plenty cystein floating around. If you want to raise glutathione, simply take glycine as it combined with cysteine to form glutathione, and it lowers free cysteine in the process. I suspect this is one of the mechanisms behind glycine's beneficial effects on thyroid - inhibiting absorption of tryptophan, methionine and cysteine and ability to deplete body stored of methionine and cysteine.
     
  4. DennisX

    DennisX Member

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    Thanks. You mentioned in a metergoline post that metergoline has a half life of about 12h. So either metergoline or cyproheptadine would cancel out cabergoline's agonism of 5-HT2B? Would cypro be better or worse than metergoline for this cancellation?
     
  5. haidut

    haidut Member

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    Cypro has been studied directly for 5-HT2B cancellation so it has more evidence behind it. Metergoline SHOULD also work as it is know to be 5-HT2B antagonist as well but I don't have much in vivo evidence to back it up with.
     
  6. Stryker

    Stryker Member

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    "Metergoline (MCE), an ergoline derivative with anti-serotoninergic activity was used in rats to determine its effect on the release of prolactin (PRL) and, possibly, the mechanism(s) of this neuroendocrine effect. MCE given by oral, intraperitoneal or subcutaneous route to reserpinized male and female rats proved to be an effective and long-lasting anti-prolactin agent. MCE lowered PRL in hypophysectomized (hypox) rats bearing an ectopic anterior pituitary (AP) when administered parenterally but was completely ineffective when administered orally. In rats with CNS-AP disconnection, blockade of pituitary dopamine (DA) receptors by pimozide completely prevented the PRL-lowering effect of parenterally administered MCE"

    "The parietal peritoneum lines the abdominal wall and extends to the organs, whereas the visceral peritoneum covers the organs. The peritoneal cavity lies between these two peritoneal layers. It contains a thin layer of fluid that lubricates the peritoneal surfaces."

    Interesting....
     
  7. Mufasa

    Mufasa Member

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    Taking metergoline for 3 weeks. Im feeling better than ever, while putting more demands on my body than I have also ever done in my life (40 office programming hours a week). This product just seems a perfect with me. Taking 4-8 drops twice a day.

    One great thing about this, is that the effect seems to stay if I stop using it, like it is helping my body in a more fundamental way instead of a quick fix.

    I keep experimenting with this, but initial reaction is super super positive. Feeling more social, more energy to do stuff after work. I feel no need or very little need to recover in the weekend. I wake up earlier. I sleep in better. Feeling more calm and grounded. Digestion had improved last couple of days, really hope that stays. Feeling more confident.

    I could actually go on with stuff that seems to have improved noticably.

    Hope you keep offering this product @haidut! I like it better than ritanserin, after some time it felt like working less, and it became to feel a bit like what reminded me about ritalin.
     
  8. haidut

    haidut Member

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    Awesome, thanks for sharing! We should have it restocked this week.
     
  9. bruschi11

    bruschi11 Member

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    @Mufasa how long did you go without taking it without really having a rebound as you stated?

    Have you measured blood pressure on it compared to ritanserin?
    I'm trying to lower cortisol and thus systolic blood pressure and I read that ritanserin can be more stimulating.
     
  10. DennisX

    DennisX Member

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    Just curious if there are any studies that compare metergoline to cabergoline for prolatin antagonism. For instance would your best guess applying 3.3mg transdermal metergoline per day to my rat be equivalent to giving the rat 0.5mg of cabergolin twice a week?
     
  11. haidut

    haidut Member

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    The studies I have seen show that metergoline is only slightly less effective then bromocriptine at the same dose. So, 3.3mg metergoline will probably equal the effects of 2.5mg bromocriptine. Not sure if you can compare with cabergoline given the much longer half life of the latter but 2.5mg bromocriptine daily have been shown to cause similar drop in prolactin as 0.5mg cabergoline twice weekly.
     
  12. DennisX

    DennisX Member

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    Pramipexole has no binding affinities for 5HT2a,2b,2c, 5HT1a,1b,1d nor the D1 receptor and D5 receptor. It's an agonist for the D2 , D3 and D4 receptors with it's strongest affinity for the D3.
    With 1mg of prami, oral, my rat gets a very strong libido and very short refractory period. With 3.3mg of metergoline, transdermal, my rat feels nothing. @haidut what would be your opinion of why there is this difference of effects? 1mg prami per day is equivalent to 0.5 cabergoline twice a week for prolactin suppression.

    A caution to those who those who wish to try prami, the primi dose MUST be titrated for a week to 10days starting at 0.25mg, else very uncomfortable side effects will occur if one was to start at 1mg.


    @haidut, Question: Since oral prami has to go through the liver, would transdermal primi eliminate the side effects?
     
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