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Metergoline - Serotonin Antagonist & Dopamine Agonist For R&D

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

  1. Quality

    Quality Member

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    Has anyone tried to stop using it for a few days after use yet? Are there any form of come downs?
    Also to Haidut, how do you feel metergoline would affect the serotonin receptors? down or upregulation, ive read that serotonin receptors are kinda odd and dont always upregulate when using receptor blockers.
     
  2. OP
    haidut

    haidut Member

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    Unlike cyproheptadine, I have not seen studies with metergoline showing it upregulates the serotonin receptors it antagonizes. So, yes, some chemicals acting as antagonists may not upregulate receptor density. But it could be just that metergoline is not a very widely used chemical so it has not been discovered yet. I personally like metergoline a lot more then ritanserin and cypro even though their subjective effects are quite distinct.
     
  3. Pointless

    Pointless Member

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    Acute and chronic effects of serotonin (5HT) antagonists on serotonin binding sites. - PubMed - NCBI
     
  4. OP
    haidut

    haidut Member

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    Thanks. Interestingly, in the acute administration test metergoline was the only drug that did not affect receptor density.

    "...The administration of 14 daily doses of cyproheptadine, BC-105, metergoline and methysergide induced a marked decrease in the number (Bmax) of 3H-spiroperidol binding sites (5HT2 sites) in frontal cortex, when assayed 48 h after the last dose; the apparent affinity (KD) of 3H-spiroperidol was not changed. The same treatment schedules failed to modify the KD and Bmax values for 3H-5HT binding to the 5HT1 site in the hippocampus. Cyproheptadine, BC-105 and methysergide, but not metergoline, decreased the density of 5HT2 sites in frontal cortex 48 h after a single dose."
     
  5. Brooks Esq.

    Brooks Esq. Member

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    Hello, I'am brand new to this forum and was hoping you guys could field a couple questions for me. I just purchased some Metergoline for research purposes, I study Post-SSRI Side effects.
    1. Does Metergoline have any specific affect on 5ht1A Serotonin Receptors? I have had difficulty locating any data to support that it can in fact antagonize this particular receptor, I was optimistic it would.
    2. Does Metergoline cause fatigue, or cause any delay in cognitive/memory function? Thank you in advance for answering my questions.
     
  6. Pointless

    Pointless Member

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    Here's an example study from the first page. Stimulation of serotonin1A receptors increases release of prolactin in the rat. - PubMed - NCBI It's about prolactin secretion increased by 5-HT1 agonists and decreased by antagonists including Metergoline. The binding profile was posted on the first page, also, about half way down the page. It's just the affinity, but we know that it's an antagonist. If you're looking for more information on its receptor activity, you'll have to dive into the studies for yourself.

    Quite the opposite. In general, it causes mental clarity. It feels like methylene blue.

    I think you could've found these answers just by reading the thread. There's a lot of reading expected here.
     
  7. khismet

    khismet Member

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    24 hrs later, still in a bliss bubble from one dose. Have to remind myself to eat as I'm feeling fine w very little food. Prefer napping to long sleep cycles.
     
  8. Brooks Esq.

    Brooks Esq. Member

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    Thank you very much for your correspondence. I did read this thread very thoroughly prior to asking my question. I also did some Pubmed researching. I found the study you are referring too with the 5ht1a agonists and prolactin. I understand Metergoline lowered the prolactin caused by the 1a agonist, but I was unsure if that was due to the serotonin antagonism or dopamine agonism. Cabergoline can also lower prolactin, but its effect is due to dopamine agonism. I just didnt know if somebody else maybe stumbled across something I didn't regarding 5ht1a.
    And thank you for also answering my questions regarding mental clarity.
     
  9. Quality

    Quality Member

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    Caber is also a pretty good 5ht1a agonist, this is why theres quite alot of people out there saying caber does not increase their libido.
    Ive experimented with it, some mixed results, takes about 1-2 weeks to somewhat build in your system, it definatly raises T though mine gone through the roof on it, I can attest to that as I had blood taken at the time, but T and libido are not always the same.
    For me personality, it made too arrogant, I felt superior to everything and everyone, I absolutely hated it and had not much desire to have sex with women, eventhough my T was very high at the time..
     
  10. Quality

    Quality Member

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    Will be ordering this tomorrow when I up my prepaid creditcard.
    What would be the best way recommended to take it, empty stomach? sublingual?
     
  11. OP
    haidut

    haidut Member

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    People experimenting on rats usually apply topically, but if you read through the thread you will find other testimonials as well.
     
  12. Quality

    Quality Member

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    Uhmmmm I never done any topical things before besides magnesium oil, how would you recommend using it? like on the wrists where the skin is thin? also, just let it dry completely? need some more info tbh.

    Khismet, would you mind sharing how it was dosed?
     
  13. OP
    haidut

    haidut Member

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    If you read through the thread you will find everything you need to know. Nothing complicated about it. And please do not ask about human application, the chemical is marketed for research/lab use only.
     
  14. Quality

    Quality Member

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    Well im trying to buy something...?
     
  15. Orion

    Orion Member

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    Put drops on your rats wrists and inside elbow, I find at the rats hip is nice too.
     
  16. Quality

    Quality Member

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    Thanks bud, thats all I wanted to know, Im new to this :)
     
  17. Orion

    Orion Member

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    No worries, can be daunting to read through the vast amount of posts and all the comments when getting started. Been a year for me and still digesting!
     
  18. cardochav

    cardochav Member

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    Haidut, do you see anything wrong with taking five drops in the morning and five drops at night to get about 2 mg in the morning and 2 mg at night? this would be daily long term. or is the half life long enough to take a single dose daily?
     
  19. Quality

    Quality Member

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    Im sure this would mess with your rats sleeping patern though? serotonin is necessary for melatonin production.
    Its all about balance imo, anyway you can try it once on your rat once and report back to us, but by reading some experiences of other people who tested it on their rats I doubt dosing late afternoon/evening would be a good idea.
    Metergoline apparantly has an half-life of about 11-12 hours, so plenty would still be in your rats system if you was to dose then.
     
  20. OP
    haidut

    haidut Member

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    I don't think it matter much, but given that serotonin rises at night it is probably a good idea to administer a bit before bed (as shown by the cypro studies). Whether it is done as a single larger dose or as a portion of a daily dose split throughout the day depends on the individual. Some people like the energy boosting effects it gives their rats when used in the morning and other like the serotonin, prolactin, and cortisol antagonism when used at night when there hormones/amines rise. Both use scenarios are valid. There is no single optimal regimen or dose for every rat.
     
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