Metergoline - Liquid Serotonin Antagonist For Lab/R&D

[Momado965]

Did anyone notice weight loss on it?

 

[ecstatichamster]

Metergoline lowered iop for a relative suffering glaucoma. She couldn’t handle the sedation so switched medications.

 

[Wagner83]

Metergoline lowered iop for a relative suffering glaucoma. She couldn’t handle the sedation so switched medications.

I remember reading that, the relative had applied it next to the eye, was the IOP measured shortly after application?

 

[ecstatichamster]

I remember reading that, the relative had applied it next to the eye, was the IOP measured shortly after application?

Applied just in the orbit not on the eyeball. Yes iop measured often, before and after application.

 

[Wagner83]

Applied just in the orbit not on the eyeball. Yes iop measured often, before and after application.

Thank you.

______________________

Behavioural effects of long term inhibition of 5-hydroxytryptamine receptors using metergoline. - PubMed - NCBI

Spoiler: Abstract

J Physiol (Paris). 1981;77(2-3):385-8.
Behavioural effects of long term inhibition of 5-hydroxytryptamine receptors using metergoline.
Stolz JF, Marsden CA.
Abstract
1. Rats were treated with acute and chronic schedules of metergoline (2.5 mg/kg I.P. twice daily) and acutely with dl-propranolol (15 mg/kg), amitriptyline (12.5 mg/kg) and fluoxetine (2 mg/kg). 2. Metergoline given both acutely and chronically blocked the behavioural response to the 5-hydroxytryptamine receptor agonist 5-methoxy-N1, N1-dimethyltryptamine (5MeODMT) (2.5 mg/kg I.P.). The response to 5MeODMT) was also blocked by acute administration of dl-propranolol and amitriptyline, but not fluoxetine. 3. Rats given chronic treatment with metergoline and then withdrawn from drug treatment for 3 days showed an enhanced response to 5MeODMT. 4. Chronic metergoline treatment caused an increase in ambulatory movement following 5MeODMT administration. 5. Exploratory behaviour, when measured under dark conditions, was reduced by chronic metergoline treatment. 6. The results suggest that supersensitivity to 5-hydroxytryptamine agonists can be induced by chronic treatment with an antagonist . Furthermore, metergoline and 5-methoxy-N1, N1-dimethyltryptamine may not act on identical receptor populations.

A few cases on metergoline are discussed:
https://europepmc.org/backend/ptpmcrender.fcgi?accid=PMC1415939&blobtype=pdf

Pharmacokinetics and bioavailability of metergoline in healthy volunteers after single i.v. and oral administration. - PubMed - NCBI

 

[haidut]

Yeah, and what could be causing that anxiety?

I am not answering because metergoline is sold as a lab chemical and I cannot discuss its use openly. In general, anxiety is sometimes experienced with anti-serotonin chemicals, especially when used on empty stomach. How long ago did you stop the SSRI drugs? Some of them have withdrawal effects that last months. Did you tell your doctor about stopping them or did you just quit cold-turkey?

 

[haidut]

@haidut looking to start using a dopamine agonist either lisuride or metergoline? Which one would you recommend? Whats the difference that people generally notice? Also is it gpod or bad idea to combine any of these two with cyphroheptadine?
Thanks in advance!

I my experience, metergoline is milder and more of serotonin antagonist than lisuride. The latter seems to have some serotonergic effects and may cause insomnia in some people. It really depends on the need. Lisuride is probably much better at lowering prolactin, but the 2 molecules are very similar to each other.

 

[haidut]

@haidut
Something that has been confounding me about LSD. I don't feel like the "trip" per se is from serotonin agonism, but rather serotonin antagonism. As Alduous Huxley once said LSD removes the filters of perception or something along those lines and that is my experience. Doesn't make sense to me that serotonin agonism would lead to all of these beautiful/profound experiences. LSD mostly feels like heightened dopaminergic function to me and not something that is truly "psychedelic". Colors are more vibrant, my senses are sharper, sight, sound, taste, smell. You can see gas exchange in plants, your intuition is strong, and I once could see air hitting the wings of a plane as it was landing from a great distance. I do not feel like these were hallucinations per se, but rather my metabolic rate had been raised to a point that I was able to perceive things that normal 2018 stress does not allow. We know that the ergots especially LSD are a mixed bag, but their net effect is usually dopamine agonism. So, yes, I have had cypro cut a "trip" in the traditional sense. But, rather than cutting a trip in the beautiful profound sense, I think it is just blocking the stress response you can get from highly dopaminergic substances. It's kind of like what happens when you have too much coffee without food. I always make sure I have access to orange juice if I know I'm taking LSD, it keeps it from getting too stressful. Just my two cents :)

That is a very interesting point. I also don't think the serotonin agonism explains the trips as serotonin agonists induce psychosis in higher doses, which is something LSD does not and often can even treat it. So, just because it is an agonist on a serotonin receptor it does not mean it has systemic serotonergic effects. As you said, its dopamine agonism probably dominates and also some serotonin receptors form negative feedback for serotonin release so an agonist on them will decrease systemic serotonin burden. It is pity we know so little of LSD due to restrictions on research with it. Hopefully, now that Big Pharma has its eyes on it as a drug for so many conditions we will learn more...but at the price of LSD becoming a VERY expensive prescription drug with enforcement against its use probably intensifying greatly due to a push from Big Pharma to preserve profits from its "legal" sales.

 

[am00]

I my experience, metergoline is milder and more of serotonin antagonist than lisuride. The latter seems to have some serotonergic effects and may cause insomnia in some people. It really depends on the need. Lisuride is probably much better at lowering prolactin, but the 2 molecules are very similar to each other.

Thanks for answering, I quit metergoline after a week, since it was strong substance for me. Side effects were harsh and I couldn't take it. I started forskolin, and I feel more energetic, more aggressive even, which is a good thing because I don't fear confronting people as before.

 

[am00]

I am not answering because metergoline is sold as a lab chemical and I cannot discuss its use openly. In general, anxiety is sometimes experienced with anti-serotonin chemicals, especially when used on empty stomach. How long ago did you stop the SSRI drugs? Some of them have withdrawal effects that last months. Did you tell your doctor about stopping them or did you just quit cold-turkey?

I quit 7 yrs ago :) I quit cold turkey, because I had enough of visiting doctors and taking whatever they prescribe me (Lexapro was the worst of SSRI's I tried). I know I made a mistake, I should have taper off slowly and then see what consequences it brings along, but after 7 yrs, don't you think my brain should had adapt at least to some percentage of preSSRI state? At that time, I was anxious but without brain fog and libido problems. 31 yrs old. I started a new thread about NSAID which helps me a lot with anxiety, but creates stomach issues due to it's antiplatelet action - Dexketoprofen - NSAID Drug Eliminates My Anxiety Did you ever hear of this phenomenon?

 

[haidut]

I quit 7 yrs ago :) I quit cold turkey, because I had enough of visiting doctors and taking whatever they prescribe me (Lexapro was the worst of SSRI's I tried). I know I made a mistake, I should have taper off slowly and then see what consequences it brings along, but after 7 yrs, don't you think my brain should had adapt at least to some percentage of preSSRI state? At that time, I was anxious but without brain fog and libido problems. 31 yrs old. I started a new thread about NSAID which helps me a lot with anxiety, but creates stomach issues due to it's antiplatelet action - Dexketoprofen - NSAID Drug Eliminates My Anxiety Did you ever hear of this phenomenon?

Many NSAID drugs have anti-serotonin, anti-cortisol, and anti-estrogenic effects. Don't know much about ketoprofen but based on its structure I would not be surprised if it antagonizes the GR, and that would explain the anti-anxiety effects.

 

[am00]

Many NSAID drugs have anti-serotonin, anti-cortisol, and anti-estrogenic effects. Don't know much about ketoprofen but based on its structure I would not be surprised if it antagonizes the GR, and that would explain the anti-anxiety effects.

It's remarkable how it works fast and efficient. Unfortunately, I have bad stomachaches after taking this and I'm afraid of stomach bleeding.

 

[am00]

Btw, @haidut, what's influence of forskolin on dopamine? I know it enhances production of SERT. What's GR?

 

[haidut]

Btw, @haidut, what's influence of forskolin on dopamine? I know it enhances production of SERT. What's GR?

Not a fan of forskolin and don't know much about its dopamine effects.

 

[am00]

Not a fan of forskolin and don't know much about its dopamine effects.

What did you take with best effects?

 

[haidut]

What did you take with best effects?

Best effects for what?

 

[am00]

Anxiety, anhedonia, low libido. All of this that are symptoms of PSSD

 

[haidut]

Anxiety, anhedonia, low libido. All of this that are symptoms of PSSD

I don't have any of these issues, so can't provide much feedback. Personally, I like metergoline the best, mostly for its effects improving digestion.

 

[Ron J]

@haidut
Read all 32 pages and no one has reported weight gain; is it safe to say that it doesn't make you gain weight, unlike cypro?
And does the anti-fibrotic properties only reduce/halt further fibrosis, or can it reverse fibrosis prior to supplementation?

 

[haidut]

@haidut
Read all 32 pages and no one has reported weight gain; is it safe to say that it doesn't make you gain weight, unlike cypro?
And does the anti-fibrotic properties only reduce/halt further fibrosis, or can it reverse fibrosis prior to supplementation?

Yes, to the first question. This is one of the serotonin antagonists that is not known to lead to weight gain.
Can't legally answer the second question but 5-HT2B antagonists like terguride are currently in clinical trials for reversing as well as preventing fibrosis in organs.