Metergoline - Liquid Serotonin Antagonist For Lab/R&D

[Pointless]

Subject took 1 drop under the tongue, left it there for 15 seconds, and then swallowed. He felt nauseous for hours after that, so nausea might be a problem with oral administration.

 

[haidut]

Subject took 1 drop under the tongue, left it there for 15 seconds, and then swallowed. He felt nauseous for hours after that, so nausea might be a problem with oral administration.

Good to know, thanks.

 

[Jsaute21]

Good reviews, but am curious to the effects on pulse and how long it lasts.

 

[PUTFOT]

Interested in a dopamine agonist/ serotonin antagonist for cognitive improvement/euphoria/more happiness but still concerned with a few things that weren't yet clarified or consistent, receptor sensitivity loss, discontinuation, safety, weight gain reported by some, and not sure which one would be best for my goals.

 

[Jsaute21]

Good reviews, but am curious to the effects on pulse and how long it lasts.

Any comments on the cognitive effects of metergoline?

 

[whit]

Off the subject Regina but....
Air quality in the city is usually pretty poor. Exertion on top of that can really lower already low co2.
I'm no expert but what's the elevation of Chicago?
This might be a factor. A carbonated beverage might be in order or nebulized bicarb perhaps.

 

[Regina]

Off the subject Regina but....
Air quality in the city is usually pretty poor. Exertion on top of that can really lower already low co2.
I'm no expert but what's the elevation of Chicago?
This might be a factor. A carbonated beverage might be in order or nebulized bicarb perhaps.

Ah thx whit -
I've been thinking about that too. But cannot move. Chicago is cold; so we are stuck inside a lot. I've also had a lot of work on my house (which I work from and which gets very little natural light) in the last couple of years--so the ducts are ongoing polluted. lol Hard to resolve this. Construction makes me feel at home (I grew up in a family of builders). Open window weather is coming soon though. Time to make changes....

 

[fkj]

I have ordered my first batch and was hoping someone could give some advice on how to administer metergoline, be it orally, sublingual etc. It seems people have been experimenting different methods, is there an agreed preference?

Has anyone observed any cognitive improvements and sexual?

 

[whit]

Administered two drops to subjects hip 8am this morning with two drops stressnon.
Good motor control was observed and clairity.
Sleepiness was aparent within two hours.
Administered some food and coffee aspirin 10am still groggy.
Two more drops applied at dinner 5pm
More clarity without sleepiness.
Subject was hungry all day.
Will try different location/dose tomorrow.

 

[haidut]

Administered two drops to subjects hip 8am this morning with two drops stressnon.
Good motor control was observed and clairity.
Sleepiness was aparent within two hours.
Administered some food and coffee aspirin 10am still groggy.
Two more drops applied at dinner 5pm
More clarity without sleepiness.
Subject was hungry all day.
Will try different location/dose tomorrow.

Thanks for the feedback.

 

[khan]

Has anyone ordered metergoline to Nordic countries?

 

[Experienced]

This chemical metergoline is a very interesting substance and is a continuation of my search for chemicals that combine several beneficial characteristics into a single molecule/entity. Metergoline belongs to the same class of drugs as bromocriptine, lisuride, cabergoline, terguride, etc. However, unlike them it is a potent antagonist on the serotonin receptors 5-HT1, 5-HT2, 5-HT6, and 5-HT7. Most ergot drugs are agonists on those receptors with the possible (and partial) exception of lisuride. More importantly, just like lisuride metergoline is a potent antagonist on the dreaded 5-HT2B receptor. This endows it with anti-fibrotic properties similar to lisuride, terguride, ritanserin and cyproheptadine. In addition, unlike other serotonin antagonist that simply block serotonin receptors metergoline is actually capable of also reducing serotonin synthesis. The putative dopamine agonism is probably responsible at least partially for this effect. Furthermore, metergoline has been consistently shown to lower prolactin in humans and animal models, with effectiveness similar to bromocriptine when used in the same doses. Preliminary research suggests that metergoline is an agonist at the D2 receptor, which is not surprising given its similarity to lisuride, bromocriptine, etc. However, its exact dopamine receptor agonism profile is not well-known. What is even more interesting is that metergoline is capable of lowering prolactin through a (currently unknown) non-dopaminergic mechanism. So, it represents a viable alternative for experiments where lowering of prolactin is desirable but WITHOUT agonism (and potential downregulation) of dopamine receptors.
Some other interesting properties include ability to lower cortisol in doses as low as 2mg daily, improve insulin sensitivity in animal models, and act as a potent antidepressant in humans.
Finally, metergoline possesses potent activity against the Candida strain of fungi and especially the potentially lethal strain Candida krusei, which typically kills 50% - 60% of the people it infects and is naturally resistant to antifungals like fluconazole. As far as I know, metergoline is unique among all ergot derivatives in its anti-fungal properties.

Metergoline - Wikipedia, the free encyclopedia
metergoline (CHEBI:64216)
metergoline
"...Summary: A dopamine agonist and serotonin antagonist. It has been used similarly to BROMOCRIPTINE as a dopamine agonist and also for MIGRAINE DISORDERS therapy."

The units listed on the label are based on the studies that used metergoline in human and animal studies. In general, doses of metergoline found to have clinically meaningful effect are virtually the same as the doses for bromocriptine, which is in the range of 2mg - 4mg daily. In fact, both chemicals can be used together for an even more potent effect. Other dopamine agonists such as lisuride also synergize greatly with metergoline. However, please note that similar to the products sold by companies like BluePeptides, this product if for lab/research use only. The product can be ordered from the link below:
www.idealabsdc.com/lab

*******************************************************************************
Metergoline is a potent serotonin antagonist and putative dopamine agonist. As a serotonin antagonist it targets the 5-HT1, 5-HT2, 5-HT6, and 5-HT7 receptors but due to its general antiserotonin effects it is considered a non-specific serotonin antagonist just like cyproheptadine. The dopamine agonism profile of metergoline is not well-known except some evidence for D2 receptor agonism. Metergoline is capable of lowering prolactin through both dopaminergic and non-dopaminergic mechanisms and displays similar effectiveness to bromocriptine in the same dose range, and the two drugs are considered synergistic. One of the most interesting properties of metergoline is its antifungal activity against Candida strains, which are naturally resistant to anti-fungal drugs.

Units per container: about 30
Unit size: 8 drops
Each unit contains the following ingredients:

Metergoline: 3.3 mg

Other ingredients: DMSO, ethanol
*******************************************************************************

References:

Miscellaneous
https://www.ncbi.nlm.nih.gov/pubmed/24909513
The effects of metergoline and 8-OH-DPAT injections into arcuate nucleus and lateral hypothalamic area on feeding in female rats during the estrous... - PubMed - NCBI
Serotonin antagonist-induced lowering of prolactin secretion does not affect the pattern of pulsatile secretion of follicle-stimulating hormone and... - PubMed - NCBI
Serotoninergic modulation of sodium appetite in the rat. - PubMed - NCBI
Further evidence for an inhibitory role of central 5-HT in male rat sexual behavior. - PubMed - NCBI


Neurological/Brain
https://www.ncbi.nlm.nih.gov/pubmed/16921395
Naloxone and metergoline effects on growth hormone response to gamma-hydroxybutyric acid. - PubMed - NCBI
The effects of metergoline combined with PGF2alpha treatment on luteal function and gestation in pregnant ********. - PubMed - NCBI
Stimulation of serotonin1A receptors increases release of prolactin in the rat. - PubMed - NCBI
Does metergoline selectively attenuate 5-HT mediated prolactin release? - PubMed - NCBI
Metergoline abolishes the prolactin response to buspirone. - PubMed - NCBI
Activation of 5-HT 1 serotonin receptors in the medial basal hypothalamus stimulates prolactin secretion in the unanaesthetized rat. - PubMed - NCBI
Metergoline as an inhibitor of prolactin release. - PubMed - NCBI
The effect of metergoline on endocrine responses to L-tryptophan. - PubMed - NCBI
The behavioural effects of intravenously administered tryptamine in mice. - PubMed - NCBI
Serotonin initiates and autoamplifies its own synthesis during mouse central nervous system development. - PubMed - NCBI
Treatment of hyperprolactinemic amenorrhea with Metergoline. - PubMed - NCBI
Metergoline, pirenperone and pizotifen alter dopamine and 5-hydroxytryptamine synthesis in discrete rat brain nuclei. - PubMed - NCBI
Intolerance of bromocriptine: is metergoline a satisfactory alternative? - PubMed - NCBI
Metergoline as an alternative to bromocriptine in amenorrhoea. - PubMed - NCBI
Effect of metergoline on prolactin, follicle stimulating hormone, luteinizing hormone and thyroid stimulating hormone response to TRH and LHRH in n... - PubMed - NCBI
Treatment of hyperprolactinaemia with metergoline for periods up to 5 years: clinical and biological tolerability. - PubMed - NCBI
Metergoline as a lactation inhibitor. - PubMed - NCBI
Treatment of hyperprolactinemic states with different drugs: a study with bromocriptine, metergoline, and lisuride. - PubMed - NCBI
Metergoline and cyproheptadine suppress prolactin release by a non-5-hydroxytryptaminergic, non-dopaminergic mechanism. - PubMed - NCBI
Effect of metergoline on serum prolactin stimulated by TRH. - PubMed - NCBI
Prolactin suppression by serotonin antagonists in man: further evidence for serotoninergic control of prolactin secretion. - PubMed - NCBI
Growth hormone and prolactin release in acromegalic patients following metergoline administration. - PubMed - NCBI

https://www.ncbi.nlm.nih.gov/pubmed/3924253
"...As metergoline acts predominantly as a serotonin antagonist it might be expected to have additive or synergistic effects when combiend with bromocriptine. Although it has some dopaminergic activity, this is probably not the mechanism that suppressed prolactin. Interestingly, the prolactin concentration in one patient was reduced further when 2.5mg bromocriptine was added to treatment...Metergoline provides satisfactory treatment for many patients unable to tolerate bromocriptine and should beuseful in the management of hyperprolactinaemia either alone or combined with a small dose of bromocriptine."

https://www.ncbi.nlm.nih.gov/pubmed/662027 (MET decreases serotonin synthesis as well)
Metergoline inhibition of thyrotrophin and prolactin secretions in primary hypothyroidism. - PubMed - NCBI (prometabolic - lowers TRH)

Mood/Cognition/Behavior/Addiction
https://www.ncbi.nlm.nih.gov/pubmed/11910270
Regulation of Human Kv1.4 Channel Activity by the Antidepressant Metergoline. - PubMed - NCBI
Cocaine modulates mammalian circadian clock timing by decreasing serotonin transport in the SCN. - PubMed - NCBI
An investigation into the effects of 5-HT agonists and receptor antagonists on ethanol self-administration in the rat. - PubMed - NCBI
Metergoline antagonizes fluoxetine-induced suppression of food intake but not changes in the behavioural satiety sequence. - PubMed - NCBI
Metergoline potentiates natural feeding and antagonizes the anorectic action of medical hypothalamic 5-hydroxytryptamine. - PubMed - NCBI
Effects of 5-HT receptor antagonists on morphine-induced tolerance in mice. - PubMed - NCBI
Effects of serotonin and the serotonin blocker metergoline on meal patterns and macronutrient selection. - PubMed - NCBI
https://www.ncbi.nlm.nih.gov/pubmed/1615137
https://www.ncbi.nlm.nih.gov/pubmed/2018816
https://www.ncbi.nlm.nih.gov/pubmed/2378927
https://www.ncbi.nlm.nih.gov/pubmed/2812508
https://www.ncbi.nlm.nih.gov/pubmed/2799267
https://www.ncbi.nlm.nih.gov/pubmed/3148151
https://www.ncbi.nlm.nih.gov/pubmed/504319


CVD/Circulation/Hypertension/Calcification
https://www.ncbi.nlm.nih.gov/pubmed/2412045
https://www.ncbi.nlm.nih.gov/pubmed/6350721
https://www.ncbi.nlm.nih.gov/pubmed/6986577


Fibrosis/Cancer
https://www.ncbi.nlm.nih.gov/pubmed/7805767
https://www.ncbi.nlm.nih.gov/pubmed/8221698
https://www.ncbi.nlm.nih.gov/pubmed/3101016


Metabolism/Diabetes/Cortisol/Insulin/Obesity
https://www.ncbi.nlm.nih.gov/pubmed/499287
https://www.ncbi.nlm.nih.gov/pubmed/477605
https://www.ncbi.nlm.nih.gov/pubmed/21600959
https://www.ncbi.nlm.nih.gov/pubmed/9831297
https://www.ncbi.nlm.nih.gov/pubmed/8386213
https://www.ncbi.nlm.nih.gov/pubmed/1658112
https://www.ncbi.nlm.nih.gov/pubmed/2787501
https://www.ncbi.nlm.nih.gov/pubmed/2956114
https://www.ncbi.nlm.nih.gov/pubmed/181396
https://www.ncbi.nlm.nih.gov/pubmed/1149950

Digestion/GI
https://www.ncbi.nlm.nih.gov/pubmed/17965538
https://www.ncbi.nlm.nih.gov/pubmed/7932163


Immune/Antirival/Antibacterial/Antiparasitic
https://www.ncbi.nlm.nih.gov/pubmed/21354537
https://www.ncbi.nlm.nih.gov/pubmed/19538518
http://journals.plos.org/plosntds/article?id=10.1371/journal.pntd.0004063

they only have in NL Cabergoline ??

 

[haidut]

they only have in NL Cabergoline ??

Cabergoline is different and more similar to bromocriptine in effects. It is an agonist on 5-HT1 and 5-HT2B, while metergoline is an antagonist on both. As far as I know metegoline is the only pure serotonin antagonist from the ergot family, all others have some serotonin agonist activity.

 

[Experienced]

Cabergoline is different and more similar to bromocriptine in effects. It is an agonist on 5-HT1 and 5-HT2B, while metergoline is an antagonist on both. As far as I know metegoline is the only pure serotonin antagonist from the ergot family, all others have some serotonin agonist activity.

then there is only one option and thats ordering it from an worldwide shipping site any ideas? does Raw Carrot boost Dopamine and lower Serotonin because after eating heavy of raw carrots I notice that my prolactine is getting lowered

 

[haidut]

then there is only one option and thats ordering it from an worldwide shipping site any ideas? does Raw Carrot boost Dopamine and lower Serotonin because after eating heavy of raw carrots I notice that my prolactine is getting lowered

I don't know of any sources. The raw carrot can lower endotoxin, which lowers serotonin and prolactin and this may result in higher dopamine.

 

[Experienced]

I don't know of any sources. The raw carrot can lower endotoxin, which lowers serotonin and prolactin and this may result in higher dopamine.

owhkay thanks buddy as always you helped me with everything

 

[fkj]

Does anyone know if administering metergoline with agamelotine is safe/not safe?

Also - if anyone has any updates on their trials of metergoline I'd be grateful

Thanks

 

[PUTFOT]

Anybody get weight gain from metergoline?

 

[Bodhi]

Started today with 4 drops dissolved in some water and gave it orally to my Rat.
Before starting the experiment i decided to stop giving the Rat any other supplements i also stopped giving it thyroid.

The first thing i noticed is that the bottle is not the same as on the idealabs picture/ website, must say that this is the first dropper that drops pretty accurate.
Supplements like Tyronene, Tyromix, Kuinone and Retinil seemed very thin liquids and very hard to dose precisely so Metergoline drops very nicely.

Rat is what i call migraine sensitive (which means he gets symptoms of something which seems like a subclinical type of migraine, with mild migraine symptoms)
Also Rat suffers from a form of high sensitivity from external stimulation, feels very overwhelmed in crowds, and gets migraines after exercises.

Rat had a good lunch with eggs, OJ, oxtail stock wih seasalt.... Coffee with milk , took the drops after 1 hour.

I took the Rat outside to buy some shoes and see how Rat is doing in an extremely busy Saturday afternoon shop....
Rat felt some anxiety but i guess that was Placebo i noticed Rat was afraid that the Metergoline would create some freaky reaction...

Rat was making squeaky noises before entering the Rat Shoe Shop and the Rat seem to experience some mild Migraine like symptoms (weird acoustics inside it's head while squeaking).

When Rat was inside the shop it seemed no difference from other shopping experiences, it did notice slight increase in Libido and sexually interested (curious) even in female rats who usually do not attract this specimen...

After the shop i took Rat outside to walk trough the busy city centre and as me and my Rat live in the Netherlands most shopping streets have Belgian/French fry vendors and my Rat was jumping and craving for a big bag of Belgian fries with mayonnaise, raw onions, and peanut sauce..
I had to tame my rat not to let it indulge into this PUFA sin and decided to walk to a place where they sell beef stew Empanadas.
After giving my rat the amazingly good tasting Empanadas and two cappuccinos, rat started to feel very calm, warm and not too overstimulated in this very busy coffee place....
Rat did noticed slight enhanced anxiety when ordering and paying the bill while interacting with very attractive female rat, my rat even had a weird slip of its squeak (which happens sometimes before a migraine sets in) while communicating when asked if it was nice....

When me and my rat got home , my rat was craving sweet things and so i gave it to him...
Rat feels a bit exhausted like after a work out, it feels ok but notices a slight shiver on the right side of its head every now an then like a very mild pain in one spot... (migrainy like)
But it seems to go very quickly....

In about 30 minutes from here i will feed my Rat some wild salmon, with baked potatoes and Tzatziki yoghurt....

Rat is ok now but pretty tired and relaxed, see how Rat goes after dinner...

I decide to do a similar experiment tomorrow but increase the dose with 2 more drops.

 

[haidut]

Started today with 4 drops dissolved in some water and gave it orally to my Rat.
Before starting the experiment i decided to stop giving the Rat any other supplements i also stopped giving it thyroid.

The first thing i noticed is that the bottle is not the same as on the idealabs picture/ website, must say that this is the first dropper that drops pretty accurate.
Supplements like Tyronene, Tyromix, Kuinone and Retinil seemed very thin liquids and very hard to dose precisely so Metergoline drops very nicely.

Rat is what i call migraine sensitive (which means he gets symptoms of something which seems like a subclinical type of migraine, with mild migraine symptoms)
Also Rat suffers from a form of high sensitivity from external stimulation, feels very overwhelmed in crowds, and gets migraines after exercises.

Rat had a good lunch with eggs, OJ, oxtail stock wih seasalt.... Coffee with milk , took the drops after 1 hour.

I took the Rat outside to buy some shoes and see how Rat is doing in an extremely busy Saturday afternoon shop....
Rat felt some anxiety but i guess that was Placebo i noticed Rat was afraid that the Metergoline would create some freaky reaction...

Rat was making squeaky noises before entering the Rat Shoe Shop and the Rat seem to experience some mild Migraine like symptoms (weird acoustics inside it's head while squeaking).

When Rat was inside the shop it seemed no difference from other shopping experiences, it did notice slight increase in Libido and sexually interested (curious) even in female rats who usually do not attract this specimen...

After the shop i took Rat outside to walk trough the busy city centre and as me and my Rat live in the Netherlands most shopping streets have Belgian/French fry vendors and my Rat was jumping and craving for a big bag of Belgian fries with mayonnaise, raw onions, and peanut sauce..
I had to tame my rat not to let it indulge into this PUFA sin and decided to walk to a place where they sell beef stew Empanadas.
After giving my rat the amazingly good tasting Empanadas and two cappuccinos, rat started to feel very calm, warm and not too overstimulated in this very busy coffee place....
Rat did noticed slight enhanced anxiety when ordering and paying the bill while interacting with very attractive female rat, my rat even had a weird slip of its squeak (which happens sometimes before a migraine sets in) while communicating when asked if it was nice....

When me and my rat got home , my rat was craving sweet things and so i gave it to him...
Rat feels a bit exhausted like after a work out, it feels ok but notices a slight shiver on the right side of its head every now an then like a very mild pain in one spot... (migrainy like)
But it seems to go very quickly....

In about 30 minutes from here i will feed my Rat some wild salmon, with baked potatoes and Tzatziki yoghurt....

Rat is ok now but pretty tired and relaxed, see how Rat goes after dinner...

I decide to do a similar experiment tomorrow but increase the dose with 2 more drops.

Thanks!