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
"...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:
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
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
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
"...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)
https://www.ncbi.nlm.nih.gov/pubmed/627092 (prometabolic - lowers TRH)
Just wanted to say that the first batch we have is limited, so please don't get mad if we run out over the weekend There is a federal holiday on Monday in the USA and that can delay shipments. Doing our best to avoid interruptions but just wanted to let people know. Thanks for the understanding.