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Ghrelin agonists

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Deleted member 170540

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I thought I should make a thread about this, because it looks interesting and has not been discussed before... Ghrelin is a peptide that is produced in the stomach and takes part in the regulation of appetite and food intake. There are ghrelin receptors (GHSR receptors) in several parts of the CNS, including the mesolimbic dopamine pathway.

Systemically administered ghrelin has been shown to increase accumbal dopamine, induce conditioned place preference and locomotor stimulation and increase novelty-seeking behavior (sounds similar to the effects of amphetamines): http://www.ncbi.nlm.nih.gov/pubmed/18782383
http://www.ncbi.nlm.nih.gov/pubmed/23227170

Ghrelin also seems to have a nootropic effect: http://www.ncbi.nlm.nih.gov/pubmed/16491079

One effect of ghrelin is the stimulation of growth hormone secretion. Several synthetic GHSR agonists have been made for this purpose, and there have even been concerns that they might be used as performance-enhancing drugs by athletes: see, for example http://en.wikipedia.org/wiki/SM-130,686 .

A psychostimulant that's also a nootropic and has an anabolic effect sounds definitely interesting... Anyone know what kind of side-effects were found in the clinical trials of the growth-hormone release stimulators?
 
There is a significant effect on bone growth with long term increases in GH, this is part of a endocrine condition called arcromegaly which can cause serious facial changes and jaw problems
http://en.wikipedia.org/wiki/Acromegaly

Interesting concept, but not something you'd want to guinea pig yourself with raw ghrelin IV, I haven't read up much on the other ghrelin receptor ligands however.
 
^ Ghrelin mimetics like capromorelin have been tested in some clinical trials for increasing appetite and muscle mass in elderly people who are in poor physical condition. Unfortunately, the articles about the trials don't mention anything about CNS effects like elevated mood or cognitive enhancement.

Some RC vendors seem to be selling ghrelin mimetics, too. Apparently some bodybuilders are making themselves guinea pigs and using these compounds.
 
I know I'm not often found posting here (I lurk though) I can give you my experience with growth hormone releasing peptides.

Ghrp2- used approximately 100 mcg 2 daily subacute injections. In the course of a month of daily usage: better sleep, increase in lean body mass (increased muscle mass and decreased overall fat), more energy (possibly due to better sleep) and very slight hunger about 30 min post injection.

I am currently using Ghrp6 in combination with sermorelin (combined administration of a Ghrp and ghrh provides a multiplicative increase of serum gh levels.
I've been using this for approximately 3 weeks at the 100 mcg twice a day. The only difference between Ghrp2 and Ghrp6 Is that 6 provides an incredible increase of hunger about 30 min post injection.

There's a lot of info pertaining to gremlin mimicking peptides in bodybuilding and performance enhancing literature with a lot of first hand accounts and dosing protocols, etc. I believe there are a few threads in steroid discussion on the topic. Sorry if this is off topic/not the info you all were in search of.

Edit:
Administration of ghrps increase prolactin and cortisol levels to the "high normal range" as well as cause the usual hgh side effects such as water retention, sore joints, carpal tunnel syndrome, etc obviously due to the larger gh "pulses".
 
Thanks for the info Serotonin101, that was just what I was looking for. I was mainly interested in knowing how strong the stimulant/mood lifting effect of those compounds is in humans. Sounds like its rather mild. Probably good drugs for bodybuilding, though.

I also found out that here in Finland the government has recently classified the ghrelin mimetics as "compounds comparable to prescription medications", making it illegal to order them from internet sources. Too bad, I might even have tested them otherwise.
 
Don't get me wrong though. 100 mcg of Ghrp6 will induce a hunger resembling having not eaten for days in some people. My caloric intake when administering Ghrp6 can increase by 1000+kcals/day if so chosen. There are also ipamorelin which is weaker in action and can be "boomed" which means very high doses can be used with lesser diminishing returns on gh release along with less impact on cortisol and prolactin and also doesn't cause as much desensitization of the pituitary gland. Then there is also so hexarelin: the strongest Ghrp. Causes the most gh release but also impacts cortisol and prolactin the most. Hexarelin causes pituitary desensitization at all doses. Those two ghrps do not trigger the hunger mechanism as Ghrp2 and Ghrp6 do. I am not too knowledgeable of how gh release and grehlin are related.
 
Apparently, certain types of receptors are responsible for mediating the release of Gherlin. For instance - Muscarinic agonism causes secretion of Gherlin in the stomach. Apparently, this is why your stomach hurts when you haven't eaten in a while. Adrenergic receptors are an interesting phenomena though. According to the study - alpha-adrenergic agonism causes a decrease in Gherlin release (which explains it's appetite suppressing effects) while beta-adrenergic agonism actually increases Gherlin levels.

http://www.researchgate.net/publica...m_regulates_gastric_ghrelin_secretion_in_rats
http://www.ncbi.nlm.nih.gov/pubmed/19067721

That's quite fascinating because it was always thought that Adrenaline (which is the natural ligand of beta-adrenergic receptors) greatly suppressed appetite. One can assume that this means that Beta agonism attenuates the release of Dopamine as well as Acetylcholine.
 
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