Potentially interesting new secretagogue MK-677

[phaeton66]

Fountain of Youth: Drug Restores Muscles | LiveScience

"The drug mimics the action of ghrelin, a peptide that stimulates a growth hormone called secretagogue receptor (GHSR). Drug developers are focusing on GHSR because it plays an important role in the regulation of growth hormone and appetite. They think it may prove to be an excellent treatment target for metabolic disorders such as those related to body weight and body composition. "


I think it's an oral, which would be a neat trick if it actually works.

[papapumpsd]

Fountain of Youth: Drug Restores Muscles | LiveScience

"The drug mimics the action of ghrelin, a peptide that stimulates a growth hormone called secretagogue receptor (GHSR). Drug developers are focusing on GHSR because it plays an important role in the regulation of growth hormone and appetite. They think it may prove to be an excellent treatment target for metabolic disorders such as those related to body weight and body composition. "


I think it's an oral, which would be a neat trick if it actually works.

This has been discussed. Orals, while they work, require very large quantities which are just not sensible when you can inject mcgs vs consume 50g.

[datBtrue]

Nice find phaeton66!

The article was weak but it references a new study where elderly were given MK-677 for one year.

I'm tired of reading DatBtrue's tired refrain so lets take a look at the Nov. 4th study in Annals of Internal Medicine and see if there is anything cool in it.

Okay they gave them 25mgs of MK-677 per day.

The "them" were 65 healthy adults (men, women receiving hormone replacement therapy, and women not receiving hormone replacement therapy) ranging from 60 to 81 years of age.

The results were "daily administration of MK-677 significantly increased growth hormone and insulin-like growth factor I levels to those of healthy young adults without serious adverse effects."

A graph tells the story:

Figure 2. Growth hormone (GH) and insulin-like growth factor I (IGF-I) levels at baseline and at 6 and 12 months, and a representative GH profile.

Growth hormone and IGF-I data were not normally distributed and were analyzed on the natural logarithmic scale. Line graphs show geometric means and 95% CIs.

A. Mean 24-hour GH levels. The dashed line indicates 24-hour mean GH level for young men and women combined (~1.3 µg/L). *P < 0.001 for MK-677 versus placebo.

B. Serum IGF-I levels. The lower dotted line indicates the lower limit of the IGF-I normal range for older adults (59 to 225 µg/L), and the upper dashed line indicates the lower limit in adults age 21 to 25 years (116 to 358 µg/L).

C. Representative 24-hour GH profile in a 70-year-old man with a body mass index of 23.2 kg/m2 who received MK-677 for 1 year. His 24-hour mean GH levels were 0.37, 1.0, and 0.86 µg/L at baseline, 6 months, and 12 months, respectively. The pulsatile pattern of GH secretion at baseline is maintained and enhanced at 6 and 12 months, primarily because of increased secretion per peak rather than peak frequency.

There is something new and really cool in that study! It took six months to build up but in the end GH & IGF-1 were elevated and remained so for the remainder of the year of continued use. As expected one month after discontinuing levels declined.

There was no demonstrated desensitization in this study.

The study: Effects of an Oral Ghrelin Mimetic on Body Composition and Clinical Outcomes in Healthy Older Adults, Ralf Nass, MD et al., Annals of Internal Medicine 4 November 2008 | Volume 149 Issue 9 | Pages 601-611

[babyblu]

This isnt new and it isnt a peptide either. But the studies do appear promising but unless you can convince a chinese supplier to manufacture, you wont ever see it.

bb

[papapumpsd]

My mistake. I thought I had covered this particular substance in another post (GHRP-2 / Ghrelin antagonist --> HGH benefits?). It was not MK-677 in that post.

But, in the above post, the participants did use an oral GH releaser dosed at a max. of 0.5mg/kg. So, if you're 200lbs, that is equivalent to ~91kg and the dose would have been 45.5mg of oral GH releaser. FYI only.

[datBtrue]

This isnt new and it isnt a peptide either. But the studies do appear promising but unless you can convince a chinese supplier to manufacture, you wont ever see it.

bb

You're right Blu its not new, its the molecular compound Roy Smith when he was at Merck spent a lot of time and money developing. It is a peptidyl mimetic modeled after the peptide GHRP-6. In fact they used reverse pharmacology on GHRP-6 (His-D-Trp-Ala-Trp-D-Phe-Lys-NH2) to develop these types of molecules.

This molecule was instrumental in leading to the discovery of the "growth hormone secretagogue receptor" GHS-R and eventually its natural ligan, Ghrelin.

This study is cool because the participants used MK-677 for a year successfully. In other shorter studies the benefits waned after a short period of time.

You're right Blu on all counts. I don't see any plans to make this derivative or the even beter Ipamorelin (peptide) molecular mimetics into a drug anytime soon.

GHRP-6 is itself about 2% orally bioactive, so you could orally take 5mgs to achieve a saturation dose (i.e. 100mcg if injected).


* - The full story of MK-677's development as reported by Roy Smith in 2005 can be read (for free) at: http://edrv.endojournals.org/cgi/content/full/26/3/346

[findnemo]

Maybe this stuff can be purchased from the Netherlands?

MK 677 - Ibutamoren mesylate

I searched the above and found a company in Holland that might sell it, but you have to contact them.

Can't post the link because of board rules.

[datBtrue]

Maybe this stuff can be purchased from the Netherlands?

MK 677 - Ibutamoren mesylate

I searched the above and found a company in Holland that might sell it, but you have to contact them.

Can't post the link because of board rules.

Keep in mind that this is simply a growth hormone secretagogue. This category includes all ghrelin-mimetics including the peptides GHRP-6, GHRP-1, GHRP-2, Hexarelin, Ipamorelin and the smaller molecular compounds such as MK-677.

They all act by binding to the GHS-R. So MK-677 doesn't get you anything more then say GHRP-6. Sure there is difference in effaciousness but that is easily equalized by adjusting doses.

Pick a GHRH (CJC-1295 or modified GRF(1-29) ) and add it to a GHS (a peptide or smaller molecule) and administer them together and you create a big GH pulse. Adjust the dose and you release all of the pituitary store.

Wait 3 hours when the pituitary is reloaded and do it again.

Repeat up to 8 times a day or as little as 3.

Thats it. You're not going to ever be able to suck out more GH than that ...and that turns out to be a lot.

So beyond that is the matter of convenience.

GHRP-6 is 2% orally bioactive so 5mgs will be equivalent to 100mcg injected.

25mgs-50mgs of MK677 is the oral dose for that molecule.

[findnemo]

So beyond that is the matter of convenience.

Exactly. One little pill/day compared to measuring doses, injecting 3 to 8x/day, ... Also, this oral has been around for more than 10yrs and seems fairly safe (from my initial research).

I'm going to contact them and see what they say.

[pumbertot]

Exactly. One little pill/day compared to measuring doses, injecting 3 to 8x/day, ... Also, this oral has been around for more than 10yrs and seems fairly safe (from my initial research).

I'm going to contact them and see what they say.

If regular injects bother you then you are in the wrong game. Take up lawn bowls or something.

Half the fun of taking AAS, peptides etc is injecting them. S.h.i.t just swallow one pill a day instead? NEVER!!!!!!!!!!

Ive just never understood spending extra money on oral supps than much cheaper and more effective injectables.

Rant over.

[papapumpsd]

If regular injects bother you then you are in the wrong game. Take up lawn bowls or something.

Half the fun of taking AAS, peptides etc is injecting them. S.h.i.t just swallow one pill a day instead? NEVER!!!!!!!!!!

Ive just never understood spending extra money on oral supps than much cheaper and more effective injectables.

Rant over.

What about high-stakes urban croquet?

[java568]

Exactly. One little pill/day compared to measuring doses, injecting 3 to 8x/day, ... Also, this oral has been around for more than 10yrs and seems fairly safe (from my initial research).

I'm going to contact them and see what they say.

Goodluck. I know what company you are referring to and they only sell to real research companies, not individuals. It will also cost you about $50/day.

[pumbertot]

Goodluck. I know what company you are referring to and they only sell to real research companies, not individuals. It will also cost you about $50/day.

Haha costs more per day than say 10 weeks of high dose ghrp6.
Just like I was saying, enjoy burning money for less effect.

[datBtrue]

Half the fun of taking AAS, peptides etc is injecting them. S.h.i.t just swallow one pill a day instead? NEVER!!!!!!!!!!

Let me introduce you to "half the fun" caverject then.

[babyblu]

There was one UG that claimed to have MK but the man behind that operation was a crazed drug addict, popped in ORD, and known snitch, so I doubt he really had the goods (but then again he was one of those crazed genius types too).

The pharm companies have NO incentive to produce MK; with all the horrible press HGH has gotten, unless someone figures out MK677 saves the lives of midgets or something ridicuously beneficial to mankind, then forget about it. I am surprised the chinese havent started producing this one.

bb

[pumbertot]

There was one UG that claimed to have MK but the man behind that operation was a crazed drug addict, popped in ORD, and known snitch, so I doubt he really had the goods (but then again he was one of those crazed genius types too).

The pharm companies have NO incentive to produce MK; with all the horrible press HGH has gotten, unless someone figures out MK677 saves the lives of midgets or something ridicuously beneficial to mankind, then forget about it. I am surprised the chinese havent started producing this one.

bb

Saving the lives of midgets is important how exactly?

Screw that Dat, they should make the needles bigger gauge instead.

[phaeton66]

The pharm companies have NO incentive to produce MK; with all the horrible press HGH has gotten, unless someone figures out MK677 saves the lives of midgets or something ridicuously beneficial to mankind, then forget about it. I am surprised the chinese havent started producing this one.

I was kinda hoping to find out they already did. Ah well, interesting science stuff I ran across on a blog in any case. I don't really know anything about secretagogues; perhaps this will encourage me to learn more.

[jayice]

not to bring back a dead thread to life like frankenstein but this peptide is available now: http://www.gtgchem.com/MK-677-104.htm
so for anyone one still interested in it!