Are you looking to add to your muscle mass and build those biceps? If your answer is YES, then you should consider Sigma Pharmaceutical’s growth hormone secretagogues.
Growth hormone (HGH) is an effective anabolic hormone that promotes weight gain, linear growth, as well as body’s nitrogen retention. It has been seen that HGH therapy increases muscle mass in adult males. It is also considered to support protein addition in hypopituitary individuals.
Its anabolic potential is suggestive of its use in catabolic patients; in particular, catabolism brought about or increased in severity due to insufficient intake of calories. Growth hormone’s anabolic activity has been beneficial to partly revert the catabolic properties of energy restriction in diet, extreme energy exploitation by exercising vigorously, surgery, excess of glucocorticoids as well as aging.
Although recombinant human growth hormone is available, therapy using Human growth hormone (HGH) injection is expensive and needs a delivery system other than the oral route. Hence, GH secretagogues, some of which are bioavailable with oral use, such as MK 677, are utilized to incite endogenous GH secretion. These serve as cost-effective alternatives.
What Is MK 677 (Ibutamoren)?
MK-677, also called Ibutamoren Mesylate, is an effective GH secretagogue receptor (GHSR) agonist. It has a non-peptide structure and serves as an active GH secretagogue orally. Research in dogs has shown Ibutamoren mesylate brings about statistically significant upsurges in body weight and elevates levels of blood Insulin-like growth factor 1 (IGF-1) and GH while not significantly increasing their levels on days 7 or 15.
In another study, it was reported that chronic use of oral MK-0677 is linked to a substantial elevation of IGF-I and HGH, the concentrations of which are sustained during the treatment. The level of HGH post-MK677 administration shows sporadic rises as compared to the control.
Ibutamoren is found to significantly increase the peak GH profile after it is taken orally. Being a potent GH secretagogue, MK-677 stimulates an instant, hefty, and durable escalation in growth hormone levels with oral administration.
History Of The Compound
Bowers et al. synthesized Growth hormone-releasing peptide 6 (GHRP-6) first in 1977 among the serial analogs of enkephalin opiate that induced release of GH from the pituitary cells of rats, in vitro. The first found GH-releasing peptide was found to have a weak stimulatory effect on GH secretion.
Successively, it was reported that GHRPs stimulate HGH release by acting on the pituitary gland and the hypothalamus without disturbing the regular GH pathway’s negative feedback mechanisms.
However, extensive use of GHRPs clinically was narrow, partly due to the need for repeated dosing as well as its parenteral administration because of their short half-lives and inadequate bioavailability with oral administration; 20 minutes and 0.3% respectively for GHRP-6. [6] Hence, it was for the identification of a small-molecule drug with superior oral bioavailability and high strength, Merck (Kenilworth, NJ, USA) investigated non-peptide compounds having GHS potential in rat’s pituitary.
The growth hormone secretagogues (GHS) were then formulated through reverse pharmacology. The aim of their development was to create small molecules that have pharmacokinetics, which allow its one-time oral use per day (1tablet/day). This was believed to revitalize the GH/IGF-I alliance. Because both the receptor and the ligand controlling the hormone release pulse amplitude were not known, recognizing principal structures was done depending on function.
Therefore, L-692,429 or Ibutamoren was produced as a minor-sized peptidomimetic agonist for the Growth hormone-releasing peptide 6 (GHRP-6). While its bioavailability and serum half-life were greater as compared to GHRP-6, the general pharmacokinetic potential was not adequate for a single dose a day with oral administration.
The researchers’ persistent efforts lead to the modification of its structure that brought about the development of compound L163,191. This compound had a high oral bioavailability and was established to be GHS receptor-specific. Finally, no side effects were seen of L-163,191 for the duration of the 14-day research, and it clinically found itself as MK-0677, also called ibutamoren mesylate.
In humans, oral administration of ibutamoren healthy and GH-deficient adults or GH-deficient children elevates serum IGF-I, GH, and IGFBP-3 levels, serving as a potential therapy for growth disorders. Nevertheless, recurrent use of GHRP has been associated with desensitization of its inductive effects on the secretion of GH. Plus, there is no presence of studies confirming its growth-promoting potential with long-term use, hence limiting its clinical use. [8]
Benefits Of The MK-0677 (Ibutamoren) In Bodybuilding
Why ibutamoren is precious for bodybuilders is also reflected from its improvement in the lower extremity function after a hip fracture, reduced LDL (bad cholesterol), augmented REM sleep, and shortened sleep latency.
The key benefits it offers for bodybuilding and weight training are as follows:
- Enhanced muscle retention rates
- Superior water retention that supports muscle development and physique
- Development of muscle quality
- Augmented rate of muscle development and growth
Other benefits include increased bone density, improved cognitive activity, delay in the aging process, and accelerated healing process.
Side Effects Of Ibutamoren
The most common side effects of ibutamoren include:
- Increased appetite
- Temporary, minor edema in lower the extremities
- Muscle pain
- A transient rise in prolactin and cortisol
- Fluid retention
- Increased sensitivity to insulin
- Weight gain
How To Use Ibutamoren?
You need to know what dose and frequency of ibutamoren you should use to get an idea of when you will see its benefits. Data has shown that its optimal dose ranges from 20 to 25 mg/day. The half-life of ibutamoren is 24 hours, which means that taking it once per day is enough.
It has been shown that the higher its dosage, the superior the effects experienced. A study reported that taking 25 mg of MK-677 lead to a rise in serum IGF-1 levels by 60.1% at six weeks and 72.9% at one year.
Thus, you should use ibutamoren for extended periods, like 3 to 6 months, for it to add up in your system for the best results.
