Review of GHRH-Related Compounds
GHRH: Natural 44-amino-acid peptide hormone that stimulates GH secretion in humans. All GHRH family drugs are based on this.
GRF 1 -29: Better known as sermorelin.This is a spliced form of GHRH, consisting of its active 29-amino-acid sequence.
Mod GRF 1-29: This is GRF 1-29 (sermorelin) with four amino acid substitutions. It is also known as a tetrasubstituted GRF 1-29.
CJC-1295: This is Mod GRF 1 -29 (tetrasubstituted GRF 1 -29) with an added Drug Affinity Complex (DAC) to extend its half-life.
MOD GRF 1-29 Key Points
- Very Short Acting.
- Moderate Effect on GH
- No Effect on Cortisol, Prolactin
MOD GRF 1-29 History
Mod GRF 1-29 was first described in 2005 by Jette et al. This drug is ultimately based on a much earlier discovery about growth hormone releasing hormone (GHRH), namely that its full pharmacological activity is retained in its terminal segment of 29 amino acids. This led to the development of numerous truncated analogs. First, the active 29 amino acids of GHRH were synthesized in a compound called GRF 1-29. Today we know it as sermorelin, an approved drug product. Though viable, scientists still struggled with its short half-life, and continued to seek out alternatives.
Jette et al sought to further modify the 29 amino acids that make up sermorelin in ways that might reduce its tendency for cleavage, yet still retain biological activity as a GH secretagogue. A tetrasubstituted derivative called CJC-1295 was one of the most promising compounds to result from their work. This is the same peptide Mod GRF 1-29 that is described here, but with an additional Drug Affinity Complex to slow its distribution. Subsequent work on this substance continued as CJC-1295. Documentation on actual Mod GRF 1-29 is hard to come by. Neither form of this peptide is presently an approved drug product, in spite of some favorable early human studies. Its potential future as a pharmaceutical agent, likewise, remains unclear.
Mod GRF 1-29 is on the World Anti-Doping Agency's (WADA) list of prohibited substances. Methods for detecting the misuse of this compound are available.
Structural Characteristics MOD GRF 1-29
Mod GRF 1-29 is a tetrasubstituted analog of growth hormone releasing fragment 1-29 (GRF 1-29, sermorelin). Its full structural sequence is: Tyr-D-Ala-Asp-Ala-lle-Phe-Thr-GIn-Ser-Tyr-Arg-Lys-Val-Leu-Ala-GIn-Leu-Ser-Ala-Arg-Lys-Leu-Leu-Gln-Asp-lle-Leu-Ser-Arg-NFI2. Four substitutions to GRF 1 -29 create this new peptide: D-Ala at the 2-position, Gin at the 8-position, Ala at position 15,and Leu at position 27. These modifications reduce this compound's susceptibility to enzymatic breakdown, and increase its bioactivity. Still, Mod GRF 1-29 has a short half-life, which usually necessitates administering the drug several times per day for optimal effect.
MOD GRF 1-29 Warnings
Mod GRF 1-29 is an unapproved new drug. A thorough understanding of its safety and propensity for side effects in humans is lacking at this time.
Obesity, uncontrolled hypothyroidism, hyperglycemia, or elevated plasma fatty acids may impair the effectiveness of Mod GRF 1-29. This drug should never be used during pregnancy, with cancer, a history of cancer, diabetic retinopathy, sclerosing diseases of the liver or lungs, intracranial hypertension, or uncontrolled diabetes.
How is MOD GRF 1-29 Supplied
This drug is not available as a pharmaceutical product. Standard dosage information is unavailable.
Mod GRF 1-29 can be purchased as a research compound or gray market supplement only. It is typically supplied in multi-dose vials containing 2 mg of dry lyophilized powder. This must be reconstituted with saline or bacteriostatic water before use. All unused portions of this drug should be kept under refrigeration.
MOD GRF 1-29 Side Effects (General)
Common side effects to Mod GRF 1-29 include flushing, warmth, dizziness, and transient hypotension following injection. Other common side effects include sleepiness, headache, diarrhea, nausea, and abdominal pain. Also frequently reported are adverse effects typically associated with other types of growth hormone therapy, such as water retention (edema), joint pain (arthralgias), carpal tunnel syndrome, and numbness or tingling in the extremities. Note that the incidence of GH-related side effects tends to be lower with GHRP therapy as compared to traditional hGFI. This is because GFI/IGF-1 release is subject to the limits of endogenous synthesis, and as such the drug is less amenable to overdosing.
MOD GRF 1-29 Side Effects (Injection site)
The subcutaneous administration of this drug may cause redness, itching, pain, or lumps at the site of injection.
MOD GRF 1-29 Administration
Mod GRF 1-29 may be given by subcutaneous injection, intramuscular injection, or IV infusion. The subcutaneous route is most often applied.
This drug has not been approved for use in humans. Prescribing guidelines are unavailable.
When used for physique- or performance-enhancing purposes, Mod GRF 1-29 is generally administered at a dosage of 50-100 meg. This is given 1-3 times per day. If single episode dosing is preferred, this is taken before sleep. Day dose(s) are taken on an empty stomach, 30-60 minutes before feeding. This is to preserve optimal GH release, as elevated plasma fatty acids and/or glucose may blunt the GH elevating effects of Mod GRF 1 -29.Total daily dosage generally does not exceed 300 meg.
Cycles of Mod GRF 1-29 usually last 3-4 months, though programs of 6 months or longer are not uncommon.
MOD GRF 1-29 Combination Therapy
Mod GRF 1-29 (a GHRH family drug) is usually combined with a drug from the GHRP (Growth Hormone Releasing Peptides) class, such as such as GHRP-2, GHRP-6, hexarelin, ipamorelin, or MK-677. These two drug types alter GH release through distinct and complimentary mechanisms. Such combination therapy tends to produce substantial synergy with regard to GH release. When another short acting GHRP peptide is used with Mod GRF 1-29, the two are generally administered at the same time to maximize the resulting GH peak.
MOD GRF 1-29 Availability
Mod GRF 1-29 is not available as a prescription drug product. It is sold exclusively as a "research compound" or gray market supplement. Note that the quality of gray market products can be difficult to assure.
References
Wlliam Llewellyn (2017) - Anabolics