Sermorelin
Synthetic GHRH(1-29) analog for diagnosing and treating growth hormone deficiency in children.
Chemical Identity
| Property | Value |
|---|---|
| Chemical Formula | C149H246N44O42S |
| Molecular Weight | 3358 Da |
| CAS Number | 86168-78-7 |
| Peptide Class | GHRH Fragment (1-29) |
| Route | SC, IV |
Structure
Sermorelin (Geref) is the synthetic N-terminal 29-amino acid fragment of human GHRH, representing the minimum sequence required for full biological activity. It lacks the C-terminal extension of full-length GHRH(1-44) but retains complete receptor binding and activation capacity.
Mechanism of Action
Sermorelin binds GHRH receptors on pituitary somatotrophs, stimulating GH release through cAMP/PKA signaling. It preserves physiological pulsatile GH secretion patterns and is subject to negative feedback by IGF-1, making GH excess unlikely. It also preserves the normal somatostatin-GHRH regulatory axis.
Clinical Applications
- Growth hormone deficiency: Diagnostic stimulation test in children
- Pediatric GHD: Treatment when GH replacement not available or contraindicated
- Anti-aging medicine: Off-label use for GH decline
- Body composition: Investigational for sarcopenia
Pharmacokinetics
- Half-life: 12-19 minutes
- Onset: 15-30 minutes (GH peak at 30-60 minutes)
- Duration: 2-3 hours
- Metabolism: DPP-4 cleavage
- Route: SC or IV
Safety and Side Effects
Flushing, injection site reactions, headache, dysgeusia, and rarely allergic reactions. Preserves physiological GH regulation, reducing risk of GH excess. Contraindicated in pituitary tumors.
References
- Thorner, M.O., et al. (1989). Sermorelin for GH deficiency. Journal of Pediatrics, 115, 73-78.
- Prakash, A., & Goa, K.L. (1999). Sermorelin: a review. BioDrugs, 12, 139-157.
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