Ipamorelin Chemische Eigenschaften,Einsatz,Produktion Methoden
Beschreibung
Ipamorelin (INN) (developmental code name NNC 26-0161) is a peptide selective agonist of the ghrelin/growth hormone secretagogue receptor (GHS) and a growth hormone secretagogue.It is a pentapeptide with the amino acid sequence Aib-His-D-2-Nal-D-Phe-Lys-NH2 that was derived from GHRP-1.
Verwenden
Ipamorelin was originally developed by Novo Nordisk, and was investigated in phase II clinical trials by Helsinn Therapeutics for the treatment of postoperative ileus, but was discontinued due to lack of efficacy.Ipamorelin has been used by athletes as a performance enhancing drug.
Biochem/physiol Actions
Ipamorelin is a highly selective, potent pentapeptide (Aib-His-D-2-Nal-D-Phe-Lys-NH2) and gastrin mimetic with growth hormone (GH) releasing activity. It mimics gastrin and binds to the gastrin receptor (or growth hormone secretion receptor, GHSR) in the brain, which selectively stimulates the pituitary gland to release growth hormone. This leads to elevated plasma GH levels, which affects many biological processes. In addition to being found in the brain, GHSR is found in the gastrointestinal tract, heart, lungs, liver, kidneys, pancreas, adipose tissue and immune cells. Unlike other growth hormone releasing peptides, ipamorelin stimulates the release of growth hormone only in a manner very similar to that of growth hormone releasing hormone
[1].
Nebenwirkungen
Ipamorelin is generally considered safe and well tolerated, with common side effects including dizziness, headache, nausea, diarrhoea and flushing. Allergic or serious adverse reactions are rare.
Synthese
Ipamorelin was prepared from a total of 4.53 g of the peptide resin Boc-Aib-His (Trt)-D-2Nal-DPhe-Lys (Boc)-NH-resin according to the Fmoc strategy on an Applied Biosystems 431A peptide synthesizer in two identical runs (to obtain sufficient material) in 1 mmol scale using the FastMoc UV protocols supplied by the manufacturer, that employ HBTU mediated couplings in NMP and UV monitoring of the deprotection of the Fmoc protection group.
Ipamorelin Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
