Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C45H55N9O6.2ClH |
Molecular Weight | 890.897 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 6 / 6 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.Cl.C[C@@H](N)C(=O)N[C@H](CC1=CC2=CC=CC=C2C=C1)C(=O)N[C@@H](C)C(=O)N[C@@H](CC3=CNC4=C3C=CC=C4)C(=O)N[C@H](CC5=CC=CC=C5)C(=O)N[C@@H](CCCCN)C(N)=O
InChI
InChIKey=ILOHMCCDCAUTQF-JESKXYQHSA-N
InChI=1S/C45H55N9O6.2ClH/c1-27(47)41(56)52-38(24-30-19-20-31-14-6-7-15-32(31)22-30)43(58)50-28(2)42(57)53-39(25-33-26-49-35-17-9-8-16-34(33)35)45(60)54-37(23-29-12-4-3-5-13-29)44(59)51-36(40(48)55)18-10-11-21-46;;/h3-9,12-17,19-20,22,26-28,36-39,49H,10-11,18,21,23-25,46-47H2,1-2H3,(H2,48,55)(H,50,58)(H,51,59)(H,52,56)(H,53,57)(H,54,60);2*1H/t27-,28+,36+,37-,38-,39+;;/m1../s1
Pralmorelin [GPA 748, GHRP 2, growth hormone-releasing peptide 2, KP-102 D, KP 102 LN] is an orally active, synthetic growth hormone-releasing peptide from a series of compounds that were developed by Polygen in Germany and Tulane University in the US. The use of pralmorelin as a diagnostic agent for GH deficiency is based on its ability to markedly increase plasma levels of GH in healthy subjects irrespectively of gender, obesity or age. However, in patients with GH deficiency, the effect of pralmorelin on GH levels is significantly lower compared with healthy controls. Pralmorelin is marketed under the brand name GHRP in Japan. It is used as a diagnostic agent in a single-dose formulation for the assessment of growth hormone deficiency (GHD). Pralmorelin (GHRP-2) acts to endogenously increase growth hormone release from the pituitary. With the increase of serum growth hormone, downstream effects occur. A notable hormone that is commonly used as a surrogate for growth hormone therapy, insulin like growth factor 1 (IGF-1), is known to increase with the infusion of GHRP-2. Administration of GHRP-2 results in amplification of the naturally occurring growth hormone secretion peaks, regulated by the hypothalamus and pituitary. After the release of growth hormone, a cascade of signaling events occurs in many body tissues, continuous exposure to growth hormone elicits long-term physiological changes. Of particular interest, especially in the case of the use of GHRP-2 as an alternative growth hormone therapy, hepatic production of IGF-1 occurs as result of endogenously released growth hormone from GHRP-2. GHRP-2 acts on the growth hormone secretagogue receptor (GHSR1a) in pituitary and hypothalamic tissues. The growth hormone secretagogue receptor (GHSR) is the natural receptor for the endogenous hormone Ghrelin, a stress hormone produced mainly by the lining of the stomach. This receptor among many other functions, controls and growth hormone release.
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL4616 Sources: https://www.ncbi.nlm.nih.gov/pubmed/9092793 |
9.3 null [pKi] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Diagnostic | GHRP Kaken 100 Approved UseAssessment of growth hormone deficiency (GHD) |
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/17609397
After overnight fasting, a 100 ug dose of GHRP-2 was administered intravenously.
Route of Administration:
Intravenous
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/15646370
In cultured primary rat anterior pituitary cells, Pralmorelin (KP-102)
(1 × 10(−11) − 1 × 10(−8) mol/l) dose-dependently increased the concentration of GH in the medium.
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Classification Tree | Code System | Code | ||
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NCI_THESAURUS |
C76358
Created by
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FDA ORPHAN DRUG |
372912
Created by
admin on Fri Dec 15 15:38:53 GMT 2023 , Edited by admin on Fri Dec 15 15:38:53 GMT 2023
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m9094
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HH-28
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158827-34-0
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CHEMBL106593
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C74356
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9940988
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R4AVR27MM8
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1492038
Created by
admin on Fri Dec 15 15:38:53 GMT 2023 , Edited by admin on Fri Dec 15 15:38:53 GMT 2023
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PRIMARY | RxNorm |
ACTIVE MOIETY
SUBSTANCE RECORD