Compound monograph
Anamorelin
Anamorelin is a nonpeptide small-molecule agonist at the ghrelin receptor, structurally unrelated to the peptide secretagogues that share its target.
01
Identity & nomenclature
Anamorelin is a nonpeptide small-molecule agonist at the ghrelin receptor, structurally unrelated to the peptide secretagogues that share its target.
The CAS recorded here is the parent free base. The hydrochloride requires separate salt accounting; chloride is not part of this formula. Describing anamorelin as a ghrelin mimetic says nothing about sequence homology with ghrelin, of which it has none.
Declared aliases and development codes: ONO-7643, RC-1291, ST-1291.
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Molecular properties
| Molecular formula | C31H42N6O3 |
|---|---|
| Molecular mass | 546.72 Da |
| CAS Registry Number | 249921-19-5 |
| PubChem CID | 9828911 |
| UNII | DD5RBA1NKF |
Not a conventional peptide and no sequence string is published here. A 3R-substituted piperidine-3-carbohydrazide bearing a benzyl group and an N,N',N'-trimethylhydrazide, acylated through a D-Trp-derived 2R centre and an Aib-derived aminoacyl unit. No lipid conjugation and no macrocycle.
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Structural characteristics
Receptor-bound structural work reports anamorelin behaving as a superagonist in the system studied, and separate structures place it alongside macimorelin in the same bifurcated binding pocket. A comparison across two assay formats found it a full agonist in both. 'Full agonist' versus 'superagonist' is a question of assay context, not two chemical identities; a single assay-independent intrinsic-activity or signalling-bias label is not established.
- trimethylhydrazide
- 2R and 3R stereocentres
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Molecular targets & mechanisms
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Analytical considerations
Matching molecular mass excludes neither epimers nor connectivity isomers, and a receptor activation assay cannot distinguish anamorelin from macimorelin or any other active ligand. NMR should establish the piperidine, hydrazide and aminoacyl connectivity, with a chiral method for the 2R and 3R centres. For hydrochloride material, quantify chloride independently rather than inferring it from the parent ion.
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Verified bibliography
- Molecular recognition of two approved drugs Macimorelin and Anamorelin by the growth hormone secretagogue receptor.current
Wang RL, Sun J, Liu H, Guo SM, Zhang Y, Hu W, Wang J, Liu H, Zhuang YW, Jiang Y, Xie X, Xu HE, Wang Y
Acta pharmacologica Sinica · 2025-06-20 · Journal Article
- The structure and function of the ghrelin receptor coding for drug actions.current
Shiimura Y, Im D, Tany R, Asada H, Kise R, Kurumiya E, Wakasugi-Masuho H, Yasuda S, Matsui K, Kishikawa JI, Kato T, Murata T, Kojima M, Iwata S, Masuho I
Nature structural & molecular biology · 2025-01-20 · Journal Article
- In vitro pharmacological characterization of growth hormone secretagogue receptor ligands using the dynamic mass redistribution and calcium mobilization assays.current
Sturaro C, Ruzza C, Ferrari F, Pola P, Argentieri M, Frezza A, Marzola E, Bettegazzi B, Cattaneo S, Pietra C, Malfacini D, Calò G
European journal of pharmacology · 2024-08-10 · Journal Article
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Methodology & citation verification
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