| Identification | Back Directory | [Name]
Relamorelin | [CAS]
661472-41-9 | [Synonyms]
BIM28131
BIM28163
BIM-28163
BIM-28131
BIM 28131
BIM 28163
Relamorelin
661472-41-9
4-Piperidinecarboxamide, 3-benzo[b]thien-3-yl-N-(4-piperidinylcarbonyl)-D-alanyl-D-tryptophyl-L-phenylalanyl-4-amino-
4-[[(2S)-2-[[(2R)-2-[[(2R)-3-(1-benzothiophen-3-yl)-2-(piperidine-3-carbonylamino)propanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-3-phenylpropanoyl]amino]piperidine-4-carboxamide | [Molecular Formula]
C43H50N8O5S | [MDL Number]
MFCD30747945 | [MOL File]
661472-41-9.mol | [Molecular Weight]
790.97 |
| Hazard Information | Back Directory | [Uses]
Relamorelin (RM-131), a pentapeptide ghrelin analog, is a selective ghrelin/growth hormone secretagogue receptor (GHSR) agonist with a Ki of 0.42 nM for GHS-1a receptor. Relamorelin is centrally penetrant. Relamorelin increases growth hormone levels and accelerates gastric emptying. Relamorelin has the potential for cachexia, gastroparesis, and gastric/intestinal dysmobility disorders research[1][2][3][4]. | [in vivo]
Relamorelin (RM-131; 50-500 nmol/kg/day; s.c.; continuous infusion for 5 days) decreases the loss of body mass and fat mass. Relamorelin (500 nmol/kg/day; continuous infusion for 5 days) increases the food intake and weight gain in rats[1].
RM-131 (250-500?nmol/kg; a single s.c.) stimulates acute food intake in wt but not growth hormone secretagogue receptor (GHR) ko mice[2]. | Animal Model: | F344/NTacfBR male rats implanted with tumor[1] | | Dosage: | 50, 500 nmol/kg/day | | Administration: | SC; continuous infusion at a rate of 0.5 μL/h for 5 d | | Result: | Resulted in an increase in food intake (tumor/saline 41.4 g, tumor/BIM-28131 72.5 g) and weight gain (tumor/saline -10.3%, tumor/BIM-28131 +19.5%).
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| [References]
[1] DeBoer MD, et, al. Ghrelin treatment causes increased food intake and retention of lean body mass in a rat model of cancer cachexia. Endocrinology. 2007 Jun;148(6):3004-12. DOI:10.1210/en.2007-0016
[2] Fischer K, et, al. The Pentapeptide RM-131 Promotes Food Intake and Adiposity in Wildtype Mice but Not in Mice Lacking the Ghrelin Receptor. Front Nutr. 2015 Jan 12;1:31. DOI:10.3389/fnut.2014.00031
[3] Zatorski H, et, al. Relamorelin and other ghrelin receptor agonists - future options for gastroparesis, functional dyspepsia and proton pump inhibitors-resistant non-erosive reflux disease. J Physiol Pharmacol. 2017 Dec;68(6):797-805. PMID:29550791
[4] Matthew Heckroth, et al. Nausea and Vomiting in 2021: A Comprehensive Update. J Clin Gastroenterol. 2021 Apr 1;55(4):279-299. DOI:10.1097/MCG.0000000000001485
[5] Victor Chedid, et al. Relamorelin for the treatment of gastrointestinal motility disorders. Expert Opin Investig Drugs. 2017 Oct;26(10):1189-1197. DOI:10.1080/13543784.2017.1373088 |
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