Anamorelin - CAS 249921-19-5
Catalog number: 249921-19-5
Category: Inhibitor
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Anamorelin, also known as RC-1291 or ONO-7643, is the orally bioavailable, small-molecule ghrelin mimetic with appetite-stimulating and anabolic activities. Anamorelin binds to and stimulates the growth hormone secretagogue receptor (GHSR) centrally, thereby mimicking the appetite-stimulating and growth hormone-releasing effects of grhelin. Stimulation of GHSR may also reduce the production of the pro-inflammatory cytokines TNF-alpha and interleukin-6, which may play a direct role in cancer-related loss of appetite.
RC-1291; ONO-7643; RC1291; ONO7643; RC 1291; ONO 7643
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1.Evidence for partial pharmaceutical reversal of the cancer anorexia-cachexia syndrome: the case of anamorelin.
Anker SD1, Coats AJ2, Morley JE3. J Cachexia Sarcopenia Muscle. 2015 Dec;6(4):275-7. doi: 10.1002/jcsm.12063. Epub 2015 Aug 30.
A major component of the cancer anorexia-cachexia syndrome is a decline in food intake. Up until now none of the drugs that improve appetite also improve skeletal muscle. Recent studies have suggested that the oral ghrelin-analog, anamorelin, increased food intake and muscle mass. Unfortunately, it does not increase muscle power. Its regulatory future is uncertain, although it has important clinical effects.
2.Simplifying and expanding the screening for peptides <2 kDa by direct urine injection, liquid chromatography, and ion mobility mass spectrometry.
Thomas A1, Görgens C1, Guddat S1, Thieme D2, Dellanna F3, Schänzer W1, Thevis M1. J Sep Sci. 2016 Jan;39(2):333-41. doi: 10.1002/jssc.201501060. Epub 2015 Dec 15.
The analysis of low-molecular-mass peptides in doping controls has become a mandatory aspect in sports drug testing and, thus, the number of samples that has to be tested for these analytes has been steadily increasing. Several peptides <2 kDa with performance-enhancing properties are covered by the list of prohibited substances of the World Anti-Doping Agency including Desmopressin, LH-RH, Buserelin, Triptorelin, Leuprolide, GHRP-1, GHRP-2, GHRP-3, GHRP-4, GHRP-5,GHRP-6, Alexamorelin, Ipamorelin, Hexarelin, ARA-290, AOD-9604, TB-500 and Anamorelin. With the presented method employing direct urine injection into a liquid chromatograph followed by ion-mobility time-of-flight mass spectrometry, a facile, specific and sensitive assay for the aforementioned peptidic compounds is provided. The accomplished sensitivity allows for limits of detection between 50 and 500 pg/mL and thus covers the minimum required performance level of 2 ng/mL accordingly.
3.Mechanisms of anorexia-cachexia syndrome and rational for treatment with selective ghrelin receptor agonist.
Esposito A1, Criscitiello C1, Gelao L1, Pravettoni G2, Locatelli M1, Minchella I1, Di Leo M1, Liuzzi R1, Milani A1, Massaro M1, Curigliano G3. Cancer Treat Rev. 2015 Nov;41(9):793-7. doi: 10.1016/j.ctrv.2015.09.002. Epub 2015 Sep 11.
Cancer cachexia is a multi-organ, multifactorial and often irreversible syndrome affecting many patients with cancer. Cancer cachexia is invariably associated with weight loss, mainly from loss of skeletal muscle and body fat, conditioning a reduced quality of life due to asthenia, anorexia, anaemia and fatigue. Treatment options for treating cancer cachexia are limited. The approach is multimodal and may include: treatment of secondary gastrointestinal symptoms, nutritional treatments, drug, and non-drug treatments. Nutritional counselling and physical training may be beneficial in delaying or preventing the development of anorexia-cachexia. However, these interventions are limited in their effect, and no definitive pharmacological treatment is available to address the relevant components of the syndrome. Anamorelin is a first-in-class, orally active ghrelin receptor agonist that binds and stimulates the growth hormone secretagogue receptor centrally, thereby mimicking the appetite-enhancing and anabolic effects of ghrelin.
4.An open-label clinical trial of the effects of age and gender on the pharmacodynamics, pharmacokinetics and safety of the ghrelin receptor agonist anamorelin.
Leese PT1, Trang JM2, Blum RA3, de Groot E4. Clin Pharmacol Drug Dev. 2015 Mar;4(2):112-120. Epub 2015 Feb 9.
PURPOSE: To assess the effect of age and gender on the pharmacokinetics (PK) of the ghrelin receptor agonist anamorelin.
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