Z-505, an Oral Ghrelin Receptor Agonist, Attenuates Anorexia After Total Gastrectomy in Rats

Shiomi, Yoshihiro; Yoshimura, Masashi; Hori, Yûko; Ohira, Yuta; Nagahama, Kenji; Ozaki, Tomoko; Takei, Makoto; Tanaka, Takao; Uno, Tomohide

doi:10.1016/j.jss.2019.09.035

Cited by 4 publications

(5 citation statements)

References 43 publications

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“…Des-acyl ghrelin directly inhibits the ARC in a ghrelin receptor-independent manner to impair the orexigenic effect of ghrelin [130]. A recent study showed that oral ghrelin receptor agonist (z-505) attenuates anorexia after total gastrectomy in rats [131].…”

Section: Appetite Regulationmentioning

confidence: 99%

Physiological Effect of Ghrelin on Body Systems

Akalu

Molla

Dessie

et al. 2020

International Journal of Endocrinology

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Ghrelin is a relatively novel multifaceted hormone that has been found to exert a plethora of physiological effects. In this review, we found/confirmed that ghrelin has effect on all body systems. It induces appetite; promotes the use of carbohydrates as a source of fuel while sparing fat; inhibits lipid oxidation and promotes lipogenesis; stimulates the gastric acid secretion and motility; improves cardiac performance; decreases blood pressure; and protects the kidneys, heart, and brain. Ghrelin is important for learning, memory, cognition, reward, sleep, taste sensation, olfaction, and sniffing. It has sympatholytic, analgesic, antimicrobial, antifibrotic, and osteogenic effects. Moreover, ghrelin makes the skeletal muscle more excitable and stimulates its regeneration following injury; delays puberty; promotes fetal lung development; decreases thyroid hormone and testosterone; stimulates release of growth hormone, prolactin, glucagon, adrenocorticotropic hormone, cortisol, vasopressin, and oxytocin; inhibits insulin release; and promotes wound healing. Ghrelin protects the body by different mechanisms including inhibition of unwanted inflammation and induction of autophagy. Having a clear understanding of the ghrelin effect in each system has therapeutic implications. Future studies are necessary to elucidate the molecular mechanisms of ghrelin actions as well as its application as a GHSR agonist to treat most common diseases in each system without any paradoxical outcomes on the other systems.

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Section: Appetite Regulationmentioning

confidence: 99%

Physiological Effect of Ghrelin on Body Systems

Akalu

Molla

Dessie

et al. 2020

International Journal of Endocrinology

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“…Serotonin, a neurotransmitter synthesized from tryptophan, is often thought to play a vital role in vomiting, and 5-HT receptor 3 (5-HT3R) antagonists (such as ondansetron) are one of the most widely used antiemetics [ 42 ]. Ghrelin, an endogenous appetite-stimulating hormone, can stimulate food intake by promoting the expression of NPY/AgRP [ 43 ].…”

Section: Discussionmentioning

confidence: 99%

Analysis of Acupoints Combination for Cancer-Related Anorexia Based on Association Rule Mining

Tang

Liang

Wang

et al. 2022

Evidence-Based Complementary and Alternative Medicine

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We investigated the acupoint selection regulations and workable core acupoint combinations in cancer-related anorexia (CA) treatment. The Apriori algorithm, complemented by the FP-growth algorithm, was used to mine association rules based on retrieved randomized control trials (RCTs) and clinical control trials (CCTs). We searched the following databases for acupuncture treatment regimens for CA: PubMed, Embase, Cochrane Central, Web of Science, WanFang Data, VIP, China Journal Full-Text Database (CNKI), and SinoMed (CBM). We extracted acupoints prescriptions from the 27 enrolled RCTs and CCTs for analysis. There have been 38 acupoints refined from 27 prescriptions. The pinnacle three regularly chosen acupoints were Zusanli (ST36), Zhongwan (RN12), and Sanyinjiao (SP6). We investigated 10 association rules, and the consequences confirmed that {RN4} ≥ {RN12}, {PC6} ≥ {ST36}, {RN12, SP6} ≥ {RN4}, {HT7} ≥ {RN12}, and {DU20} ≥ {RN12} had been the most frequent associated rules in the adoption literature. Zusanli (ST36), Sanyinjiao (SP6), Guanyuan (RN4), Zhongwan (RN12), Neiguan (PC6), Shenmen (HT7), and Baihui (DU20) would be regarded as acupuncture prescriptions in the treatment of CA.

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“…109 Compound 62 was also demonstrated to decrease anorexia after total gastrectomy in rats. 110 Several clinical studies have reported that GHS-R1a agonists can be effective in improving anorexia and cachexia with limited side effects in healthy young adults and cancer patients, and in particular compound 6 represents a promising agent for the treatment of such pathologies. 111−115 In December 2020, it was approved in Japan for cancer cachexia.…”

Section: Pharmacological Potential Of Ghs-r1a Ligandsmentioning

confidence: 99%

“…Due to the established lipogenic and orexigenic effects of AG, various preclinical and clinical studies were performed and supported the beneficial role of AG or GHS-R1a agonists in the treatment of anorexia and cachexia. , Prevention of tissue wasting and increased food intake have been observed in a series of studies evaluating the role of known GHS-R1a agonists, such as compound 6 , HM01 ( 61 ), and Z-505 ( 62 ) (Figure ) in rodents bearing tumors associated with cachexia. − Recently, it has been reported that both compounds 6 and 61 potently induce Ca 2+ mobilization, but as compound 6 is more effective in the β-arrestin recruitment and GHS-R1a internalization, it is potentially more susceptible than compound 61 to treatment-induced tolerance, highlighting the importance of signaling bias characterization in the future development of GHS-R1a ligands . Compound 62 was also demonstrated to decrease anorexia after total gastrectomy in rats …”

Section: Pharmacological Potential Of Ghs-r1a Ligandsmentioning

confidence: 99%

Advances in the Development of Nonpeptide Small Molecules Targeting Ghrelin Receptor

et al. 2022

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Ghrelin is an octanoylated peptide acting by the activation of the growth hormone secretagogue receptor, namely, GHS-R1a. The involvement of ghrelin in several physiological processes, including stimulation of food intake, gastric emptying, body energy balance, glucose homeostasis, reduction of insulin secretion, and lipogenesis validates the considerable interest in GHS-R1a as a promising target for the treatment of numerous disorders. Over the years, several GHS-R1a ligands have been identified and some of them have been extensively studied in clinical trials. The recently resolved structures of GHS-R1a bound to ghrelin or potent ligands have provided useful information for the design of new GHS-R1a drugs. This perspective is focused on the development of recent nonpeptide small molecules acting as GHS-R1a agonists, antagonists, and inverse agonists, bearing classical or new molecular scaffolds, as well as on radiolabeled GHS-R1a ligands developed for imaging. Moreover, the pharmacological effects of the most studied ligands have been discussed.

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Z-505, an Oral Ghrelin Receptor Agonist, Attenuates Anorexia After Total Gastrectomy in Rats

Cited by 4 publications

References 43 publications

Physiological Effect of Ghrelin on Body Systems

Physiological Effect of Ghrelin on Body Systems

Analysis of Acupoints Combination for Cancer-Related Anorexia Based on Association Rule Mining

Advances in the Development of Nonpeptide Small Molecules Targeting Ghrelin Receptor

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