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GHRP-6

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https://www.readbyqxmd.com/read/29137815/local-injection-of-d-lys-3-ghrp-6-in-the-rat-amygdala-dentate-gyrus-or-ventral-tegmental-area-impairs-memory-consolidation
#1
Siamak Beheshti, Neda Aslani
It is well known that the hormone ghrelin affects learning and memory in different experimental models of learning. Though, the effect of antagonism of ghrelin receptor type 1a (GHS-R1a) in various regions of the brain and on different stages of learning has not been examined. In this study the effect of injection of a GHS-R1a selective antagonist (d-Lys-3-GHRP-6) into the basolateral amygdala, dentate gyrus or ventral tegmental area was examined on memory consolidation in the passive avoidance task. Adult male Wistar rats weighing 230-280g were used...
November 4, 2017: Neuropeptides
https://www.readbyqxmd.com/read/29028172/influences-of-histidine-1-and-azaphenylalanine-4-on-the-affinity-anti-inflammatory-and-antiangiogenic-activities-of-azapeptide-cluster-of-differentiation-36-receptor-modulators
#2
Kelvine Chignen Possi, Mukandila Mulumba, Samy Omri, Yesica Garcia-Ramos, Houda Tahiri, Sylvain Chemtob, Huy Ong, William D Lubell
Azapeptide analogues of growth hormone releasing peptide-6 (GHRP-6) exhibit promising affinity, selectivity, and modulator activity on the cluster of differentiation 36 receptor (CD36). For example, [A(1), azaF(4)]- and [azaY(4)]-GHRP-6 (1a and 2b) were previously shown to bind selectively to CD36 and exhibited respectively significant antiangiogenic and slight angiogenic activities in a microvascular sprouting assay using choroid explants. The influences of the 1- and 4-position residues on the affinity, anti-inflammatory, and antiangiogenic activity of these azapeptides have now been studied in detail by the synthesis and analysis of a set of 25 analogues featuring Ala(1) or His(1) and a variety of aromatic side chains at the aza-amino acid residue in the 4-position...
November 1, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28993142/ghrelin-upregulates-the-phosphorylation-of-the-glun2b-subunit-of-the-nmda-receptor-by-activating-ghsr1a-and-fyn-in-the-rat-hippocampus
#3
Liza Berrout, Masako Isokawa
Ghrelin and its receptor GHSR1a have been shown to exert numerous physiological functions in the brain, in addition to the well-established orexigenic role in the hypothalamus. Earlier work indicated that ghrelin stimulated the phosphorylation of the GluN1 subunit of the NMDA receptor (NMDAR) and enhanced synaptic transmission in the hippocampus. In the present study, we report that the exogenous application of ghrelin increased GluN2B phosphorylation. This increase was independent of GluN2B subunit activity or NMDAR channel activity...
October 6, 2017: Brain Research
https://www.readbyqxmd.com/read/28985965/ghrelin-projection-from-the-lateral-hypothalamus-area-to-the-dorsal-vagal-complex-and-its-regulation-of-gastric-motility-in-cisplatin-treated-rats
#4
Yanling Gong, Yang Liu, Yaoyao Guo, Manqing Su, Yifan Zhong, Luo Xu, Feifei Guo, Shengli Gao
OBJECTIVE: To investigate ghrelin projection from the lateral hypothalamus area (LHA) to the dorsal vagal complex (DVC) and its regulation of gastric motility in cisplatin-treated rats. MATERIALS AND METHODS: In the present study, the protein and mRNA expression of ghrelin and its receptor GHSR-1a were measured by Western blot and PCR, respectively. The ghrelin fiber projections arising from the LHA and projecting to the DVC were investigated by retrograde tracing combined with fluoro-immunohistochemical staining...
September 28, 2017: Neuropeptides
https://www.readbyqxmd.com/read/28930716/antinociceptive-effect-of-ghrelin-in-a-rat-model-of-irritable-bowel-syndrome-involves-trpv1-opioid-systems
#5
Yuqing Mao, Zhengyang Li, Kan Chen, Huafang Yu, Shaoren Zhang, Miao Jiang, Yuanhua Ma, Chunli Liang, Hongyan Liu, Huanqing Li, Qian Hua, Hao Zhou, Yonghong Sun, Xiaoming Fan
BACKGROUND/AIMS: Irritable bowel syndrome (IBS), defined as recurrent abdominal pain and changes in bowel habits, seriously affects quality of life and ability to work. Ghrelin is a brain-gut hormone, which has been reported to show antinociceptive effects in peripheral pain. We investigated the effect of ghrelin on visceral hypersensitivity and pain in a rat model of IBS. METHODS: Maternal deprivation (MD) was used to provide a stress-induced model of IBS in Wistar rats...
2017: Cellular Physiology and Biochemistry
https://www.readbyqxmd.com/read/28903914/long-term-treatment-with-the-ghrelin-receptor-antagonist-d-lys3-ghrp-6-does-not-improve-glucose-homeostasis-in-non-obese-diabetic-mkr-mice
#6
Rasha Mosa, Lili Huang, Hongzhuo Li, Michael Grist, Derek LeRoith, Chen Chen
Ghrelin secretion has been associated with increased caloric intake and adiposity. The expressions of ghrelin and its receptor (GHS-R1a) in pancreas have raised the interest about the role of ghrelin in glucose homeostasis. Most of the studies showed that ghrelin promoted hyperglycaemia and inhibited insulin secretion. This raised the interest in using GHS-R1a antagonists as therapeutic targets for type 2 diabetes. Available data of GHS-R antagonists are on a short-term basis. Moreover, the complexity of GHS-R1a signalling makes it difficult to understand the mechanism of action of GHS-R1a antagonists...
September 13, 2017: American Journal of Physiology. Regulatory, Integrative and Comparative Physiology
https://www.readbyqxmd.com/read/28893476/growth-hormone-releasing-peptide-6-enhanced-antibody-titers-against-subunit-antigens-in-mice-balb-c-tilapia-oreochromis-niloticus-and-african-catfish-clarias-gariepinus
#7
Rebeca Martínez, Liz Hernández, Lázaro Gil, Yamila Carpio, Antonio Morales, Fidel Herrera, Alina Rodríguez-Mallón, Yeny Leal, Aracelys Blanco, Mario Pablo Estrada
Modern subunit vaccines have excellent safety profiles and improved tolerability, but do not elicit strong immune responses without the addition of adjuvants. Developing a safe and affective adjuvant remains a challenge for peptide-based vaccine design. Growth Hormone Releasing Peptide-6 (GHRP-6) is one of the earliest-developed, synthetic, peptidyl growth hormone secretagogue receptor agonists. These compounds mimic the effect of the endogenous ligand, ghrelin. In the present study, we evaluated the ability of GHRP-6 to enhance the humoral immune response against co-injected antigens in mice, tilapia and African catfish...
September 8, 2017: Vaccine
https://www.readbyqxmd.com/read/28830317/growth-hormone-secretagogue-treatment-in-hypogonadal-men-raises-serum-insulin-like-growth-factor-1-levels
#8
John T Sigalos, Alexander W Pastuszak, Andrew Allison, Samuel J Ohlander, Amin Herati, Mark C Lindgren, Larry I Lipshultz
Realizing the reported misuse of human growth hormone (GH), investigation of a safe alternative mechanism for increasing endogenous GH is needed. Several GH secretagogues are available, including GH-releasing peptides (GHRPs) GHRP-2 and GHRP-6, and the GH-releasing hormone analog, sermorelin (SERM). Insulin-like growth factor 1 (IGF-1) serves as a surrogate marker for GH. Here, the effect of GHRP/SERM therapy on IGF-1 levels is evaluated. A retrospective review of medical records was performed for 105 men on testosterone (T) therapy seeking increases in lean body mass and fat loss who were prescribed 100 mcg of GHRP-6, GHRP-2, and SERM three times daily...
November 2017: American Journal of Men's Health
https://www.readbyqxmd.com/read/28751159/ghrelin-ameliorates-acute-lung-injury-induced-by-oleic-acid-via-inhibition-of-endoplasmic-reticulum-stress
#9
Xiuli Tian, Zhijun Liu, Ting Yu, Haitao Yang, Linlin Feng
AIMS: Acute lung injury (ALI) is associated with excessive mortality and lacks appropriate therapy. Ghrelin is a novel peptide that protects the lung against ALI. This study aimed to investigate whether endoplasmic reticulum stress (ERS) mediates the protective effect of ghrelin on ALI. MAIN METHODS: We used a rat oleic acid (OA)-induced ALI model. Pulmonary impairment was detected by hematoxylin and eosin (HE) staining, lung mechanics, wet/dry weight ratio, and arterial blood gas analysis...
July 24, 2017: Life Sciences
https://www.readbyqxmd.com/read/28750241/a-polypeptide-mediated-synthesis-of-green-fluorescent-gold-nanoclusters-for-fe-3-sensing-and-bioimaging
#10
Hua Li, Hong Huang, Jiu-Ju Feng, Xiliang Luo, Ke-Ming Fang, Zhi-Gang Wang, Ai-Jun Wang
In this paper, growth hormone releasing peptide-6 (GHRP-6) is a bioactive polypeptide and acts as the reducing agent and capping ligand for synthesis of bright green fluorescent gold nanoclusters (GHRP-6-Au NCs) by a simple and environmental-friendly aqueous method, with the assistance of NaBr as the fluorescent sensitizer. The obtained GHRP-6-Au NCs had high fluorescent quantum yield (10.7%), and the fluorescence was strongly quenched by the existence of trace Fe(3+). Thus, a new and highly sensitive sensor for the assay of Fe(3+) was constructed based on the analyte-induced fluorescent quenching mechanism...
November 15, 2017: Journal of Colloid and Interface Science
https://www.readbyqxmd.com/read/28598597/azapeptide-synthesis-methods-for-expanding-side-chain-diversity-for-biomedical-applications
#11
Ramesh Chingle, Caroline Proulx, William D Lubell
Mimicry of bioactive conformations is critical for peptide-based medicinal chemistry because such peptidomimetics may augment stability, enhance affinity, and increase specificity. Azapeptides are peptidomimetics in which the α-carbon(s) of one or more amino acid residues are substituted by nitrogen. The resulting semicarbazide analogues have been shown to reinforce β-turn conformation through the combination of lone pair-lone pair repulsion of the adjacent hydrazine nitrogen and urea planarity. Substitution of a semicarbazide for an amino amide residue in a peptide may retain biological activity and add benefits such as improved metabolic stability...
June 9, 2017: Accounts of Chemical Research
https://www.readbyqxmd.com/read/28513740/l-ornithine-stimulates-growth-hormone-release-in-a-manner-dependent-on-the-ghrelin-system
#12
Yee Yin Ho, Junya Nakato, Takafumi Mizushige, Ryuhei Kanamoto, Mamoru Tanida, Saori Akiduki, Kousaku Ohinata
We found that intraduodenal administration of l-ornithine (l-Orn) stimulates growth hormone (GH) secretion in Wistar rats, and then investigated its mechanism. GH-releasing activity after intraduodenal administration of l-Orn was blocked by [d-Lys(3)]-GHRP-6, an antagonist of the ghrelin receptor; however, l-Orn (100 μM) has no affinity for the ghrelin receptor, suggesting that the GH-releasing activity of l-Orn is mediated via ghrelin release and activation of the ghrelin receptor. Intraduodenally administered l-Orn increased ghrelin mRNA expression in the duodenum but not in the stomach or hypothalamus...
June 1, 2017: Food & Function
https://www.readbyqxmd.com/read/28506816/ghrelin-suppresses-cholecystokinin-cck-peptide-yy-pyy-and-glucagon-like-peptide-1-glp-1-in-the-intestine-and-attenuates-the-anorectic-effects-of-cck-pyy-and-glp-1-in-goldfish-carassius-auratus
#13
Ayelén Melisa Blanco, Juan Ignacio Bertucci, Ana Isabel Valenciano, María Jesús Delgado, Suraj Unniappan
Ghrelin is an important gut-derived hormone with an appetite stimulatory role, while most of the intestinal hormones, including cholecystokinin (CCK), peptide YY (PYY) and glucagon-like peptide-1 (GLP-1), are appetite-inhibitors. Whether these important peptides with opposing roles on food intake interact to regulate energy balance in fish is currently unknown. The aim of this study was to characterize the putative crosstalk between ghrelin and CCK, PYY and GLP-1 in goldfish (Carassius auratus). We first determined the localization of CCK, PYY and GLP-1 in relation to ghrelin and its main receptor GHS-R1a (growth hormone secretagogue 1a) in the goldfish intestine by immunohistochemistry...
May 18, 2017: Hormones and Behavior
https://www.readbyqxmd.com/read/28462451/complexity-of-stomach-brain-interaction-induced-by-molecular-hydrogen-in-parkinson-s-disease-model-mice
#14
Yusuke Yoshii, Taikai Inoue, Yuya Uemura, Yusaku Iwasaki, Toshihiko Yada, Yusaku Nakabeppu, Mami Noda
Molecular hydrogen (H2), as a new medical gas, has protective effects in neurological disorders including Parkinson's disease (PD). In our previous report, the neuroprotective effect of drinking water with saturated H2 (H2 water) in PD mice might be due to stomach-brain interaction via release of gastric hormone, ghrelin. In the present study, we assessed the effect of H2-induced ghrelin more precisely. To confirm the contribution of ghrelin in H2 water-drinking PD model mice, ghrelin-knock out (KO) mice were used...
September 2017: Neurochemical Research
https://www.readbyqxmd.com/read/28338019/ghrelin-facilitates-glut2-sglt1-and-sglt2-mediated-intestinal-glucose-transport-in-goldfish-carassius-auratus
#15
Ayelén Melisa Blanco, Juan Ignacio Bertucci, Naresh Ramesh, María Jesús Delgado, Ana Isabel Valenciano, Suraj Unniappan
Glucose homeostasis is an important biological process that involves a variety of regulatory mechanisms. This study aimed to determine whether ghrelin, a multifunctional gut-brain hormone, modulates intestinal glucose transport in goldfish (Carassius auratus). Three intestinal glucose transporters, the facilitative glucose transporter 2 (GLUT2), and the sodium/glucose co-transporters 1 (SGLT1) and 2 (SGLT2), were studied. Immunostaining of intestinal sections found colocalization of ghrelin and GLUT2 and SGLT2 in mucosal cells...
March 24, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28321024/the-growth-hormone-secretagogue-hexarelin-protects-rat-cardiomyocytes-from-in-vivo-ischemia-reperfusion-injury-through-interleukin-1-signaling-pathway
#16
Jiannan Huang, Yi Li, Juan Zhang, Yusheng Liu, Qinghua Lu
Hexarelin, a synthetic growth hormone-releasing peptide, has been proven to possess cardioprotective actions through its binding to the growth hormone secretagogue receptor (GHSR) 1a and the non-GHSR receptor CD36. However, its effect on myocardial ischemia/reperfusion (I/R) injury has not been fully clarified in vivo. We aimed to determine whether hexarelin treatment could protect cardiomyocytes from I/R injury and to examine the underlying mechanisms. In vivo hearts of male SD rats underwent 30 minutes of ischemia by left coronary artery ligation followed by reperfusion...
April 6, 2017: International Heart Journal
https://www.readbyqxmd.com/read/28245976/ghrelin-alleviates-anxiety-and-depression-like-behaviors-induced-by-chronic-unpredictable-mild-stress-in-rodents
#17
Hui-Jie Huang, Xiao-Cang Zhu, Qiu-Qin Han, Ya-Lin Wang, Na Yue, Jing Wang, Rui Yu, Bing Li, Gen-Cheng Wu, Qiong Liu, Jin Yu
As a regulator of food intake, ghrelin also plays a key role in mood disorders. Previous studies reported that acute ghrelin administration defends against depressive symptoms of chronic stress. However, the effects of long-term ghrelin on rodents under chronic stress hasn't been revealed. In this study, we found chronic peripheral administration of ghrelin (5nmol/kg/day for 2 weeks, i.p.) could alleviate anxiety- and depression-like behaviors induced by chronic unpredictable mild stress (CUMS). The depression-like behaviors were assessed by the forced swimming test (FST), and anxiety-like behaviors were assessed by the open field test (OFT) and the elevated plus maze test (EPM)...
May 30, 2017: Behavioural Brain Research
https://www.readbyqxmd.com/read/28214691/dlitiazem-inhibits-the-oxidative-stress-induced-by-angiotensin-ii-through-growth-hormone-secretagogue-receptor-type-1a-in-human-umbilicus-vein-endothelial-cells
#18
Lingyun Zhou, Meng Yang, Shanru Zuo, Xiaofeng Guan, Jianglin Wang, Qingjie Chen, Xiaocong Zuo, Sujie Jia, Ren Guo
Diltiazem has been used for post-transplant hypertension, but the mechanism underlying its protective effect of endothelial cells against angiotensin II (Ang II) - induced impairment remains unclear. Human umbilicus vein endothelial cells (HUVECs) were cultured and divided into seven groups: control, Ang II (10(-6)M), diltiazem (10(-6)M), [D-Lys3]-GHRP-6(25μM), diltiazem (10(-6)M)+Ang II (10(-6)M), losartan (10(-6)M)+Ang II (10(-6)M), [D-Lys3]-GHRP-6 (25μM) + Dil(10(-6)M)+Ang II (10(-6)M) groups. Nitric oxide (NO) production, intracellular reactive oxygen species (ROS) levels, protein and mRNA expressions of endothelial nitric oxide synthase (eNOS) and p47 phox subunit of NADPH were evaluated...
May 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28090719/diversity-oriented-synthesis-of-cyclic-azapeptides-by-a-3-macrocyclization-provides-high-affinity-cd36-modulating-peptidomimetics
#19
Jinqiang Zhang, Mukandila Mulumba, Huy Ong, William D Lubell
Macrocyclization has enabled the use of peptides in drug discovery creating a need for methods to synthesize diverse peptide macrocycles. Azapeptides have advanced to clinically used drugs, however, few cyclic azapeptides have been studied. A multiple component "A(3) -macrocyclization" strategy is described for the preparation of diverse cyclic azapeptides and is demonstrated by the synthesis of 15 growth hormone releasing hormone-6 (GHRP-6) analogs. Certain cyclic aza-GHRP-6 analogs exhibited unprecedented affinity for the CD36 receptor, and capacity to modulate Toll-like receptor agonist-induced overproduction of nitric oxide, and reduce pro-inflammatory cytokine and chemokine production in macrophages...
January 16, 2017: Angewandte Chemie
https://www.readbyqxmd.com/read/28042022/ghrelin-modulates-gene-and-protein-expression-of-digestive-enzymes-in-the-intestine-and-hepatopancreas-of-goldfish-carassius-auratus-via-the-ghs-r1a-possible-roles-of-plc-pkc-and-ac-pka-intracellular-signaling-pathways
#20
Ayelén Melisa Blanco, Juan Ignacio Bertucci, Aída Sánchez-Bretaño, María Jesús Delgado, Ana Isabel Valenciano, Suraj Unniappan
Ghrelin, a multifunctional gut-brain hormone, is involved in the regulation of gastric functions in mammals. This study aimed to determine whether ghrelin modulates digestive enzymes in goldfish (Carassius auratus). Immunofluorescence microscopy found colocalization of ghrelin, GHS-R1a and the digestive enzymes sucrase-isomaltase, aminopeptidase A, trypsin and lipoprotein lipase in intestinal and hepatopancreatic cells. In vitro ghrelin treatment in intestinal and hepatopancreas explant culture led to a concentration- and time-dependent modulation (mainly stimulatory) of most of the digestive enzymes tested...
February 15, 2017: Molecular and Cellular Endocrinology
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