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To apply the recently developed GPR ligands
2022-09-16

To apply the recently developed GPR35 ligands to CNS disorders, it is necessary to understand whether GPR35 is expressed by any identified cell types in the 5-aminosalicylic acid australia and whether activation or blockade of this receptor has any consequence on the activity of the neuronal circuit
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Because of the commercial availability of some acetamide phe
2022-09-16

Because of the commercial availability of some acetamide phenol starting materials, a few acetamide final products (such as and , ) were directly synthesized via a Mitsunobu reaction with chloropyrimidine piperidinyl cyclopropyl alcohol . The 3-pyridinyl analogue was synthesized by a nucleophilic
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Overall ABC transporters are hypothesised to prevent the pen
2022-09-16

Overall, ABC transporters are hypothesised to prevent the penetration of AEDs and other pharmacological compounds into the brain, being a hurdle for therapeutic delivery in neurological diseases. DRE is thought to be in part related to an increased expression of efflux transporters in the BBB, altho
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Up to now the research about the effect of PAs
2022-09-16

Up to now, the research about the effect of PAs on inhibiting carbohydrase activity in vitro or reducing blood sugar level in vivo was mainly reported in PAs from grape seeds, Lepisanthes alata (Malay cherry) leaves, sorghum, pomegranate, cranberry and persimmon (Banerji and Banerjee, 2016, Barrett
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The ER EK polymorphism is located
2022-09-16

The ER22/23EK polymorphism is located in the transactivation domain of the GR gene. A single nucleotide polymorphisms (SNPs) has been identified in both of the two adjacent codons (22 and 23). These SNPs are fully linked and are associated with relative GC resistance[32], [44]. Although no associati
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Two pathways have emerged to
2022-09-16

Two pathways have emerged to explain the beneficial metabolic effect of Roux-en-Y bypass [Fig. 3]. Firstly, the rapid delivery of nutrients to the distal small intestine and bowel might up-regulate secretion of a physiological stimulus that improves glucose homeostasis. As such, GLP-1 represents an
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GHSR A s have high levels of
2022-09-16

GHSR-1A's have high levels of constitutive activity and recent investigations show that constitutively active GHSR-1As in the absence of ligand (ghrelin) binding can have effects on feeding and energy balance (Mear et al., 2013, Petersen et al., 2009). Furthermore, GHSR-1As are capable of dimerizing
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Free fatty acids FFAs which are obtained from
2022-09-15

Free fatty acids (FFAs), which are obtained from dietary fat or endogenous synthesis, function as nutrients and signaling molecules. Studies have shown that free fatty glucocorticoid receptors receptors 1–4 which are G-protein coupled receptors, bind free fatty acids and serve as receptors for these
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All of the abovementioned effects of
2022-09-15

All of the abovementioned effects of PUFAs signal their involvement in a cellular phenotype switching phenomenon, which is increasingly recognized as a potential target for future pharmacotherapies of atherosclerosis, especially for individuals who do not respond to the classical lipid-lowering stra
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The molecular target of N BPs is farnesyl diphosphate
2022-09-15

The molecular target of N-BPs is farnesyl diphosphate synthase (FPPS), a crucial enzyme at the branch point of cholesterol and isoprenoid synthesis in the mevalonate pathway [5]. Because they bind calcium ions, N-BPs accumulate quickly in the skeleton and are internalised by osteoclasts, leading to
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br Materials and methods Patients charts were reviewed retro
2022-09-15

Materials and methods Patients’ charts were reviewed retrospectively, and 165 consecutive patients (82 with cancer and 83 without cancer) who either started edoxaban (Lixiana®, Daiichi-Sankyo, Tokyo, Japan) therapy for the treatment of VTE or were switched from other oral anticoagulants to edoxab
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Not only does G a GLP
2022-09-15

Not only does G9a/GLP complex appear to play a role (albeit a seemingly conflicting one) in LTP maintenance, it may also be involved in long-term depression (LTD) (). At hippocampal CA1 synapses, LTD can be induced by pharmacological or synaptic stimulation of Group 1 metabotropic glutamate receptor
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br Results br Discussion The present
2022-09-15

Results Discussion The present findings outline a novel regulatory mechanism for fasting-induced ketogenesis, which involves histamine release from mast NU 7026 into the hepatic portal system, H1 receptor-mediated stimulation of liver OEA biosynthesis, and recruitment of the nuclear receptor P
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br Introduction Nicotinic acid has been used
2022-09-09

Introduction Nicotinic Anisomycin has been used clinically for more than 50 years [1] since it has anti-atherogenic effects, including the ability to reduce triglyceride (TG) and low-density lipoprotein cholesterol (LDL-C), and elevate high-density lipoprotein cholesterol (HDL-C) [2]. Nicotinic
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br Materials and methods br Results br Discussion
2022-09-09

Materials and methods Results Discussion and conclusions Our data demonstrate that native and 2-OMe-LPC analogues are GPR119 ligands and activate insulin secretion from βTC-3 pancreatic cells. LPC 18:1 was the first proposed endogenous ligand for GPR119 [1], however natural LPC has limited
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