l-Lysine hydrochloride was transformed to ethyl l-lysine dihydrochloride. This salt was reacted with trimellitic anhydride to yield the corresponding diacid (1). Interfacial polycondensation results novel poly(ester-imide)s (PEIa–i). These polymers have inherent viscosities in the range of 0.23...

Hydrogels have attracted much attention in cancer therapy and tissue engineering due to their sustained gene delivery ability. To obtain an injectable and high-efficiency gene delivery hydrogel, methoxypolyethylene glycol (MPEG) was used to conjugate with the arginine-functionalized poly(l-lysin...

As the exopeptidase over-expressed in the cell surface of endothelial cells, aminopeptidase N (APN/CD13) is an essential target for tumor angiogenesis and metastasis. Based on the previous work of l-lysine amide derivatives in our laboratory, we designed and synthesized two series of l-lysine ur...

ObjectiveTo prepare a floating type dosage form for the anti-diabetic drug repaglinide using polycarbonate (PC) microspheres capable of floating in the gastro-intestinal fluid to improve the biological half life and bioavailability of the drug.

Tropical starches from Dioscorea dumetorum (bitter) and Dioscorea oppositifolia (Chinese) yams were acetylated with acetic anhydride in pyridine medium and utilized as polymers for the delivery of repaglinide in microsphere formulations in comparison to ethyl cellulose. Acetylated starches of bi...

Repaglinide, an oral antidiabetic agent, has a rapid onset of action and short half–life of approximately 1 h. Developing a controlled and prolonged release delivery system is required to maintain its therapeutic plasma concentration and to eliminate its adverse effects particularly hypoglycemi...

This work is the first, according to our knowledge, complete structural report on the solid-state supramolecular architecture of antidiabetic drug repaglinide. Here, we present a series of four crystal structures, namely: an un-solvated form of repaglinide (1), repaglinide hydrochloride (2), rep...

Experimental and theoretical conformational study of repaglinide in chloroform and dimethyl sulfoxide was investigated. By applying potential energy scanning (PES) at B3LYP/6-311++g** and B3LYP-D3/6-311++g** level of theory on rotatable single bonds, four stable conformers (R1-R4) were identifie...

Repaglinide is a nonsulfonylurea, oral hypoglycemic agent used in the treatment of type 2 diabetes mellitus. It stimulates insulin secretion by binding to the sulfonylurea receptor (SUR1) subunit of the KATP channel, thus blocking the channel, resulting in depolarization of the beta-cell membran...

The present manuscript highlights the structural insight into the repaglinide polymorphs. The experimental screening for the possible crystal forms were carried out using various solvents, which generated three forms. The crystal structure of Form II and III was determined using PXRD pattern whe...

Glioblastoma multiforme (GBM) is a highly aggressive brain tumor with a median survival time of only 14 months after treatment. It is urgent to find new therapeutic drugs that increase survival time of GBM patients. To achieve this goal, we screened differentially expressed genes between long-te...

The dynamics of insulin secretion stimulated by repaglinide, a glinide, and the combinatorial effects of repaglinide and incretin were investigated. At 4.4 mM glucose, repaglinide induced insulin secretion with a gradually increasing first phase, showing different dynamics from that induced by g...

SummaryRepaglinide (RPG) is a short-acting insulin secretagogue widely prescribed for the treatment of type 2 diabetes. It boosts insulin secretion by inhibiting the pancreatic ATP-sensitive potassium channel (KATP). However, the mechanisms by which RPG binds to the KATP channel are poorly under...

IntroductionThe N-methyl-D-Aspartate (NMDA) receptor plays an important role in learning and memory. Overactivation is thought to play an important role in neurodegenerative disorders such as Alzheimer's disease. Currently, it is not possible to assess N-methyl-D-aspartate receptor (NMDAr) ...

Secretin is a linear 27-aa peptide which was initially discovered from the porcine intestine based on its activities in stimulating pancreatic juice. Secretin is highly conserved among mammalian species, but the sequence identity in non-mammalian species up to avians is lower, and secretin-like ...

BackgroundSocial recognition underlies social behavior in animals, and patients with psychiatric disorders associated with social deficits show abnormalities in social recognition. Oxytocin is implicated in social behavior and has received attention as an effective treatment for sociobehavioral ...

Activation of the secretin (Sct)/secretin receptor (SR) axis stimulates ductular reaction and liver fibrosis, which are hallmarks of cholangiopathies. Our aim was to define the role of Sct-regulated cellular senescence, and we demonstrated that both ductular reaction and liver fibrosis are signi...

Drug shortages and recalls are often caused due to particulate growth in parenteral products and can have serious clinical implications. Root cause analysis of such recalls and shortages may arise due to insufficient understanding of process, formulations issues and environmental effects than of...

The discovery of secretin initiated the field of endocrinology. Over the past century, multiple gastrointestinal functions of secretin have been extensively studied, and it was discovered that the principal function of this peptide in the gastrointestinal system is to facilitate digestion and to...

Secretin and the secretin receptor have been reported to play an important role in regulating pancreatic water and bicarbonate secretion in mammals; however, little is known about their expression, structure, and biological functions in non-mammalian vertebrates including birds. In this study, t...