g -aminobutiric acid (gaba), the major inhibitory neurotransmitter in the central nervous system has two major receptor subtypes (gabaa and gabab). gabab receptors are activated by the antispastic and muscle relaxant agent, baclofen, which is a lipophilic derivative of gaba. since 1962 several strategies have been reported for the synthesis of baclofen.in this study an approach has been made to...

Diabetes is a major risk factor for the development of stroke. Glucagon-like peptide-1 receptor (GLP-1R) agonists have been in clinical use for the treatment of diabetes and also been reported to be neuroprotective in ischemic stroke. The quinoxaline 6,7-dichloro-2-methylsulfonyl-3-N-tert- butylaminoquinoxaline (DMB) is an agonist and allosteric modulator of the GLP-1R with the potential to inc...

Peptidic mimics of the gut hormone glucagon-like peptide (GLP) 1, exemplified by the recently approved drug exenatide, show promise as therapies for type 2 diabetes. Such "incretin mimetics" regulate glucose appearance in the plasma and can restore glucose-stimulated insulin secretion without excess risk of hypoglycemia. The need for injection, which may limit the use of peptidic GLP-1 receptor...

OBJECTIVE Glucagon-like peptides (GLPs) are secreted from enteroendocrine cells in response to nutrients and bile acids and control metabolism via actions on structurally-related yet distinct G protein coupled receptors. GLP-1 regulates gut motility, appetite, islet function, and glucose homeostasis, whereas GLP-2 enhances intestinal nutrient absorption. GLP-1R agonists are used to treat diabet...

Glucagon and the glucagon-like peptides are derived from a common proglucagon precursor, and regulate energy homeostasis through interaction with a family of distinct G protein coupled receptors. Three proglucagon-derived peptides, glucagon, GLP-1, and GLP-2, play important roles in energy intake, absorption, and disposal, as elucidated through studies utilizing peptide antagonists and receptor...

Activation of the receptor for advanced glycation end products (RAGE) axis may have an important role in apoptosis. Glucagon-like peptide-1 (GLP-1) is a gut hormone that has been proposed as a therapeutic target for the treatment of diabetes, and GLP-1 receptor agonists have been reported to protect against myocardial injury associated with diabetes. The aim of the present study was to investig...

INTRODUCTION Regulatory requirements mandate that new drugs for treatment of patients with type 2 diabetes mellitus (T2DM), such as dipeptidyl peptidase-4 (DPP-4) inhibitors and glucagon-like peptide-1 (GLP-1) receptor agonists, are evaluated to show that they do not increase cardiovascular (CV) risk. METHODS A systematic review was undertaken to evaluate the association between DPP-4 inhibit...

AIMS To determine the effects of glucagon-like peptide-1 receptor agonists compared with placebo and other anti-diabetic agents on weight loss in overweight or obese patients with type 2 diabetes mellitus. METHODS Electronic searches were conducted for randomised controlled trials that compared a glucagon-like peptide-1 receptor agonist therapy at a clinically relevant dose with a comparator ...

This is a case of a severe hypoglycemia caused by an excess of GLP-1 receptors on a benign insulinoma in an individual with type 2 diabetes. The hypoglycemia was likely induced by a GLP-1 receptor agonist. The patient is a 54-year-old Caucasian female evaluated for “reactive” hypoglycemia that had worsened over the past 10 years. She had gained 20 pounds and reported intermittent episodes of “l...

INTRODUCTION Our main aim was to assess the level of persistence and adherence to therapy with glucagon-like peptide-1 (GLP-1) receptor agonists in type 2 diabetes mellitus (T2DM) patients in the United Kingdom (UK) and Germany, also by comparing once- (OD) with twice-a-day (BID) therapy. METHODS We used two large retrospective datasets: a German claims dataset and the UK General Practitioner...