Understanding the incretin pathway has led to significant advancements in the treatment of type 2 diabetes (T2D). Still, the exact mechanisms are not fully understood. In a randomized, placebo-controlled, four-period, crossover study in 24 patients with T2D, dipeptidyl peptidase-4 (DPP-4) inhibition and its glucose-lowering actions were tested after an oral glucose tolerance test (OGTT). The co...

Adenosine receptors (nomenclature as agreed by the NC-IUPHAR Subcommittee on Receptors [112]) are activated endogenous ligand adenosine (potentially inosine also at A3 receptors). Crystal structures for antagonist-bound [155, 316, 224, 62], agonist-bound [379, 205, 206] and G protein-bound A2A [49] have been described. The of an A1 receptor [130] adenosine-bound receptor-Gi complex [87] resolve...

Objective(s): Atherosclerosis is an important risk factor for coronary heart disease. Neuropeptide Y (NPY) and its receptors, located in peripheral tissue such as white adipose tissue, have been linked to obesity and fat storage. The role of NPY in atherosclerosis has not yet been fully studied, so this study was conducted to further investigate the effect of BIIE 0246, an NPY receptor antagoni...

Objective(s): Traumatic brain injury (TBI) is one of the most common causes of death and disability in modern societies. The role of steroids and melatonin is recognized as a neuroprotective factor in traumatic injuries. This study examined the role of melatonin receptors in the neuroprotective effects of estrogen. Materials and Methods: Seventy female ovariectomized Wistar rats were divided in...

Glucocorticoid (GC)-based therapies can cause insulin resistance (IR), glucose intolerance, hyperglycemia and, occasionally, overt diabetes. Understanding the mechanisms behind these metabolic disorders could improve the management of glucose homeostasis in patients undergoing GC treatment. For this purpose, adult rats were treated with a daily injection of dexamethasone (1 mg/kg b.w., i.p.) (D...

The effects of caerulin, a CCK receptor agonist, and proglumide, a receptor antagonist, on hyperalgesia induced by sciatic nerve ligation, was studied in mice. Tolerance to the morphine response was obtained 3,7, 14,21 and 28 days after unilateral sciatic nerve ligation. Maximum hyperalgesia was found 14 days after nerve ligation. Caerulin increased morphine antinociception in nerve-ligated ani...

In the present study, interactions of dopamine receptor agonists and antagonists with water swimming stress (WSS) on naloxone-induced jumping in morphine-dependent mice were examined. Mice were rendered dependent as described in the methods section. The opioid receptor antagonist, naloxone (1 mg/kg), was injected to elicit jumping (as a withdrawal sign). The first group exposed to WSS in the pr...

Atypical antipsychotic drugs such as Olanzapine (Olan) induce weight gain and metabolic changes associated with the development of type 2 diabetes. The mechanisms underlying these undesired side-effects are currently unknown. It has been shown that peripheral injections of Olan activate neurons in the lateral hypothalamus/perifornical area and that a large part of these neurons are orexin (Ox) ...

A complementary DNA for a glucagon-like peptide-1 receptor was isolated from a human pancreatic islet cDNA library. The isolated clone encoded a protein with 90% identity to the rat receptor. In stably transfected fibroblasts, the receptor bound [125I]GLP-1 with high affinity (Kd = 0.5 nM) and was coupled to adenylate cyclase as detected by a GLP-1-dependent increase in cAMP production (EC50 = ...