Selective alpha-1 and alpha-2 adrenergic agonists were used to test the hypothesis that both receptor subtypes increase transcellular Na+ transport in the nephron. Oxygen consumption (QO2) was used as an index of transcellular transport and provided a continuous dynamic record of the tubules' response to an agonist. Both alpha-1 and alpha-2 adrenoceptor agonists produced a linear dose-related i...

A cation-π interaction between the ammonium group of an agonist and a conserved tryptophan termed TrpB is a near universal feature of agonist binding to nicotinic acetylcholine receptors (nAChRs). TrpB is one of five residues that form the aromatic box of the agonist binding site, and for the prototype agonists ACh and nicotine, only TrpB makes a functional cation-π interaction. We report that,...

PPARγ (peroxisome proliferator activated receptor γ) is a ligand activated transcription factor of the nuclear receptor superfamily that controls the expression of a variety of genes involved in fatty acid metabolism, adipogenesis, and insulin sensitivity. While endogenous ligands of PPARγ include fatty acids and eicosanoids, synthetic full agonists of the receptor, including members of the thi...

This article gives an overview of current pharmacological treatment of paraphilias and sex offenders focusing on the situation in Germany. Information about selective serotonin reuptake inhibitors (SSRI) is followed by data about established antihormonal substances (cyproterone acetate/CPA, and medroxyprogesterone acetate/MPA), as well as a more detailed account on luteinizing hormone-releasing...

Alpha2-adrenergic agonists have been shown to reduce the incidence of perioperative myocardial morbidity and mortality. The purpose of this review article is to summarize the current data pertaining to alpha2-adrenergic agonists and their role in the prevention of perioperative adverse cardiac events. The MEDLINE and Cochrane databases were searched for randomized trials from 1980 to 2006 that ...

N-Formyl peptide receptors (FPRs) are G protein-coupled receptors (GPCRs) involved in host defense and sensing cellular dysfunction. Thus, FPRs represent important therapeutic targets. In the present studies, we screened 32 ligands (agonists and antagonists) of unrelated GPCRs for their ability to induce intracellular Ca²+ mobilization in human neutrophils and HL-60 cells transfected with human...

The ability of muscarinic cholinergic agonists to interact with muscarinic receptors in nerve ending preparations and elicit an increased labeling of phosphatidate and phosphatidylinositol from 32Pi has been investigated. Two groups of brain muscarinic agonists are distinguished. Addition of acetylcholine, carbamylcholine, methacholine, or muscarine resulted in a 2-fold stimulation of phosphati...

Activation of FFA1 (GPR40), a member of G protein-coupling receptor family A, is mediated by medium- and long-chain fatty acids and leads to amplification of glucose-stimulated insulin secretion, suggesting a potential role for free fatty acid 1 (FFA1) as a target for type 2 diabetes. It was assumed previously that there is a single binding site for fatty acids and synthetic FFA1 agonists. Howe...

Because of their wide range of actions on glucose homeostasis, lipid metabolism and vascular inflammation, peroxisome proliferator-activated receptors (PPARs) are promising targets for the development of new drugs for the treatment of metabolic disorders such as diabetes, dyslipidemia and atherosclerosis. In clinical practice, PPARalpha agonists, such as the already available fibrates, improve ...

κ opioid receptor agonists that do not readily cross the blood-brain barrier are peripherally restricted and distribute poorly to the central nervous system after systemic administration. Peripherally restricted κ agonists have promise as candidate analgesics, because they may produce antinociception mediated by peripheral κ receptors more potently than they produce undesirable sedative and psy...