Showing papers in "Trends in Pharmacological Sciences in 1995"

TL;DR: Recent advances in this field are reviewed and the therapeutic potential of this novel, non-genomic effect of steroids is discussed and whether they may influence behaviour under physiological, or pathophysiological, conditions is investigated.

TL;DR: There is evidence to suggest that receptors with seven transmembrane domains can exist in G protein-activating conformations, but how many activated receptor forms exist for each receptor is not known.

TL;DR: It is acknowledged that much more data from endogenous receptors in whole tissues are needed before further recommendations on somatostatin receptor nomenclature can be made, but a promising approach is discussed.

TL;DR: The use of the elevated plus maze as a model of anxiety has some limitations, and although anxiolytics, such as the benzodiazepine receptor agonist chlordiazepoxide and the partial 5-HT1A receptor agonists 2, produce reliable and reproducible effects, other anxIOlytics do not.

TL;DR: The predictions of the two-state model of receptor activation are explained and the impact on the analysis and interpretation of agonist-receptor interactions is discussed.

TL;DR: Recent affinity labelling and site-directed mutagenesis studies on GABAA receptors that have identified amino acid residues essential for binding of agonists and allosteric modulators as well as the ion channel wall formation are discussed.

TL;DR: In large conducting arteries, EDHF may provide a secondary system to NO, which assumes primary importance in some disease states such as pulmonary hypertension and atherosclerosis, however, in small resistance arteries (100-300 microns), EDHF appears to be a major determinant of vascular calibre under normal conditions, and may therefore be ofprimary importance in the regulation of vascular resistance.

TL;DR: The properties of melatonin receptors are discussed, and the basis for their classification into at least two subtypes, the ML1 and ML2 are discussed.

TL;DR: The pharmacology of both officially recognized and atypical 5- HT2 receptor subtypes is examined and a number of novel selective agents are highlighted, some of which may prove useful for 5-HT2 receptor classification and clarify the mechanistic basis for current and future therapeutic strategies which target this receptor family.

TL;DR: Findings indicate that a large proportion of the neurotoxic Ca2+ that enters nerve cells following NMDA receptor activation originates from an intracellular Ca 2+ pool that is sensitive to the skeletal muscle relaxant dantrolene, and this may constitute a novel and alternative therapeutic approach againstNMDA receptor-mediated excitotoxicity.

TL;DR: The radical nature of NO cannot account for its cytotoxicity, but its reaction with superoxide to form peroxynitite and highly reactive hydroxyl radicals may be important in this context.

TL;DR: In this article, Pierre Sokoloff and Jean-Charles Schwartz discuss the functional significance of such diversity of dopamine receptors, as well as the new therapeutic perspectives it offers.

TL;DR: Evidence indicating that Na+ channel modulators are neuroprotective is reviewed and recent ideas for the molecular sites of action of voltage-dependentNa+ channel blockers are described.

TL;DR: Experimental support for the SBB is summarized, and pharmacological modulation of Ca2+ transport in the superficial sarcoplasmic reticulum presents an alternative means of controlling smooth muscle tone dependent on Ca2- entry.

TL;DR: The emerging evidence relating to the function of the 5-HT4 receptor in the brain, along with neurochemical and electrophysiological data, suggests a role in cognition.

TL;DR: The prospects of receptor antagonists, enzyme inhibitors, tumour suppressor genes and vascular targeted approaches, especially that of gene therapy, in the future development of angiotherapy are discussed.

TL;DR: It is suggested that Ca2+ channel drugs act by blocking or, in some cases, activating channel function via binding directly or indirectly to the pore structure of the channel.

TL;DR: Kelvin Chan overviews the TCM practitioners' concepts of how TCM natural products work and attempts to suggest the pharmacological interpretation of their mechanisms of action, and critically assessing the authenticity, quality, toxicity and clinical efficacy of these natural products.

TL;DR: The findings of recent cloning studies are summarized, the impact of these on the understanding of the function of the G protein-coupled P2 purinoceptors in several types of cells and tissues are assessed.

TL;DR: There is increasing evidence that the cysteinyl leukotrienes also produce several pro-inflammatory effects and alter the activity of neuronal pathways in the airways, and the therapeutic possibilities of cysteine receptor antagonists and 5-lipoxygenase inhibitors are discussed.

TL;DR: A generic method of performing nonlinear regression using spreadsheet applications is described and how this approach can be used to create automated systems of data analysis is demonstrated.

TL;DR: Terry Kenakin discusses a basic question in receptor pharmacology, namely the nature of ligand efficacy, and the way in which ligands change receptor populations to impart signals to cells remains to be determined.

TL;DR: Approaches that use antisense oligodeoxynucleotides provide an opportunity to characterize the pharmacology of short cDNA fragments without necessitating the cloning of the entire cDNA and can assess the role of the products of specific exons in a receptor, providing an approach for the study of alternative splicing as demonstrated with the mu- and kappa 3-opioid receptor clones.

TL;DR: In this review, David Tyrell, Stephen Kilfeather and Clive Page examine some of the activities of Heparin (and heparin derivatives) beyond its effects as an anticoagulant, and discuss the therapeutic potential of this old, but certainly not antiquated, drug.

TL;DR: In vitro, vanadium salts mimic most effects of insulin on the main target tissues of the hormone, and in vivo they induce a sustained fall in blood glucose levels in insulin-deficient diabetic rats, and improve glucose homeostasis in obese, insulin-resistant diabetic rodents.

TL;DR: Recent results that indicate that the established classification of P2X purinoceptors is no longer valid and needs redefinition are discussed.

TL;DR: The major models of acute cerebral ischaemia are reviewed, and rational protocols for examining novel neuroprotective agents are proposed.

TL;DR: The likelihood that cADPR-activated Ca2+ release is mediated by one of the recognized isoforms of the ryanodine receptor-Ca2+ channel complex is discussed.

TL;DR: It is now apparent that the binding site for most allosteric ligands is close to thebinding site for acetylcholine but that it is located at a more extracellular position.