A tachykinin antagonist inhibits gastric emptying and gastrointestinal transit in the rat.

abstract：BACKGROUND AND PURPOSE:Although the stoichiometry of the major synaptic αβγ subunit-containing GABAA receptors has consensus support for 2α:2β:1γ, a clear view of the stoichiometry of extrasynaptic receptors containing δ subunits has remained elusive. Here we examine the subunit stoichiometry of recombinant α4β3δ recep...

journal_title：British journal of pharmacology

authors： Patel B,Mortensen M,Smart TG

更新日期：2014-02-01 00:00:00

abstract：:The Concise Guide to PHARMACOLOGY 2017/18 provides concise overviews of the key properties of nearly 1800 human drug targets with an emphasis on selective pharmacology (where available), plus links to an open access knowledgebase of drug targets and their ligands (www.guidetopharmacology.org), which provides more deta...

journal_title：British journal of pharmacology

authors： Alexander SP,Christopoulos A,Davenport AP,Kelly E,Marrion NV,Peters JA,Faccenda E,Harding SD,Pawson AJ,Sharman JL,Southan C,Davies JA,CGTP Collaborators.

更新日期：2017-12-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Marijuana smoking is widespread in many countries, and the use of smoked synthetic cannabinoids is increasing. Smoking a marijuana joint leads to bronchodilation in both healthy subjects and asthmatics. The effects of Δ(9) -tetrahydrocannabinol and synthetic cannabinoids on human bronchus reactiv...

journal_title：British journal of pharmacology

authors： Grassin-Delyle S,Naline E,Buenestado A,Faisy C,Alvarez JC,Salvator H,Abrial C,Advenier C,Zemoura L,Devillier P

更新日期：2014-06-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Pancreatic cancer is characterized by alterations in several key signalling proteins, including increased expression and activity of the Src tyrosine kinase and focal adhesion kinase (FAK), which have been linked to its chemoresistance. Sustained Src inhibition reactivates survival pathways regul...

journal_title：British journal of pharmacology

authors： Pathania D,Kuang Y,Sechi M,Neamati N

更新日期：2015-01-01 00:00:00

abstract：:1. The involvement of peripheral nitric oxide (NO) in febrigenic signaling to the brain has been proposed because peripherally administered NO synthase (NOS) inhibitors attenuate lipopolysaccharide (LPS)-induced fever in rodents. However, how the unstable molecule of NO can reach the brain to trigger fever is unclear....

journal_title：British journal of pharmacology

authors： Steiner AA,Rudaya AY,Ivanov AI,Romanovsky AA

更新日期：2004-04-01 00:00:00

abstract：:1. A single i.p. injection of bacterial endotoxin in rats (3.5 mg kg-1) caused lung injury assessed as changes in lung dry:wet weight ratio and leukopaenia over the subsequent 28 h. 2. This treatment also slowed the efflux of 14C from [14C]-prostaglandin E2 (PGE2), i.e., increased t1/2 and increased the survival of PG...

journal_title：British journal of pharmacology

authors： Izumi T,Bakhle YS

更新日期：1988-04-01 00:00:00

abstract：:1. The potencies of some beta-adrenoreceptor blocking drugs in reducing noradrenaline uptake by the isolated heart were compared with their potencies in reducing the release of noradrenaline from the heart by tyramine.2. Of the drugs tested, propranolol, pronethalol and dichloroisoprenaline were the most potent in blo...

journal_title：British journal of pharmacology

authors： Foo JW,Jowett A,Stafford A

更新日期：1968-09-01 00:00:00

abstract：:1. We have investigated the effects of chlorpheniramine, atropine and capsaicin pretreatment on inhaled sodium metabisulphite (MBS)-induced airway microvascular leakage and bronchoconstriction in anaesthetized guinea-pigs in order to clarify the mechanisms involved in these responses. The effects of frusemide and nedo...

journal_title：British journal of pharmacology

authors： Sakamoto T,Elwood W,Barnes PJ,Chung KF

更新日期：1992-10-01 00:00:00

abstract：:1. Peroxynitrite, a potent cytotoxic oxidant formed by the reaction of nitric oxide with superoxide anion, and hydroxyl radical, formed in the iron-catalysed Fenton reaction, are important mediators of reperfusion injury. In in vitro studies, DNA single strand breakage, triggered by peroxynitrite or by hydroxyl radica...

journal_title：British journal of pharmacology

authors： Cuzzocrea S,Zingarelli B,Costantino G,Szabó A,Salzman AL,Caputi AP,Szabó C

更新日期：1997-07-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Diabetes is a risk factor for the development of coronary artery disease but it is not known whether the functions of endothelium-derived nitric oxide (NO) and endothelium-derived hyperpolarizing factor (EDHF) in coronary arteries are altered in the early stage of diabetes. Such alterations and t...

journal_title：British journal of pharmacology

authors： Kajikuri J,Watanabe Y,Ito Y,Ito R,Yamamoto T,Itoh T

更新日期：2009-09-01 00:00:00

abstract：:1 New 2H-1,4-benzoxazine derivatives were synthesized and tested for their agonist properties on the ATP-sensitive K(+) channels (K(ATP)) of native rat skeletal muscle fibres by using the patch-clamp technique. The novel modifications involved the introduction at position 2 of the benzoxazine ring of alkyl substituent...

journal_title：British journal of pharmacology

authors： Tricarico D,Barbieri M,Antonio L,Tortorella P,Loiodice F,Camerino DC

更新日期：2003-05-01 00:00:00

abstract：:The response to vasoactive agents of microvessels of the rat was tested in vivo by direct microscopic observation of the exteriorized mesentery and assessment of cutaneous vascular permeability changes with Evans blue. The constrictor response to a standard amount of noradrenaline in mesenteric microvessels was fully ...

journal_title：British journal of pharmacology

authors： Fortes ZB,Garcia Leme J,Scivoletto R

更新日期：1984-11-01 00:00:00

abstract：:1. The type of endothelin (ET) receptor located on the myenteric neurones of guinea-pig ileum was determined by receptor autoradiography and function of the receptor was examined by release experiments of acetylcholine (ACh) from the longitudinal muscle myenteric plexus (LM-MP) preparations. 2. Specific [125I]-ET-1 bi...

journal_title：British journal of pharmacology

authors： Yoshimura M,Yamashita Y,Kan S,Niwa M,Taniyama K

更新日期：1996-07-01 00:00:00

abstract：:1. Recombinant human ETA receptors were expressed in a mouse fibroblast cell line (Ltk- cell) and functional coupling of the receptors with Ca2+ permeable channels at low concentrations of endothelin-1 (ET-1) was investigated using whole-cell recordings and monitoring the changes in intracellular free Ca2+ concentrati...

journal_title：British journal of pharmacology

authors： Enoki T,Miwa S,Sakamoto A,Minowa T,Komuro T,Kobayashi S,Ninomiya H,Masaki T

更新日期：1995-06-01 00:00:00

abstract：UNLABELLED:Cell movement is a fundamental process of normal cellular physiology and pathophysiology. Abnormal regulation of cell migration is a common denominator of many medical disorders, including cancer metastasis, autoimmune disease and inflammation. Increased interest in the targeting of cell migration and invasi...

journal_title：British journal of pharmacology

authors： Detchokul S,Frauman AG

更新日期：2014-12-01 00:00:00

abstract：:The characteristics of the rat epidydimal adipocyte beta-adrenoceptor have been examined using lipolysis and cyclic AMP accumulation in adipocytes as well as adenylate cyclase activity in fat cell membranes. The pA2 values corrected for binding to bovine serum albumin of the selective antagonists betaxolol (beta 1-sel...

journal_title：British journal of pharmacology

authors： Bojanic D,Jansen JD,Nahorski SR,Zaagsma J

更新日期：1985-01-01 00:00:00

abstract：:Association between staphylococcal infection and pathogenesis of upper airways disease has been reported. This study aimed to investigate the mechanisms underlying the rat pulmonary inflammation induced by airway exposure to staphylococcal enterotoxin A (SEA). SEA (0.3-10 ng trachea(-1)) caused dose-dependent neutroph...

journal_title：British journal of pharmacology

authors： Desouza IA,Franco-Penteado CF,Camargo EA,Lima CS,Teixeira SA,Muscará MN,De Nucci G,Antunes E

更新日期：2005-11-01 00:00:00

abstract：:1. Orexin-containing neurons have been implicated in feeding, sleep-wake cycles and more recently in drug-seeking behaviour. 2. Pretreatment of alcohol-preferring (iP) rats with an orexin1 receptor antagonist (SB-334867, 20 mg kg(-1), intraperitoneally) completely abolished an olfactory cue-induced reinstatement of al...

journal_title：British journal of pharmacology

authors： Lawrence AJ,Cowen MS,Yang HJ,Chen F,Oldfield B

更新日期：2006-07-01 00:00:00

abstract：:Schizophrenia remains an elusive multifaceted disorder with all evidence of its onset and aetiology pointing to a complex interplay of genetic, nutritional, environmental and developmental factors. Although several molecular and structural abnormalities have been reported for schizophrenia, no diagnostic test or other...

journal_title：British journal of pharmacology

authors： Schwarz E,Bahn S

更新日期：2008-03-01 00:00:00

abstract：:1. Fenclozic acid (2-(4-chlorophenyl)thiazol-4-ylacetic acid; I.C.I. 54,450; "Myalex") is one representative of a new class of compounds with antiinflammatory, analgesic and antipyretic properties as evidenced by its activity in a variety of tests in rats, mice and guinea-pigs.2. In tests of short duration the potency...

journal_title：British journal of pharmacology

authors： Newbould BB

更新日期：1969-03-01 00:00:00

abstract：:Using a rat model which allows serial blood sampling and concurrent brain microdialysis sampling, we have investigated the temporal kinetic inter-relationship of levetiracetam in serum and brain extracellular fluid (frontal cortex and hippocampus) following systemic administration of levetiracetam, a new antiepileptic...

journal_title：British journal of pharmacology

authors： Tong X,Patsalos PN

更新日期：2001-07-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Although trace amines (TAs) are historically considered 'false neurotransmitters' on the basis of their ability to induce catecholamine release, there is evidence that they directly affect neuronal activity via TA receptors, ligand-gated receptor channels and/or sigma receptors. Here, we have inv...

journal_title：British journal of pharmacology

authors： Ledonne A,Federici M,Giustizieri M,Pessia M,Imbrici P,Millan MJ,Bernardi G,Mercuri NB

更新日期：2010-07-01 00:00:00

abstract：:1. We have used the whole-cell patch clamp technique to study the effect of the partial anti-oestrogens clomiphene and nafoxidine, the pure anti-oestrogens ICI 182,780 and RU 58,668 and the oestrogen ss-estradiol, on the volume-regulated anion channel (VRAC) in cultured pulmonary artery endothelial (CPAE) cells. 2. In...

journal_title：British journal of pharmacology

authors： Maertens C,Droogmans G,Chakraborty P,Nilius B

更新日期：2001-01-01 00:00:00

abstract：:Adrenomedullin (AM) has two known receptors formed by the calcitonin receptor-like receptor (CL) and receptor activity-modifying protein (RAMP) 2 or 3: we report the effects of the antagonist fragments of human AM and CGRP (AM22-52 and CGRP8-37) in inhibiting AM at human (h), rat (r) and mixed species CL/RAMP2 and CL/...

journal_title：British journal of pharmacology

authors： Hay DL,Howitt SG,Conner AC,Schindler M,Smith DM,Poyner DR

更新日期：2003-10-01 00:00:00

abstract：:1. It has previously been shown that the antimigraine drug, sumatriptan, a putative 5-HT1D receptor agonist, decreases porcine common carotid and arteriovenous anastomotic blood flows, but slightly increases the arteriolar (capillary) blood flow to the skin and ears. Interestingly, such responses, being mediated by 5-...

journal_title：British journal of pharmacology

authors： De Vries P,Heiligers JP,Villalón CM,Saxena PR

更新日期：1996-05-01 00:00:00

abstract：:1. Electrically-evoked contractions in different regions of the rabbit isolated pulmonary artery have been investigated using stimulation parameters generally assumed to stimulate nerves selectively. 2. In extrapulmonary artery, trains of stimuli (10 Hz; pulse width 0.1 ms) evoked monophasic contractions. In contrast,...

journal_title：British journal of pharmacology

authors： Jackson VM,Trout SJ,Cunnane TC

更新日期：2002-10-01 00:00:00

abstract：:The effect of propranolol, a beta-adrenoceptor blocking agent, has been investigated on gastric acid secretion in pylorus and cardiac-ligated rats. Compared to the control group, propranolol significantly diminished the gastric acid secretion, and inhibited the formation of gastric ulceration. ...

journal_title：British journal of pharmacology

authors： Danhof IE,Geumei A

更新日期：1972-09-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Pancreatic cancer is a solid tumour that is often fatal. Hence, there is an urgent need to identify new drug targets for this disease. Highly proliferating cancer cells have an increased demand for nutrients and, therefore, need to up-regulate selective amino acid transporters. Here, we investiga...

journal_title：British journal of pharmacology

authors： Coothankandaswamy V,Cao S,Xu Y,Prasad PD,Singh PK,Reynolds CP,Yang S,Ogura J,Ganapathy V,Bhutia YD

更新日期：2016-12-01 00:00:00

abstract：:The concentration-dependence of the negative and positive inotropic effect of choline esters and of oxotremorine was studied in isometrically contracting papillary muscles of the guinea-pig. The preparations were obtained from reserpine-pretreated animals and were electrically driven at a frequency of 0.2 Hz. In the p...

journal_title：British journal of pharmacology

authors： Korth M,Kühlkamp V

更新日期：1987-01-01 00:00:00

abstract：:1. A series of analogues of angiotensin II (AT(II)) has been used in the present experiments to characterize receptors for AT(II) in intestinal (rat stomach strip, rat colon) and vascular (rabbit aorta) smooth muscles. Two types of compounds have been chosen: (a) agonists with reduced potency, in which 4-Tyr, 6-His or...

journal_title：British journal of pharmacology

authors： Park WK,Regoli D,Rioux F

更新日期：1973-06-01 00:00:00