The mechanism of action of cantharidin in smooth muscle.

abstract：:The effects of dopamine receptor and alpha-adrenoceptor agonists and antagonists on the stimulation-evoked overflow of radioactivity from strips of dog saphenous vein previously loaded with [3H]-noradrenaline have been examined alone and in combination. In the presence of neuronal and extraneuronal catecholamine uptak...

journal_title：British journal of pharmacology

authors： Baker DJ,Drew GM,Hilditch A

更新日期：1984-03-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Memantine and ketamine are clinically used, open-channel blockers of NMDA receptors exhibiting remarkable pharmacodynamic similarities despite strikingly different clinical profiles. Although NMDA channel gating constitutes an important difference between memantine and ketamine, it is unclear how...

journal_title：British journal of pharmacology

authors： Emnett CM,Eisenman LN,Mohan J,Taylor AA,Doherty JJ,Paul SM,Zorumski CF,Mennerick S

更新日期：2015-03-01 00:00:00

abstract：:1 Nateglinide, a novel oral hypoglycemic agent, rapidly reaches the maximum serum concentration after oral administration, suggesting that it is rapidly absorbed in the gastrointestinal tract. The aim of this work is to clarify the intestinal absorption mechanism of nateglinide by means of in vitro studies. 2 We exami...

journal_title：British journal of pharmacology

authors： Okamura A,Emoto A,Koyabu N,Ohtani H,Sawada Y

更新日期：2002-10-01 00:00:00

abstract：:1. A technique for the close-arterial administration of substances to the rat stomach in vivo has been developed. 2. Intra-arterial infusion of platelet-activating factor (Paf, 10-50 ng kg-1 min-1 for 10 min) induced macroscopically assessed damage in the corpus mucosa, characterized as vasocongestion and necrosis. 3....

journal_title：British journal of pharmacology

authors： Esplugues JV,Whittle BJ

更新日期：1988-01-01 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：:Mitochondrial permeability transition pore (mPTP) opening plays a critical role in cardiac reperfusion injury and its prevention is cardioprotective. Tumour cell mitochondria usually have high levels of hexokinase isoform 2 (HK2) bound to their outer mitochondrial membranes (OMM) and HK2 binding to heart mitochondria ...

journal_title：British journal of pharmacology

authors： Halestrap AP,Pereira GC,Pasdois P

更新日期：2015-04-01 00:00:00

abstract：:1 Amodiaquine was found to be a potent inhibitor in vitro of gastric histamine methyltransferase from human and canine corpus and from pig antrum. The ID50 for the enzyme, purified from pig antrum mucosa by ultracentrifugation and chromatography on DEAE-cellulose, was 2.5 muM. 2 In six dogs with Heidenhanin pouches th...

journal_title：British journal of pharmacology

authors： Barth H,Lorenz W,Troidl H

更新日期：1975-11-01 00:00:00

abstract：:1. Pharmacological inhibitors of protein kinase A (PKA) and protein phosphatases 1/2A were used to determine whether basal L-type Ca(2+) current (I(Ca)) observed in the absence of exogenous beta-adrenergic receptor stimulation is sustained by PKA-mediated phosphorylation. Amphotericin B was used to record whole-cell I...

journal_title：British journal of pharmacology

authors： Bracken N,Elkadri M,Hart G,Hussain M

更新日期：2006-08-01 00:00:00

abstract：:1 The possible involvement of N-methyl-D-aspartate (NMDA)-receptors in epileptiform synaptic activity in the kainic acid (KA) lesioned hippocampus was investigated. In this chronic model of epilepsy there is a loss of both the early and the late components of synaptic inhibition as well as changes in the membrane prop...

journal_title：British journal of pharmacology

authors： Ashwood TJ,Wheal HV

更新日期：1987-08-01 00:00:00

abstract：:1.--The small protein Bv8, isolated from the amphibian skin, belongs to a novel family of secreted proteins linked to several biological effects. We describe the expression of Bv8/prokineticins and their receptors in mouse macrophages, and characterize their proinflammatory activities. 2.--The rodent analogue of Bv8, ...

journal_title：British journal of pharmacology

authors： Martucci C,Franchi S,Giannini E,Tian H,Melchiorri P,Negri L,Sacerdote P

更新日期：2006-01-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Methylene blue (MB) is commonly employed as a treatment for methaemoglobinaemia, malaria and vasoplegic shock. An increasing number of studies indicate that MB can cause 5-HT toxicity when administered with a 5-HT reuptake inhibitor. MB is a potent inhibitor of monoamine oxidases, but other targe...

journal_title：British journal of pharmacology

authors： Oz M,Isaev D,Lorke DE,Hasan M,Petroianu G,Shippenberg TS

更新日期：2012-05-01 00:00:00

abstract：:1. Optimal dipeptide and peptidomimetic drug transport across the intestinal mucosal surface is dependent upon the co-operative functional activity of the di/tripeptide transporter hPepT1 and the Na(+)/H(+) exchanger NHE3. The ability of the anti-absorptive enteric neuropeptide VIP (vasoactive intestinal peptide) to m...

journal_title：British journal of pharmacology

authors： Anderson CM,Mendoza ME,Kennedy DJ,Raldua D,Thwaites DT

更新日期：2003-02-01 00:00:00

abstract：:1. The kinetics of glycine-sensitive, N-methyl-D-aspartate (NMDA) receptor desensitization were investigated in cultured neurones with the patch clamp technique. 2. The degree of fast NMDA-receptor desensitization was inversely related to glycine concentration. Thus, increasing concentrations of glycine from 30 nM to ...

journal_title：British journal of pharmacology

authors： Parsons CG,Zong X,Lux HD

更新日期：1993-05-01 00:00:00

abstract：:Nociceptive tail flick latencies (TFL) were recorded in response to noxious thermal stimuli applied to lightly anaesthetized rats. The effects of intrathecally administered dopamine receptor agonists alone and combined with dopamine receptor antagonists were examined upon the TFL. Experiments were repeated on animals ...

journal_title：British journal of pharmacology

authors： Barasi S,Ben-Sreti MM,Clatworthy AL,Duggal KN,Gonzalez JP,Robertson J,Rooney KF,Sewell RD

更新日期：1987-01-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Small molecule glucokinase activators (GKAs) have been associated with potent antidiabetic efficacy and hepatic steatosis in rodents. This study reports the discovery of S 50131 and S 51434, two novel GKAs with an original scaffold and an atypical pharmacological profile. EXPERIMENTAL APPROACH:A...

journal_title：British journal of pharmacology

authors： De Ceuninck F,Kargar C,Charton Y,Goldstein S,Perron-Sierra F,Ilic C,Caliez A,Rolin JO,Sadlo M,Harley E,Vinson C,Ktorza A

更新日期：2013-07-01 00:00:00

abstract：:1. The possibility that tachykinin NK1 receptors are involved in the plasma extravasation evoked by intradermal (i.d.) injection of Phoneutria nigriventer venom (PNV) in rat dorsal skin in vivo has been investigated. 2. Local oedema formation induced by the i.d. injection of test agents was measured by the extravascul...

journal_title：British journal of pharmacology

authors： Palframan RT,Costa SK,Wilsoncroft P,Antunes E,de Nucci G,Brain SD

更新日期：1996-05-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Catechol-O-methyltransferase (COMT) metabolizes compounds containing catechol structures and has two forms: soluble (S-COMT) and membrane-bound (MB-COMT). Here we report the generation of a mouse line that expresses MB-COMT but not S-COMT. We compared the effects of deleting S-COMT only or both C...

journal_title：British journal of pharmacology

authors： Käenmäki M,Tammimäki A,Garcia-Horsman JA,Myöhänen T,Schendzielorz N,Karayiorgou M,Gogos JA,Männistö PT

更新日期：2009-12-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Fibrosis, a pathological accumulation of collagen in tissues, represents a major global disease burden. Effective characterization of potential antifibrotic drugs has been constrained by poor formation of the extracellular matrix in vitro, due to tardy procollagen processing by collagen C-protein...

journal_title：British journal of pharmacology

authors： Chen CZ,Peng YX,Wang ZB,Fish PV,Kaar JL,Koepsel RR,Russell AJ,Lareu RR,Raghunath M

更新日期：2009-11-01 00:00:00

abstract：:G protein-coupled receptors are the largest group of membrane proteins and are the targets for approximately 30% of drugs currently used therapeutically. These 7-transmembrane-spanning proteins continue to provide new opportunities to develop therapeutics based on emerging knowledge of their structure, signalling prop...

journal_title：British journal of pharmacology

authors： Summers RJ

更新日期：2010-03-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Immunomodulatory tetracyclines are well-characterized drugs with a pharmacological potential beyond their antibiotic properties. Specifically, minocycline and doxycycline have shown beneficial effects in experimental colitis, although pro-inflammatory actions have also been described in macrophag...

journal_title：British journal of pharmacology

authors： Garrido-Mesa J,Rodríguez-Nogales A,Algieri F,Vezza T,Hidalgo-Garcia L,Garrido-Barros M,Utrilla MP,Garcia F,Chueca N,Rodriguez-Cabezas ME,Garrido-Mesa N,Gálvez J

更新日期：2018-12-01 00:00:00

abstract：:1. ICI D7114 is a novel, beta-adrenoceptor agonist which stimulates whole body oxygen consumption in conscious rats, cats and dogs and brown adipose tissue (BAT) activity in conscious rats. Treatment of rats with ICI D7114 stimulated oxygen consumption (ED50, 0.04 mg kg-1, p.o.) and BAT mitochondrial guanosine diphosp...

journal_title：British journal of pharmacology

authors： Holloway BR,Howe R,Rao BS,Stribling D,Mayers RM,Briscoe MG,Jackson JM

更新日期：1991-09-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Non-alcoholic hepatic fatty liver disease (NAFLD) is a manifestation of the metabolic syndrome in the liver and non-alcoholic steatohepatitis (NASH) represents its advanced stage. R17 derived from bouchardatine, shows benefits in the metabolic syndrome, but has not been tested in the liver. The p...

journal_title：British journal of pharmacology

authors： Rao Y,Lu YT,Li C,Song QQ,Xu YH,Xu Z,Hu YT,Yu H,Gao L,Gu LQ,Ye JM,Huang ZS

更新日期：2019-08-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Angiotensin AT1 receptor antagonists induce weight loss; however, the mechanism underlying this phenomenon is unknown. The Mas receptor agonist angiotensin-(1-7) is a metabolite of angiotensin I and of angiotensin II . As an agonist of Mas receptors, angiotensin-(1-7) has beneficial cardiovascula...

journal_title：British journal of pharmacology

authors： Schuchard J,Winkler M,Stölting I,Schuster F,Vogt FM,Barkhausen J,Thorns C,Santos RA,Bader M,Raasch W

更新日期：2015-08-01 00:00:00

abstract：:Histamine-induced contractions of small airways from human lung were substantially augmented by the cyclo-oxygenase inhibitor, indomethacin, whereas the contraction of larger airways was not. Mixed cyclo-oxygenase/lipoxygenase inhibitors of arachidonic acid metabolism did not modify histamine-induced contractions of s...

journal_title：British journal of pharmacology

authors： Adcock JJ,Garland LG

更新日期：1982-12-01 00:00:00

abstract：BACKGROUND AND PURPOSE:N-docosahexaenoylethanolamine (DHEA) is the ethanolamine conjugate of the long-chain polyunsaturated n-3 fatty acid docosahexaenoic (DHA; 22: 6n-3). Its concentration in animal tissues and human plasma increases when diets rich in fish or krill oil are consumed. DHEA displays anti-inflammatory pr...

journal_title：British journal of pharmacology

authors： Meijerink J,Poland M,Balvers MG,Plastina P,Lute C,Dwarkasing J,van Norren K,Witkamp RF

更新日期：2015-01-01 00:00:00

abstract：:1. Nociceptive thresholds to noxious mechanical (paw pressure) and thermal (tail flick) stimuli were recorded in conscious rats. The effects of three selective kappa-opioid receptor agonists on the responses to these stimuli were determined following intravenous, intracerebroventricular or intrathecal administration. ...

journal_title：British journal of pharmacology

authors： Leighton GE,Rodriguez RE,Hill RG,Hughes J

更新日期：1988-03-01 00:00:00

abstract：:Effects of isoprenaline (Isop) on the contractile properties of the smooth muscle cells of cat trachea were investigated using intact and chemically skinned muscle preparations and an isometric tension recording method. In the intact muscle preparations, Isop 3 X 10(-10) or 3 X 10(-9) M significantly suppressed the am...

journal_title：British journal of pharmacology

authors： Ito Y,Itoh T

更新日期：1984-11-01 00:00:00

abstract：:1. Behavioural activity (delayed differentiation and spatial delayed alternation) and pharmacokinetics of diazepam and its metabolites, N-desmethyldiazepam (nordiazepam), 3-hydroxydiazepam (temazepam) and 3-hydroxy-N-desmethyldiazepam (oxazepam), and of dipotassium clorazepate (clorazepate), were studied in the monkey...

journal_title：British journal of pharmacology

authors： Curry SH,Whelpton R,Nicholson AN,Wright CM

更新日期：1977-11-01 00:00:00

abstract：:1. This study describes the effects of hypoxia on relaxing responses and cAMP production induced by the known vasodilator peptides: alphaCGRP, amylin (AMY) and adrenomedullin (AM) on isolated pig coronary arteries in vitro. 2. Hypoxic incubation increased the vasorelaxant effect of alphaCGRP (four-fold; P<0.05), AMY (...

journal_title：British journal of pharmacology

authors： Hasbak P,Eskesen K,Schifter S,Edvinsson L

更新日期：2005-07-01 00:00:00

abstract：BACKGROUND AND PURPOSE:It has been extensively reported that the leading anti-diabetic drug, metformin, exerts significant anticancer effects. This hydrophilic, cationic drug requires cation transporters for cellular entry where it activates its intracellular target, the AMPK signalling pathway. However, clinical resul...

journal_title：British journal of pharmacology

authors： Cai H,Everett RS,Thakker DR

更新日期：2019-08-01 00:00:00