In vitro and in vivo profile of SB 206553, a potent 5-HT2C/5-HT2B receptor antagonist with anxiolytic-like properties.

abstract：:1. The haemodynamic effects of propranolol, practolol and 4-hydroxypropranolol have been compared in anaesthetized dogs both at free heart rates and at heart rates fixed by electrical pacing. All three drugs produced a fall in heart rate at the lowest dose of 0.09 mg/kg.2. Practolol caused less change in dP/dt, cardia...

journal_title：British journal of pharmacology

authors： Fitzgerald JD,O'Donnell SR

更新日期：1972-06-01 00:00:00

abstract：:The opioid receptors are key targets in the treatment of acute and chronic pain, and the development of novel analgesics with reduced side effects is crucial in the search for more effective medications. The crystal structures of opioid receptors have provided a wealth of knowledge on many aspects of opioid receptor p...

journal_title：British journal of pharmacology

authors： Marino KA,Shang Y,Filizola M

更新日期：2018-07-01 00:00:00

abstract：:The Secretin family of GPCRs are endocrine peptide hormone receptors that share a common genomic organization and are the subject of a wide variety of alternative splicing. All GPCRs contain a central seven transmembrane domain responsible for transducing signals from the outside of the cell as well as extracellular a...

journal_title：British journal of pharmacology

authors： Furness SG,Wootten D,Christopoulos A,Sexton PM

更新日期：2012-05-01 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：AIMS:The trace amine-associated receptor (Taar) family displays high species- and subtype-specific pharmacology. Several trace amines such as β-phenylethylamine (β-PEA), p-tyramine and tryptamine are agonists at TA(1) but poorly activate rat and mouse Taar4. PRINCIPAL RESULTS:Using rat TA(1) and Taar4 chimera, we id...

journal_title：British journal of pharmacology

authors： Stäubert C,Bohnekamp J,Schöneberg T

更新日期：2013-03-01 00:00:00

abstract：:1. Sarcolemmal membranes were isolated from normal and from denervated muscles and the specific binding of [125I]-alpha-bungarotoxin to the membranes was determined. 2. Cytosol prepared from either slow (soleus) or fast (extensor digitorum longus) muscle increased the toxin binding. Similar effects were seen with cyto...

journal_title：British journal of pharmacology

authors： Harborne AJ,Smith ME

更新日期：1988-07-01 00:00:00

abstract：:1. The effects of different K+ channel blockers were studied on nitric oxide (NO)-mediated non-adrenergic non-cholinergic (NANC) relaxations in the canine ileocolonic junction. 2. The non-selective blockers of K+ channels, 4-aminopyridine (4-AP) and tetraethylammonium (TEA) and the blocker of large conductance Ca(2+)-...

journal_title：British journal of pharmacology

authors： De Man JG,Boeckxstaens GE,Pelckmans PP,De Winter BY,Herman AG,Van Maercke YM

更新日期：1993-10-01 00:00:00

abstract：:Binding of the 5-HT(7) receptor antagonist radioligand [(3)H]-SB-269970 to human 5-HT(7(a)) receptors expressed in HEK293 cell membranes (h5-HT(7(a))/293) and to guinea-pig cerebral cortex membranes, was characterized and compared with [(3)H]-5-CT binding. [(3)H]-SB-269970 (1 nM) showed full association with h5-HT(7(a...

journal_title：British journal of pharmacology

authors： Thomas DR,Atkinson PJ,Ho M,Bromidge SM,Lovell PJ,Villani AJ,Hagan JJ,Middlemiss DN,Price GW

更新日期：2000-05-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Protease-activated receptor 1 (PAR1) has been demonstrated to be involved in the pathogenesis of viral diseases. However, its role remains controversial. The goal of our study was to investigate the contribution of PAR1 to respiratory syncytial virus (RSV) and human metapneumovirus (hMPV) infecti...

journal_title：British journal of pharmacology

authors： Lê VB,Riteau B,Alessi MC,Couture C,Jandrot-Perrus M,Rhéaume C,Hamelin MÈ,Boivin G

更新日期：2018-01-01 00:00:00

abstract：:1. We studied the effects of various K+ channel blockers on the vasodilator responses of guinea-pig isolated basilar arteries to nitrergic nerve stimulation, the nitric oxide (NO) donor sodium nitroprusside (SNP), and the membrane permeable guanosine-3',5'-cyclic monophosphate (cyclic GMP) analogue 8-bromo-cyclic GMP ...

journal_title：British journal of pharmacology

authors： Jiang F,Li CG,Rand MJ

更新日期：1998-01-01 00:00:00

abstract：:1. Poly(2-vinylpyridine 1-oxide) counteracts the pathogenic effects normally produced when quartz is injected into or inhaled by animals and the cytotoxic effects when quartz is added to macrophage cultures. The protective action of this polymer has been attributed variously to the formation of an adsorbed layer on th...

journal_title：British journal of pharmacology

authors： Holt PF,Lindsay H,Beck EG

更新日期：1970-01-01 00:00:00

abstract：:1 Acetylcholine, substance P, prostaglandin E1 and the nitrovasodilator glyceryl trinitrate induced concentration-dependent relaxations of endothelium-intact strips of rabbit coeliac artery precontracted with noradrenaline. 2 Endothelium-denuded strip preparations contracted to acetylcholine and showed no response to ...

journal_title：British journal of pharmacology

authors： Alheid U,Dudel C,Förstermann U

更新日期：1987-09-01 00:00:00

abstract：:The concentrations of catecholamines and the activities of dopamine-beta-hydroxylase were measured in blood obtained from decapitated diabetic and aged-matched control rats. The activity of dopamine-beta-hydroxylase in blood from diabetic rats was much greater (5 fold) than that seen for control rats. For both diabeti...

journal_title：British journal of pharmacology

authors： Berkowitz BA,Head RJ

更新日期：1978-09-01 00:00:00

abstract：:1. The effector mechanism of intestinal necrosis in rat anaphylaxis was studied following several complementary approaches: (i) the use of monoclonal antibodies (mAb) belonging to different classes (IgG1, IgG2b and IgE anti-DNP), (ii) the assay of mediators, and (iii) the use of pharmacological tools. 2. Lethality and...

journal_title：British journal of pharmacology

authors： Pellón MI,Steil AA,Furió V,Sánchez Crespo M

更新日期：1994-08-01 00:00:00

abstract：:Since its discovery over 50 years ago, cAMP has been the archetypal second messenger introducing students to the concept of cell signalling at the simplest level. As explored in this review, however, there are many more facets to cAMP signalling than the path from Gs-coupled receptor to adenylyl cyclase (AC) to cAMP t...

journal_title：British journal of pharmacology

authors： Billington CK,Hall IP

更新日期：2012-05-01 00:00:00

abstract：:1. To see if arachidonic acid (AA) plays a role in the sustained suppression of voltage-gated calcium channel currents produced by muscarinic receptor stimulation by carbachol (CCh), the effects of AA on membrane currents were examined in whole-cell voltage-clamped smooth muscle cells of the guinea-pig ileum. 2. In ce...

journal_title：British journal of pharmacology

authors： Unno T,Komori S,Ohashi H

更新日期：1996-09-01 00:00:00

abstract：:1. The possible involvement of nitric oxide (NO) in the induction and expression of morphine tolerance and dependence was studied in mice. A two-day repeated injection regimen was used to induce morphine tolerance and dependence. Tolerance was assessed by the tail flick test and physical dependence by naloxone challen...

journal_title：British journal of pharmacology

authors： Dambisya YM,Lee TL

更新日期：1996-03-01 00:00:00

abstract：:1 The influence of the external calcium concentration on the effect of harmine 2 x 10(-5) M upon the guinea-pig atrial muscle was analysed. Transmembrane potentials of contractile fibres were measured during exposure to the drug at 30 degrees C. 2 In preparations superfused with 1.35 mM Ca2+-Tyrode solution and driven...

journal_title：British journal of pharmacology

authors： Carpentier RG

更新日期：1981-10-01 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：:The effects of treatment with rolipram, a specific phosphodiesterase IV inhibitor, on learning and memory function and on the cyclic AMP/PKA/CREB signal transduction system were examined in rats with microsphere embolism (ME)-induced cerebral ischaemia. Sustained cerebral ischaemia was induced by the injection of 900 ...

journal_title：British journal of pharmacology

authors： Nagakura A,Niimura M,Takeo S

更新日期：2002-04-01 00:00:00

abstract：:In this issue, BJP is proud to publish an Endothelium Themed Section to celebrate the life of Robert F. Furchgott, who died on May 19th 2009. It is 30 years since he discovered endothelium-derived relaxant factor and a decade since he was awarded the Nobel Prize for this work. His discovery has led to an array of new ...

journal_title：British journal of pharmacology

authors： McGrath JC

更新日期：2009-06-01 00:00:00

abstract：:1. Possible interactions between non-steroidal anti-inflammatory drugs (NSAIDs) and endogenous opioids were examined in electrophysiological experiments in alpha-chloralose anaesthetized spinalized rats without or with carrageenan-induced acute inflammation of one hindpaw. Spinal reflex responses, monitored as single ...

journal_title：British journal of pharmacology

authors： Herrero JF,Headley PM

更新日期：1996-06-01 00:00:00

abstract：:1. Endotoxin shock is accompanied by an increase in peripheral vascular permeability. It has been postulated that most biological activities of LPS are derived from lipid A moiety. Here we examined the effect of lipid A analogue ONO-4007 in increasing vascular permeability and the possible mediators in mouse skin by a...

journal_title：British journal of pharmacology

authors： Ishida H,Fujii E,Irie K,Yoshioka T,Muraki T,Ogawa R

更新日期：2000-07-01 00:00:00

abstract：:1. The presence of an endogenous digitalis-like factor (EDLF) in the plasma of both normal and volume expanded animals is well documented. In this study we have used ouabain and bufalin as pharmacological analogues to mimic the renal effects of EDLF and to investigate whether any interaction occurs between atrial natr...

journal_title：British journal of pharmacology

authors： Yates NA,McDougall JG

更新日期：1993-03-01 00:00:00

abstract：:The antioestrogen, tamoxifen, blocks volume-regulated chloride channels and reduces transparency in bovine lenses maintained in vitro. In contrast to tamoxifen, the steroidal antioestrogen, ICI 182780, did not block volume-regulated chloride currents in three cultured cell lines and required 10 fold higher concentrati...

journal_title：British journal of pharmacology

authors： Zhang JJ,Jacob TJ,Hardy SP,Higgins CF,Valverde MA

更新日期：1995-08-01 00:00:00

abstract：:1 alpha-Monofluoromethyldopa (MFMD, RMI 71963), a potent and selective enzyme-activated irreversible inhibitor of aromatic L-amino acid decarboxylase produces a substantial and long-lasting decrease in the catecholamine content of mouse brain, heart and kidney. 2 Single doses of MFMD reduce the 5-hydroxytryptamine con...

journal_title：British journal of pharmacology

authors： Bey P,Jung MJ,Koch-Weser J,Palfreyman MG,Sjoerdsma A,Wagner J,Zraïka M

更新日期：1980-12-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Kyotorphin (KTP; L-Tyr-L-Arg), an endogenous neuropeptide, is potently analgesic when delivered directly to the central nervous system. Its weak analgesic effects after systemic administration have been explained by inability to cross the blood-brain barrier (BBB) and detract from the possible cl...

journal_title：British journal of pharmacology

authors： Ribeiro MM,Pinto A,Pinto M,Heras M,Martins I,Correia A,Bardaji E,Tavares I,Castanho M

更新日期：2011-07-01 00:00:00

abstract：BACKGROUND AND PURPOSE:The regulation of vascular soluble guanylyl cyclase (sGC) expression by nitric oxide (NO) is still under discussion. In vitro, NO has been shown to downregulate the expression of sGC but it is unclear if this mechanism is operative in vivo and occurs during nitrate treatment. EXPERIMENTAL APPROA...

journal_title：British journal of pharmacology

authors： Oppermann M,Dao VT,Suvorava T,Bas M,Kojda G

更新日期：2008-10-01 00:00:00

abstract：:The effects of injection of 3,4-methylenedioxymethamphetamine (MDMA), 3,4-methylenedioxyamphetamine (MDA) and N-ethyl-3,4-methylenedioxyamphetamine (MDEA) (all 20 mg kg(-1)) on blood pressure, heart rate, core body temperature and locomotor activity in conscious rats were investigated using radiotelemetry. MDMA and MD...

journal_title：British journal of pharmacology

authors： Bexis S,Docherty JR

更新日期：2006-04-01 00:00:00

abstract：:1. Interactions of bath-applied pentobarbitone and gamma-aminobutyric acid (GABA) on neurones in isolated superior cervical ganglia of the rat have been examined with intracellular microelectrodes. 2. Pentobarbitone itself (30 micrometer-1 mM) showed no clear or consistent GABA-like effects: changes in resting input c...

journal_title：British journal of pharmacology

authors： Brown DA,Constanti A

更新日期：1978-05-01 00:00:00