The 5-HT4 receptor antagonist ML10375 inhibits the constitutive activity of human 5-HT4(c) receptor.

abstract：:1. Intrathecal (i.t.) administration of nociceptin and high doses of morphine induced allodynia in response to innocuous tactile stimuli, and i.t. nociceptin evoked hyperalgesia in response to noxious thermal stimuli in conscious mice. Here we have characterized the nociceptin-induced allodynia and compared it with th...

journal_title：British journal of pharmacology

authors： Hara N,Minami T,Okuda-Ashitaka E,Sugimoto T,Sakai M,Onaka M,Mori H,Imanishi T,Shingu K,Ito S

更新日期：1997-06-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Inhaled glucocorticoid (ICS)/long-acting β2 -adrenoceptor agonist (LABA) combination therapy is a recommended treatment option for patients with moderate/severe asthma in whom adequate control cannot be achieved by an ICS alone. Previously, we discovered that LABAs can augment dexamethasone-induc...

journal_title：British journal of pharmacology

authors： Joshi T,Johnson M,Newton R,Giembycz MA

更新日期：2015-05-01 00:00:00

abstract：:1. The aim of the present study was to examine whether ramipril induces delayed myocardial protection against free radical injuries ex vivo and to determine the possible role of the bradykinin B2-nitric oxide (NO) pathway, prostaglandins(PGs) and protein synthesis in this delayed adaptive response. 2. Rats were pretre...

journal_title：British journal of pharmacology

authors： Jin ZQ,Chen X

更新日期：1998-10-01 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：:1. Idioventricular rate responses and adrenoceptor number have been examined in normal Langendorff hearts perfused at 70 cmH2O and in 'ischaemic' hearts perfused at 10 cmH2O. 2. In hearts perfused at normal pressure, ventricular rate responses to phenylephrine in the presence of propranolol were biphasic with low conc...

journal_title：British journal of pharmacology

authors： Butterfield MC,Chess-Williams R

更新日期：1990-07-01 00:00:00

abstract：:1. The purpose of this investigation was to determine whether enhanced contractile responses to noradrenaline (NA) of mesenteric arteries from rats with chronic streptozotocin-induced diabetes are associated with increases in mean cytosolic [Ca(2+)]i. 2. [Ca(2+)]i was measured with fura 2-AM, and was monitored simulta...

journal_title：British journal of pharmacology

authors： Chow WL,Zhang L,MacLeod KM

更新日期：2001-09-01 00:00:00

abstract：:The arterial endothelium critically contributes to blood pressure control by releasing vasodilating autacoids such as nitric oxide, prostacyclin and a third factor or pathway termed 'endothelium-derived hyperpolarizing factor' (EDHF). The nature of EDHF and EDHF-signalling pathways is not fully understood yet. However...

journal_title：British journal of pharmacology

authors： Grgic I,Kaistha BP,Hoyer J,Köhler R

更新日期：2009-06-01 00:00:00

abstract：:1 The butyrophenone tranquilizer, azaperone, was administered intramuscularly, at dose levels of 0.4 and 0.8 mg/kg, to ponies and its effects on cardiovascular and respiratory functions assessed. 2 Arterial blood pH, CO2 tension (PaCO2) and O2 tension (PaO2) remained relatively constant throughout the course of action...

journal_title：British journal of pharmacology

authors： Lees P,Serrano L

更新日期：1976-03-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Pulmonary arterial hypertension (PAH) is characterized by enhanced pulmonary vascular resistance, right ventricular hypertrophy and increased right ventricular systolic pressure. Here, we investigated the effects of a N-acylhydrazone derivative, 3,4-dimethoxyphenyl-N-methyl-benzoylhydrazide (LASS...

journal_title：British journal of pharmacology

authors： Alencar AK,Pereira SL,Montagnoli TL,Maia RC,Kümmerle AE,Landgraf SS,Caruso-Neves C,Ferraz EB,Tesch R,Nascimento JH,de Sant'Anna CM,Fraga CA,Barreiro EJ,Sudo RT,Zapata-Sudo G

更新日期：2013-07-01 00:00:00

abstract：:The effects of 10 mM caffeine (CAF) on intramembrane charge movements (ICM) were studied in isolated guinea-pig ventricular heart cells with the whole-cell patch-clamp technique. In the presence of CAF, the properties (voltage dependence, maximum Q(ON) [Q(max)], availability with voltage) of Q(ON) charge activated fro...

journal_title：British journal of pharmacology

authors： Leroy J,Lignon JM,Gannier F,Argibay JA,Malécot CO

更新日期：2002-02-01 00:00:00

abstract：:Botulinum toxin (Type A) depressed or abolished transmission from postganglionic nerves to smooth muscle of isolated preparations of guinea-pig and mouse vas deferens. The time course of blockade was 2 to 6 times slower than that observed with the same concentration of the same batch of toxin on the rat diaphragm. Spo...

journal_title：British journal of pharmacology

authors： Holman ME,Spitzer NC

更新日期：1973-02-01 00:00:00

abstract：:Irritable bowel syndrome is characterized by visceral hyperalgesia commonly associated with stress and inflammatory processes. We investigated the role of tachykinin NK2 receptors in the ability of trinitrobenzenesulphonic acid (TNBS) and stress to enhance the sensitivity of the rat rectum to distension using a select...

journal_title：British journal of pharmacology

authors： Toulouse M,Coelho AM,Fioramonti J,Lecci A,Maggi C,Buéno L

更新日期：2000-01-01 00:00:00

abstract：BACKGROUND AND PURPOSE:The Na+/Ca2+ exchanger (NCX) may contribute to triggered activity and transmural dispersion of repolarization, which are substrates of torsades de pointes (TdP) type arrhythmias. This study examined the effects of selective inhibition of the NCX by SEA0400 on the occurrence of dofetilide-induced ...

journal_title：British journal of pharmacology

authors： Farkas AS,Makra P,Csík N,Orosz S,Shattock MJ,Fülöp F,Forster T,Csanády M,Papp JG,Varró A,Farkas A

更新日期：2009-03-01 00:00:00

abstract：:1. The interaction between endogenous nitric oxide (NO) and factors from the rat submandibular salivary gland such as epidermal growth factor (EGF) on gastric mucosal integrity in the rat has been investigated. 2. Bolus administration of the NO synthase inhibitor, NG nitro-L-arginine methyl ester (L-NAME; 6.25-50 mg k...

journal_title：British journal of pharmacology

authors： Tepperman BL,Soper BD

更新日期：1993-09-01 00:00:00

abstract：:Strips of human pulmonary arteries from patients undergoing surgery for lung tumour were incubated with [3H]-noradrenaline. Subsequently, they were superfused with physiological salt solution containing cocaine and corticosterone. Tritium overflow from the strips was stimulated by transmural electrical impulses (2 Hz)...

journal_title：British journal of pharmacology

authors： Göthert M,Hentrich F

更新日期：1985-08-01 00:00:00

abstract：:Burimamide, an H(2)-receptor blocking agent, has been shown capable of blocking the uptake and metabolism of [(14)C]-histamine, both in the guinea-pig isolated atrium and in murine neoplastic mast cells. This occurs even at concentrations far below the dose range capable of blocking the positive chronotropic effect of...

journal_title：British journal of pharmacology

authors： Fantozzi R,Mannaioni PF,Moroni F

更新日期：1973-10-01 00:00:00

abstract：BACKGROUND AND PURPOSE:In mammalian cells, the anti-parasitic drug ivermectin is known as a positive allosteric modulator of the ATP-activated ion channel P2X4 and is used to discriminate between P2X4- and P2X7-mediated cellular responses. In this paper we provide evidence that the reported isoform selectivity of iverm...

journal_title：British journal of pharmacology

authors： Nörenberg W,Sobottka H,Hempel C,Plötz T,Fischer W,Schmalzing G,Schaefer M

更新日期：2012-09-01 00:00:00

abstract：:There is evidence that cannabinoid-based medicines that are selective for different targets in the cannabinoid signalling system (e.g. receptors, inactivation mechanism, enzymes) might be beneficial in basal ganglia disorders, namely Parkinson's disease (PD) and Huntington's disease (HD). These benefits not only inclu...

journal_title：British journal of pharmacology

authors： Fernández-Ruiz J

更新日期：2009-04-01 00:00:00

abstract：:1. In Ca-free solution, the contractile response of guinea-pig taenia caecum to 10(-4) M carbachol was mediated through muscarinic receptors and was reduced time-dependently by desensitization with 10(-4) M carbachol, but not 10(-4) M histamine. On the other hand, the response to 10(-4) M histamine was shown to be med...

journal_title：British journal of pharmacology

authors： Hishinuma S,Uchida MK

更新日期：1988-07-01 00:00:00

abstract：:1. We have investigated the effects of RP 73401, a novel, potent and highly selective cyclic nucleotide phosphodiesterase (PDE) type IV inhibitor, in guinea-pig and rat models of bronchoconstriction and allergic inflammation. In some models, the effects of RP 73401 have been compared with those of the standard PDE typ...

journal_title：British journal of pharmacology

authors： Raeburn D,Underwood SL,Lewis SA,Woodman VR,Battram CH,Tomkinson A,Sharma S,Jordan R,Souness JE,Webber SE

更新日期：1994-12-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Stress is believed to be associated with the development of neuropsychiatric disorders, including Alzheimer's disease (AD). We have studied mechanisms implicated in vulnerability to stress and the relationship with changes in AD-related markers. EXPERIMENTAL APPROACH:Anhedonia induced by a chron...

journal_title：British journal of pharmacology

authors： Briones A,Gagno S,Martisova E,Dobarro M,Aisa B,Solas M,Tordera R,Ramírez M

更新日期：2012-02-01 00:00:00

abstract：:The effect of trimetazidine (TMZ), an anti-anginal drug, on the mechanical response of the guinea-pig ductus arteriosus placed under conditions of mild hypoxia (PO2 approximately equal to 75 mmHg) was investigated. When the PO2 of the bathing solution was 75 mmHg, TMZ caused a dose-dependent increase in tension. The m...

journal_title：British journal of pharmacology

authors： Garnier D,Roulet MJ

更新日期：1985-02-01 00:00:00

abstract：BACKGROUND AND PURPOSE:The chemokine receptor CXCR3 directs migration of T-cells in response to the ligands CXCL9/Mig, CXCL10/IP-10 and CXCL11/I-TAC. Both ligands and receptors are implicated in the pathogenesis of inflammatory disorders, including atherosclerosis and rheumatoid arthritis. Here, we describe the molecul...

journal_title：British journal of pharmacology

authors： Nedjai B,Li H,Stroke IL,Wise EL,Webb ML,Merritt JR,Henderson I,Klon AE,Cole AG,Horuk R,Vaidehi N,Pease JE

更新日期：2012-06-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Diabetes causes sensory polyneuropathy with associated pain in the form of tactile allodynia and thermal hyperalgesia which are often intractable and resistant to current therapy. This study tested the beneficial effects of the non-peptide and orally active kinin B(1) receptor antagonist SSR24061...

journal_title：British journal of pharmacology

authors： Dias JP,Ismael MA,Pilon M,de Champlain J,Ferrari B,Carayon P,Couture R

更新日期：2007-09-01 00:00:00

abstract：:1. In order to characterize the neuropeptide Y (NPY) Y1 receptors known to be present in rabbit isolated vas deferens and saphenous vein, the pharmacological activity of the selective NPY Y1 receptor agonists, [Leu31,Pro34] NPY and various other peptide agonists, together with the putative NPY antagonist, benextramine...

journal_title：British journal of pharmacology

authors： Palea S,Corsi M,Rimland JM,Trist DG

更新日期：1995-05-01 00:00:00

abstract：:Extensive in vitro and in vivo studies have shown that cannabinoid drugs have neuroprotective properties and suggested that the endocannabinoid system may be involved in endogenous neuroprotective mechanisms. On the other hand, neurotoxic effects of cannabinoids in vitro and in vivo were also described. Several possib...

journal_title：British journal of pharmacology

authors： Sarne Y,Asaf F,Fishbein M,Gafni M,Keren O

更新日期：2011-08-01 00:00:00

abstract：BACKGROUND AND PURPOSE:MLN4924 prevents the formation of active cullin-RING ubiquitin ligase complexes and thus inhibits NF-κB signalling. Here, we evaluated the effects of this compound on monocytes and dendritic cells (DCs). EXPERIMENTAL APPROACH:Monocytes and DCs were challenged with TNF or LPS in the presence and ...

journal_title：British journal of pharmacology

authors： El-Mesery M,Seher A,Stühmer T,Siegmund D,Wajant H

更新日期：2015-03-01 00:00:00

abstract：:1. The drug HA-966 (1-hydroxy-3-amino-pyrrolidone-2), which chemically resembles the cyclic form of GABA, has been studied for neuro-pharmacological properties and for effects on the catecholamine content of the corpus striatum.2. The acute effects on spontaneous behaviour of rodents included flaccid catalepsy and rev...

journal_title：British journal of pharmacology

authors： Bonta IL,De Vos CJ,Grijsen H,Hillen FC,Noach EL,Sim AW

更新日期：1971-11-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Uridine 5'-triphosphate (UTP) is a potent vasoconstrictor of cerebral arteries and induces Ca(2+) waves in vascular smooth muscle cells (VSMCs). This study aimed to determine the mechanisms underlying UTP-induced Ca(2+) waves in VSMCs of the rat basilar artery. EXPERIMENTAL APPROACH:Isometric fo...

journal_title：British journal of pharmacology

authors： Syyong HT,Yang HH,Trinh G,Cheung C,Kuo KH,van Breemen C

更新日期：2009-02-01 00:00:00

abstract：:1 A procedure involving two guinea-pig isolated hearts perfused in series is described for detecting in the recipient heart the release of a possible coronary vasodilator metabolite from the donor heart. 2 Adrenaline and isoprenaline stimulated the rate and force of contraction and produced a multiphasic coronary vasc...

journal_title：British journal of pharmacology

authors： Broadley KJ

更新日期：1976-09-01 00:00:00