Anti-arrhythmic activities of opioid agonists and antagonists and their stereoisomers.

abstract：BACKGROUND:5-HT(2B) receptors are localized within the myenteric nervous system, but their functions on motor/sensory neurons are unclear. To explore the role of these receptors, we further characterized the 5-HT(2B) receptor antagonist RS-127445 and studied its effects on peristalsis and defecation. EXPERIMENTAL APPR...

journal_title：British journal of pharmacology

authors： Bassil AK,Taylor CM,Bolton VJ,Gray KM,Brown JD,Cutler L,Summerfield SG,Bruton G,Winchester WJ,Lee K,Sanger GJ

更新日期：2009-09-01 00:00:00

abstract：BACKGROUND AND PURPOSE:We previously reported that NCX 2057, a compound comprising a nitric oxide (NO)-releasing moiety and the natural antioxidant, ferulic acid (FA), inhibits pro-inflammatory mediators through NO-mediated gene regulation. Here, we have assessed the activities of NCX 2057 in models of inflammatory and...

journal_title：British journal of pharmacology

authors： Ronchetti D,Borghi V,Gaitan G,Herrero JF,Impagnatiello F

更新日期：2009-09-01 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：:1. The effects of several agonists of the metabotropic glutamate receptor (mGluR) were studied in adult rat striatal slices by measuring (i) KCl (30 mM)-induced output of previously taken up D-[3H]-aspartate (Asp), (ii) forskolin (30 microM)-induced adenosine 3':5'-cyclic monophosphate (cyclic AMP) accumulation and (i...

journal_title：British journal of pharmacology

authors： Lombardi G,Alesiani M,Leonardi P,Cherici G,Pellicciari R,Moroni F

更新日期：1993-12-01 00:00:00

abstract：:1. The effects of the nitrosothiol, S-nitroso N-acetylpenicillamine (SNAP) which liberates nitric oxide (NO), on ethanol-mediated gastric damage, blood flow and cyclic GMP levels in siaoloadenectomized (SALX) rats have been investigated. 2. Intraluminal instillation of ethanol (5-50% w/v) dose-dependently induced haem...

journal_title：British journal of pharmacology

authors： Tripp MA,Tepperman BL

更新日期：1995-05-01 00:00:00

abstract：:Alzheimer's disease (AD) is the most common age related neurodegenerative disease. Currently, there are no disease modifying drugs, existing therapies only offer short-term symptomatic relief. Two of the pathognomonic indicators of AD are the presence of extracellular protein aggregates consisting primarily of the Aβ ...

journal_title：British journal of pharmacology

authors： Kenche VB,Barnham KJ

更新日期：2011-05-01 00:00:00

abstract：:1. Action potentials from guinea-pig single ventricular myocytes were interrupted by application of a 300 ms voltage clamp to -40 mV in order to evoke the Ca-activated tail current which is thought to be carried by Na:Ca exchange. Stimulation frequency was 1 Hz and temperature 36 degrees C. 2. The actions of ryanodine...

journal_title：British journal of pharmacology

authors： White E,Terrar DA

更新日期：1990-10-01 00:00:00

abstract：:1 The ability of drugs to inhibit noradrenaline accumulation and to release noradrenaline was studied in the isolated anococcygeus muscle of the rat. 2 Noradrenaline, tyramine, 2-amino,6,7-dihydroxy-1,2,3,4-tetrahydronaphthalene (ADTN), 2-amino,6,7-dimethoxy-1,2,3,4-tetrahydronaphthalene (dimethyl ADTN), and 5-hydroxy...

journal_title：British journal of pharmacology

authors： Doggrell SA,Woodruff GN

更新日期：1978-07-01 00:00:00

abstract：:1. The effect of adenosine triphosphate (ATP) and its stable analogues, alpha, beta-methylene-ATP and beta, gamma-methylene-ATP, on the efferent function of capsaicin-sensitive non-adrenergic, non-cholinergic (NANC) nerves was tested in guinea-pig isolated atria. 2. Transmural nerve stimulation of atria isolated from ...

journal_title：British journal of pharmacology

authors： Rubino A,Amerini S,Ledda F,Mantelli L

更新日期：1992-03-01 00:00:00

abstract：:1. The effects of forskolin, a direct activator of adenylate cyclase and sodium nitroprusside, a direct activator of guanylate cyclase, were studied on rabbit isolated ear arteries preconstricted with 80 mM potassium. 2. Bolus injection of these two compounds resulted in vasodilatation. They had similar potencies in t...

journal_title：British journal of pharmacology

authors： Wood LM,Owen DA

更新日期：1989-03-01 00:00:00

abstract：:The ability of beta-adrenoceptor agonists to reduce the fusion of incomplete tetanic contractions of the soleus muscle of the cat has been used previously as a model to assess the potential tremor producing effect of sympathomimetic bronchodilators. The ability of (-)-isoprenaline, (-)-adrenaline, (+/-)-soterenol and ...

journal_title：British journal of pharmacology

authors： Nott MW,Raper C

更新日期：1972-03-01 00:00:00

abstract：:1. Platelet-activating factor (PAF), an inflammatory mediator, plays an important role in mediating intestinal injury. However, it remains unclear whether PAF has a function in the intestine. The production of PAF by normal intestine and by unstimulated intestinal epithelial cell lines suggests that PAF may have a reg...

journal_title：British journal of pharmacology

authors： Tan XD,Chang H,Qu XW,Caplan M,Gonzalez-Crussi F,Hsueh W

更新日期：2000-04-01 00:00:00

abstract：:Following identification of the human motilin receptor, we isolated the rabbit orthologue by PCR amplification and found this to be 85% identical to the open reading frame of the human receptor. The protein encoded was 84% identical to the human polypeptide. In HEK293T cells transfected with the rabbit receptor, motil...

journal_title：British journal of pharmacology

authors： Dass NB,Hill J,Muir A,Testa T,Wise A,Sanger GJ

更新日期：2003-11-01 00:00:00

abstract：:1. 8-Hydroxy-2-(di-n-propylamino) tetralin (8-OH-DPAT), gepirone, buspirone and ipsapirone dose-dependently antagonized the head-shakes induced by 1-(2,5-dimethoxy 4-iodophenyl)-2-amino propane hydrochloride (DOI) (1.0 mg kg-1) in mice, when these agents were given i.p. 10 min beforehand. 2. para-Chlorophenylalanine (...

journal_title：British journal of pharmacology

authors： Dursun SM,Handley SL

更新日期：1993-08-01 00:00:00

abstract：:The past two decades have seen an immense increase in our appreciation of the vast range of signalling processes and supporting machinery that occur in cells. Pivotal to this is the notion of signal compartmentalization (compartmentation). Targeting by protein domains is critical in allowing signalling complexes to be...

journal_title：British journal of pharmacology

authors： Houslay MD

更新日期：2009-09-01 00:00:00

abstract：:1. The present study investigated the central effects of the selective serotonin reuptake inhibitor (SSRI) fluoxetine and the role of 5-hydroxytryptamine(3) (5-HT(3)) receptors in the core of the nucleus accumbens (NAc) on cocaine-induced behavioural changes in rats. 2. The 5-HT(3) receptor antagonist ondansetron (1 o...

journal_title：British journal of pharmacology

authors： Herges S,Taylor DA

更新日期：2000-12-01 00:00:00

abstract：:Endothelin constricted human isolated cerebral arteries in a concentration-dependent manner. The maximal tension developed, as well as EC50 values were similar in arteries with and without endothelium. Removal of extracellular calcium or addition of the calcium antagonist nicardipine (10(-6)M), attenuated but did not ...

journal_title：British journal of pharmacology

authors： de Aguilera EM,Irurzun A,Vila JM,Aldasoro M,Galeote MS,Lluch S

更新日期：1990-03-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Saponins isolated from Panax notoginseng (Burk.) F.H. Chen have been shown to relieve thrombogenesis and facilitate haemostasis. However, it is not known which saponin accounts for this haemostatic effect. Hence, in the present study we aimed to identify which saponins contribute to its haemostat...

journal_title：British journal of pharmacology

authors： Gao B,Huang L,Liu H,Wu H,Zhang E,Yang L,Wu X,Wang Z

更新日期：2014-01-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Pituitary adenylate cyclase-activating polypeptide (PACAP) is an excitatory neuropeptide with central and peripheral cardiovascular actions. Intrathecal PACAP increases splanchnic sympathetic nerve activity and heart rate, but not mean arterial pressure (MAP). We hypothesize that the three PACAP ...

journal_title：British journal of pharmacology

authors： Inglott MA,Lerner EA,Pilowsky PM,Farnham MM

更新日期：2012-11-01 00:00:00

abstract：:1. Bepridil (BPD) is a pharmacological compound able to bind to the Ca2+ sensor protein troponin C (TnC), which triggers skeletal muscle contraction upon Ca2+-binding. BPD can thereby modulate the Ca2+-affinity of this protein. 2. The Ca2+-sensitizing action of bepridil was investigated on slow and fast isoforms of Tn...

journal_title：British journal of pharmacology

authors： Kischel P,Stevens L,Mounier Y

更新日期：1999-10-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Cigarette smoke is a major cause for chronic obstructive pulmonary disease (COPD). Andrographolide is an active biomolecule isolated from the plant Andrographis paniculata. Andrographolide has been shown to activate nuclear factor erythroid-2-related factor 2 (Nrf2), a redox-sensitive antioxidant...

journal_title：British journal of pharmacology

authors： Guan SP,Tee W,Ng DS,Chan TK,Peh HY,Ho WE,Cheng C,Mak JC,Wong WS

更新日期：2013-04-01 00:00:00

abstract：:Rats were placed on either a low sodium intake (low sodium diet 0.025% dry weight, tap water for drinking) or a high sodium intake (normal sodium diet 0.45% dry weight, 0.9% saline for drinking) for 10 days. The pressor-response curve to angiotensin II in rats previously on a high sodium intake was shifted to the left...

journal_title：British journal of pharmacology

authors： Jones DR,Penner SB,Smyth DD

更新日期：1985-12-01 00:00:00

abstract：:Homocysteine is a sulphur-containing non-proteinogenic amino acid. Hyperhomocysteinaemia (HHcy), the pathogenic elevation of plasma homocysteine as a result of an imbalance of its metabolism, is an independent risk factor for various vascular diseases, such as atherosclerosis, hypertension, vascular calcification and ...

journal_title：British journal of pharmacology

authors： Fu Y,Wang X,Kong W

更新日期：2018-04-01 00:00:00

abstract：:1 A series of cationic, lipophilic histamine H1-receptor antagonists, neuroleptics, antidepressants and monoamine oxidase inhibitors were tested for their effects on anti-IgE-induced histamine release from human lung fragments in vitro. 2 They had a biphasic effect: at low concentrations a dose-related inhibition of h...

journal_title：British journal of pharmacology

authors： Church MK,Gradidge CF

更新日期：1980-08-01 00:00:00

abstract：:After many years of effort, recent technical breakthroughs have enabled the X-ray crystal structures of three G-protein-coupled receptors (GPCRs) (beta1 and beta2 adrenergic and adenosine A(2a)) to be solved in addition to rhodopsin. GPCRs, like other membrane proteins, have lagged behind soluble drug targets such as ...

journal_title：British journal of pharmacology

authors： Congreve M,Marshall F

更新日期：2010-03-01 00:00:00

abstract：:Relaxin is a small heterodimeric peptide hormone of the insulin/relaxin superfamily produced mainly in female and male reproductive organs. It has potent antifibrotic, vasodilatory and angiogenic effects and regulates the normal function of various physiological systems. Preclinical studies and recent clinical trials ...

journal_title：British journal of pharmacology

authors： Agoulnik AI,Agoulnik IU,Hu X,Marugan J

更新日期：2017-05-01 00:00:00

abstract：:1. The pathological features of Gram-positive shock can be mimicked by the co-administration of two cell wall components of Staphylococcus aureus, namely lipoteichoic acid (LTA) and peptidoglycan (PepG). This is associated with the expression of the inducible isoform of nitric oxide synthase (iNOS) in various organs. ...

journal_title：British journal of pharmacology

authors： Kengatharan KM,De Kimpe SJ,Thiemermann C

更新日期：1996-12-01 00:00:00

abstract：:1. Elevated plasminogen activator inhibitor 1 (PAI-1) is a risk factor for thrombosis, and inhibitors of the interaction between PAI-1 and tissue plasminogen activator (t-PA) have antithrombotic and prothrombolytic activity in animals. We describe the antithrombotic effects in the rat of a monoclonal antibody (MA33H1)...

journal_title：British journal of pharmacology

authors： Berry CN,Lunven C,Lechaire I,Girardot C,O'Connor SE

更新日期：1998-09-01 00:00:00

abstract：:1. The effects of the nitric oxide synthase inhibitor NG-nitro-L-arginine methyl ester (L-NAME) on vasoconstrictor responses to transmural electrical nerve stimulation and noradrenaline were examined in the rabbit isolated renal artery with and without an intact endothelium. In addition, the effect of removing the end...

journal_title：British journal of pharmacology

authors： Vials AJ,Crowe R,Burnstock G

更新日期：1997-05-01 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