Pharmacological evidence for the 5-HT7 receptor mediating smooth muscle relaxation in canine cerebral arteries.

abstract：BACKGROUND AND PURPOSE:Translation of non-clinical markers of delayed ventricular repolarization to clinical prolongation of the QT interval corrected for heart rate (QTc) (a biomarker for torsades de pointes proarrhythmia) remains an issue in drug discovery and regulatory evaluations. We retrospectively analysed 150 d...

journal_title：British journal of pharmacology

authors： Park E,Gintant GA,Bi D,Kozeli D,Pettit SD,Pierson JB,Skinner M,Willard J,Wisialowski T,Koerner J,Valentin JP

更新日期：2018-02-01 00:00:00

abstract：BACKGROUND AND PURPOSE:In cardiac myocytes, cAMP produced by both β1 and β2 -adrenergic receptors (ARs) results in an increase in L-type Ca2+ channel activity and myocyte contraction. However, only cAMP produced by β1 ARs is able to enhance myocyte relaxation through phospholamban-dependent regulation of the sarco/endo...

journal_title：British journal of pharmacology

authors： Rudokas MW,Post JP,Sataray-Rodriguez A,Sherpa RT,Moshal KS,Agarwal SR,Harvey RD

更新日期：2021-01-21 00:00:00

abstract：BACKGROUND AND PURPOSE:The free fatty acid receptor 1 (FFAR1) plays an important role in glucose-stimulated insulin secretion making it an attractive anti-diabetic target. This study characterizes the pharmacological profile of HWL-088 (2-(2-fluoro-4-((2'-methyl-[1,1'- biphenyl]-3-yl)methoxy)phenoxy)acetic acid), a nov...

journal_title：British journal of pharmacology

authors： Chen Y,Ren Q,Zhou Z,Deng L,Hu L,Zhang L,Li Z

更新日期：2020-05-01 00:00:00

abstract：:1 Prolonged exposure (6-12 h) of rat aorta to alpha1-adrenergic receptor (alpha(1)AR) agonist phenylephrine (Phe) leads to a decrease in alpha(1)AR-mediated vasoconstriction. This reduced responsiveness to alpha(1)AR stimulation was strongly dependent on the intactness of the endothelium. 2 We examined the effect of P...

journal_title：British journal of pharmacology

authors： Gürdal H,Can A,Uğur M

更新日期：2005-05-01 00:00:00

abstract：:1. We previously demonstrated that cyclopiazonic acid (CPA), an inhibitor of Ca(2+)-ATPase in the sarcoplasmic reticulum, induced rhythmic relaxations of active tension in the endothelium-denuded small arteries of the mesentery and the ear of the rabbit, but that this agent failed to induce rhythmic responses in the e...

journal_title：British journal of pharmacology

authors： Omote M,Mizusawa H

更新日期：1996-05-01 00:00:00

abstract：:The detrimental actions of leptin on cardiovascular function are well established. Smith et al. report the novel finding of a reduction of infarct size by exogenous leptin when given at reperfusion. The involvement of the reperfusion injury salvage kinase (RISK) pathway in such reduction of infarct size and its relati...

journal_title：British journal of pharmacology

authors： Heusch G

更新日期：2006-09-01 00:00:00

abstract：:1 The effects of general anaesthetics on the responses of neurones to iontophoretically applied L-glutamate have been examined in slices of the guinea-pig olfactory cortex in vitro. 2 Concentrations of pentobarbitone, ether, methoxyflurance, trichloroethylene and alphaxalone that are known to depress synaptic transmis...

journal_title：British journal of pharmacology

authors： Richards CD,Smaje JC

更新日期：1976-11-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Hydrogen sulphide (H(2)S) is a labile, endogenous metabolite of cysteine, with multiple biological roles. The development of sulphide-based therapies for human diseases will benefit from a reliable method of quantifying H(2)S in blood and tissues. EXPERIMENTAL APPROACH:Concentrations of reactive...

journal_title：British journal of pharmacology

authors： Wintner EA,Deckwerth TL,Langston W,Bengtsson A,Leviten D,Hill P,Insko MA,Dumpit R,VandenEkart E,Toombs CF,Szabo C

更新日期：2010-06-01 00:00:00

abstract：:The present study examined the ability of the selective imidazoline I(2)-site ligands 2-(-2-benzofuranyl)-2-imidazoline (2-BFI) and 2-[4,5-dihydroimidaz-2-yl]-quinoline (BU224) and selected monoamine oxidase (MAO) inhibitors to evoke locomotor activity in rats bearing a lesion of the nigrostriatal pathway. Male Spragu...

journal_title：British journal of pharmacology

authors： Macinnes N,Duty S

更新日期：2004-12-01 00:00:00

abstract：BACKGROUND AND PURPOSE:A fluorinated derivative (2F-MT-45) of the synthetic μ-opioid receptor agonist MT-45 (1-cyclohexyl-4-(1,2-diphenylethyl)piperazine) was recently identified in a seized illicit tablet. While MT-45 is a Class A drug, banned in a number of countries, nothing is known about the pharmacology of 2F-MT-...

journal_title：British journal of pharmacology

authors： Baptista-Hon DT,Smith M,Singleton S,Antonides LH,Nic Daeid N,McKenzie C,Hales TG

更新日期：2020-08-01 00:00:00

abstract：:1. The systemic and regional haemodynamic effects of the potassium channel activator EMD 52692 or its solvent were investigated after intravenous and after intracoronary administration in anaesthetized pigs. 2. Consecutive intravenous 10 min infusions of EMD 52692 (0.15, 0.30, 0.60, 1.20 micrograms kg-1 min-1; n = 7) ...

journal_title：British journal of pharmacology

authors： Sassen LM,Duncker DJ,Gho BC,Diekmann HW,Verdouw PD

更新日期：1990-11-01 00:00:00

abstract：:The processes underpinning post-developmental neurogenesis in the mammalian brain continue to be defined. Such processes involve the proliferation of neural stem cells and neural progenitor cells (NPCs), neuronal migration, differentiation and integration into a network of functional synapses within the brain. Both in...

journal_title：British journal of pharmacology

authors： Prenderville JA,Kelly ÁM,Downer EJ

更新日期：2015-08-01 00:00:00

abstract：:The discovery of the nitric oxide/cGMP pathway was the basis for our understanding of many normal physiological functions and the pathophysiology of several diseases. Since the discovery and introduction of sildenafil, inhibitors of PDE5 have been the first-line therapy for erectile dysfunction (ED). The success of si...

journal_title：British journal of pharmacology

authors： Andersson KE

更新日期：2018-07-01 00:00:00

abstract：:1 In cats anaesthetized with pentobarbitone and vagotomized, observations were made on the phrenic nerve action potential and the diaphragm electromyogram (EMG) at constant end-tidal Pco(2). Arterial blood pressure was stabilized by intravenous infusions of noradrenaline.2 Intravenous administration of saxitoxin (STX)...

journal_title：British journal of pharmacology

authors： Borison HL,Culp WJ,Gonsalves SF,McCarthy LE

更新日期：1980-02-01 00:00:00

abstract：:1. Bradykinin has multiple effects on differentiated NG108-15 neuroblastoma x glioma cells: it increases Ins(1,4,5)P3 production and intracellular Ca2+ concentration [Ca2+]i evokes a Ca2+ activated K+ current (IK(Ca)) and inhibits M current (IM). We studied the effect of the aminosteroid U73122 and the antibiotic neom...

journal_title：British journal of pharmacology

authors： Hildebrandt JP,Plant TD,Meves H

更新日期：1997-03-01 00:00:00

abstract：:The effects of high (20 mM) concentrations of caffeine were studied on the transmembrane voltage and currents in rat single ventricular myocytes by the whole cell configuration of the patch clamp technique. Rapid application of caffeine released Ca2+ from the sarcoplasmic reticulum and induced a Ni(2+)-sensitive trans...

journal_title：British journal of pharmacology

authors： Varro A,Hester S,Papp JG

更新日期：1993-08-01 00:00:00

abstract：:1. We showed earlier that NO inhibition caused a left-shift and augmented Emax of the concentration-response curve of AT1-mediated (angiotensin II)-induced vasoconstrictions (AII-VC) in the rat kidney. The 0.01-0.1 nM AII-VC unmasked by the potentiating effect of NO inhibition, were sensitive not only to AT1 (L158809)...

journal_title：British journal of pharmacology

authors： Muller C,Endlich K,Helwig JJ

更新日期：1998-07-01 00:00:00

abstract：:1. NaF (10 mM) produced a 2-3 fold increase in adenylate cyclase activity in homogenates of NG108-15 cells incubated in the presence of 1 microM GTP. Higher concentrations of NaF suppressed adenylate cyclase activity. 2. In the presence of the adenosine receptor agonist 5'-(N-ethyl)-carboxamidoadenosine (NECA; 100 mic...

journal_title：British journal of pharmacology

authors： Kelly E,Keen M,Nobbs P,MacDermot J

更新日期：1990-06-01 00:00:00

abstract：:1. The pharmacological characteristics of alpha 1-adrenoceptor binding sites in rat pineal gland membranes, detected by use of a selective alpha 1-adrenoceptor antagonist ([125I]-iodo-2-[beta-(4-hydroxyphenyl) ethylaminomethyl]tetralone, [125I]-HEAT), were investigated with the alkylating agent, chloroethylclonidine (...

journal_title：British journal of pharmacology

authors： Sugden D,Anwar N,Klein DC

更新日期：1996-07-01 00:00:00

abstract：:1. Acute moderate hypoxia modifies the catalytic activity and expression of certain isoenzymes of hepatic cytochrome P450 (P450). The aim of this study was to document whether hypoxia affects hepatic P450 directly or through the release of serum mediators. 2. Rabbits were subjected to a FiO(2) of 8% for 48 h, sacrific...

journal_title：British journal of pharmacology

authors： Fradette C,Bleau AM,Pichette V,Chauret N,Du Souich P

更新日期：2002-11-01 00:00:00

abstract：:[This retracts the article on p. 3702 in vol. 171, PMID: 24758388.]. ...

journal_title：British journal of pharmacology

authors：

更新日期：2015-09-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Inhibitory junction potentials (IJP) are responsible for smooth muscle relaxation in the gastrointestinal tract. The aim of this study was to pharmacologically characterize the neurotransmitters [nitric oxide (NO) and adenosine triphosphate (ATP)] and receptors involved at the inhibitory neuromus...

journal_title：British journal of pharmacology

authors： Grasa L,Gil V,Gallego D,Martín MT,Jiménez M

更新日期：2009-11-01 00:00:00

abstract：:1. This study exploited established immunoneutralization protocols and an N-terminal annexin 1 peptide (annexin 1(Ac2 - 26)) to advance our knowledge of the role of annexin 1 as a mediator of acute glucocorticoid action in the rat neuroendocrine system in vivo. 2. Rats were treated with corticosterone (500 microg kg(-...

journal_title：British journal of pharmacology

authors： Philip JG,John CD,Cover PO,Morris JF,Christian HC,Flower RJ,Buckingham JC

更新日期：2001-10-01 00:00:00

abstract：:1. This study tested the hypothesis that the systemic effects of burn include altered metabolic activity in the heart. Metabolic activity was studied by measuring alterations in cyclic nucleotide levels and protein concentrations in atrial and ventricular muscle in mice at 14 and 22 days after a 20% body surface area ...

journal_title：British journal of pharmacology

authors： Tomera JF,Martyn JA

更新日期：1990-10-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Our team previously demonstrated that diabetes induces a deterioration in vascular dynamics, in parallel with the enhanced formation of advanced glycation end products. The aim of this study was to determine whether prevention of the arterial stiffening by pyridoxamine in diabetes is associated w...

journal_title：British journal of pharmacology

authors： Chang KC,Liang JT,Tsai PS,Wu MS,Hsu KL

更新日期：2009-08-01 00:00:00

abstract：:In the present study we tested the effects of the antihyperalgesic compound gabapentin on dorsal horn neurones in adult spinal cord. Slices were taken from control and hyperalgesic animals suffering from streptozocin-induced diabetic neuropathy. At concentrations up to 100 microM, bath application failed to affect the...

journal_title：British journal of pharmacology

authors： Patel MK,Gonzalez MI,Bramwell S,Pinnock RD,Lee K

更新日期：2000-08-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Betulinic acid (BA) is a naturally occurring triterpenoid widely distributed throughout the plant kingdom. We previously reported that BA inhibits lipopolysaccharide (LPS)-induced interleukin-6 production through modulation of nuclear factor κB (NF-κB) in human peripheral blood mononuclear cells ...

journal_title：British journal of pharmacology

authors： Viji V,Helen A,Luxmi VR

更新日期：2011-03-01 00:00:00

abstract：:1. Porcine neuromedin U-8 produced a concentration (0.3 nM-1 microM)-dependent contraction of the longitudinal muscle of the human isolated ileum, which was unaffected by either atropine (1 microM) or tetrodotoxin (1 microM). 2. By contrast, neuromedin U-8 had only a weak effect on the circular muscle of the human iso...

journal_title：British journal of pharmacology

authors： Maggi CA,Patacchini R,Giuliani S,Turini D,Barbanti G,Rovero P,Meli A

更新日期：1990-01-01 00:00:00

abstract：:1. The effects of sodium nitroprusside (SNP, a nitric oxide donor) and authentic nitric oxide (NO) on superoxide anion (O2-) generation were investigated in human polymorphonuclear leukocytes (PMNs). 2. Neither SNP (10 nM to 10 microM) nor NO (40 nM to 40 microM) alone induced O2- generation or change of intracellular...

journal_title：British journal of pharmacology

authors： Morikawa M,Inoue M,Tokumaru S,Kogo H

更新日期：1995-08-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Botulinum toxin type A (BoNT/A) injections into hyperactive muscles provide effective treatment for spasticity and dystonias, presumably due to its local effects on extrafusal and intrafusal motor fibres. A recent discovery of toxin's retrograde axonal transport to CNS might suggest additional ac...

journal_title：British journal of pharmacology

authors： Matak I

更新日期：2020-01-01 00:00:00