Assessment of selective beta-adrenoceptor blockade in man.

abstract：BACKGROUND AND PURPOSE:The human prostacyclin receptor (hIP), a G-protein coupled receptor (GPCR) expressed mainly on platelets and vascular smooth muscle cells, plays important protective roles in the cardiovascular system. We hypothesized that significant insights could be gained into the structure and function of th...

journal_title：British journal of pharmacology

authors： Stitham J,Arehart E,Gleim SR,Li N,Douville K,Hwa J

更新日期：2007-10-01 00:00:00

abstract：:The kallikrein-kinin system is subdivided into the plasma and tissue-kallikrein-kinin system, with bradykinin (BK) and kallidin (KAL) (Lys(0)-bradykinin) as functional peptides. This occurs in both humans and other mammals. Both peptides are released by plasma and tissue-kallikrein. BK, but not KAL, has been detected ...

journal_title：British journal of pharmacology

authors： Hilgenfeldt U,Stannek C,Lukasova M,Schnölzer M,Lewicka S

更新日期：2005-12-01 00:00:00

abstract：:1. The stimulatory effect of neuropeptide Y (NPY) on food intake is well established but the roles of the receptor subtypes Y(1) and Y(5) have been difficult to define. We have studied the effects of two novel Y(1)-preferring and two Y(5)-preferring agonists on feeding in guinea pigs. 2. The Y(1)-preferring receptor a...

journal_title：British journal of pharmacology

authors： Lecklin A,Lundell I,Salmela S,Männistö PT,Beck-Sickinger AG,Larhammar D

更新日期：2003-08-01 00:00:00

abstract：BACKGROUND AND PURPOSE:The use of tubulin-binding compounds, which act in part by inhibiting tumour angiogenesis, has become an integral strategy of tumour therapy. Recently, tubulysins were identified as a novel class of natural compounds of myxobacterial origin, which inhibit tubulin polymerization. As these compound...

journal_title：British journal of pharmacology

authors： Rath S,Liebl J,Fürst R,Ullrich A,Burkhart JL,Kazmaier U,Herrmann J,Müller R,Günther M,Schreiner L,Wagner E,Vollmar AM,Zahler S

更新日期：2012-11-01 00:00:00

abstract：:1. By use of patch-clamp techniques, the effects of SD-3212, a novel antiarrhythmic drug, on the calcium current (Ica), the sodium current (INa) and the muscarinic acetylcholine-receptor-operated potassium current (IK.ACh) were examined and compared with those of bepridil in guinea-pig single atrial cells. 2. SD-3212 ...

journal_title：British journal of pharmacology

authors： Hara Y,Nakaya H

更新日期：1995-11-01 00:00:00

abstract：:The effects of several anticonvulsant drugs on sodium-dependent high affinity choline uptake (HACU) in mouse hippocampal synaptosomes was investigated. HACU was measured in vitro after in vivo administration of the drug to mice. HACU was inhibited by drugs which have in common the ability to facilitate gamma-aminobuty...

journal_title：British journal of pharmacology

authors： Miller JA,Richter JA

更新日期：1985-01-01 00:00:00

abstract：:1. Plasma exudation and blood flow changes induced by intradermal injection of prostaglandins E2 (PGE2), I2 (PG12), D2 (PGD2) and F2 alpha (PGF2 alpha) were measured in rabbit dorsal skin by the use of [131I]-albumin and 133Xe. 2. Little plasma exudation was produced by any of the prostaglandins when injected alone. 3...

journal_title：British journal of pharmacology

authors： Williams TJ

更新日期：1979-03-01 00:00:00

abstract：:1. Inhalational anaesthetics modulate ligand-gated ion channels at clinical concentrations. In this paper we address submolecular mechanisms for gamma-aminobutyric acid (GABA) receptor modulation by isoflurane. 2. Wild-type Drosophila melanogaster homo-oligomeric GABA receptors were characterized and compared with an ...

journal_title：British journal of pharmacology

authors： Edwards MD,Lees G

更新日期：1997-10-01 00:00:00

abstract：:Bradykinin, angiotensin II, arginine vasopressin (AVP) or des-amino-D-arginine vasopressin (DDAVP) were administered by intravenous infusion to 10 healthy men. The concentration of 6-oxo-prostaglandin F1 alpha (6-oxo-PGF1 alpha), the stable hydrolysis product of prostacyclin (PGI2), was measured in plasma using gas ch...

journal_title：British journal of pharmacology

authors： Barrow SE,Dollery CT,Heavey DJ,Hickling NE,Ritter JM,Vial J

更新日期：1986-01-01 00:00:00

abstract：:The physiological regulation of the immune system encompasses comprehensive anti-inflammatory mechanisms that can be harnessed for the treatment of infectious and inflammatory disorders. Recent studies indicate that the vagal nerve, involved in control of heart rate, hormone secretion and gastrointestinal motility, is...

journal_title：British journal of pharmacology

authors： de Jonge WJ,Ulloa L

更新日期：2007-08-01 00:00:00

abstract：:1. The effect on membrane currents of infection of mouse neuroblastoma NA cells with rabies virus was studied by using the whole-cell patch clamp technique. 2. Three types of membrane currents, namely voltage-dependent Na+ current (I(Na)), delayed rectifier K+ current (I(K-DR)) and inward rectifier K+ current (I(K-IR)...

journal_title：British journal of pharmacology

authors： Iwata M,Komori S,Unno T,Minamoto N,Ohashi H

更新日期：1999-04-01 00:00:00

abstract：:1. A study has been made of the modulation of high-voltage activated transient and sustained calcium currents in cultured neurones of avian ciliary ganglia by nitric oxide (NO) and arachidonic acid. 2. Sodium nitroprusside (100 microM) reduced the transient calcium current (ICa) on average by 31% and the sustained ICa...

journal_title：British journal of pharmacology

authors： Khurana G,Bennett MR

更新日期：1993-06-01 00:00:00

abstract：:1. Ca currents in rat and mouse sensory dorsal root ganglion (DRG) neurones were inhibited by concentrations of (-)-baclofen as low as 1 micron. The proportion of neurones responding to baclofen was low (less than 20%), except in young cultures of neonate rat DRG neurones (3 days in culture), where 86% of the neurones...

journal_title：British journal of pharmacology

authors： Green KA,Cottrell GA

更新日期：1988-05-01 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：:1. Inhibition of rat platelet aggregation by the nitric oxide (NO) donor MAHMA NONOate (Z-1-N-methyl-N-[6-(N-methylammoniohexyl)amino]diazen-1-ium-1,2-diolate) was investigated. The aims were to compare its anti-aggregatory effect with vasorelaxation, to determine the effects of the soluble guanylate cyclase inhibitor...

journal_title：British journal of pharmacology

authors： Homer KL,Wanstall JC

更新日期：2002-12-01 00:00:00

abstract：BACKGROUND AND PURPOSE:In endothelial dysfunction, signalling by nitric oxide (NO) is impaired because of the oxidation and subsequent loss of the soluble guanylyl cyclase (sGC) haem. The sGC activator 4-[((4-carboxybutyl){2-[(4-phenethylbenzyl)oxy]phenethyl}amino)methyl[benzoic]acid (BAY 58-2667) is a haem-mimetic abl...

journal_title：British journal of pharmacology

authors： Hoffmann LS,Schmidt PM,Keim Y,Schaefer S,Schmidt HH,Stasch JP

更新日期：2009-07-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Tetracyclines were recently found to induce tumour cell death, but the early processes involved in this cytotoxic effect remain unclear. EXPERIMENTAL APPROACH:Viability of human and mouse melanoma cells was determined by MTT assay and flow cytometry. Kinase/protein/caspase activation was measure...

journal_title：British journal of pharmacology

authors： Shieh JM,Huang TF,Hung CF,Chou KH,Tsai YJ,Wu WB

更新日期：2010-07-01 00:00:00

abstract：:1. The rat spinal cord in vitro has been used to assess the effect of 6-cyano-7-nitroquinoxaline-2,3-dione (CNQX) on the dorsal root evoked extracellular ventral root reflex (DR-VRR) and the intracellular excitatory postsynaptic potential (e.p.s.p.) in ventral horn neurones and motoneurones. 2. CNQX (1-5 microM) produ...

journal_title：British journal of pharmacology

authors： King AE,Lopez-Garcia JA,Cumberbatch M

更新日期：1992-10-01 00:00:00

abstract：:1. Chronic administration of the benzodiazepine inverse agonist FG 7142 has previously been shown to induce seizure activity in mice. In the present study we have investigated the effects of acute and chronic treatment with FG 7142 in mice on the levels of acetylcholinesterase activity in cortex, hippocampus, midbrain...

journal_title：British journal of pharmacology

authors： Appleyard ME,Taylor SC,Little HJ

更新日期：1990-11-01 00:00:00

abstract：:The phenanthrene-derivative 9-phenanthrol is a recently identified inhibitor of the transient receptor potential melastatin (TRPM) 4 channel, a Ca(2+) -activated non-selective cation channel whose mechanism of action remains to be determined. Subsequent studies performed on other ion channels confirm the specificity o...

journal_title：British journal of pharmacology

authors： Guinamard R,Hof T,Del Negro CA

更新日期：2014-04-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Cholecystokinin (CCK) stimulates the release of amylase and lipase from the normal pancreas. However, it is not clear to what extent this occurs in the early stages of pancreatitis induced by biliary tract obstruction in the rat and whether CCK initiates an inflammatory cascade in this condition....

journal_title：British journal of pharmacology

authors： Barrett TD,Yan W,Freedman JM,Lagaud GJ,Breitenbucher JG,Shankley NP

更新日期：2008-04-01 00:00:00

abstract：:1. The effect of prolonged anti-hypertensive drug treatment on the blood pressure of conscious spontaneously hypertensive rats (SH-rats), and of age-matched normotensive Sprague-Dawley rats was determined during the development of hypertension in SH-rats and in the early stages of established hypertension. A compariso...

journal_title：British journal of pharmacology

authors： Hamilton TC

更新日期：1975-08-01 00:00:00

abstract：:1. The pharmacological characteristics of cloned mammalian alpha 1A/D-, alpha 1B- and alpha 1C-adrenoceptor subtypes expressed in rat 1 fibroblasts were determined in comparison to the binding and functional properties of these subtypes in rat tissues. 2. Analysis of [3H]-prazosin binding to membrane homogenates from ...

journal_title：British journal of pharmacology

authors： Kenny BA,Naylor AM,Greengrass PM,Russell MJ,Friend SJ,Read AM,Wyllie MG

更新日期：1994-04-01 00:00:00

abstract：:1. Two-electrode voltage clamp was used to study the effects of adenosine 3':5'-cyclic monophosphate (cyclic AMP) and guanosine 3':5'-cyclic monophosphate (cyclic GMP) on voltage-dependent ion channels in salivary gland cells of the leech, Haementeria ghilianii. 2. Intracellular cyclic AMP specifically blocked delayed...

journal_title：British journal of pharmacology

authors： Everill B,Berry MS

更新日期：1995-09-01 00:00:00

abstract：:1. We studied the inhibitory effect of pituitary adenylate cyclase activating polypeptide (PACAP 1-27) on the increase in total pulmonary resistance (RL) caused either by allergen or histamine in anaesthetized, ventilated guinea-pigs. 2. PACAP 1-27 given via i.v. infusion (0.045-4.5 nmol kg-1 min-1) dose-dependently r...

journal_title：British journal of pharmacology

authors： Lindén A,Yoshihara S,Chan B,Nadel JA

更新日期：1995-07-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Peptides from venomous animals have long been important for understanding pain mechanisms and for the discovery of pain treatments. Here, we hypothesized that Phα1β, a peptide from the venom of the armed spider Phoneutria nigriventer, produces analgesia by blocking the TRPA1 channel. EXPERIMENTA...

journal_title：British journal of pharmacology

authors： Tonello R,Fusi C,Materazzi S,Marone IM,De Logu F,Benemei S,Gonçalves MC,Coppi E,Castro-Junior CJ,Gomez MV,Geppetti P,Ferreira J,Nassini R

更新日期：2017-01-01 00:00:00

abstract：:1. We compared the relaxant effect of pituitary adenylate cyclase activating peptide (PACAP) 1-27 with that of a newly developed PACAP 1-27 analogue, [Arg15,20,21Leu17]-PACAP-Gly-Lys-Arg-NH2, in the guinea-pig trachea and primate bronchi in vitro (n = 4-5). 2. In the guinea-pig trachea precontracted by a submaximally ...

journal_title：British journal of pharmacology

authors： Yoshihara S,Lindén A,Kashimoto K,Nagano Y,Ichimura T,Nadel JA

更新日期：1997-08-01 00:00:00

abstract：:1. [35S]t-butylbicyclophosphorothionate (TBPS) is a high affinity ligand for the picrotoxin site of GABA(A) receptors. Here we examined TBPS binding to the cloned receptors made of alpha 1, alpha 3 or alpha 6 in combination with beta 2 or beta 2 and gamma 2 subunits, in the presence of GABA and several allosteric liga...

journal_title：British journal of pharmacology

authors： Im WB,Pregenzer JF,Thomsen DR

更新日期：1994-08-01 00:00:00

abstract：:1. The purpose of this study was to compare the pharmacological properties (i.e. the AV nodal depressant, vasodilator, and inotropic effects) of two AV nodal blocking agents belonging to different drug classes; a novel A1 adenosine receptor (A1 receptor) agonist, N-(3(R)-tetrahydrofuranyl)-6-aminopurine riboside (CVT-...

journal_title：British journal of pharmacology

authors： Snowdy S,Liang HX,Blackburn B,Lum R,Nelson M,Wang L,Pfister J,Sharma BP,Wolff A,Belardinelli L

更新日期：1999-01-01 00:00:00

abstract：:1 A method is described for repeated sampling of plasma noradrenaline (NA) in freely moving rats. Na concentration does not change during the day or after adrenalectomy. 2 Exogenous NA has a half-life of 1.5 min; drugs which block neuronal and extra-neuronal uptake lengthen this to 6.3 min. 3 Swim-stress leads to a st...

journal_title：British journal of pharmacology

authors： Benedict CR,Fillenz M,Stanford C

更新日期：1978-10-01 00:00:00