Alterations of the benzodiazepine site of rat alpha 6 beta 2 gamma 2-GABAA receptor by replacement of several divergent amino-terminal regions with the alpha 1 counterparts.

abstract：:Specific [125I]-angiotensin II (AII) and [125I]-bradykinin (Bk) binding sites have been identified within epithelial membranes from rat jejunum and descending colon. These high affinity intestinal sites exhibited KD values of 0.64 +/- 0.16 nM for [125I]-AII and 0.69 +/- 0.13 nM for [125I]-Bk, which were similar to tho...

journal_title：British journal of pharmacology

authors： Cox HM,Munday KA,Poat JA

更新日期：1986-01-01 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:As the pathogenesis of postoperative ileus (POI) involves inflammation and oxidative stress, comparable to ischaemia/reperfusion injury which can be ameliorated with nitrite, we investigated whether nitrite can protect against POI and explored the mechanisms involved. EXPERIMENTAL APPROACH:We us...

journal_title：British journal of pharmacology

authors： Cosyns SM,Shiva S,Lefebvre RA

更新日期：2015-10-01 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：:1. Protein phosphorylation is involved in the induction of nitric oxide synthase II (NOS II, iNOS) in several types of animal cells. Here we have investigated the possible involvement of major protein kinases in the induction of NOS II expression in human DLD-1 cells. 2. In DLD-1 cells, interferon--gamma alone induced...

journal_title：British journal of pharmacology

authors： Kleinert H,Euchenhofer C,Fritz G,Ihrig-Biedert I,Förstermann U

更新日期：1998-04-01 00:00:00

abstract：:Rat vas deferens preparations became desensitized to the alpha 1-adrenoceptor antagonist thymoxamine: after 6 h in vitro, the t 1/2 value (time to attain half the occupancy of receptors occupied at equilibrium) of the response to this drug was 1.50 fold greater in control strips (strips exposed to thymoxamine at 6 h) ...

journal_title：British journal of pharmacology

authors： Onnen I

更新日期：1984-09-01 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 The cardiovascular effects of the anthelmintic drug diethylcarbamazine citrate (DECC) were examined in cats anaesthetized with pentobarbitone. There were two quite distinct haemodynamic responses, an initial transient hypotension (occurring within 10 s of an intravenous injection) and a pronounced secondary hyperten...

journal_title：British journal of pharmacology

authors： Abaitey AK,Parratt JR

更新日期：1976-02-01 00:00:00

abstract：:1. Transcriptional control of the human beta(2) adrenergic receptor gene (ADRB2) predominantly resides within a 549 base pair region immediately 5' to the start of translation. Within this region, four naturally occurring polymorphisms, -468 C-->G, -367 T-->C, -47 T-->C, and -20 T-->C, have been identified. 2. To dete...

journal_title：British journal of pharmacology

authors： Johnatty SE,Abdellatif M,Shimmin L,Clark RB,Boerwinkle E

更新日期：2002-12-01 00:00:00

abstract：BACKGROUND AND PURPOSE:The dietary trace amines tyramine and beta-phenylethylamine (beta-PEA) can increase blood pressure. However, the mechanisms involved in the vascular effect of trace amines have not been fully established. The purpose of this study was to evaluate whether trace amine-dependent vasoconstriction was...

journal_title：British journal of pharmacology

authors： Herbert AA,Kidd EJ,Broadley KJ

更新日期：2008-10-01 00:00:00

abstract：:Ryanodine (1 microM) suppressed or abolished contraction in response to step depolarization in voltage-clamped cells isolated from adult rat ventricular myocardium. The step depolarizations evoked the second inward current, which is carried largely by Ca ions under these conditions, and there was little or no change i...

journal_title：British journal of pharmacology

authors： Mitchell MR,Powell T,Terrar DA,Twist VW

更新日期：1984-01-01 00:00:00

abstract：:Midbrain dopaminergic (DA) neurones sustain important physiological functions such as control of motricity, signalling of the error in prediction of rewards and modulation of emotions and cognition. Moreover, their degeneration leads to Parkinson's disease and they may be dysfunctional in other pathological states, su...

journal_title：British journal of pharmacology

authors： Seutin V

更新日期：2005-09-01 00:00:00

abstract：:1. Effects were studied of 6-(3-dimethylaminopropionyl) forskolin (NKH477), a water-soluble forskolin derivative and of dibutyryl-cyclic AMP, a membrane-permeable cyclic AMP analogue on noradrenaline (NA)-induced Ca2+ mobilization in smooth muscle strips of the rabbit mesenteric artery. The intracellular concentration...

journal_title：British journal of pharmacology

authors： Ito S,Suzuki S,Itoh T

更新日期：1993-11-01 00:00:00

abstract：:5-Lipoxygenase (5-LO) is a crucial enzyme in the synthesis of the bioactive leukotrienes (LTs) from arachidonic acid (AA), and inhibitors of 5-LO are thought to prevent the untowarded pathophysiological effects of LTs. In this study, we present the molecular pharmacological profile of the novel nonredox-type 5-LO inhi...

journal_title：British journal of pharmacology

authors： Fischer L,Steinhilber D,Werz O

更新日期：2004-07-01 00:00:00

abstract：:1 The spasmogenic and spasmolytic effects of beta-lipotropin (LPH) fragments and one analogue were investigated on different parts of the gastro-intestinal tract of guinea-pig and rat in vitro.2 Changes in muscle tone were observed in colon and rectum and to a lesser extent in jejunum and ileum of both species. Rat co...

journal_title：British journal of pharmacology

authors： Nijkamp FP,Van Ree JM

更新日期：1980-04-01 00:00:00

abstract：:Two prostaglandin endoperoxide analogues, EP 035 and EP 157, behave as specific thromboxane receptor antagonists on isolated smooth muscle preparations such as rabbit aorta, dog saphenous vein and guinea-pig trachea. However, in human platelet-rich plasma (PRP) they produce an unsurmountable block of aggregation induc...

journal_title：British journal of pharmacology

authors： Armstrong RA,Jones RL,MacDermot J,Wilson NH

更新日期：1986-03-01 00:00:00

abstract：:1. Partial agonists of the beta2-adrenoceptor which activate adenylyl cyclase are widely used as bronchodilators for the relief of bronchoconstriction accompanying many disease conditions, including bronchial asthma. The bronchodilator salmeterol has both a prolonged duration of action in bronchial tissue and the abil...

journal_title：British journal of pharmacology

authors： January B,Seibold A,Allal C,Whaley BS,Knoll BJ,Moore RH,Dickey BF,Barber R,Clark RB

更新日期：1998-02-01 00:00:00

abstract：BACKGROUND AND PURPOSE:As a hallmark of glioblastoma multiforme (GBM), CD44 plays a crucial role in promoting glioblastoma stem cell (GSC) stemness phenotypes and multiple drug resistance. The therapeutic potential of CD44 has been validated by the clinical successes of several CD44 inhibitors, including antibodies and...

journal_title：British journal of pharmacology

authors： Wang C,Wang Z,Chen C,Fu X,Wang J,Fei X,Yan X,Xu R

更新日期：2020-07-01 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：:Tyrosine sulfation is a post-translational modification of secreted and transmembrane proteins, including many GPCRs such as chemokine receptors. Most chemokine receptors contain several potentially sulfated tyrosine residues in their extracellular N-terminal regions, the initial binding site for chemokine ligands. Su...

journal_title：British journal of pharmacology

authors： Ludeman JP,Stone MJ

更新日期：2014-03-01 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：:1. The role of endogenous ADP in platelet aggregation in vivo remains unclear due to the lack of suitable P2T-antagonist probes. This paper describes the potency, selectivity and specificity of the novel P 2T-purinoceptor antagonist, FPL 67085 (2-propylthio-D-beta,gamma-dichloromethylene ATP) both in vitro and in the ...

journal_title：British journal of pharmacology

authors： Humphries RG,Tomlinson W,Clegg JA,Ingall AH,Kindon ND,Leff P

更新日期：1995-07-01 00:00:00

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：:1. Extracellular recording of the stimulus-evoked population spike in the CA1 region of rat hippocampal slices in vitro was performed in order to investigate whether lappaconitine affects neuronal excitability. Lappaconitine is a diterpene alkaloid of plants of the Aconitum genus and has analgesic properties. 2. The r...

journal_title：British journal of pharmacology

authors： Ameri A,Metzmeier P,Peters T

更新日期：1996-06-01 00:00:00

abstract：:1. The influence of angiotensin II (AII) on resting blood pressure and on sympathetic nerve-mediated pressor responses in the pithed rat was investigated either by inhibiting the renin-angiotensin system or by infusing AII. 2. Plasma AII levels in the pithed rat were approximately 20 fold higher than in normotensive r...

journal_title：British journal of pharmacology

authors： Grant TL,McGrath JC

更新日期：1988-12-01 00:00:00

abstract：:We have performed a systematic mutagenesis of three hydrophobic rings (17', 13' and 9') within transmembrane region (TM) 2 of the alpha9alpha10 nicotinic cholinergic receptor (nAChR) to a hydrophilic (threonine) residue and compared the properties of mutant receptors reconstituted in Xenopus laevis oocytes. Phenotypic...

journal_title：British journal of pharmacology

authors： Plazas PV,De Rosa MJ,Gomez-Casati ME,Verbitsky M,Weisstaub N,Katz E,Bouzat C,Elgoyhen AB

更新日期：2005-08-01 00:00:00

abstract：:1. SB 206553 (5-methyl-1-(3-pyridylcarbamoyl)-1,2,3,5-tetrahydropyrrolo[2 ,3-f]indole) displays a high affinity (pK1 7.9) for the cloned human 5-HT2C receptor expressed in HEK 293 cells and the 5-HT2B receptor (pA2 8.9) as measured in the rat stomach fundus preparation. SB 206553 has low affinity for cloned human 5-HT...

journal_title：British journal of pharmacology

authors： Kennett GA,Wood MD,Bright F,Cilia J,Piper DC,Gager T,Thomas D,Baxter GS,Forbes IT,Ham P,Blackburn TP

更新日期：1996-02-01 00:00:00

abstract：:1. Release-regulating alpha 2-autoreceptors in human brain were characterized pharmacologically in cortical slices from patients undergoing neurosurgery to remove subcortical tumours; the slices were prelabelled with [3H]-noradrenaline ([3H]-NA) and stimulated electrically (3 Hz, 2 ms, 24 mA) under superfusion conditi...

journal_title：British journal of pharmacology

authors： Raiteri M,Bonanno G,Maura G,Pende M,Andrioli GC,Ruelle A

更新日期：1992-12-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Angiotensin II (AngII) induces migration and growth of vascular smooth muscle cell (VSMC), which is responsible for vascular remodelling in some cardiovascular diseases. Ang II also activates a Cl(-) current, but the underlying mechanism is not clear. EXPERIMENTAL APPROACH:The A10 cell line and ...

journal_title：British journal of pharmacology

authors： Ma MM,Lin CX,Liu CZ,Gao M,Sun L,Tang YB,Zhou JG,Wang GL,Guan YY

更新日期：2016-02-01 00:00:00

abstract：:1. Electroconvulsive treatment (ECT) of rabbits produced ocular inflammation consisting of conjunctival hyperaemia, miosis and protein extravasation into the aqueous humour, reflected by the so-called aqueous flare response (AFR): the maximal reduction in pupil size was 3.8 +/- 0.1 mm (s.e. of mean, n = 16) while the ...

journal_title：British journal of pharmacology

authors： Wang ZY,Waldeck K,Grundemar L,Håkanson R

更新日期：1997-04-01 00:00:00