Inhibition of histamine release from human lung in vitro by antihistamines and related drugs.

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. Measurements were made of the in vivo formation of inositol phosphates in the brains of C57/B1/601a mice treated acutely or chronically with lithium chloride (LiCl). 2. A single injection of LiCl (10 mEquiv kg-1, s.c.) 18 h before death increased the accumulation of [3H]-inositol phosphates ([3H]-Ins P's) in the br...

journal_title：British journal of pharmacology

authors： Whitworth P,Heal DJ,Kendall DA

更新日期：1990-09-01 00:00:00

abstract：:1. Several amino-acid esters and amides have been prepared and their toxicological and pharmacological properties have been investigated. Some of the quaternary esters and amides were lethal to mice at doses below 1 mg/kg; this lethality was usually associated with high nicotinic activity. None of the compounds showed...

journal_title：British journal of pharmacology

authors： Barrass BC,Brimblecombe RW,Parkes DC,Rich P

更新日期：1968-10-01 00:00:00

abstract：:1. In the present study the effect of N-methyl-D-aspartate (NMDA) on thromboxane B2 synthesis and on [Ca2+]i was studied in human platelets. 2. NMDA (10(-7) M) completely inhibited the synthesis of thromboxane B2 from exogenous arachidonic acid (AA), while it did not interfere with the aggregating effect of the thromb...

journal_title：British journal of pharmacology

authors： Franconi F,Miceli M,Alberti L,Seghieri G,De Montis MG,Tagliamonte A

更新日期：1998-05-01 00:00:00

abstract：:The variety of factors and events involved in neurodegeneration renders the subject a major challenge. Neurodegenerative disorders include a number of different pathological conditions, which share similar critical metabolic processes, such as protein aggregation and oxidative stress, both of which are associated with...

journal_title：British journal of pharmacology

authors： Gaeta A,Hider RC

更新日期：2005-12-01 00:00:00

abstract：:Multidrug transporters play a dual role in haematopoietic cells, mediating the efflux of xenobiotics and regulating cell migration. For several reasons including the lack of specific antibodies, reports of multidrug transporter distribution on lymphocytes conflict. Murine B cells have been reported to completely lack ...

journal_title：British journal of pharmacology

authors： Elliott JI,Raguz S,Higgins CF

更新日期：2004-12-01 00:00:00

abstract：:1. The brain cytoprotective effects of a putative calcium-associated protein kinase inhibitor, HA1077, as well as a calcium entry blocker nicardipine were evaluated in models of cerebral ischaemia in Mongolian gerbils. Morphological changes characterizing delayed neuronal death of selectively vulnerable CA1 pyramidal ...

journal_title：British journal of pharmacology

authors： Asano T,Ikegaki I,Satoh S,Mochizuki D,Hidaka H,Suzuki Y,Shibuya M,Sugita K

更新日期：1991-08-01 00:00:00

abstract：:1. The effects of dimethothiazine have been studied on the response of afferent fibres from primary and secondary endings of muscle spindles in the soleus muscle of the decerebrate cat during stretching of the muscle under controlled conditions.2. Dimethothiazine in doses of 1 to 4 mg/kg intravenously reduced the disc...

journal_title：British journal of pharmacology

authors： Maxwell DR,Rhodes KF

更新日期：1970-07-01 00:00:00

abstract：:1 Prostaglandin and thromboxane release from the term pregnant (Day 22) rat uterus in vitro has been measured by radioimmunoassay and gas chromatography combined with mass spectrometry. 2 Prostacyclin (prostaglandin I2, PGI2) and thromboxane A2 (TXA2) (measured as their metabolites, 6-oxo-PGF1 alpha and TXB2, respecti...

journal_title：British journal of pharmacology

authors： Phillips CA,Poyser NL

更新日期：1981-05-01 00:00:00

abstract：:1. The effects of various metabotropic glutamate receptor agonists on [3H]-cyclic AMP accumulation and phosphoinositide hydrolysis were investigated in guinea-pig cerebral cortical slices prelabelled with [3H]-adenine or [3H]-inositol. 2. 1-Aminocyclopentane-1S,3R-dicarboxylate (1S,3R-ACPD), L-2-amino-4-phosphonobutan...

journal_title：British journal of pharmacology

authors： Cartmell J,Kemp JA,Alexander SP,Shinozaki H,Kendall DA

更新日期：1994-01-01 00:00:00

abstract：BACKGROUND AND PURPOSE:There is increasing evidence that potassium channels are involved in the cardiovascular dysfunction of sepsis. This evidence was obtained after the systemic inflammation, cardiovascular dysfunction and organ damage had developed. Here we have studied the consequences of early interference with po...

journal_title：British journal of pharmacology

authors： Sordi R,Fernandes D,Heckert BT,Assreuy J

更新日期：2011-07-01 00:00:00

abstract：:1. General anaesthetics disrupt normal cell receptivity and responsiveness while sparing vital respiratory processes. Ultimate elucidation of the molecular basis of general anaesthesia presumes the identification of one or more subcellular components with appropriate sensitivity to the entire array of anaesthetics. 2....

journal_title：British journal of pharmacology

authors： LaBella FS,Chen QM,Stein D,Queen G

更新日期：1997-03-01 00:00:00

abstract：:1 The effects of electrical stimulation, changes in external ion concentrations and various drugs on acetylcholine release from the myenteric plexus were measured by bioassay in the presence of physostigmine and by recording the responses of the longitudinal muscle. In preparations from the guinea-pig, the acetylcholi...

journal_title：British journal of pharmacology

authors： Cowie AL,Kosterlitz HW,Waterfield AA

更新日期：1978-12-01 00:00:00

abstract：:1. The release of prostaglandin D2 (PGD2) during immediate allergic reactions in human skin was investigated in vivo and in vitro. 2. Skin exudates were collected from abraded sites on the thigh of atopic subjects sensitive to D. pteronyssinus antigen and from non-atopic control subjects. Challenge with antigen caused...

journal_title：British journal of pharmacology

authors： Barr RM,Koro O,Francis DM,Black AK,Numata T,Greaves MW

更新日期：1988-07-01 00:00:00

abstract：BACKGROUND:Macrophage elastase (MMP-12) is involved in the inflammatory process of chronic obstructive pulmonary disease (COPD). The aim of this study was to investigate in mice the effect of MMP-12 inhibition on the inflammatory process induced by cigarette smoke (CS) or by lipopolysaccharide (LPS) exposure of the air...

journal_title：British journal of pharmacology

authors： Le Quément C,Guénon I,Gillon JY,Valença S,Cayron-Elizondo V,Lagente V,Boichot E

更新日期：2008-07-01 00:00:00

abstract：:1. To characterize the muscarinic receptors on human pulmonary veins associated with the acetylcholine (ACh)-induced relaxation, isolated venous and arterial preparations were pre-contracted with noradrenaline (10 microM) and were subsequently challenged with ACh in the absence or presence of selective muscarinic anta...

journal_title：British journal of pharmacology

authors： Walch L,Gascard JP,Dulmet E,Brink C,Norel X

更新日期：2000-05-01 00:00:00

abstract：:Resting blood flow, arterio-venous glucose and oxygen (A-V)O2 differences, glucose uptake and oxygen consumption by a segment of the upper jejunum were measured in anaesthetized dogs. Systemic arterial pressure was also measured. The effect of nicotine infusion (25 micrograms kg-1 i.v., over 10 min) on these measureme...

journal_title：British journal of pharmacology

authors： Grayson J,Oyebola DD

更新日期：1985-08-01 00:00:00

abstract：:1. The diversity of alpha(2) and purinergic autoreceptor actions on action potential evoked calcium transients in single varicosities has been investigated using the calcium indicator Oregon Green 488 BAPTA-1. 2. During long trains of impulses (10 Hz for 30 s), the change in calcium concentration in varicosities from ...

journal_title：British journal of pharmacology

authors： O'Connor SC,Brain KL,Bennett MR

更新日期：1999-12-01 00:00:00

abstract：:We investigated the action of the phenylalkylamines verapamil and N-methyl-verapamil on the Kv1.3 potassium channel using the whole-cell configuration of the patch-clamp technique. Our goal was to identify their binding as a prerequisite for using the phenylalkylamines as small, well-defined molecular probes, not only...

journal_title：British journal of pharmacology

authors： Rauer H,Grissmer S

更新日期：1999-07-01 00:00:00

abstract：:We have studied the recovery of receptor binding and of isoprenaline-stimulated cyclic AMP responses after chronic (2-5 days) exposure of tissue-cultured living rat heart cells to several beta-adrenoceptor antagonists. Most experiments were performed with [3H]- (+/-)-carazolol and [3H]-(+/-)-CGP 12177, as prototypes o...

journal_title：British journal of pharmacology

authors： Becker C,Porzig H

更新日期：1984-07-01 00:00:00

abstract：:1. Preparations were developed whereby the hypogastric ganglion of the rat or guinea-pig was perfused through its vasculature with saline solutions. Drugs were injected into the perfusion stream, and their effects were indicated by contractions of the vas deferens. The base of this organ could be ligated to prevent th...

journal_title：British journal of pharmacology

authors： Bentley GA

更新日期：1972-03-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Although picrotoxin is a well-established antagonist of GABA(A) receptors, detailed studies of its action on inhibitory synaptic transmission have not previously been made. EXPERIMENTAL APPROACH:Electrophysiological techniques were used to study the action of picrotoxin on inhibitory postsynapti...

journal_title：British journal of pharmacology

authors： Korshoej AR,Holm MM,Jensen K,Lambert JD

更新日期：2010-02-01 00:00:00

abstract：:1 The metabolism of extracellular nucleotides plays an important role in nucleotide signalling mediated by P2 receptors. The nucleotide sequence encoding a putative human ecto-ATPase named CD39L1 was reported recently. However, the biological activity of this protein has not been established. 2 Based on the sequence o...

journal_title：British journal of pharmacology

authors： Mateo J,Harden TK,Boyer JL

更新日期：1999-09-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Adrenoceptors can associate with cardiac caveolae. To investigate the function of vascular caveolae, adrenoceptor-mediated effects were compared in the saphenous artery of caveolin-1 knockout (cav-1KO) and wild-type (WT) mice. EXPERIMENTAL APPROACH:Electronmicroscopy was used to detect caveolae....

journal_title：British journal of pharmacology

authors： Neidhold S,Eichhorn B,Kasper M,Ravens U,Kaumann AJ

更新日期：2007-02-01 00:00:00

abstract：BACKGROUND AND PURPOSE:The ω-3 polyunsaturated fatty acids (PUFAs) mediate protective effects on several metabolic disorders. However, the functions of their metabolites in the early stage of nonalcoholic fatty liver disease (NAFLD) are largely unknown. EXPERIMENTAL APPROACH:Mice were fed a control diet, high-fat diet...

journal_title：British journal of pharmacology

authors： Wang C,Liu W,Yao L,Zhang X,Zhang X,Ye C,Jiang H,He J,Zhu Y,Ai D

更新日期：2017-07-01 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：:Muscarinic receptors in the rat cerebral cortex, reacted with p-chloromercuribenzoate (PCMB) under different conditions (Phase I and II), have modified binding sites. These exhibit remarkable changes in the structural dependence of the binding of drugs. In Phase I, the structure-binding profile of agonists for both th...

journal_title：British journal of pharmacology

authors： Birdsall NJ,Burgen AS,Hulme EC,Wong EH

更新日期：1983-09-01 00:00:00

abstract：:1. In order to define the electrophysiological mechanism(s) responsible for bradykinin (BK)-induced positive inotropic and chronotropic responses in isolated guinea-pig atria, effects of BK on the membrane currents were examined in isolated atrial cells using patch clamp techniques. 2. BK (0.1-1000 nM) increased the L...

journal_title：British journal of pharmacology

authors： Sakamoto N,Uemura H,Hara Y,Saito T,Masuda Y,Nakaya H

更新日期：1998-09-01 00:00:00

abstract：:1 Neuropeptide Y (NPY), peptide YY (PYY) and pancreatic polypeptide (PP) differentially activate three Y receptors (Y(1), Y(2) and Y(4)) in mouse and human isolated colon. 2 The aim of this study was to characterise Y(2) receptor-mediated responses in colon mucosa and longitudinal smooth muscle preparations from wild ...

journal_title：British journal of pharmacology

authors： Hyland NP,Sjöberg F,Tough IR,Herzog H,Cox HM

更新日期：2003-06-01 00:00:00

abstract：:1 The activation of tachykinin NK(1) receptors in the rat spinal cord produced a transient drop in arterial blood pressure followed by a more prolonged pressor effect which is mediated by the stimulation of the sympatho-adrenal system. This study aims at characterizing the spinal mechanism of that initial hypotension ...

journal_title：British journal of pharmacology

authors： Brouillette J,Couture R

更新日期：2002-08-01 00:00:00