Relationship between internal Na + -K + and the accumulation of 14 C-5-hydroxytryptamine by rat platelets.

abstract：BACKGROUND AND PURPOSE:Inflammation associated with the tumour microenvironment (TME) plays a critical role in the cancer development, and immunotherapeutic strategies that aim to modulate the immune response in cancer have been crucial. In this study, a Methotrexate-loaded (MTX) poly (lactic-co-glycolic acid)-based (P...

journal_title：British journal of pharmacology

authors： Cavalcante RS,Ishikawa U,Silva ES,Silva Júnior AA,Araújo AA,Cruz LJ,Chan AB,Araújo Júnior RF

更新日期：2021-01-12 00:00:00

abstract：:1 delta'-trans-Tetrahydrocannabinol (THC) is more active orally in mice than previously thought, as cataleptic responses occur at doses from 0.06 mg/kg upwards, with peak activity at 2 to 4 h after dosing. These doses and peaks correspond well with the effects in man. 2 Comparison with chlorpromazine in mice shows tha...

journal_title：British journal of pharmacology

authors： Fairbairn JW,Pickens JT

更新日期：1979-11-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Cloxyquin (5-cloroquinolin-8-ol) has been described as an activator of TRESK (K2P 18.1, TWIK-related spinal cord K+ channel) background potassium channel. We have examined the specificity of the drug by testing several K2P channels. We have investigated the mechanism of cloxyquin-mediated TRESK a...

journal_title：British journal of pharmacology

authors： Lengyel M,Dobolyi A,Czirják G,Enyedi P

更新日期：2017-07-01 00:00:00

abstract：:1. To see if arachidonic acid (AA) plays a role in the sustained suppression of voltage-gated calcium channel currents produced by muscarinic receptor stimulation by carbachol (CCh), the effects of AA on membrane currents were examined in whole-cell voltage-clamped smooth muscle cells of the guinea-pig ileum. 2. In ce...

journal_title：British journal of pharmacology

authors： Unno T,Komori S,Ohashi H

更新日期：1996-09-01 00:00:00

abstract：:1. In the present study, the properties of glaucine (an aporphine structurally related to papaverine) were compared with those of papaverine, diltiazem, nifedipine and prazosin. The work includes functional studies on rat isolated aorta contracted with noradrenaline, caffeine or KCl, and a determination of the affinit...

journal_title：British journal of pharmacology

authors： Ivorra MD,Lugnier C,Schott C,Catret M,Noguera MA,Anselmi E,D'Ocon P

更新日期：1992-06-01 00:00:00

abstract：:Gut inflammation occurring in patients with inflammatory bowel diseases (IBD) is associated with an excessive immune response that is directed against constituents of the normal bacterial flora and results in the production of large amounts of inflammatory cytokines. Anti-cytokine compounds, such as the neutralizing T...

journal_title：British journal of pharmacology

authors： Caprioli F,Caruso R,Sarra M,Pallone F,Monteleone G

更新日期：2012-02-01 00:00:00

abstract：:1. The effect of intradermally injected endotoxin on skin blood flow was investigated in anaesthetized male Wistar rats in vivo. 2. Local skin blood flow changes were measured hourly for 6 h in the shaved dorsal skin with a laser-Doppler flow probe and compared to changes in control sites which had been injected with ...

journal_title：British journal of pharmacology

authors： Warren JB,Coughlan ML,Williams TJ

更新日期：1992-08-01 00:00:00

abstract：:The non-peptide NK1 receptor antagonist, CP-96,345, and its 2R,3R enantiomer CP-96,344, which is not an NK1 receptor antagonist (IC50 > 10 microM), were evaluated for antinociceptive and anti-inflammatory activities in several classical models of pain and inflammation in the rat. Both CP-96,345 and CP-96,344 reduced c...

journal_title：British journal of pharmacology

authors： Nagahisa A,Asai R,Kanai Y,Murase A,Tsuchiya-Nakagaki M,Nakagaki T,Shieh TC,Taniguchi K

更新日期：1992-10-01 00:00:00

abstract：:1. An investigation into the effects of cholecystokinin octapeptide (CCK-8S) and its pentapeptide analogue, pentagastrin, on neurones located in ventromedial nuclei of rat hypothalamic slices maintained in vitro has been undertaken. 2. CCK-8S (0.01-1.0 microM) applied in the perfusion medium produced a concentration-d...

journal_title：British journal of pharmacology

authors： Boden P,Hill RG

更新日期：1988-05-01 00:00:00

abstract：:1 Nine antibiotic compounds in common use were studied to determine their ability to affect intestinal motility in vitro, in the guinea-pig ileum and rabbit colon. 2 Ampicillin, doxycycline, mecillinam and metronidazole were without effect over a concentration range which included typical serum levels found when these...

journal_title：British journal of pharmacology

authors： Lees GM,Percy WH

更新日期：1981-06-01 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:The P2X(7) receptor exhibits complex pharmacological properties. In this study, binding of a [(3)H]-labelled P2X(7) receptor antagonist to human P2X(7) receptors has been examined to further understand ligand interactions with this receptor. EXPERIMENTAL APPROACH:The P2X(7) receptor antagonist, ...

journal_title：British journal of pharmacology

authors： Michel AD,Chambers LJ,Clay WC,Condreay JP,Walter DS,Chessell IP

更新日期：2007-05-01 00:00:00

abstract：:1. The effects of 1,3-di(2-tolyl)guanidine (DTG) were examined on the responses of cultured hippocampal neurones to the excitatory amino acid analogues N-methyl-D-aspartate (NMDA), kainate, quisqualate and (RS)-alpha-amino-3-hydroxy-5-methylisoxazole-4-propionate (AMPA). 2. In rat hippocampal neurones loaded with the ...

journal_title：British journal of pharmacology

authors： Fletcher EJ,Church J,Abdel-Hamid K,MacDonald JF

更新日期：1993-08-01 00:00:00

abstract：BACKGROUND AND PURPOSE:5-HT receptor agonists have variable nociceptive effects within the spinal cord. While there is some evidence for 5-HT(1A) spinally-mediated analgesia, the role of other 5-HT(1) receptor subtypes remains unclear. In the present study, we examined the spinal actions of a range of 5-HT(1) agonists,...

journal_title：British journal of pharmacology

authors： Jeong HJ,Mitchell VA,Vaughan CW

更新日期：2012-03-01 00:00:00

abstract：:Calcitonin gene-related peptide (CGRP) is believed to play a pivotal role in the pathogenesis of migraine via activation of CGRP receptors in the trigeminovascular system. The CGRP receptor antagonist, BIBN4096BS, has proven efficacy in the acute treatment of migraine attacks and represents a new therapeutic principle...

journal_title：British journal of pharmacology

authors： Petersen KA,Birk S,Doods H,Edvinsson L,Olesen J

更新日期：2004-11-01 00:00:00

abstract：:GPCRs can interact with each other to form homomers or heteromers. Homomers involve interactions with the same receptor type while heteromers involve interactions between two different GPCRs. These receptor-receptor interactions modulate not only the binding but also the signalling and trafficking properties of indivi...

journal_title：British journal of pharmacology

authors： Fujita W,Gomes I,Devi LA

更新日期：2014-09-01 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. The effect of basal tension (transmural tensions 235 +/- 29 mg wt (low tension: equivalent to approximately 16 mmHg) and 305 +/- 34 mg wt (high tension: equivalent to 35 mmHg)) on rat pulmonary resistance artery responses to endothelin-1 (ET-1) and the selective ET(B)-receptor agonist sarafotoxin S6c (S6c) were stu...

journal_title：British journal of pharmacology

authors： MacLean MR,McCulloch KM

更新日期：1998-03-01 00:00:00

abstract：BACKGROUND AND PURPOSE:The development of subtype-selective ligands to inhibit voltage-sensitive sodium channels (VSSCs) has been attempted with the aim of developing therapeutic compounds. Tetrodotoxin (TTX) is a toxin from pufferfish that strongly inhibits VSSCs. Many TTX analogues have been identified from marine an...

journal_title：British journal of pharmacology

authors： Tsukamoto T,Chiba Y,Wakamori M,Yamada T,Tsunogae S,Cho Y,Sakakibara R,Imazu T,Tokoro S,Satake Y,Adachi M,Nishikawa T,Yotsu-Yamashita M,Konoki K

更新日期：2017-11-01 00:00:00

abstract：:1. Acetylcholine mustard (N-2-chloroethyl-N-methyl-2-acetoxyethylamine), a potent muscarinic agonist, binds virtually irreversibly to muscarinic receptors in longitudinal muscle strips from guinea-pig small intesting, as shown by the inhibition of the binding of E13-H]-propylbenzilycholine mustard ([3-H-PrBCM), an aff...

journal_title：British journal of pharmacology

authors： Robinson DA,Taylor JG,Young JM

更新日期：1975-03-01 00:00:00

abstract：:We studied the effects of the novel Na(+)/Ca(2+) exchange inhibitor KB-R7943, 2-[2-[4-(4-nitrobenzyloxy)phenyl]ethyl]isothiourea methanesulphonate, on the native nicotinic receptors present at the bovine adrenal chromaffin cells, as well as on rat brain alpha(3)beta(4) and alpha(7) nicotinic acetylcholine receptors (A...

journal_title：British journal of pharmacology

authors： Pintado AJ,Herrero CJ,García AG,Montiel C

更新日期：2000-08-01 00:00:00

abstract：:1. Calcium entry via neuronal calcium channels is essential for the process of neurotransmission. We investigated the calcium channel subtypes involved in the operation of cardiac autonomic neurotransmission by examining the effects of selective calcium channel blockers on the inotropic responses to electrical field s...

journal_title：British journal of pharmacology

authors： Serone AP,Angus JA

更新日期：1999-06-01 00:00:00

abstract：:1. The serine/threonine protein phosphatase (PP) inhibitors, okadaic acid and calyculin, attenuated the IgE-mediated release of histamine from human lung mast cells (HLMC) and basophils in a dose-dependent manner whereas an alternative PP inhibitor, microcystin, was ineffective. Calyculin was more potent than okadaic ...

journal_title：British journal of pharmacology

authors： Peirce MJ,Munday MR,Peachell PT

更新日期：1998-11-01 00:00:00

abstract：BACKGROUND AND PURPOSE:In humans and non-human primates, the 7TM receptor GPR17 exists in two isoforms differing only by the length of the N-terminus. Of these, only the short isoform has previously been characterized. Hence, we investigated gene expression and ligand-binding profiles of both splice variants and furthe...

journal_title：British journal of pharmacology

authors： Benned-Jensen T,Rosenkilde MM

更新日期：2010-03-01 00:00:00

abstract：:1 alpha-Monofluoromethyldopa (MFMD, RMI 71963), a potent and selective enzyme-activated irreversible inhibitor of aromatic L-amino acid decarboxylase produces a substantial and long-lasting decrease in the catecholamine content of mouse brain, heart and kidney. 2 Single doses of MFMD reduce the 5-hydroxytryptamine con...

journal_title：British journal of pharmacology

authors： Bey P,Jung MJ,Koch-Weser J,Palfreyman MG,Sjoerdsma A,Wagner J,Zraïka M

更新日期：1980-12-01 00:00:00

abstract：:Extracellular nucleotides can activate a common purinoceptor mediating various cell responses. In this study we report that stimulation of rat mesangial cells with ATP and UTP leads to a rapid activation of the protein kinase B/Akt (PKB) pathway. Time-course studies reveal a rapid and transient phosphorylation of both...

journal_title：British journal of pharmacology

authors： Huwiler A,Rölz W,Dorsch S,Ren S,Pfeilschifter J

更新日期：2002-06-01 00:00:00

abstract：:1. This study investigates the effect of partially metabolic controlled long-term (34 weeks) streptozotocin (STZ)-induced diabetes on relaxation and contractile responses of isolated coronary arteries to seven different vasoactive agents. 2. The average fasting and non-fasting blood glucose concentrations (mM) were si...

journal_title：British journal of pharmacology

authors： Sheykhzade M,Dalsgaard GT,Johansen T,Nyborg NC

更新日期：2000-03-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Sublesional osteoporosis predisposes individuals with spinal cord injury (SCI) to an increased risk of low-trauma fracture. The aim of the present work was to investigate the effect of treatment with resveratrol (RES) on sublesional bone loss in spinal cord-injured rats. EXPERIMENTAL APPROACH:Co...

journal_title：British journal of pharmacology

authors： Wang HD,Shi YM,Li L,Guo JD,Zhang YP,Hou SX

更新日期：2013-10-01 00:00:00

abstract：:Des-Arg9-bradykinin (des-Arg9-BK) caused endothelium-dependent relaxations in human, isolated coronary arteries which upregulated with in vitro incubation time. Relaxations to des-Arg9-BK were inhibited by the B1 receptor antagonist, des-Arg9-[Leu3]-BK (pK(B), 6.14 +/- 0.11) but were unaffected by the B2 receptor anta...

journal_title：British journal of pharmacology

authors： Drummond GR,Cocks TM

更新日期：1995-12-01 00:00:00

abstract：:1. Intracellular recordings were made from neurones in vitro in the rat substantia nigra zona compacta and ventral tegmental area; the neurones had the characteristic properties of dopamine-containing cells, and fired action potentials spontaneously. 2. Cocaine (1-10 microM) inhibited spontaneous firing, hyperpolarize...

journal_title：British journal of pharmacology

authors： Lacey MG,Mercuri NB,North RA

更新日期：1990-04-01 00:00:00