Abstract：
:Recombinant P2X2 receptor was observed by atomic force microscope in the aqueous phase. The P2X2 receptor was expressed in an insect cell line, and recombinant proteins were prepared under native conditions. The membrane fractions were extracted, and histidine-tagged receptor protein was purified from the fractions by column chromatography. When the purified protein fraction was diluted with water and served for atomic force microscopy, dispersed particles of about 3 nm in height were observed. In the presence of 1 mM ATP, the assembly-like images of the particles were obtained. More densely assembled images of the particles were achieved when the protein was dissolved in a Tris buffer containing 1 mM ATP. Under this condition, imaging of the surface of the particles exhibited a circular structure with a diameter of about 10 nm having a pore-like structure. These results suggest that atomic force microscopy provides structural information about P2X2 receptor in aqueous phase.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Nakazawa K,Yamakoshi Y,Tsuchiya T,Ohno Ydoi
10.1016/j.ejphar.2005.06.018keywords:
subject
Has Abstractpub_date
2005-08-22 00:00:00pages
107-10issue
2-3eissn
0014-2999issn
1879-0712pii
S0014-2999(05)00670-9journal_volume
518pub_type
杂志文章abstract：:(-)Baclofen, a GABAB receptor agonist, and GABA attenuated by 60% the high K+-evoked 45Ca2+ uptake into cultured cerebellar granule cells with an EC50 of 110 +/- 18 nM and 2.4 +/- 0.2 microM, respectively. The attenuation by baclofen of 45Ca2+ uptake was stereospecific and the effect of GABA was unaffected by bicucull...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(87)90557-7
更新日期：1987-09-23 00:00:00
abstract：:The involvement of delta opioid receptors in supraspinal analgesia was investigated. With this aim, opioids that produced analgesia in the tail immersion test were administered i.c.v. to mice a few minutes before the irreversible antagonist, beta-funaltrexamine (beta-FNA). Protection of the respective analgesic effect...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(89)90038-1
更新日期：1989-01-02 00:00:00
abstract：:Hypovolemic shock was produced in rats by withdrawing about 50% of the estimated total blood volume. Following mean arterial pressure stabilization in the range of 22-23 mm Hg, the rats were given an i.v. bolus injection of L-6-ketopiperidine-2-carbonyl-L-leucyl-L-proline amide (RGH-2202) to be compared with thyrotrop...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(90)90511-4
更新日期：1990-06-21 00:00:00
abstract：:Alternaria alternata is a fungal allergen linked to the development of severe asthma in humans. In view of the clinical relationship between A. alternata and asthma, we sought to investigate the allergic activity of this antigen after direct application to the lungs of Brown Norway rats. Here we demonstrate that a sin...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2014.09.021
更新日期：2014-11-15 00:00:00
abstract：:A comparison has been made of the abilities of salbutamol, forskolin and prenalterol to relax guinea-pig tracheal rings contracted equivalently with either prostaglandin F2 alpha (PGF2 alpha) or carbachol. In the absence of spontaneous tension, 10(-6) M PGF2 alpha and 4 X 10(-7) M carbachol induced equivalent contract...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(86)90559-5
更新日期：1986-08-22 00:00:00
abstract：:Foot shocks applied to the rat on a grid floor caused brain noradrenaline depletion. Hemicholinium-3 injected intracerebroventricularly (i.c.v.) blocked the noradrenaline depletion and this blockade was reversed by choline (i.c.v.). Physostigmine (i.c.v.) had different effects according to the age of the rats: "young"...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(77)90067-x
更新日期：1977-08-01 00:00:00
abstract：:Geniposide (GE) can effectively inhibit diabetic nephropathy (DN), but its mechanism is unclear. The objective of this study was to explore the antidiabetic nephropathy effects of GE both in high fat diet/streptozotocin-induced DN mice and in high glucose-induced podocyte model. Renal function in DN mice was evaluated...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2020.173449
更新日期：2020-11-05 00:00:00
abstract：:Fructose-2,6-bisphosphate is a potent activator of 6-phosphofructo-1-kinase, a key enzyme in glycolysis. We previously revealed that sulfonylureas stimulate fructose-2,6-bisphosphate production in the rat liver by activating 6-phosphofructo-2-kinase. In the present study, we show that CS-045, a new antidiabetic agent,...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(94)90462-6
更新日期：1994-03-21 00:00:00
abstract：:Recently, down-regulation of vascular endothelial growth factor (VEGF) in the heart was suggested as a potential molecular explanation for the increased risk of cardiovascular morbidity and mortality in patients with diabetes. Increased endothelin-1 production is reported in diabetes. Here, we report that down-regulat...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2006.04.041
更新日期：2006-08-07 00:00:00
abstract：:Vagal motor outflow from the dorsal vagal complex is important in the regulation of intestinal motility. The aim of our study was to test the hypothesis that within the dorsal vagal complex, tonic GABA(A)-receptor mediated neurotransmission modulates intestinal motility. The GABA(A) receptor antagonist, bicuculline (m...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(98)00071-5
更新日期：1998-04-10 00:00:00
abstract：:Glucocorticoids can reverse hemodynamic disturbances and dependence on catecholamines in septic shock. The relevant beneficial mechanisms of steroids in septic shock are unknown, although inducible nitric oxide synthase could account for them. The aim of this study was to compare the effects of dexamethasone, a glucoc...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(03)02035-1
更新日期：2003-08-15 00:00:00
abstract：:The present study examines the effect of three adenosine receptor antagonists on tremulous jaw movements (TJMs), an animal model of tremor. Forty-five rats were pre-treated with one adenosine antagonist: caffeine (0.0, 5.0, or 10.0 mg/kg; non-selective adenosine receptor antagonist), 8-cyclopentyltheophylline (CPT; 0....
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2018.06.004
更新日期：2018-08-15 00:00:00
abstract：:The anticancer drugs camptothecin (CPT) and topotecan (TPT) are known DNA topoisomerase I inhibitors which cause DNA damage and lead to cell death. In this study we provide evidence that CPT and TPT also interfere with the elements of cytoskeleton - microtubules and actin filaments which could be partly responsible fo...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2016.07.044
更新日期：2016-10-15 00:00:00
abstract：:This review selectively explores some areas of pain research that, until recently, have been poorly understood. We have chosen four topics that relate to clinical pain and we discuss the underlying mechanisms and related pathophysiologies contributing to these pain states. A key issue in pain medicine involves crucial...
journal_title：European journal of pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.ejphar.2013.01.069
更新日期：2013-09-15 00:00:00
abstract：:We have examined the effects of intrathecally (i.t.) administered CP-96,345, a non-peptide NK1 receptor ligand, on the spinal nociceptive flexor reflex and on the facilitation of this reflex evoked by i.t. substance P (SP), neurokinin A (NKA) and electrical conditioning stimulation of cutaneous C-afferents. CP-96,345 ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(92)90428-7
更新日期：1992-06-17 00:00:00
abstract：:Mouse peritoneal inflammatory macrophages have a saturable binding site for [3H]flunitrazepam with a KD of 43 +/- 7 nM and Bmax of 391 +/- 58 fmol per 10(6) cells, which corresponds to 250 000 sites per cell. The IC50 values for PK 11195, Ro 5-4864, diazepam, flunitrazepam, clonazepam, ethyl-beta carboline 3-carboxyla...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(84)90059-1
更新日期：1984-11-27 00:00:00
abstract：:We have tested for anti-nociceptive effects of the anticonvulsant KCNQ channel opener, N-(2-amino-4-(4-fluorobenzylamino)-phenyl)carbamic acid ethyl ester (retigabine), in rat models of experimental pain. In the chronic constriction injury and spared nerve models of neuropathic pain, injection of retigabine (5 and 20 ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(02)02924-2
更新日期：2003-01-24 00:00:00
abstract：:Cultured retina cells released accumulated [3H]GABA (gamma-aminobutyric acid) when stimulated by L-glutamate, N-methyl-D-aspartate (NMDA) and kainate. In the absence of Mg2+, dopamine at 200 microM (IC50 60 microM), inhibited in more than 50% the release of [3H]GABA induced by L-glutamate and NMDA, but not by kainate....
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(97)01522-7
更新日期：1998-02-05 00:00:00
abstract：:Opiates impair neutrophil-mediated host defense, but the involvement of kappa-opioid receptors in this action has not been defined. The selective kappa-opioid receptor agonist [trans-(+)3,4-dichloro-N-methyl-N[2-(1-pyrrolidinyl)-cyclohexyl]benzeneacetamide methanesulfonate inhibited macrophage inflammatory protein-2-i...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(01)00727-0
更新日期：2001-03-02 00:00:00
abstract：:Our laboratory recently reported that a group of novel indole quinuclidine analogs bind with nanomolar affinity to cannabinoid type-1 and type-2 receptors. This study characterized the intrinsic activity of these compounds by determining whether they exhibit agonist, antagonist, or inverse agonist activity at cannabin...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2014.05.007
更新日期：2014-08-15 00:00:00
abstract：:Angiotensin-converting enzymes, ACE and ACE2, are key members of renin angiotensin system. Activation of ACE2/Ang-(1-7) pathway enhances cardiovascular protective functions of bone marrow-derived stem/progenitor cells. The current study evaluated the selectivity of ACE2 inhibitors, MLN-4760 and DX-600, and ACE and ACE...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2016.01.007
更新日期：2016-03-05 00:00:00
abstract：:Single myelinated nerve fibres of Rana esculenta were investigated under current and potential clamp conditions at 20 degrees C. Under 2.5 mM phenobarbital, the amplitude of the action potential was reversibly reduced to 85.5 +/- 5% (n = 6), and the threshold potential was raised by 32% of the control in Ringer soluti...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(79)90432-1
更新日期：1979-06-01 00:00:00
abstract：:Animal models of arthritis are widely used to de-convolute disease pathways and to identify novel drug targets and therapeutic approaches. However, the high attrition rates of drugs in Phase II/III rates means that a relatively small number of drugs reach the market, despite showing efficacy in pre-clinical models. Th...
journal_title：European journal of pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.ejphar.2015.03.047
更新日期：2015-07-15 00:00:00
abstract：:There is controversy concerning the inhibitory effect of arginine-vasopressin (AVP) on human platelet adenylate cyclase activity, which putatively involves Gi as the G-protein. To clarify this point, the effects of AVP on human platelet membranes were studied by measuring the activities of the high-affinity GTPase, as...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(88)90020-9
更新日期：1988-06-10 00:00:00
abstract：:Kappa- and mu-opioid binding site affinities of the kappa-selective ligand U62066 and its optical isomers, (+)-U63639 and (-)-U63640 were compared with those of the structurally related ligand PD117302 and its respective isomers, (+)-PD123497 and (-)-PD123475. The relative efficacies of each compound were also establi...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(89)90512-8
更新日期：1989-12-07 00:00:00
abstract：:The protective potency of ischemic preconditioning decreases with increasing age. A key step in ischemic preconditioning is the opening of mitochondrial Ca(2+) sensitive K(+) (mK(Ca)) channels, which causes mild uncoupling of mitochondrial respiration. We hypothesized that aging reduces the effects of mK(Ca) channel o...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2007.09.008
更新日期：2008-01-14 00:00:00
abstract：:Some effects of Org GC 94 (1,3,4,14b-tetrahydro-2,7-dimethyl-2H-dibenzo[b,f]pyrazino[1,2-d][1,4]oxazepine maleate) on human platelets have been investigated. Without pretreatment with ADP, 5-HT-induced aggregation of humam platets was completely inhibited by 2.5 x 10(-8) M of Org GC 94. Aggregation triggered by noradr...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(77)90290-4
更新日期：1977-04-07 00:00:00
abstract：:The effects of hyperosmotic solutions of xylitol were tested on acid and bicarbonate outputs from the rat stomach as well as on acid back-diffusion. Hyperosmotic solutions were instilled into anesthetized rats by an esophageal cannula and drained through a duodenal catheter. Spontaneously secreting and histamine-stimu...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(84)90258-9
更新日期：1984-07-13 00:00:00
abstract：:Loss of body weight was proved to be a convenient and reliable way to predict the degree of reserpine-induced amine depletion after i.p. injections of reserpine (2.5, 5 and 10 mg/kg) and it thus helps reduce variability. Two populations of animals were sharply distinguished lying on either side of the 5% cutoff point ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(75)90327-1
更新日期：1975-05-01 00:00:00
abstract：:Cannabinoid CB(2) receptors have been implicated in antinociception in animal models of both acute and chronic pain. We evaluated the role both cannabinoid CB(1) and CB(2) receptors in mechanonociception in non-arthritic and arthritic rats. The antinociceptive effect of Delta(9)-tetrahydrocannabinol (Delta(9)THC) was ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2007.05.024
更新日期：2007-09-10 00:00:00
