Abstract：
:The goal of our study was to determine whether GPR55 agonists, O-1602, could reverse the cyclophosphamide (CYP)-induced changes in cystometric and inflammatory parameters, indicative of the development of bladder inflammation and overactivity. If confirmed, the stimulation of novel cannabinoid receptor - GPR55, could be a reasonable strategy as a treatment of CYP-induced haemorrhagic cystitis. The experiments were conducted in female Wistar rats. Based on the methodology of our published studies on CYP-induced heamorrhagic cystitis we performed experiments after administration of CYP, O-1602 or CYP plus O-1602. These included surgical procedures, conscious cystometry, measurements of bladder oedema and urothelium thickness using the Evans Blue dye leakage technique, as well as biochemical analyses with particular ELISA kits. O-1602 ameliorated the symptoms of CYP-induced detrusor overactivity leading to an increase in voided volume (0.59 vs. 0.93 ml), and lowering the detrusor overactivity index (703 vs. 115 cm H2O/ml). Intravenous administration of the GPR55 agonist to animals that received CYP significantly decreased Evans Blue extravasation and increased urothelium thickness. O-1602 also reversed the pro-inflammatory activity of CYP by restoring concentrations of brain-derived neurotrophic factor, nerve growth factor, calcitonin gene related peptide, interleukin 1-beta, interleukin-6, tumour necrosis factor alpha, malondialdehyde, nitrotyrosine, occludin, and organic cation transporter 3. GPR55 agonist, O-1602, represents a novel class of uroprotective agents, targeting the inflammatory basis of cystitis. To our knowledge, this is the first paper proposing O-1602 agent, as a candidate for future studies in the treatment of CYP-induced cystitis.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Wróbel A,Zapała Ł,Zapała P,Piecha T,Radziszewski Pdoi
10.1016/j.ejphar.2020.173321subject
Has Abstractpub_date
2020-09-05 00:00:00pages
173321eissn
0014-2999issn
1879-0712pii
S0014-2999(20)30413-1journal_volume
882pub_type
杂志文章abstract：:Honokiol and magnolol, two major phenolic constituents of Magnolia sp., have been known to exhibit antibacterial activities. However, until now, their antibacterial activity against Propionibacterium sp. has not been reported. To this end, the antibacterial activities of honokiol and magnolol were detected using the d...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2004.05.047
更新日期：2004-08-02 00:00:00
abstract：:The pre- and postsynaptic actions of the calcium entry facilitator Bay K 8644 were investigated in the rat isolated vas deferens. Bay K 8644 had no presynaptic effect on adrenergic neurotransmission in the epididymal portion. Bay K 8644 and alpha 1-adrenoceptor agonists potentiated, and the calcium entry blocker nifed...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(84)90414-x
更新日期：1984-09-17 00:00:00
abstract：:Extravasation elicited in rat skin by antidromic electrical stimulation of the saphenous nerve was dose dependently inhibited by the intravenous (i.v.) application of the mu-opioid receptor agonists, morphine and [D-Ala2,Me-Phe4,Gly-ol5]enkephalin (DAGO), and the kappa-opioid receptor agonists (-)-U 50488H, (-)-ICI 19...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(93)90233-8
更新日期：1993-05-12 00:00:00
abstract：:In this study, the anti-inflammatory effects of flavonoids isolated from the roots of Glycyrrhiza uralensis (Leguminosae), namely, isoliquiritin (the glycoside of isoliquirigenin) and isoliquiritigenin (the aglycone of isoliquiritin) were evaluated on lipopolysaccharide (LPS)-treated RAW 264.7 macrophages. Isoliquirit...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2008.01.032
更新日期：2008-04-14 00:00:00
abstract：:Platelet serotonin (5HT) uptake was measured in 18 subjects administered physostigmine salicylate in a double-blind, placebo crossover design. In comparison to placebo, the drug caused a significant transient depression in mood, as measured by self- and observer-rated depression scores. In addition, physostigmine sign...
journal_title：European journal of pharmacology
pub_type： 临床试验,杂志文章
doi：10.1016/0014-2999(85)90543-6
更新日期：1985-02-12 00:00:00
abstract：:Paeoniflorin (PF) is the main active ingredients of radix paeoniae rubra and radix paeoniae alba, which are used widely in Traditional Chinese Medicine. This study aimed to assess the capacity of PF to inhibit imiquimod (IMQ)-induced psoriasis. Mice treated with IMQ were divided into four groups and administered 240mg...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2015.12.040
更新日期：2016-02-05 00:00:00
abstract：:Inhibition by antipsychotic drugs of voltage-gated L-type Ca2+ channels was characterized in rat neuronal cell line pheochromocytoma PC12 cells. Under whole-cell voltage-clamp, haloperidol and chlorpromazine (1-100 microM) inhibited Ba2+ current permeating through Ca2+ channels. Fluspirilene and pimozide the Ba2+ curr...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(96)00500-6
更新日期：1996-10-24 00:00:00
abstract：:In the present study, the mechanism of relaxant response of nitric oxide precursor, L-arginine, was investigated in goat isolated coronary artery. L-arginine (1 mM) reversed the U-46619 (1 microM)-induced contraction both in endothelium-intact and endothelium-denuded arterial ring preparations. L-arginine analogues, L...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2009.03.031
更新日期：2009-05-01 00:00:00
abstract：:The role of dopamine transmission on striatal acetylcholine release was investigated by using brain microdialysis. Blockade of dopamine D2 receptors with (-)-sulpiride or haloperidol increased acetylcholine release to a maximum of 80% (after 50 and 0.5 mg/kg, respectively). This effect was prevented by blockade of dop...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(94)90409-x
更新日期：1994-01-14 00:00:00
abstract：:3,5-Dihydroxyphenylglycine (DHPG), (S)-3-hydroxyphenylglycine and (S)-4-carboxy-3-hydroxyphenylglycine (S-4C3HPG) stimulated phosphoinositide hydrolysis in neonatal rat cortical slices, but with lower maximal effect, in comparison with 2S,1'S,2'S-2-(2'-carboxycyclopropyl)glycine (L-CCG I) or (1S,3R)-1-aminocyclo-penta...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(97)01192-8
更新日期：1997-09-10 00:00:00
abstract：:The present experiments were devoted to analyzing the mechanisms involved in the captopril-dependent inhibition of human mesangial cell proliferation. Studies were performed in cultured human mesangial cells incubated with captopril, an angiotensin II-converting enzyme inhibitor with antioxidant properties, lisinopril...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(97)01250-8
更新日期：1997-10-08 00:00:00
abstract：:Two clinically effective anticonvulsants, phenobarbitone and diazepam, protected 5-day old chicks against picrotoxin convulsions without reducing brain GABA-transaminase activity or raising brain GABA concentration. Ethanolamine-O-sulphate and amino-oxyacetic acid, in doses which inhibited GABA-transminase by at least...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(76)90359-9
更新日期：1976-11-01 00:00:00
abstract：:Vasopressin ([Arg(8)]vasopressin)-induced contraction was characterized using receptor agonists and antagonists for vasopressin and channel blockers in the rat basilar artery ring preparations. Vasopressin induced rhythmic contractions superimposed on a contraction in endothelium-intact preparations but not in denuded...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(01)00781-6
更新日期：2001-03-23 00:00:00
abstract：:Effects of two typical neuroleptics haloperidol and loxapine, and an atypical antipsychotic clozapine on excitatory synaptic transmission were examined in the CA1 area of rat hippocampal slices. Haloperidol (10 mumol) and loxapine (10 mumol) increased extracelllar evoked field potentials by an average of 57 and 125% o...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(93)90151-7
更新日期：1993-04-28 00:00:00
abstract：:Disturbances in myocyte calcium homeostasis are hypothesized to be one cause for cardiac arrhythmia. The full development of this hypothesis requires (i) the identification of all sources of arrhythmogenic calcium and (ii) an understanding of the mechanism(s) through which calcium initiates arrhythmia. To these ends w...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2013.12.020
更新日期：2014-02-05 00:00:00
abstract：:The effects of endothelin, a potent endogenous vasoconstrictor peptide, were examined in a range of vascular and non-vascular tissues. At concentrations that cause vasoconstriction in portal vein and aorta, the peptide strongly contracted rat uterus, trachea and vas deferens, but not guinea pig ileum. Nifedipine, a di...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(89)90716-4
更新日期：1989-06-20 00:00:00
abstract：:The aim of this study was to investigate role of the N-Methyl-D-Aspartate (NMDA) receptors in the decrease of morphine analgesia in mice after nociceptive sensitization. We used a hot plate test to assess effects of morphine on pain behavior in male NMRI mice. All drugs were administered through an intraperitoneal rou...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2014.04.048
更新日期：2014-08-15 00:00:00
abstract：:The concentration of blood glucose was measured in rats after administration of a number of drugs characterized as dopamine agonists. Compounds that cause release of dopamine, or agents that block the reuptake of dopamine, did not elevate blood glucose. Some direct dopamine receptor stimulants (lergotrile, bromocripti...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(83)90234-0
更新日期：1983-06-03 00:00:00
abstract：:The effects of brief actinomycin D treatment (0.1 microgram/ml, 0.5 h) on inhibition of cell growth and colony formation were studied in synchronized HeLa cells. Cells in late S and G2 phases were found to be maximally sensitive to inhibition of cell growth and colony formation after short exposure to actinomycin D. C...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0926-6917(94)90064-7
更新日期：1994-04-04 00:00:00
abstract：:Local infusions of PYY (3-100 pmol.min-1) caused a slowly developing vasoconstriction of a long duration in the cat submandibular salivary gland. The vasoconstrictor action of PYY was also present after alpha-adrenoceptor blockade and in sympathectomized animals. Local APP infusions caused only weak vasoconstriction. ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(82)90300-4
更新日期：1982-09-10 00:00:00
abstract：:Hydroxytyrosol (HT), a polyphenol widely contained as an ester in olive fruits and olive leaves, exhibits a broad spectrum of effectiveness. The present study was designed to investigate the effect of HT alone as well as in the combination with cisplatin on the House Ear Institute-Organ of Corti 1 cells (HEI-OC1) and ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2020.173338
更新日期：2020-11-15 00:00:00
abstract：:The contractile actions of imidazoline alpha-adrenoceptor agonists were investigated in human vas deferens longitudinal and circular muscle. The effects of phenoxybenzamine were studied in comparison to dibenamine and SZL-49 (4-amino-6,7-dimethoxy-2-quinazolinyl-4-(2-bicyclo[2,2,2]octa-2,5-dienylcarbonyl-2-piperazine)...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(03)01346-3
更新日期：2003-02-21 00:00:00
abstract：:The present study concerns previously unreported effects of menthol, a cyclic terpene alcohol produced by the peppermint herb, on anion transporters in polarized human airway Calu-3 epithelia. Application of menthol (0.01-1mM) attenuated transepithelial anion transport, estimated as short-circuit currents (I(SC)), aft...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2010.03.032
更新日期：2010-06-10 00:00:00
abstract：:The aim of the study was to reveal general characteristics of the ligand-receptor interaction in the binding and displacement of radiolabeled ligands. The binding and displacement of DL-[3H]propranolol hydrochloride ([3H]propranolol) and L-[propyl-2,3, -3H]dihydroalprenolol ([3H]dihydroalprenolol), beta-adrenoceptor a...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(99)00679-2
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abstract：:The effects of ICS 205-930 [3 alpha-tropanyl)-1H-indole-3-carboxylic acid ester), an antagonist of 5-HT at neuronal M receptors, were examined in anaesthetised greyhounds subject to acute coronary artery occlusion and reperfusion. Intravenous administration of 0.3 or 2.0 mg kg-1 of ICS 205-930 did not significantly al...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(86)90366-3
更新日期：1986-08-15 00:00:00
abstract：:Behavioural evidence has accumulated that supports the hypothesis that specific territories of the striatum contribute differentially to the control of motor behaviours. The present experiments compare the behavioural effects of microinjections of amphetamine (20 microg/0.5 microl) with those elicited by the D2-class ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(98)00752-3
更新日期：1998-12-04 00:00:00
abstract：:[123I]Iodobenzofuran ([123I]IBF) is a new single photon emission computed tomography (SPECT) tracer for visualization of the dopamine D2 receptors. A tracer constant infusion paradigm was developed to measure the binding potential, density (Bmax) and affinity (KD) of the dopamine D2 receptor in baboons. Three baboons ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(94)90521-5
更新日期：1994-09-22 00:00:00
abstract：:The glutamate receptor agonists, kainate and N-methyl-D-aspartate (NMDA) result in the elevation of intracellular calcium levels ([Ca2+]i) in primary cultures of cerebellar granule neurons. Several tricyclic antidepressants (TCAs), amitriptyline (0.5-1 microM), desipramine (1 microM) and doxepine (1 microM) partially ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(92)90579-s
更新日期：1992-08-14 00:00:00
abstract：:Hydrogen sulfide (H2S) is a gasotransmitter synthesized in peripheral tissues by the enzyme cystathionine gamma-lyase (CSE). This gas has been documented to be involved in a wide variety of processes including inflammation and nociception. The aim of the present study was to investigate the role of the peripheral H2S ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2014.05.023
更新日期：2014-09-05 00:00:00
abstract：:A single dose of methamphetamine (25 mg/kg i.p.) was administered to young adult gerbils (Meriones unguiculatus) aged 90 days and the number of spices was determined along 40-microns segments of basal, lateral and apical dendrites of pyramidal cells in layers III and V of the prefrontal cortex, after 1.5, 7, 20 and 30...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(93)90937-d
更新日期：1993-09-07 00:00:00
