Abstract:
:The involvement of essential sulfhydryl groups in alpha 2-adrenoceptor function was investigated in the cerebral cortex of 7 and 70 day old rats. N-Ethylmaleimide (NEM) inhibited specific [3H]clonidine binding to cerebral cortical membranes in a concentration-dependent and biphasic manner in both infant and adult rats. The inhibitory effect of NEM was attenuated by simultaneous addition of dithiothreitol 30 microM and 1 mM, though dithiothreitol up to 1 mM did not affect the binding. p-Chloromercuriphenylsulfonic acid also caused a significant reduction in [3H]clonidine binding at both stages. Scatchard analysis of [3H]clonidine binding showed that NEM 10 and 100 microM caused a significant decrease in Bmax of high affinity binding sites without changing KD. Neither Bmax nor KD values were changed by NEM 10 and 100 microM in low affinity sites. The treatment with NEM 10 and 100 microM significantly reduced the increase of binding induced by Mn2+ 10 and 100 microM which was observed on day 70 but not on day 7. It is suggested that two distinct categories of essential sulfhydryl groups are involved in cerebral cortical alpha 2-adrenoceptors and are functionally mature by day 7. Furthermore, sulfhydryl groups are involved in the Mn2+-induced increase of alpha 2-receptors in adult rats.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Kawai M,Nomura Ydoi
10.1016/0014-2999(83)90169-3subject
Has Abstractpub_date
1983-08-05 00:00:00pages
449-54issue
4eissn
0014-2999issn
1879-0712pii
0014-2999(83)90169-3journal_volume
91pub_type
杂志文章abstract::We have already demonstrated that arachidonic acid (AA) inhibits carrageenin-induced granuloma growth in vivo and that this effect is related to an increase in prostaglandin E2 formation. As prostaglandin E1 has been shown to be more effective in inhibiting granuloma growth than prostaglandin E2 we investigated the ef...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(86)90234-7
更新日期:1986-05-27 00:00:00
abstract::Preparations of cauda epididymides were taken from rats unilaterally vasectomised by medial transection of the vas deferens. Responses of preparations from the operated side to field stimulation (10 pulses, 70 V, 1 ms, 0.1-20 Hz) declined in parallel with decreases in catecholamine fluorescence. There were leftward sh...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(89)90315-4
更新日期:1989-12-19 00:00:00
abstract::CPP has a potent anticonvulsant effect against sound-induced seizures in audiogenic DBA/2 mice. Pretreatment with CPP (0.01-10 nmol i.c.v., 45 min) protects against successive phases of sound-induced seizures in a dose-dependent fashion (ED50, tonic phase, 0.023 nmol; clonic phase, 0.039 nmol; wild running, 0.17 nmol)...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(87)90501-2
更新日期:1987-07-02 00:00:00
abstract::The effects of intracellular and extracellular application of bretylium tosylate on outward potassium current and fast inward Na+ current have been studied in single ventricular cells of chick embryo (18-day-old) using the whole-cell voltage clamp technique. Extracellular superfusion with bretylium (3 x 10(-4) M) decr...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(88)90535-3
更新日期:1988-07-14 00:00:00
abstract::The cocaine analog 3 beta-(4-iodophenyl)tropane-2 beta-carboxylic acid methyl ester (RTI-55 or beta CIT) has a higher affinity for the dopamine transporter and may be potentially useful in interfering with cocaine's actions in brain. However, imaging studies have demonstrated displacement of tracer doses of [123I]RTI-...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(95)00698-2
更新日期:1996-01-25 00:00:00
abstract::Cathelicidins are a class of gene-encoded multifunctional factors in host defence systems. They have recently attracted a great deal of attention as promising drug candidates. Cathelicidins are well studied in vertebrates, yet no studies have been reported concerning gecko cathelicidin. Recently, we identified a novel...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2020.173649
更新日期:2021-01-05 00:00:00
abstract::Vasoconstrictor responses elicited by periarterial electrical nerve stimulation were analyzed pharmacologically in the canine isolated, perfused intermediate auricular artery. Phentolamine (10 microM) significantly inhibited the vasoconstrictor responses to stimulation at 5 Hz and over but not those to stimulation at ...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/s0014-2999(97)01121-7
更新日期:1997-08-27 00:00:00
abstract::Eosinophils and their granular proteins are crucial for combating allergic airway diseases. Eosinophils derived from HL-60 clone 15 (HC15) cells have been established as a feasible alternative cell model for human primary eosinophils. Simvastatin, a cholesterol-lowering agent, has been shown to exhibit anti-inflammato...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2019.05.029
更新日期:2019-08-05 00:00:00
abstract::Acetylcholine releases a non-prostanoid endothelium-derived hyperpolarizing factor (EDHF) and nitric oxide from physiological salt solution perfused rat mesenteric arteries. This study reports an impairment in EDHF-mediated vasodilation in deoxycorticosterone acetate (DOCA)-salt hypertensive versus control normotensiv...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2003.09.005
更新日期:2003-11-14 00:00:00
abstract::Ischemia reperfusion (I/R) injury is a cellular damage in a hypoxic organ following the restoration of oxygen delivery. It may occur during organ transplantation, trauma and hepatectomies. Nitric oxide (NO) effects during hepatic I/R are complicated. The iNOS-derived NO has a deleterious effect, whereas eNOS-derived N...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2017.09.037
更新日期:2017-11-15 00:00:00
abstract::The central dopamine system plays a prominent role in the effect of psychostimulants such as methamphetamine, cocaine and nicotine. l-3,4-Dihydroxyphenylalanine (DOPA), a precursor of dopamine, has been proposed as a neurotransmitter in the central nervous system. We have studied the effects of these psychostimulants ...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2006.08.031
更新日期:2006-11-07 00:00:00
abstract::The actions of gamma-aminobutyric acid (GABA) and the receptor selective agonists, muscimol (GABAA) and baclofen (GABAB), on motor activity of the longitudinal muscle-myenteric plexus of guinea-pig distal colon were studied in vitro. Preparations exhibited spontaneous contractions that were blocked by scopolamine (1 m...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(93)90801-n
更新日期:1993-01-12 00:00:00
abstract::In the present study we investigated the in vivo pharmacological profile of the benz[e]indole cis-8-hydroxy-3-(n-propyl)],2,3a,4,5,9b-hexahydro-1H-benz[e]indole (cis-8-OH-PBZI), which has been described as a preferential dopamine D3 receptor agonist in vitro. The compound inhibited spontaneous locomotor activity in mi...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/s0014-2999(97)01494-5
更新日期:1998-01-26 00:00:00
abstract::The aim of the study was to investigate whether diabetes mellitus modulated the function and expression of P-glycoprotein and the distribution of phenobarbital in the brain of 3-week streptozotocin-induced diabetic mice. P-glycoprotein function in blood-brain barrier was assessed by measuring the brain-to-plasma conce...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2007.01.062
更新日期:2007-04-30 00:00:00
abstract::We investigated, in murine colon circular muscle, the role of adenosine 5'-triphosphate (ATP) and pituitary adenylate cyclase activating peptide (PACAP) as inhibitory neurotransmitters of the fast component of nerve-evoked inhibitory junction potential (fast IJP). Fast IJP was antagonised by apamin or suramin, abolish...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/s0014-2999(02)02923-0
更新日期:2003-01-24 00:00:00
abstract::Little research has been conducted investigating the long-term impact of opioid exposure during adolescence. These experiments were conducted to determine the behavioral effects of morphine exposure during periadolescence (postnatal days 30-32) versus young adulthood (postnatal days 65-67) on subsequent sensitivity to...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2005.10.026
更新日期:2005-12-28 00:00:00
abstract::Dextrans of molecular weight 10(4) to 2 x 10(6) induced histamine release from rat peritoneal mast cells in the presence of calcium (1 mM) and phosphatidyl serine (10 micrograms/ml). Glucose and low molecular weight dextrans inhibited the histamine release induced by high molecular weight dextrans but the inhibition c...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(82)90287-4
更新日期:1982-09-10 00:00:00
abstract::Induction of mRNA or protein for immediate-early genes, such as c-fos, is used to identify brain areas, specific cell types, and neuronal circuits that become activated in response to various stimuli including psychoactive drugs. The objective of the present study was to identify the cell types in the prefrontal corte...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2007.12.031
更新日期:2008-03-31 00:00:00
abstract::The effects of indapamide on contractile responses in various isolated artery rings and on spontaneous mechanical activity in portal vein segments were investigated. Arteries used were: rabbit aorta, mesenteric (fifth branch), femoral and basilar, and sheep coronary arteries. 45Ca2+ uptake was also analysed in rabbit ...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(93)90630-z
更新日期:1993-11-30 00:00:00
abstract::The maximal number of binding sites (Bmax) and the equilibrium dissociation constant (KD) values for [3H]PK 11195 binding were determined in the platelet membranes of epileptic patients before and after 4 weeks of carbamazepine (CBZ) treatment, as well as in healthy controls. There was a decrease of 17.1% in the Bmax ...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(87)90567-x
更新日期:1987-09-23 00:00:00
abstract::Acute lung injury (ALI) is a common severe clinical syndrome in intensive care unit. Inflammation has been reported to play a critical role in the development of ALI. Cordycepin, an active component isolated from Cordyceps militaris, has been reported to have anti-inflammatory effects. However, the anti-inflammatory e...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2017.10.029
更新日期:2018-01-05 00:00:00
abstract::The toxicity of glutamate in neuronal cultures has been attributed in part to a mitochondrial dysfunction involving the permeability transition pore. The participation of the permeability transition pore in this process has been pharmacologically demonstrated by the use of cyclosporin A, which inhibits pore opening by...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/s0014-2999(00)00584-7
更新日期:2000-09-15 00:00:00
abstract::Thapsigargin (TG), an inhibitor of Ca(2+) ATPase pumps in the endoplasmic reticulum (ER), inhibits replication of human vascular smooth muscle cell (hVSMC) at low nM concentrations. TG blocks replication of other cell types through promotion of ER stress (ERS). In order to determine whether ERS may mediate the cytosta...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2013.05.036
更新日期:2013-08-15 00:00:00
abstract::Emodin, 1,3,8-trihydroxy-6-methyl-anthraquinone, is an anthraquinone derivative from the roots of Rheum officinale Baill that has been used to treat many diseases in digestive system for thousands of years. This study is to disclose the mechanism of Emodin to treat cholestatic hepatitis via anti-inflammatory pathway. ...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2008.06.044
更新日期:2008-08-20 00:00:00
abstract::Rats were treated with 10 mg/kg tetrahydroaminoacridine (THA) twice daily for 14 days. THA (10 mg/kg) induced a significant decrease in the number of muscarinic receptors (both M1 and M2) in the cortex and striatum, whereas the number of nicotinic receptors in the cortex and hippocampus increased. Rats treated with ph...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(90)90448-f
更新日期:1990-09-21 00:00:00
abstract::Non-peptide antagonists of the NK1 and NK2 receptors were tested as inhibitors of the reaction time in the rat tail-flick and on the decrease of reaction time induced by the intrathecal injection of the NK1 receptor selective agonist [Sar9,Met(O2)11]SP or of the NK2 selective agonist NKA-(4-10). The decrease in reacti...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(93)90782-d
更新日期:1993-03-02 00:00:00
abstract::The direct relaxing effect of halothane on airway smooth muscle has been reported to involve the reduction of the cytosolic Ca2+ concentration ([Ca2+]i) and the [Ca2+]i-independent inhibitory mechanism. To clarify the extent of the contribution of these mechanisms, the effect of halothane on the [Ca2+]i-tension relati...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/s0014-2999(96)00617-6
更新日期:1996-11-21 00:00:00
abstract::PK20M (Dmt-D-Lys-Phe-Phe-OH) is a novel modified endomorphin-2 (EM-2) peptide producing strong dose- and time-dependent antinociceptive activity. Yet its prototype, endogenous EM-2, has been reported to trigger respiratory and vascular effects such as apnea and hypotension. The purpose of this study was to investigate...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2020.173514
更新日期:2020-10-15 00:00:00
abstract::The effect of progesterone on isolated rabbit coronary arteries and its possible mechanism was investigated by measuring changes of isometric tension. Progesterone (1, 3, 10 and 30 microM) induced significant coronary relaxation in K+ (30 mM)-, prostaglandin F2 alpha (3 microM)- or Bay K 8644 (1 microM plus 15 mM K+)-...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(92)90524-8
更新日期:1992-02-11 00:00:00
abstract::The effect of eliprodil on P-type Ca2+ channels was investigated in acutely dissociated rat Purkinje neurons, by using the whole-cell patch-clamp technique. Eliprodil inhibited in a reversible manner the omega-agatoxin-IVA-sensitive Ba2+ current elicited by step depolarizations from a -80 mV holding voltage (IC50 = 1....
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(95)00511-0
更新日期:1995-12-27 00:00:00