Abstract:
:Administration of methyl-beta-carboline-3-carboxamide (FG 7142, 15 mg/kg i.p.) to rats has previously been shown to cause a selective increase in the levels of 3,4-dihydroxy-phenylacetic acid (DOPAC) in the prefrontal cortex and ventral tegmental area (VTA) via an interaction with benzodiazepine receptors. On withdrawal 3 days following chronic treatment with diazepam for 21 days, FG 7142 no longer increased DOPAC levels in either the prefrontal cortex or the VTA. Chronic diazepam treatment alone was ineffective in altering dopamine metabolism in the eight brain regions examined. The present findings indicate that chronic diazepam treatment may cause changes at the level of GABA/benzodiazepine receptor macromolecular complex, which is normally functionally integrated with the mesoprefrontal dopaminergic neurons, so that FG 7142 can no longer exert its intrinsic actions.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Ida Y,Roth RHdoi
10.1016/0014-2999(87)90221-4subject
Has Abstractpub_date
1987-06-04 00:00:00pages
185-90issue
2-3eissn
0014-2999issn
1879-0712pii
0014-2999(87)90221-4journal_volume
137pub_type
杂志文章abstract::The binding of the tritiated derivative of the 5-HT3 receptor agonist meta-chlorophenylbiguanide ([3H]mCPBG) to rat cortical homogenates and whole rat brain sections was assessed in an attempt to further investigate the binding of agonists to the 5-HT3 receptor. In crude homogenates of rat cortex, no reproducible spec...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(93)90161-a
更新日期:1993-10-12 00:00:00
abstract::This study investigated whether increased polyol pathway activity could contribute to alterations in nitrergic neurotransmission in anococcygeus muscles from 8-week diabetic rats. In the presence of guanethidine (10-30 microM) and clonidine (0.01-0.05 microM), relaxations obtained to nitrergic nerve stimulation (0.5-5...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/s0014-2999(96)00751-0
更新日期:1996-12-27 00:00:00
abstract::The purpose of the present study was to test whether kava extract and its constituents kawain, dihydrokawain, methysticin, dihydromethysticin and yangonin provide protection against ischemic brain damage. To this end, we used a model of focal cerebral ischemia in mice and rats. Ischemia was induced by microbipolar coa...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(92)90037-5
更新日期:1992-05-14 00:00:00
abstract:UNLABELLED:This study analyzed the role of nitric oxide (NO) and endothelium-derived hyperpolarizing factor (EDHF) in gender differences in the renal vascular reactivity of rats. Renal responses to vasoconstrictors and vasodilators were studied in isolated kidneys from male and female rats under basal conditions, after...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2003.12.036
更新日期:2004-02-23 00:00:00
abstract::The potency and site of action of Ro5-3663 as a GABA antagonist were investigated in the rat cuneate slice in vitro. A Schild plot for Ro5-3663 was clearly non-linear but enabled a pA2 value of 3.97 to be calculated. Combination studies using the 'classical' GABA antagonists bicuculline and picrotoxin indicated that R...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(83)90064-x
更新日期:1983-01-28 00:00:00
abstract::In WI-38 human fibroblasts, interleukin-1 beta and tumour necrosis factor-alpha (TNF-alpha) increased bradykinin B(1) receptor mRNA, which peaked between 2 and 4 h, remaining elevated for 20 h. Binding of the bradykinin B(1) receptor selective ligand [3H]des-Arg(10)-kallidin, also increased, peaking at 4 h and remaini...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/s0014-2999(00)00323-x
更新日期:2000-06-02 00:00:00
abstract::A 5-min period of cerebral ischemia induced in rats by the four-vessel occlusion method increased the number of errors (attempts to pass through two incorrect panels of the three panel-gates at four choice points) assessed by a working memory procedure applied in a three-panel runway task. The protein kinase C (PKC) i...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(91)90844-g
更新日期:1991-10-29 00:00:00
abstract::Rats were treated with ethanol for 11-15 days, after which the brain neurotransmitter receptors for dopamine, acetylcholine, serotonin and noradrenaline were measured. The rats were intubated at 12 h intervals with 4 g/kg ethanol, and sacrificed 10 h after the last intubation. After ethanol treatment, the specific bin...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(80)90205-8
更新日期:1980-07-11 00:00:00
abstract::Substance-related and addictive disorders (SRADs) are characterized by compulsive drug use and recurrent relapse. The persistence of pathological drug-related memories indisputably contributes to a high propensity to relapse. Hence, strategies to disrupt reconsolidation of drug reward memory are currently being pursue...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2021.173911
更新日期:2021-01-24 00:00:00
abstract::The quantitative [14C]2-deoxyglucose autoradiographic technique was applied to the measurement of the cerebral metabolic effects of adenosine A1 and A2 receptor agonists and antagonists in adult rats. The adenosine A1 receptor agonist and antagonist, 2-chloro-N6-cyclopentyladenosine (CCPA) and 8-cyclopentyl-1,3-diprop...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(94)90057-4
更新日期:1994-06-02 00:00:00
abstract::The present study investigated the changes in NMDA receptor subunit proteins in diazepam-withdrawn rat cerebral cortex, using Western blotting analysis. The protein levels of the NR1 and NR2B, but not NR2A, subunits were significantly increased in diazepam-withdrawn rats compared to those in control rats. Therefore, a...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/s0014-2999(97)01501-x
更新日期:1998-01-12 00:00:00
abstract::We investigated the involvement of dopamine D1 and D2 receptor subtypes in the effects of GBR 12909, a selective dopamine uptake inhibitor, on latent learning in the performance of a water-finding task and on locomotor activity in mice. GBR 12909 (10 and 20 mg/kg) impaired latent learning, and this effect was countera...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(93)90949-i
更新日期:1993-04-06 00:00:00
abstract::Since its clinical inception, tamoxifen (TAM) has proved to be a powerful tool in treating estrogen receptor-positive breast cancers while exhibiting manageable side effects. Although TAM was synthesized as an estrogen receptor antagonist, reports have found that a significant fraction of women with estrogen receptor-...
journal_title:European journal of pharmacology
pub_type: 杂志文章,评审
doi:10.1016/j.ejphar.2016.04.017
更新日期:2016-06-15 00:00:00
abstract::Breast cancer is one of the main diagnosis cancers annually worldwide. It is difficult to thorough cure due to drug resistance and the high possibility of metastasis. SM934 is a novel water-soluble artemisinin analog, and has been reported to have a promising therapeutic effect on multiple autoimmune diseases. In this...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2019.05.011
更新日期:2019-09-05 00:00:00
abstract::The effects of intracerebroventricular (i.c.v.), intravenous (i.v.) and oral (p.o.) administration of trimebutine on the gastric motor inhibition induced by acoustic stress were investigated in fasted dogs fitted with strain-gauge transducers on the antrum and proximal jejunum. Started 40-50 min after the last migrati...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(88)90486-4
更新日期:1988-01-27 00:00:00
abstract::Venenum Bufonis, a traditional Chinese medicine, is widely used in the treatment of liver cancer in modern Chinese medical practices. In our search for anti-hepatoma constituents in Venenum Bufonis, bufotalin, bufalin, telocinobufagin and cinobufagin were obtained. Bufotalin was the most potent active compound among t...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2012.06.045
更新日期:2012-10-05 00:00:00
abstract::Prostate cancer is one of the most severe malignancies in men, and many genes and non-coding RNAs, included microRNAs (miRs), have been demonstrated to regulate prostate cancer progression. In the present study, we investigated the role of miR-671 in prostate cancer cell proliferation. We found that miR-671 was signif...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2018.01.016
更新日期:2018-03-15 00:00:00
abstract::We investigated the effects of the platelet activating factor (PAF) receptor antagonists, SM-12502 ((+)-cis-3,5-dimethyl-2-(pyridyl)- thiazolidin-4-one hydrochloride), WEB-2086 (3-(4-(2-chlorphenyl)-9-methyl-6H-thieno(3,2-f)-(1,2,4)triazolo(4, 3- a)(1,4)diazepin-2-yl)-1-(4-morpholinyl)-1-propanone) and RP-48740 (3-(3-...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0922-4106(94)90037-x
更新日期:1994-11-15 00:00:00
abstract::The pH dependence of the facilitation by dopamine (10 microM), 5-hydroxytryptamine (10 microM), adenosine (1 and 100 microM), Zn2+ (10 microM) and Cd2+ (1 mM) of P2X2 purinoceptor/channels was tested by expressing these channels in Xenopus oocytes. In a pH range between 6.0 and 8.5, concentration-response curves for a...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/s0014-2999(97)01293-4
更新日期:1997-10-22 00:00:00
abstract::3H-Mepyramine (3H-MEP) binds to slide-mounted tissue sections with characteristics indicating the labelling of a H1-histamine receptor. It is saturable (Bmax 12 pg/g tissue), of a high affinity (KD 0.5 mM) and possesses a drug specificity similar to that observed for H1 receptors in a variety of systems. In agreement ...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(79)90478-3
更新日期:1979-10-01 00:00:00
abstract::Tanshinone IIA, one of the main active components from Chinese herb Danshen, is widely used to treat cardiovascular diseases including arrhythmia in Asian countries especially in China. However, the mechanisms underlying its anti-arrythmia effects are not clear. In this study we investigate the effects of tanshinone I...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2008.06.005
更新日期:2008-08-20 00:00:00
abstract::Sickness behavior is a series of behavioral and psychological changes that develop in inflammatory disease, including infections and cancers. Administration of the bacterial endotoxin lipopolysaccharide (LPS) induces sickness behavior in rodents. Genipin, an aglycon derived from an iridoid glycoside geniposide extract...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2014.07.038
更新日期:2014-10-15 00:00:00
abstract::Agomelatine is an antidepressant with a novel mechanism of action. It is a melatonergic agonist for MT1 and MT2 receptors and a serotonin (5-HT2C) receptor antagonist. Agomelatine has been suggested not to have adverse effects on sexual functions. However, the effects of chronic agomelatine administration on reproduct...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2015.11.054
更新日期:2016-01-05 00:00:00
abstract::Analogues of the C-terminal octapeptide of cholecystokinin (CCK) modified in the Met28-Gly29 region, were tested for their ability to interact with peripheral cholecystokinin receptors on rat pancreatic acini and to stimulate amylase secretion. These analogues were further evaluated for their ability to recognize cent...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(90)90436-a
更新日期:1990-09-21 00:00:00
abstract::Horizontal motor activity, rearing and head dipping were recorded automatically in rats placed on a holeboard and taken as indices of locomotion and exploration. Other behaviours were assessed visually using a video camera. SKF 38393, 15-30 mg/kg (D-1 agonist), suppressed all three behavioural measures more effectivel...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(85)90014-7
更新日期:1985-11-19 00:00:00
abstract::Treatment with soterenol (0.3-300 mug/kg, i.v.) increased the mean arterial blood pressure and decreased heart rate in rabbits. Soterenol caused a dose-dependent contraction of rabbit aorta and portal vein, guinea-pig vas deferens and cat nicitating membrane which was inhibited by phentolamine. Other beta-agonists suc...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(75)90163-6
更新日期:1975-08-01 00:00:00
abstract::The spasmolytic activity of synthetic alpha-human atrial natriuretic peptide (alpha-hANP) and its related peptides was determined in vitro using the chick rectum and the rat aorta. Natriuretic activity was also measured in the anesthetized rat, alpha-hANP-(7-28), with the NH2-terminal hexapeptide truncated, had greate...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(88)90632-2
更新日期:1988-02-16 00:00:00
abstract::In isolated spontaneously beating right and left atria and in electrically driven left atrium from rat, endothelin-1 increased the rate and force of contraction, but significantly decreased the positive chronotropic and inotropic responses to sympathetic nerve stimulation. The decrease may be partly dependent on the p...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(91)90102-v
更新日期:1991-03-05 00:00:00
abstract::Nanomolar concentrations of atropine have been considered up to now to be selective for blockade of muscarinic receptors for acetylcholine. A collateral finding indicated to us that these low concentrations of atropine could also target the neuronal nicotinic receptors. We report here a detailed study on this novel pr...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2006.01.057
更新日期:2006-03-27 00:00:00
abstract::Neuromedin K, a decapeptide isolated from porcine spinal cord and suggested to have tachykinin-like activity in vitro, produced reciprocal hind-limb scratching when injected intrathecally to mice. Neuromedin K was 20-60 times less potent in producing scratching (on a molar basis) than substance P, kassinin, eledoisin ...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(84)90499-0
更新日期:1984-08-17 00:00:00