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-dipropylxanthine (DPCPX) as well as the adenosine A2 receptor agonist, 2-[p-(2-carboxyethyl)phenylethylamino]-5'-ethylcarboxamidoadenosin e (CGS 21680), were injected at the dose of 0.01 mg/kg. The adenosine A2 receptor antagonist, 3,7-dimethyl-1-proparglyxanthine (DMPX) was injected at the dose of 0.3 mg/kg. These doses were chosen in accordance with the known affinity of the drugs for their respective receptor and to avoid peripheral effects. The adenosine A1 receptor agonist, CCPA, induced decreases in glucose utilization in three brain areas, the globus pallidus and two hypothalamic nuclei. The adenosine A2 receptor agonist, CGS 21680, induced more general depressant effects on energy metabolism which were significant in 17 brain areas, such as cerebral cortex, hippocampal and white matter regions plus motor and limbic structures. The adenosine A2 receptor antagonist, DMPX, decreased glucose utilization in the globus pallidus while increasing energy metabolism in the cochlear nucleus. The adenosine A1 receptor antagonist, DPCPX, depressed glucose utilization in the globus pallidus and dentate gyrus, and increased rates of energy metabolism in six regions, mainly hypothalamic, thalamic areas and in the cochlear nucleus. There was a mismatch between cerebral metabolic consequences of adenosine A1 and A2 receptor agonists and the localization of corresponding adenosine receptors. The metabolic effects of the adenosine A2 receptor agonist and antagonist were consistent with the known involvement of that type of receptor in the control of locomotion and its effects on neuronal firing in the hippocampus and cerebral cortex. The effects of the adenosine A1 receptor agonist were very discrete and mostly related to the transient decrease in blood pressure induced by the drug. The increases in glucose utilization induced in limbic regions by the adenosine A1 receptor antagonist are probably linked to the regulation by adenosine of arousal and cardiorespiratory function. These results are in good agreement with the neuroregulatory function of the adenosine system as previously shown by other methods.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Nehlig A,Daval JL,Boyet Sdoi
10.1016/0014-2999(94)90057-4subject
Has Abstractpub_date
1994-06-02 00:00:00pages
57-66issue
1-2eissn
0014-2999issn
1879-0712pii
0014-2999(94)90057-4journal_volume
258pub_type
杂志文章abstract::GABAA receptors are pentameric chloride ion channels that are opened by GABA. We have screened a cell line derived from human glioblastoma, U3047MG, for expression of GABAA receptor subunit isoforms and formation of functional ion channels. We identified GABAA receptors subunit α2, α3, α5, β1, β2, β3, δ, γ3, π, and θ ...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2014.12.001
更新日期:2015-02-05 00:00:00
abstract::Melatonin is of considerable interest for its regulatory influence on a variety of physiological processes including biological rhythms and neuroendocrine functions. We showed that melatonin potentiates sympathetic neurotransmission in the prostatic portion of the rat vas deferens, by increasing contractions in respon...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(94)90696-3
更新日期:1994-05-12 00:00:00
abstract::The characteristics of [3H]gamma-aminobutyric acid (GABA) uptake by slices of the rabbit oviduct were studied, and the GABA-accumulating structures were identified by histoautoradiography. A high-affinity (Km = 5 microM), sodium-dependent GABA uptake system was demonstrated which showed significant segmental variation...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(86)90280-3
更新日期:1986-11-04 00:00:00
abstract::The effect of DL-propranolol on NO release in perfused rat hindquarters was studied by using oxyhemoglobin as a capture system to allow the quantitative assay of NO production. In some experiments the stable prostacyclin metabolite 6-keto-PGF1 alpha (6-keto) was simultaneously assayed. We observed that: (1) DL-propran...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(92)90686-x
更新日期:1992-03-24 00:00:00
abstract::We studied the effects of carmustine (1,3-bis(2-chloroethyl)-1-nitrosourea) on the intracellular Ca(2+) concentration ([Ca(2+)](i)) in PC12 cells using fura-2 fluorescence imaging. Carmustine (100 microM) caused a delayed increase in [Ca(2+)](i) that developed within approximately 3 h. This effect was enhanced in cell...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2004.06.043
更新日期:2004-08-16 00:00:00
abstract::The cGMP response and the accumulation of inositol monophosphate (IP) induced by carbachol were compared in slices of different rat brain structures. Basal cGMP and the responses of cGMP to carbachol appeared dependent on the concentration of added Ca2+, suggesting that distinct Ca(2+)-mediated and Ca(2+)-sensitive mu...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0922-4106(91)90029-h
更新日期:1991-07-12 00:00:00
abstract::The tachykinins substance P, neurokinin A and neurokinin B are involved in many pathophysiological processes. A reverse transcription-polymerase chain reaction (RT-PCR) assay was used to analyse the expression of TAC1 and TAC3, the genes that encode substance P/neurokinin A and neurokinin B, respectively, and the gene...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2004.05.016
更新日期:2004-06-28 00:00:00
abstract::To investigate whether argatroban ((2R,4R)-4-methyl-1-[N(2)-((RS)-3-methyl-1,2,3,4-tetrahydro-8-quinolinesulfonyl)-L-arginyl]-2-piperidinecarboxylic acid hydrate, a selective thrombin inhibitor, exerts a direct action on phenotype conversion of vascular smooth muscle cells, cultured rabbit aortic vascular smooth muscl...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/s0014-2999(03)01293-7
更新日期:2003-02-07 00:00:00
abstract::The inhibitory actions of the Ca2+ antagonist Cd2+, morphine and noradrenaline (exogenously added + endogenously released) on electrically evoked release of [3H]noradrenaline from superfused rat neocortical slices were strongly reduced when release was enhanced by 4-aminopyridine. In the presence of 4-aminopyridine th...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(83)90084-5
更新日期:1983-03-04 00:00:00
abstract::We examined the influence of streptozotocin-induced diabetes on the growth of cultured rat aortic smooth muscle cells in the presence of interleukin-1 beta. Interleukin-1 beta induced a dose-dependent biphasic effect on proliferation of diabetic and control smooth muscle cells, consistent with the data on [3H]thymidin...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(96)00398-6
更新日期:1996-09-05 00:00:00
abstract::Liver failure altered P-glycoprotein (P-gp) function and expression at blood-brain barrier (BBB), partly owing to hyperammonemia. We aimed to examine the effects of partial portal vein ligation (PVL) plus chronic hyperammonemia (CHA) on P-gp function and expression at rat BBB. Experimental rats included sham-operation...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2019.01.005
更新日期:2019-03-05 00:00:00
abstract::Adenosine 5'-triphosphate (ATP), beta, gamma-methylene ATP and alpha, beta-methylene ATP produced relaxation of carbachol-precontracted isolated trachealis muscle from the guinea-pig in the presence of indomethacin (2.8 microM) and the adenosine uptake inhibitor S-(4-nitrobenzyl)-6-thioinosine (NBTI; 300 nM). The pote...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(96)00237-3
更新日期:1996-06-27 00:00:00
abstract::18-Methoxycoronaridine, a novel iboga alkaloid congener that decreases drug self-administration in several animal models, may be a potential treatment for multiple forms of drug abuse. In previous work, 18-methoxycoronaridine was found to be a somewhat selective antagonist at alpha3beta4 nicotinic receptors; and low d...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/s0014-2999(02)01944-1
更新日期:2002-07-19 00:00:00
abstract::Vasoactive substances released from aggregating platelets inhibit beta-adrenergic neurotransmission in coronary arteries. Studies were carried out on the effects of two such vasoactive substances on canine coronary arteries, at concentrations equivalent to that released by platelets under physiological conditions. 5-H...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(87)90030-6
更新日期:1987-01-20 00:00:00
abstract::Intravenous infusions of sodium nitroprusside (SNP) at doses of 20, 40 or 80 micrograms/kg min-1 for 30 min produced dose-related decrements in blood pressure in conscious rats fitted with indwelling aortic and vena caval catheters. Immediately upon termination of SNP infusions, blood pressure rebounded to levels whic...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(79)90473-4
更新日期:1979-10-01 00:00:00
abstract::Intermittent cocaine administration induces sensitization (reverse tolerance) to its behavioral effects. The mechanism(s) mediating sensitization is not clear, however, previous research has implicated 5-HT(3) receptors in the expression of sensitization. The present experiment evaluated the ability of the 5-HT(3) rec...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/s0014-2999(99)00926-7
更新日期:2000-04-07 00:00:00
abstract::Conscious guinea-pigs received platelet activating factor (PAF, 0.03-0.25 microgram/kg, i.v.) and colloidal carbon (C, tracer for microvascular leakage). Fifteen min later the animal was killed and C-labelled microvessels (leakage) were detected in the mucosal/submucosal region of tracheal and bronchial sections. PAF ...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(87)90477-8
更新日期:1987-06-26 00:00:00
abstract::Experiments were undertaken to determine the effect of the selective histamine H3 receptor agonist (R)-alpha-methylhistamine on the amplitude of neurally evoked electrodermal (sudomotor) responses in anesthetized cats. (R)-alpha-Methylhistamine produced comparable dose-related depressions of these evoked sympathetic-c...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(94)90701-3
更新日期:1994-05-12 00:00:00
abstract::Cytokines and cytokine-induced nitric oxide (NO) play important roles in inflammatory glomerular diseases, and both platelet-derived growth factor and transforming growth factor-beta inhibit cytokine-induced NO production. In this study, we demonstrated that a selective endothelin ET(A) receptor antagonist, BQ-485 (He...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/s0014-2999(98)00849-8
更新日期:1999-01-15 00:00:00
abstract::This study investigated sex-related differences in rat papillary muscle force generation in response to altered extracellular [Ca2+] ([Ca2+](o), 0.2 to 5.0 mM) and to L-type Ca2+ channel modulators (nifedipine and Bay K8644). At all [Ca2+]o examined, contractile force was significantly greater in male than female papi...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2008.02.053
更新日期:2008-05-31 00:00:00
abstract::Administration of drugs activating cannabinoid CB(1) receptors in the brain induces memory deficit in rodents, and blockade of these receptors may restore memory capacity in these animals. Central administration of beta-amyloid or beta-amyloid fragments may also lead to memory disturbances. This study was undertaken t...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2003.08.026
更新日期:2003-09-23 00:00:00
abstract::Results from lesion studies show that selective damage to the temporal cortex or lateral entorhinal cortex impairs visual memory, whereas damage to the hippocampal region does not affect retention of a visual discrimination task. Major input pathways of the above structures use glutamate as neurotransmitter. The gluta...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/s0014-2999(01)01348-6
更新日期:2001-10-12 00:00:00
abstract::The involvement of dopamine D-1 and D-2 receptor mechanisms was investigated in the forced swimming test with rats. d,1-Sulpiride, a D-2 receptor antagonist, reported to reduce desipramine-induced anti-immobility, did not alter the brain levels of desipramine. In addition, the anti-immobility effect of desipramine was...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(88)90107-0
更新日期:1988-04-13 00:00:00
abstract::This study investigates the possible protective effects of levocetirizine against fructose-induced insulin resistance, hepatic steatosis and vascular dysfunction, in comparison to pioglitazone, a standard insulin sensitizer. Male Sprague Dawley rats (150-200 g) were divided into 4 groups. Three groups were fed on high...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2014.07.021
更新日期:2014-10-05 00:00:00
abstract::Hepatic and systemic insulin resistance form the core of metabolic syndrome which is also associated with cardiovascular abnormalities, inflammation, and dyslipidemia. Skeletal muscles and adipose tissues are two main target organs for glucose disposal and hence have been studied for insulin resistance too. The liver ...
journal_title:European journal of pharmacology
pub_type: 杂志文章,评审
doi:10.1016/j.ejphar.2019.172657
更新日期:2019-11-05 00:00:00
abstract::Postoperative cognitive dysfunction (POCD) is commonly seen in patients undergoing major surgeries and may persist. Although neuroinflammation is one of the important contributors to the development of POCD, the mechanisms underlying POCD remain unclear. We performed stabilized tibial fracture operation in male mice. ...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2018.12.034
更新日期:2019-03-05 00:00:00
abstract::[3H]Neuropeptide Y labelled neuropeptide Y receptors in rat forebrain membranes as a homogenous class of high-affinity sites. Between 80 and 85% of these receptors showed high affinity for Y1-selective antagonists such as (R)-N2-(diphenylacetyl)-N-[(4-hydroxyphenyl)methyl]-D-arginine amide (BIBP3226). While competitiv...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/s0014-2999(97)01016-9
更新日期:1997-07-23 00:00:00
abstract::Three non-steroidal antiinflammatory agents were tested for their ability to antagonize bradykinin in the rabbit jugular vein, the dog carotid artery and the guinea pig trachea. The new agents were compared with indomethacin, as well as with [Thi5,8,D-Phe7] bradykinin and [Thi6,9,D-Phe8] kallidin, two B2 receptor anta...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(88)90808-4
更新日期:1988-07-07 00:00:00
abstract::We studied the effects of 2-(allyl-1-piperazinyl)-4-n-amyloxyquinazoline fumarate (KB-5666) on brain edema and histological neuronal damage in rats with focal ischemia and on lipid peroxidation in brain homogenates and brain mitochondria in vitro. KB-5666 (3-100 microM) inhibited lipid peroxidation in brain homogenate...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(91)90367-y
更新日期:1991-05-02 00:00:00
abstract::Endogenous hydrogen sulfide is produced by cystathionine-γ-lyase and cystathionine-β-synthase in a variety of tissues and has recently been implicated in the regulation of cardiac functions. Acceleration of the heart rate in response to catecholamines is impaired in patients with cirrhosis. The present study was aimed...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2012.09.039
更新日期:2012-12-05 00:00:00