Abstract:
:The characteristics of [3H](+)-pentazocine and [3H]1,3-di(2-tolyl) guanidine (DTG) binding to mouse whole brain, cortex, cerebellum and spinal cord membranes were investigated in radioreceptor assays. [3H](+)-Pentazocine bound to a single, high affinity site (Kd = 1.2-1.6 nM) with increasing density along the neuraxis from the cortex (Bmax = 543 fmol/mg protein) to the spinal cord (Bmax = 886 fmol/mg protein). Hot saturation studies resolved the presence of one binding site for [3H]DTG showing no tissue variations in terms of density (Bmax = 1075-1264 fmol/mg protein) or affinity (Kd = 16.6-22.3 nM). Incubation with 100 nM (+)-pentazocine revealed two classes of high affinity [3H]DTG labeled binding sites corresponding to sigma 1 and sigma 2 subtypes. A preponderance of sigma 2 sites was revealed in all investigated tissues. Different pharmacological profiles were demonstrated for the sigma 2 sites in mouse whole bain compared to mouse spinal cord. However, competition studies indicated that the whole brain and spinal [3H](+)-pentazocine labeled sigma 1 binding sites exhibited similar pharmacological properties. The density of [3H](+)-pentazocine labeled sigma 1 population was found not to match that of [3H]DTG labeled sigma 1 site throughout the mouse central nervous system. The presence of low affinity [3H]DTG labeled sites was demonstrated in cold saturation experiments. Equilibrium binding data for the low affinity [3H]DTG binding site resulted in an increasing density (Bmax = 1973-11,369 fmol/mg protein) with a decreasing affinity (Kd = 242-943 nM) in mouse cortex through the spinal cord.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Kovács KJ,Larson AAdoi
10.1016/0014-2999(95)00383-vsubject
Has Abstractpub_date
1995-10-16 00:00:00pages
127-34issue
2eissn
0014-2999issn
1879-0712pii
0014-2999(95)00383-Vjournal_volume
285pub_type
杂志文章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::Increasing costs, much time consumption and high risk of failure associated with the process of de novo development of new anticancer drugs have prompted the pharmaceutical industry to seek alternative strategies that may facilitate and accelerate the whole process. In particular, the repurposing strategy, known also ...
journal_title:European journal of pharmacology
pub_type: 杂志文章,评审
doi:10.1016/j.ejphar.2019.172784
更新日期:2020-01-05 00:00:00
abstract::N-Phthaloyl gamma-aminobutyric acid, a new gamma-aminobutyric acid derivative synthesized in this laboratory, has been found to possess anticonvulsant, antinociceptive and antistress activities. Effects of this derivative on gastric lesions induced by aspirin and ethanol were studied in rats. N-Phthaloyl gamma-aminobu...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(92)90298-i
更新日期:1992-08-25 00:00:00
abstract::The highly toxic monomer 12-deoxyphorbol 13-palmitate (G) was extracted from the roots of Euphorbia fischeriana. Our experimental data confirmed studies showing that 12-deoxyphorbol 13-palmitate had certain antitumor activities. The MTT method, soft agar experiments, and nude mouse tumor experiments proved that 12-deo...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2012.11.015
更新日期:2013-01-30 00:00:00
abstract::Spinal 5-HT1A receptor subtypes are involved in regulation of nociception. This study was performed to investigate the effect of stimulation of these receptors on wide dynamic range neurones in the spinal cord. Extracellular single unit recordings of dorsal horn neurones were performed in intact urethane-anaesthetized...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/s0014-2999(96)00819-9
更新日期:1996-12-30 00:00:00
abstract::We have previously shown that, in porcine aortic smooth muscle cells, endoplasmic reticulum (ER) stressor thapsigargin simultaneously activate the mitochondrial caspase-dependent death cascade and an extracellular signal-regulated kinase (ERK)-dependent pathway, which inhibits the caspase-independent death pathway. Ou...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2012.04.015
更新日期:2012-07-05 00:00:00
abstract::The kappa-opioid receptor agonist, U50,488H (trans-(+-)-3,4-dichloro-N-methyl-[2-(1-pyrrolidinyl)-cyclohexyl]- benzeneacetamide), has recently been reported to induce dystonia after s.c. administration of 5-10 mg/kg in guinea pigs. The dystonic movements observed in response to U50,488H resembled those previously repo...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(93)90600-m
更新日期:1993-05-19 00:00:00
abstract::The anxiogenic activity of N-methyl-beta-carboline-3-carboxamide (FG 7142) is sometimes difficult to observe in rats. As the open field has recently been applied successfully to test the anxiogenic potential of n-butyl-beta-carboline-3-carboxylate (beta-CCB) in mice, a comparable experiment was performed with FG 7142 ...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(91)90685-j
更新日期:1991-07-23 00:00:00
abstract::The alpha(2)-adrenoceptor agonist, clonidine, modulates colorectal sensorimotor functions in humans and, given intrathecally, has analgesic effects in the colorectal distension (CRD) model in rats. We tested the effects of systemic clonidine on the visceral pain-related viscerosomatic and autonomic cardiovascular resp...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2008.06.056
更新日期:2008-09-04 00:00:00
abstract::The effects of nicotine, carbachol, hexamethonium and scopolamine were investigated on distress vocalizations (DBs) of acutely isolated domestic chicks. Nicotine attenuated, while the antimuscarinic scopolamine increased the frequency of separation-induced DVs. Furthermore, the stress attenuating effects of nicotine w...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(81)90283-1
更新日期:1981-06-19 00:00:00
abstract::We investigated the effects of beta-estradiol, dehydroepiandrosterone and dehydroepiandrosterone sulfate on intracellular calcium concentration ([Ca(2+)](i)) increases induced by gamma-aminobutyric acid (GABA), high K(+) and N-methyl-D-aspartate acid (NMDA) in cultured hippocampal neurons. Acute treatment with beta-es...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/s0014-2999(01)00880-9
更新日期:2001-03-30 00:00:00
abstract::The present study investigated the effects of acute and of chronic treatment with desipramine (DI) and citalopram (CT) on the alterations in rat behavior in the open field and in the forced swim tests produced by intra-hippocampal microinjections of noradrenaline (NA) and adrenoceptor agonists. Chronic but not acute t...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(85)90609-0
更新日期:1985-11-05 00:00:00
abstract::Nociceptin (orphanin FQ) is an endogenous agonist for the opioid receptor-like1 (ORL1) receptor. We investigated the effects of nociceptin on mean circulatory filling pressure, an index of venous tone. The effects of nociceptin (10, 30 nmol/kg, i.v.) and the vehicle (0.9% NaCl) on mean arterial pressure, heart rate an...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/s0014-2999(02)02617-1
更新日期:2002-11-29 00:00:00
abstract::Statins are the most common type of medicine used to treat hypercholesterolemia; however, they are associated with a low incidence of myotoxicity such as myopathy and rhabdomyolysis. The mechanisms for the adverse effects remain to be fully elucidated for safer chronic use and drug development. The results of our earl...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2011.10.044
更新日期:2012-01-15 00:00:00
abstract::The new platinum (II) and palladium (II) complexes (2-4) with ligands 5-(2-hydroxyphenyl)-1,3-dimethyl-4-(dimethoxy)phosphonyl-1H]-pyrazole (1a) and 5-(2-hydroxyphenyl)-1,3-dimethyl-4-methoxycarbonyl-1H]-2-pyrazole (1b) were screened in a search for novel anticancer agents. Thus, alkylating activity, cytotoxicity, abi...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2004.08.053
更新日期:2004-10-11 00:00:00
abstract::Perfused rabbit hearts removed 3H-5-hydroxytryptamine (3H-5-HT) from a perfusion solution containing 2.6 ng/ml and a tissue-to-medium ratio of about 10 was achieved after a 55 min perfusion period. 12.4 +/- 1.0% of the cardiac total radioactivity consisted of metabolites and metabolites appeared in the venous effluent...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(75)90291-5
更新日期:1975-06-01 00:00:00
abstract::Astragaloside IV (AS-IV) is one of the main active ingredients of Astragalus membranaceus. This study is aimed to investigate AS-IV׳s effects on Ca(2+) channel activity of single cardiomyocytes and single Ca(2+) channels. Whole-cell Ca(2+) currents in freshly dissociated cardiomyocytes were measured using the whole-ce...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2015.03.082
更新日期:2015-08-05 00:00:00
abstract::Eating high-fat chow can modify the effects of drugs acting directly or indirectly on dopamine systems and repeated intermittent drug administration can markedly increase sensitivity (i.e., sensitization) to the behavioral effects of indirect-acting dopamine receptor agonists (e.g., methamphetamine). This study examin...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2011.02.027
更新日期:2011-05-11 00:00:00
abstract::A series of tertiary amines structurally related to the potent muscarinic agent oxotremorine showed weak stimulant activity on the frog rectus abdominis preparation. The corresponding quaternary ammonium salts were more effective stimulants, the most potent being half as active as carbachol. The effects appeared to be...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(84)90239-5
更新日期:1984-03-23 00:00:00
abstract::Acute administration of fluoxetine (1, 10 and 20 mg/kg i.p.) increased extracellular levels of serotonin (5-hydroxytryptamine, 5-HT) in the frontal cortex, ventral hippocampus and raphe nuclei as measured by in vivo microdialysis in anaesthetized rats. In the frontal cortex, fluoxetine showed a marked dose-response ef...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(95)00573-4
更新日期:1995-11-14 00:00:00
abstract::Substance P and its tachykinin NK(1) receptors are highly expressed in brain regions involved in emotional control. We recently showed that NK(1)-mediated substance P neurotransmission is deeply involved in the control of aggressiveness. To get further insights into the NK(1) receptor/aggression relationship, we studi...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2009.03.050
更新日期:2009-06-02 00:00:00
abstract::The antifibrillatory and electrophysiologic actions of bepridil and butyl-methylenedioxyindene (BU-MDI), two intracellular calcium antagonists, were examined in anesthetized dogs. The administration of bepridil (1.0-10.0 mg/kg i.v.) significantly increased the electrical threshold for ventricular fibrillation determin...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(85)90107-4
更新日期:1985-04-23 00:00:00
abstract::The effects of treatment with anxiogenic or anxiolytic agents and exposure to acute restraint stress on emotional behavior in mice were examined using an automatic hole-board apparatus. Changes in the emotional state of mice were evaluated in terms of changes in exploratory activity, i.e., total locomotor activity, nu...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/s0014-2999(98)00223-4
更新日期:1998-05-29 00:00:00
abstract::The effects of the dopamine D2 receptor agonist quinpirole (LY 171555) on locomotor activity and margin time (thigmotaxis or wall-hugging) were measured for 2 h in rats injected either s.c. (vehicle, 0.02, 2.0 mg/kg) or directly into either the dorsal striatum or nucleus accumbens (vehicle, 0.1, 1.0, 10, 20 or 40 micr...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(92)90091-h
更新日期:1992-04-07 00:00:00
abstract::The purpose of this study was to investigate whether high conductance Ca2+-activated K+ channels (BK(Ca)) are mediating the vasodilator action of hydralazine. In isolated porcine coronary arteries, hydralazine (1-300 microM), like the K+ channel opener levcromakalim, preferentially relaxed contractions induced by K+ (...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/s0014-2999(98)00701-8
更新日期:1998-11-13 00:00:00
abstract::This study was designed to investigate the effects of serotonin on changes in intracellular Ca(2+) concentration ([Ca(2+)](i)) in cultured rat heart endothelial cells. Serotonin stimulated a biphasic change in cytosolic Ca(2+) of rat heart endothelial cells: an initial transient increase, which primarily reflects the ...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/s0014-2999(99)00672-x
更新日期:1999-11-12 00:00:00
abstract::Environments previously associated with drug use can become one of the most common factors triggering relapse to drug-seeking behavior. To better understand the neurochemical mechanisms potentially mediating these cues, we measured nucleus accumbens dopamine levels in animals exposed to environmental cues previously p...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/s0014-2999(01)00800-7
更新日期:2001-03-02 00:00:00
abstract::The aim of the present study was to find out the mechanism by which the inflammatory mediator, bradykinin, induces an increase of the cytosolic Ca(2+) concentration ([Ca(2+)](i)) in enteric neurons. For this purpose, ganglia in the isolated submucosa from rat colon were loaded with the Ca(2+)-sensitive dye, fura-2, an...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2012.02.001
更新日期:2012-04-15 00:00:00
abstract::Human adipose tissue-derived stromal cells (hADSCs) demonstrate promising potential in various clinical applications, including the transplantation to regenerate injured or degenerative tissues. The migration of engrafted hADSCs to the correct site of injure is essential for the curative effect of stem cell therapy. W...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2008.09.030
更新日期:2008-12-03 00:00:00
abstract::The involvement of dopamine receptors in the amnesic effects of the endogenous micro-opioid receptor agonists endomorphins 1 and 2 was investigated by observing step-down type passive avoidance learning in mice. Although the dopamine D1 receptor agonist R(+)-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepine-7,8-diol hydroc...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/s0014-2999(02)01760-0
更新日期:2002-06-20 00:00:00