Abstract:
:Saturable, high-affinity binding sites for [3H]saxitoxin were identified in equine portal vein smooth muscle membranes. These sites had a dissociation constant of 0.29 nM and a maximal binding capacity of 115 fmol.mg-1 of protein. A similar dissociation constant was obtained with cells prepared from rat portal vein. Specific binding of [3H]saxitoxin was completely displaced by unlabelled saxitoxin and tetrodotoxin, with inhibition constants of 0.42 and 2.10 nM, respectively. Tetrodotoxin blocked the fast Na+ current in single cells of rat portal vein in a concentration-dependent manner, with an IC50 of 3.15 nM. These results suggest that the high-affinity binding sites for tetrodotoxin and saxitoxin may be associated with voltage-dependent Na+ channels in vascular myocytes.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Mironneau J,Martin C,Arnaudeau S,Jmari K,Rakotoarisoa L,Sayet I,Mironneau Cdoi
10.1016/0014-2999(90)90624-fsubject
Has Abstractpub_date
1990-08-10 00:00:00pages
315-9issue
2-3eissn
0014-2999issn
1879-0712pii
0014-2999(90)90624-Fjournal_volume
184pub_type
杂志文章abstract::Activation of serotonergic 5-HT3 receptors by its selective agonist 2-methyl serotonin (2-Me-5-HT) induces vomiting, which is sensitive to selective antagonists of both 5-HT3 receptors (palonosetron) and L-type calcium channels (LTCC) (amlodipine or nifedipine). Previously we demonstrated that 5-HT3 receptor activatio...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2015.02.042
更新日期:2015-05-15 00:00:00
abstract::In isolated rat aorta, endothelin-1 induced contractions at lower concentrations than endothelin-3. The contractile effects were augmented by removing the endothelium. In contrast, endothelium-1 and endothelin-3 at similar concentrations induced endothelium-dependent relaxation in norepinephrine-stimulated aorta. IRL ...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(93)90112-u
更新日期:1993-02-16 00:00:00
abstract::Glucocorticoids bind to and activate a cytoplasmic glucocorticoid receptor. The activated glucocorticoid receptor translocates into the nucleus and binds to specific response elements in the promoter regions of anti-inflammatory genes such as lipocortin-1 and secretory leukocyte protease inhibitor (SLPI). However, the...
journal_title:European journal of pharmacology
pub_type: 杂志文章,评审
doi:10.1016/j.ejphar.2004.07.011
更新日期:2004-10-01 00:00:00
abstract::In anaesthetised guinea-pigs, bronchoconstriction induced by vagal nerve stimulation was potentiated by low doses of the antimuscarinic bronchodilator drug, ipratropium (0.01-1.0 microgram/kg); the maximum effect was obtained with 1.0 microgram/kg which doubled the bronchoconstriction. When the dose was increased abov...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(87)90251-2
更新日期:1987-07-09 00:00:00
abstract::We have analyzed the effect of quinolizidine alkaloids from Lupinus species upon insulin secretion. Isolated normal rat islets were incubated with 3.3, 8.3, and 16.7 mM glucose, in the presence or absence of different concentrations of lupanine (0.05, 0.5, and 1.0 mM), 13-alpha-OH lupanine, 17-oxo-lupanine, and 2-thio...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2004.09.008
更新日期:2004-11-03 00:00:00
abstract::The pharmacology of cannabidiol, the non-psychoactive major component of Cannabis sativa, is of growing interest as it becomes more widely prescribed. This study aimed to examine the effects of cannabidiol on a wide range of contractile agents in rat small resistance arteries, in comparison with large arteries, and to...
journal_title:European journal of pharmacology
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doi:10.1016/j.ejphar.2020.173767
更新日期:2021-01-15 00:00:00
abstract::A high dose of apomorphine, a stimulator of brain dopamine receptors, caused a reduction in total sleep, intermediate sleep and a delayed appearance of paradoxical sleep. With a lower dose, a small and not significant trend toward an increase of paradoxical sleep was observed. Spiroperidol, considered as a specific bl...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(76)90340-x
更新日期:1976-08-01 00:00:00
abstract::Recent studies suggest that endocannabinoid signaling is modulated by 17β-estradiol (17Eβ) however it is unclear if this applies to the cardiovascular actions of anandamide, a major endocannabinoid. This study examined the in vitro effects of 17Eβ on vasorelaxation to anandamide in myograph-mounted small mesenteric ar...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2013.01.002
更新日期:2013-02-15 00:00:00
abstract::SR 57746A, 4-(3-trifluoromethylphenyl)-N-[2-(naphth-2-yl)ethyl]-1,2,3,6- tetrahydropyridine HCl, was studied for its specific 5-HT1A receptor agonist action and antidepressant-like effects in the rat. The compound showed a high affinity for 5-HT1A specific binding sites in the rat hippocampus (IC50 3 nM), moderate aff...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(94)90768-4
更新日期:1994-02-21 00:00:00
abstract::The spontaneous and electrically evoked activity was examined in guinea-pig, ferret and marmoset urinary bladder. Electrical field stimulation of detrusor strips in vitro induced a rapid, frequency-dependent contraction with a maximum response at 40 Hz. This contraction was partly decreased by either atropine (0.29 mi...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(85)90375-9
更新日期:1985-08-27 00:00:00
abstract::Depression is very common in asthmatic patients and may increases risk for morbidity and mortality. The present work aimed to investigate the protective effect of fluoxetine, on behavioral and biochemical changes, associated with ovalbumin (OVA) - induced bronchial asthma and depression in rats. Rats were sensitized w...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2018.08.026
更新日期:2018-10-15 00:00:00
abstract::A decrease of 30% was observed in the density of peripheral-type benzodiazepine binding sites in platelets of nine schizophrenics maintained on chronic neuroleptic treatment as compared to platelets of six untreated schizophrenics and 15 healthy volunteers. The equilibrium dissociation constant for binding by [3H]PK 1...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(86)90500-5
更新日期:1986-02-18 00:00:00
abstract::The hypotensive activity of a series of calcium entry blockers and various other vasodilators was quantified in pentobarbitone-anesthetized rats. Hypotensive activity was correlated linearly with the potency of these vasoactive agents to depress alpha 2-adrenoceptor-induced pressor responses in pithed rats. However, v...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(83)90104-8
更新日期:1983-08-19 00:00:00
abstract::In male Swiss mice, muscimol produced myoclonic jerks. A 3 mg/kg (i.p.) dose induced this response in all of the mice tested and the peak response of 73 jerks per min was observed between 27 and 45 min. Increasing the brain serotonin levels by the administration of 5-hydroxytryptophan (80-160 mg/kg) in combination wit...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(81)90087-x
更新日期:1981-07-17 00:00:00
abstract::Several antimalarial drugs are known to produce a QT interval prolongation via a blockade of the rapidly activating delayed rectifier K+ current (IKr), encoded by the human-ether-a-go-go-related gene (hERG). We investigated the influence of lumefantrine and its major metabolite desbutyl-lumefantrine, as well as halofa...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2003.11.003
更新日期:2004-01-19 00:00:00
abstract::Phencyclidine and its derivatives bind specifically and reversibly to rat brain and peripheral organs. Binding characteristics are different in brain, lung, kidney, heart and liver. Affinities of phencyclidines for the brain receptor but not those for peripheral organs are correlated with the pharmacological activitie...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(80)90065-5
更新日期:1980-11-07 00:00:00
abstract::Cancer remains a major public health problem worldwide and was responsible for 9.6 million deaths in 2018. Oncologic treatments such as doxorubicin (Dox) and trastuzumab (Trz) are chemotherapeutic drugs used to treat several types of cancer, including solid and non-solid malignancies. Although these drugs have a signi...
journal_title:European journal of pharmacology
pub_type: 杂志文章,评审
doi:10.1016/j.ejphar.2019.172818
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abstract::Type 2 diabetes mellitus (T2DM) is one of the risk factors for Parkinson's disease (PD). Insulin desensitisation has been observed in the brains of patients, which may promote neurodegeneration. Incretins are a family of growth factors that can re-sensitise insulin signalling. We have previously shown that mimetics of...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2017.06.029
更新日期:2017-10-05 00:00:00
abstract::Using the ex vivo chick embryo retina to study the efficacy of antagonists in blocking the excitotoxic effects of excitatory amino acid agonists, we previously identified phencyclidine as the most powerful known anti-excitotoxin. Here we show that MK-801 is 5 times more powerful than phencyclidine as an anti-excitotox...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(87)90552-8
更新日期:1987-09-23 00:00:00
abstract::Toll-like receptors (TLRs) play an important role in the recognition of microbial pathogens and induce innate immune responses. The recognition of microbial components by TLRs triggers the activation of myeloid differential factor 88 (MyD88)- and toll-interleukin-1 receptor domain-containing adapter inducing interfero...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2013.09.045
更新日期:2013-12-05 00:00:00
abstract::The effects of morphine tolerance-dependence and abstinence on 5-HT1A receptors in brain regions and spinal cord of the rat were determined. Tolerance to and physical dependence on morphine was induced in male Sprague-Dawley rats by implanting six morphine pellets (each containing 75 mg of morphine free base) during a...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(90)90284-d
更新日期:1990-07-03 00:00:00
abstract::Although initial resuscitation from cardiac arrest (CA) has increased over the past years, long term survival rates remain dismal. Epinephrine is the vasopressor of choice in the treatment of CA. However, its efficacy has been questioned, as it has no apparent benefits for long-term survival or favorable neurologic out...
journal_title:European journal of pharmacology
pub_type: 杂志文章,评审
doi:10.1016/j.ejphar.2014.06.024
更新日期:2014-10-05 00:00:00
abstract::We investigated the inhibitory effects of 1 mM of the inorganic cations, La3+, Cd2+, Mn2+, Ni2+ and Co2+ on contractions induced by K+ (100 mM) and 5-hydroxytryptamine (5-HT, 10(-5) M) in the isolated rat jugular vein and on contractions induced by K+ (100 mM), 5-HT (10(-5] and noradrenaline (NA, 10(-5) M) in the rat ...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(90)90634-i
更新日期:1990-08-28 00:00:00
abstract::Sensitization to the discriminative stimulus effects of psychostimulants is not fully understood. Therefore, the present study was designed to investigate the development of sensitization to the discriminative stimulus of methamphetamine in rats. A dose-response curve for methamphetamine and a generalization test for ...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2004.07.064
更新日期:2004-09-13 00:00:00
abstract::The present work is aimed at evaluating the protective effect of eugenol against in vitro nicotine-induced toxicity in murine peritoneal macrophages, compared with N-acetylcysteine. Eugenol was isolated from Ocimum gratissimum and characterized by HPLC, FTIR, (1)H NMR. To establish most effective protective support, w...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2009.09.019
更新日期:2009-11-25 00:00:00
abstract::In the brain, various neurotransmitters such as noradrenaline and GABA regulate peripheral sympathetic functions. Previously, it has been reported that both β-adrenoceptor activation and GABAB receptor activation in the brain are involved in the elevation of plasma noradrenaline levels. However, it is unknown whether ...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2019.01.029
更新日期:2019-04-05 00:00:00
abstract::The effects of serotonin (5-HT) on a beta-adrenergic response were studied, using the voltage clamp technique, in Xenopus laevis oocytes surrounded by their follicular cells. noradrenaline induced marked hyperpolarization, with a specific increase in the permeability of the membrane toward K+. Application of 10 microM...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(93)90901-s
更新日期:1993-08-24 00:00:00
abstract::The structure-activity relationships of 35 novel derivatives of 2-(carboxypropyl)-3-amino-4-methyl-6-phenyl pyridazine (SR 95103) were examined as gamma-aminobutyric acid (GABA) antagonists in the flap preparation of the parasitic nematode, Ascaris suum, using a two-microelectrode current-clamp technique. All but one ...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(94)00778-6
更新日期:1995-03-24 00:00:00
abstract::Restraint for 1 h induced significant antinociceptive activity, as assessed by the hot plate test, in female mice. The antinociceptive activity was significant throughout the 1 h period of observation starting immediately after restraint. Prior administration of the histamine H2 receptor agonist dimaprit (1.5-6.0 mg/k...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(95)00129-9
更新日期:1995-06-12 00:00:00
abstract::Local anesthetics bind to dopamine transporters and inhibit dopamine uptake in rodent brain. Additionally, local anesthetics are self-administered in rhesus monkeys. The present study determined binding affinities of cocaine and five local anesthetics at dopamine transporters in rhesus monkey brain, and compared bindi...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/s0014-2999(98)00967-4
更新日期:1999-02-19 00:00:00