Abstract：
:alpha 2-adrenoceptor-mediated contractions of the rabbit saphenous vein were previously found to be inhibited by wortmannin, a protein kinase inhibitor which blocks receptor-dependent phospholipase D activation. Since other studies have indicated that receptor-dependent phospholipase D activation required activity of a tyrosine kinase, we examined the influence of several tyrosine kinase inhibitors on both alpha 2-adrenoceptor-mediated contractions of rabbit saphenous vein and alpha 1-adrenoceptor-mediated contractions of rabbit aorta. Methyl 2,5-dihydroxycinnamate, genistein and erbstatin each caused non-competitive inhibition of rabbit saphenous vein contractions elicited by the alpha 2-adrenoceptor-selective agonist 5-bromo-6-[2-imidazolin-2-yl-amino]-quinoxaline (UK14304), yielding complete inhibition at 100 microM and IC50 values of 15, 35 and 40 microM respectively. By contrast, phenylephrine-induced dose-response curves in rabbit aorta were largely unaffected by tyrosine kinase inhibitors at 50 microM. In a separate analysis of intracellular Ca(2+)-dependent and extracellular Ca(2+)-dependent alpha 1-adrenoceptor responses of rabbit aorta, genistein (50 microM) did partially reduce the initial intracellular Ca(2+)-dependent response, but did not reduce maximal response. Methyl 2,5-dihydroxycinnamate (25 microM) had no effect on intracellular or extracellular Ca2+ responses in rabbit aorta. High K(+)-induced contractions of both rabbit saphenous vein and aorta were unaffected by up to 100 microM of the tyrosine kinase inhibitors. These results indicate an obligatory requirement for tyrosine kinase activity in alpha 2-adrenoceptor-mediated but not alpha 1-adrenoceptor-mediated vasoconstriction.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Jinsi A,Deth RCdoi
10.1016/0014-2999(95)00053-nsubject
Has Abstractpub_date
1995-04-13 00:00:00pages
29-34issue
1eissn
0014-2999issn
1879-0712pii
001429999500053Njournal_volume
277pub_type
杂志文章abstract：:The functional role of metabotropic glutamate (mGlu) receptors in the rat dentate gyrus was investigated. By using extracellular recording techniques in slices, it was found that the depression induced by the mGlu receptor agonist (1S,3R)-1-amino-cyclopentane-1,3-dicarboxylate (ACPD) was mediated through the mGlu grou...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(95)00560-9
更新日期：1995-12-29 00:00:00
abstract：:Kinins are known to be potent releasers of histamine. In the present study, the B2 antagonist analogues of bradykinin (BK) and kallidin (KD): [( Thi6,9,D-Phe8]KD, [Thi5,8,D-Phe7]BK) were also found to be potent releasers of histamine from rat mast cells and not to exert any antagonistic effect. Similarly, two B1 recep...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(88)90051-9
更新日期：1988-04-27 00:00:00
abstract：:Drugs belonging to different chemical classes having the ability to improve behavioral performance in animal learning and memory tests may share the common ability to stimulate protein kinase C activity in rat brain cortex. In vitro acetyl-L-carnitine (100 nM) promoted in rat brain cortex slices a significant increase...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(94)90216-x
更新日期：1994-11-14 00:00:00
abstract：:The purpose of this study was to delineate the distribution of beta-adrenoceptor density in the cat heart, with an emphasis on areas within the left ventricle. beta-Adrenoceptor densities, determined for hearts obtained from five cats, were not significantly different in the left and rights atria, i.e. 47.6 +/- 7.2 an...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(86)90189-5
更新日期：1986-10-14 00:00:00
abstract：:Opiates depress the potassium-induced efflux of [3H]noradrenaline from the mouse vas deferens in a concentration-dependent (the IC50 for normorphine was 1.5 microM), stereospecific and naloxone-reversible manner. As the concentration of sodium in the extracellular fluid was reduced, the inhibitory action of opiates wa...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(81)90354-x
更新日期：1981-04-09 00:00:00
abstract：:7-Nitroindazole (a selective neuronal nitric oxide (NO) synthase inhibitor) at 25 and 50 mg/kg, 30 min before the test, did not influence the electroconvulsive threshold. However, at 50 mg/kg, it enhanced the anticonvulsive activity of phenobarbital against maximal electroshock and did not affect that of carbamazepine...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(97)01034-0
更新日期：1997-07-23 00:00:00
abstract：:Disturbances in oxidative metabolism are involved in many acute and chronic diseases, as well as in several other conditions. The objective of the present study was to examine the relationship between the level of intracellular reactive oxygen species in the peripheral blood granulocytes of mice, as evaluated by 2',7'...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2009.11.001
更新日期：2010-02-10 00:00:00
abstract：:The ability of flunarizine to terminate ouabain-induced ventricular tachycardia was investigated in conscious dogs. These arrhythmias result from triggered activity based on delayed afterdepolarizations. Sustained ventricular tachycardia was induced by ouabain (48 +/- 6 micrograms/kg) and pacing in 13 animals with sur...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(89)90780-2
更新日期：1989-06-08 00:00:00
abstract：:Chemopreventive non-steroidal anti-inflammatory drugs (NSAIDs) exhibit diverse pharmacological and biological activities mainly through their inhibitory effect on cyclooxygenase (COX). However, COX-independent mechanisms involving kinase inhibition have been proposed to explain certain therapeutic effects of NSAIDs. H...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2010.04.012
更新日期：2010-07-25 00:00:00
abstract：:Cerebral ischemia/reperfusion (I/R) is a lethal and disabling disease. Studies have suggested that hyperglycemia is a risk factor for cerebral I/R. Baicalin is a natural bioactive flavonoid extracted from Scutellaria baicalensis Georgi with neuroprotective activity. In the present study, we investigated the effects of...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2017.07.041
更新日期：2017-11-15 00:00:00
abstract：:The polyphenolic flavonoid silymarin that is the milk thistle extract has been found to possess an anti-cancer effect against various human epithelial cancers. In this study, to explore the regulative effect of silymarin on human ovarian cancer line A2780s and PA-1 cells, 3-[4, 5-dimethylthiazol-2-yl]-2, 5-diphenyltet...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2014.09.019
更新日期：2014-11-15 00:00:00
abstract：:The aims of the present study were to establish whether vasoactive intestinal polypeptide (VIP) could mobilize internally-stored Ca2+ and whether Ca2+ release could trigger Ca2+ influx from the extracellular space. Bovine pulmonary artery endothelial cells from an established cell line were loaded with fura-2/AM and c...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(97)01315-0
更新日期：1997-11-27 00:00:00
abstract：:The effects of angiotensin I-converting enzyme (ACE) inhibitors and bradykinin (BK) on prostacyclin (PGI2) production in isolated arterial tissue were investigated. Rings of rat abdominal aorta were incubated in Krebs-Ringer bicarbonate buffer and PGI2 generation was assessed by the determination of its stable hydroly...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(90)94795-y
更新日期：1990-03-13 00:00:00
abstract：:The effects of drugs that inhibit human ether-a-go-go-related gene (HERG) related cardiac potassium channels on the variability of QT duration as a sign of repolarisation instability were evaluated in conscious telemetered dogs. QT duration variability was determined using a beat-to-beat analysis before and after the ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2005.01.042
更新日期：2005-04-04 00:00:00
abstract：:The site of action of the kappa opioid receptor agonist, U-50,488H in suppressing the development of tolerance to morphine antinociception was examined by local application, either intrathecal (i.t., spinal) or intracerebroventricular (i.c.v., supraspinal) in mice. Mice given morphine s.c., i.c.v. or i.t. daily develo...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(91)90585-e
更新日期：1991-08-06 00:00:00
abstract：:The role of pertussis toxin-sensitive G proteins on the alpha 2-adrenoceptor and mu-opioid receptor-mediated inhibition of the efferent function of capsaicin-sensitive neurones was investigated in guinea-pig atria pretreated with guanethidine. In the presence of atropine, CGP 20712A (2-hydroxy-5-(2-[hydroxy-3-(4-[(1-m...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(92)90444-9
更新日期：1992-06-17 00:00:00
abstract：:Animal studies have shown that endogenous estrogens such as 17β-estradiol (E2) can modulate lipid profiles in vivo, and this effect is generally thought to be mediated by the estrogen receptors (ERs). The present study sought to test a hypothesis that some of the endogenous estrogen metabolites that have very weak est...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2017.02.032
更新日期：2017-04-05 00:00:00
abstract：:Rats were injected with 15 mg/kg (i.p.) mianserin or vehicle (saline) for 4, 10 or 21 days and 5-HT2 receptor binding and mRNA levels measured. Treatment with mianserin induced a substantial decrease in 5-HT2 radioligand binding (44-59% decrease; P less than 0.05 vs. control). No changes in the amount of 5-HT2 or, as ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0922-4106(91)90093-w
更新日期：1991-06-19 00:00:00
abstract：:Infusion of arachidonic acid through the guinea pig lung or the cat spleen causes a release of thromboxane A2 and prostaglandins, as measured by bioassay. After incubation of human platelets with arachidonate similar metabolites are formed, as demonstrated chromatographically. Infusion of imidazole (50-75 microgram/ml...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(77)90104-2
更新日期：1977-07-15 00:00:00
abstract：:Captivity-induced stereotypies in bank voles (Clethrionomys glareolus) were inhibited at the age of 1, 2, 4, 6, 8 and 10 months by 0.2 mg/kg haloperidol s.c., while 35 mg/kg naloxone s.c. only inhibited them at the age of 4-6 months. Other activities were not significantly inhibited. The change in the naloxone effect ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(88)90583-3
更新日期：1988-08-09 00:00:00
abstract：:We investigated the effects of 1-amino-5-bromouracil on the benzodiazepine-gamma-aminobutyric acid (GABA)A receptor complex to elucidate its central action. 1-Amino-5-bromouracil neither displaced nor enhanced [3H]muscimol, [35S]t-butylbicyclophosphorothionate (TBPS), or [3H]dehydroepiandrosterone sulfate binding to t...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(94)90278-x
更新日期：1994-12-12 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：:Administration of the 5-HT1C/5-HT2 receptor agonist 1-(2,5-dimethoxy-4- iodophenyl)-2-aminopropane (DOI, 0.125-2.0 mg/kg i.v.) triggered dose-dependent increases in plasma glucose; plasma insulin levels remained unchanged. Pretreatment with the 5-HT1C/5-HT2 receptor antagonists LY 53857, ritanserin, or the mixed 5-HT2...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(90)90370-l
更新日期：1990-10-23 00:00:00
abstract：:An intricate surveillance network consisting of enteroendocrine cells, immune cells and sensory nerve fibres monitors the luminal and interstitial environment in the alimentary canal. Functional bowel disorders are characterized by persistent alterations in digestive regulation and gastrointestinal discomfort and pain...
journal_title：European journal of pharmacology
pub_type： 杂志文章,评审
doi：10.1016/s0014-2999(01)01319-x
更新日期：2001-10-19 00:00:00
abstract：:We examined the effects of mammalian tachykinins on human bronchial secretion in vitro using fucose as an endogenous marker for mucus. Substance P (SP, 10(-9)-10(-5) M) increased secretion in a dose-related manner and was more potent than neurokinin A or neurokinin B. The enkephalinase (endopeptidase 24.11) inhibitor ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(89)90322-1
更新日期：1989-12-19 00:00:00
abstract：:Our recent study has shown that the intracerebroventricular administration of d-serine, an endogenous and selective agonist for the glycine site of the N-methyl-d-aspartate receptor, alone or in combination with morphine, leads to the potentiation of antinociception on the tail-flick response. Although there is a vari...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2008.02.068
更新日期：2008-05-31 00:00:00
abstract：:The effect of furosemide on carbohydrate metabolism was studied in ob/ob mice. Intraperitoneal injection of a single dose of furosemide (200 mg/kg body weight) into fasted mice resulted in acute hyperglycaemia and two days after such a single dose, the mice showed fasting hyperglycaemia and glucose intolerance. Pancre...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(88)90175-6
更新日期：1988-03-15 00:00:00
abstract：:Seroma formation is one of the most common complications following breast cancer surgery. It may lead to delay of adjuvant therapies and increasement of therapy costs. Bleomycin sulfate is a sclerosing antibiotic with antineoplastic efficacy. It is locally used in the treatment of pleural effusion. The present study a...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2013.10.067
更新日期：2014-01-15 00:00:00
abstract：:The present paper describes the effect of beta-phenylethylamine and its metabolites phenylethanolamine, tyramine, acetyl-phenylethylamine and phenylacetaldehyde on the dopaminergic nigrostriatal system. The rotational behavioural response to the i.v. injection of these drugs was quantified in animals with a unilateral...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(95)00757-1
更新日期：1996-02-22 00:00:00
abstract：:Apomorphine-induced locomotor stimulation was investigated in the developing rat following injection with 6-hydroxydopa at birth. Treatment with 6-hydroxydopa potentiated locomotor responsiveness to apomorphine in the 20-day-old rat. The 6-hydroxydopa-treated animal at 30 days, however, was less sensitive to the drug ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(78)90012-2
更新日期：1978-07-15 00:00:00
