Abstract：
:Clonidine and methysergide constrict the rabbit auricular artery by activating smooth muscle alpha-adrenoceptors. Clonidine inhibits and methysergide enhances responses to stimulation of the sympathetic nerves. Both drugs sensitise the artery to a variety of vasoconstrictor stimuli, although not to potassium chloride. This weak generalised sensitisation may depend on clonidine and methysergide themselves being vasoconstrictor since sensitisation after clonidine did not occur when vasoconstriction was abolished with phentolamine. The marked potentiation of 5-HT and tryptamine observed during clonidine perfusion may reflect a property of the tryptamines since it was observed during perfusion with histamine but not when histamine vasoconstriction was abolished with mepyramine. Cyproheptadine and pizotifen neither constrict the artery nor sensitise it to vasoconstrictor agents. They inhibit responses to nerve stimulation, alpha-adrenoceptor agonists, potassium chloride and particularly histamine. Sensitisation of blood vessels reinforced by direct vasoconstriction may contribute to the mechanism of action of clonidine and methysergide in migraine. Conversely, alterations in vascular function may be less important to the antimigraine actions of either cyproheptadine or pizotifen.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Fozard JRdoi
10.1016/0014-2999(76)90264-8keywords:
subject
Has Abstractpub_date
1976-03-01 00:00:00pages
127-139issue
1eissn
0014-2999issn
1879-0712pii
0014-2999(76)90264-8journal_volume
36pub_type
杂志文章abstract：:Many studies have demonstrated that cyclophosphamide (CPA) can affect hepatic cytochrome p450 (CYP) isoenzyme activity in animals. We have investigated the effect of CPA on gene expression of various CYP enzymes as well as beta-actin in the human acute promyelocytic leukemia cell line (HL-60S) and its multidrug-resist...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(02)01995-7
更新日期：2002-08-09 00:00:00
abstract：:To determine if an Ag(+)-induced contracture is associated with the Ca(2+)-induced Ca2+ release mechanism in the sarcoplasmic reticulum, effects of Ca(2+)-induced Ca2+ release modulators on the Ag(+)-induced contracture were studied with single fibers of frog toe skeletal muscle. The fiber treated with 1 mM caffeine c...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0926-6917(95)90036-5
更新日期：1995-03-16 00:00:00
abstract：:Sphingosine-1-phosphate (S1P) is a bioactive sphingolipid that contracts most smooth muscles. Although S1P has been shown to contract bladder smooth muscle, the mechanism(s) by which S1P initiates contraction has not been extensively investigated. The goal of this study was to determine if S1P-induced force generation...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2013.10.004
更新日期：2013-11-15 00:00:00
abstract：:We investigated the effects of three bile acids conjugated with N-acetylglucosamine, ursodeoxycholate N-acetylglucosaminide, tauroursodeoxycholate N-acetylglucosaminide and glycoursodeoxycholate N-acetylglucosaminide, on bile flow and biliary excretion of various markers in comparison with ursodeoxycholic acid, taurou...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(98)00725-0
更新日期：1998-12-11 00:00:00
abstract：:Stearoyl-CoA Desaturase 1 (SCD1) is a central enzyme that catalyzes the biosynthesis of monounsaturated fatty acids from saturated fatty acids. SCD1 is an emerging target in obesity and insulin resistance due to the improved metabolic profile obtained when the enzyme is genetically inactivated. Here, we have investiga...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2009.07.004
更新日期：2009-09-15 00:00:00
abstract：:Arteries were isolated from male DBA/2 mice and mounted on a small vessel wire myograph for isometric recording. Responses to exogenous noradrenaline were inhibited with high affinity by prazosin (pKB, 9.3) and 5-methyl-urapidil (pKB, 9.2) and with low affinity by 8-[2-[4-(2-methoxyphenyl)-1 piperazinyl]ethyl]-8-azasp...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2004.09.046
更新日期：2004-10-25 00:00:00
abstract：:5-HT and dopamine receptor antagonists have become widely used as atypical antipsychotics. Although 5-HT(2A) receptor antagonistic activity is thought to contribute to the atypical aspects of these agents, the precise mechanism remains unknown. M100907 (R(+)-alpha(2,3-dimethoxyphenyl)-1-[2(4-fluorophenyl)ethyl)]-4-pip...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(01)00926-8
更新日期：2001-04-13 00:00:00
abstract：:Endoplasmic reticulum (ER) stress and associated protein aggregation are closely associated with human diseases, including alterations in hepatic lipid metabolism. Inhibition of ER stress can have a significant effect on the prevention of hepatic dyslipidemia. Here, we studied the role of 4-phenylbutyric acid (4-PBA),...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2016.02.068
更新日期：2016-04-15 00:00:00
abstract：:Corticotropin-releasing factor (CRF) plays a major role at the level of the hypothalamus and pituitary to control the body's response mechanisms to stressful stimuli. The recent discovery of CRF outside the central nervous system suggests that CRF may well play a similar role in peripheral tissues, most likely in a pa...
journal_title：European journal of pharmacology
pub_type： 杂志文章,评审
doi：10.1016/s0014-2999(97)00057-5
更新日期：1997-03-26 00:00:00
abstract：:The prophylactic effect of serotonin uptake inhibitors, imipramine and fluoxetine, against motion sickness was investigated in Suncus murinus. Imipramine (s.c.) and fluoxetine (i.p.) inhibited motion-induced emesis dose dependently with ID50 values of 1.7 and 26 mg/kg, respectively. The results suggest that increasing...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(96)00407-4
更新日期：1996-08-01 00:00:00
abstract：:Crocetin, an aglycone of crocin, is found both in the saffron crocus (Crocus starus L.) and in gardenia fruit (Gardenia jasminoides Ellis). We evaluated the protective effects of crocetin against the retinal ischemia induced by 5h unilateral ligation of both the pterygopalatine artery (PPA) and the external carotid ar...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2013.02.007
更新日期：2013-03-05 00:00:00
abstract：:MPTP (1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine) destroys dopamine-containing nigrostriatal neurons and increases the apparent Bmax of both D1 and D2 binding sites in the striatum. However, the changes of Bmax occur at different intervals after the lesion. Up-regulation of D2 sites becomes evident about 3 weeks aft...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(90)90324-y
更新日期：1990-05-16 00:00:00
abstract：:The histamine H2-receptor antagonist cimetidine potently inhibited [3H]muscimol and enhanced [3H]flunitrazepam binding in membranes prepared from several brain regions in the rat, including the dorsal raphe nucleus. As further examined in cortical membranes, this effect on both GABA and benzodiazepine binding sites wa...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(83)90011-0
更新日期：1983-03-25 00:00:00
abstract：:The effect of prostacyclin (PGI2, 0.5 nmol . kg-1 . min-1,i.v.) on myocardial metabolism was studied in cats subjected to 5 h of myocardial ischemia (MI) and compared to vehicle-treated MI cats. MI was followed by a 52% decrease in ATP and a concomitant increase (2-3 fold) in lactate and lactate/pyruvate ratio in the ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(81)90454-4
更新日期：1981-02-19 00:00:00
abstract：:The goals of the present study were: (1) to investigate the binding properties of (R)- and (S)-procyclidine and two achiral derivatives of muscarinic M1, M2 and M4 receptor subtypes and (2) to identify the interactions which allow these receptors to discriminate between the two stereoisomers. (R)-Procyclidine showed a...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0922-4106(90)90017-r
更新日期：1990-09-18 00:00:00
abstract：:The effects of P2Y receptor agonists on smooth muscle membrane potential in isolated ring segments of rat mesenteric artery were examined by intracellular microelectrodes. In the presence of inhibitors of nitric oxide-synthase and cyclo-oxygenase, the selective P2Y1 receptor agonist adenosine 5'-O-thiodiphosphate (ADP...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(98)00848-6
更新日期：1999-01-08 00:00:00
abstract：:Membrane currents in response to the application of alpha, beta-methylene ATP (alpha,beta-meATP) were recorded by the whole-cell patch-clamp technique in human embryonic kidney 293 cells transfected with the human P2X3 receptor (HEK 293-hP2X3 cells). Trichloroethanol, the biologically active metabolite of chloral hydr...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(00)00833-5
更新日期：2000-12-15 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
abstract：:Glucagon release upon hypoglycemia is an important homeostatic mechanism utilized by vertebrates to restore blood glucose to normal. Glucagon secretion itself is triggered by Ca2+ influx through voltage-gated ion channels, and the gene inactivation of R-type Ca2+ channels, with Ca(v)2.3 as the ion conducting subunit, ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2005.01.044
更新日期：2005-03-21 00:00:00
abstract：:The toxicity of glutamate in neuronal cultures has been attributed in part to a mitochondrial dysfunction involving the permeability transition pore. The participation of the permeability transition pore in this process has been pharmacologically demonstrated by the use of cyclosporin A, which inhibits pore opening by...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(00)00584-7
更新日期：2000-09-15 00:00:00
abstract：:Inhibitors of Na(+)/H(+) exchanger (NHE) 1 have been shown to exert protective effects on various myocardial injuries. In this study, we characterized the pharmacodynamic properties of new guanidine NHE1 inhibitors (cariporide, sabiporide, KR-32511, KR-32570, and KR-33028) to analyze their myocardial protective effect...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2007.03.056
更新日期：2007-07-12 00:00:00
abstract：:The vascular effects of bradykinin were studied in rat perfused mesenteric vascular beds with active tone. Bolus injections of bradykinin (1-1000 pmol) but not des-Arg(9)-bradykinin (bradykinin B(1) receptor agonist) induced triphasic vascular responses: the initial sharp vasodilation followed by transient vasoconstri...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(01)01513-8
更新日期：2001-12-14 00:00:00
abstract：:Hyperphosphatemia is a mineral bone-disease that increases cardiovascular complications and all-cause mortality in chronic kidney disease (CKD) patients. Oral phosphate binders absorb the dietary phosphate to prevent its high plasma levels. Moreover, they can adsorb some uremic toxins and decrease inflammation. A few ...
journal_title：European journal of pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.ejphar.2019.172892
更新日期：2020-02-05 00:00:00
abstract：:Forskolin, a potent activator of adenylate cyclase, and isoprenaline, an unselective beta-adrenoceptor agonist, were studied in vitro on tissues from guinea-pig with respect to relaxation of the carbachol-contracted trachea, increase in the force of contraction of the papillary muscle and depression of subtetanic cont...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(85)90780-0
更新日期：1985-06-19 00:00:00
abstract：:Vasodilation, in vitro, evoked by atrial extracts (cardionatrin) was compared with the relaxation due to acetylcholine and papaverine in rat precontracted aortae with and without endothelium. Ventricular extracts were tested as controls. Atrial extracts and papaverine caused a similar concentration-dependent relaxatio...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(84)90040-2
更新日期：1984-05-18 00:00:00
abstract：:Transient outward K+ current, Ito, contributes to cardiac action potential generation and is primarily carried by Kv4.3 (KCND3) channels. Two Kv4.3 isoforms are expressed in human ventricle and show differential remodeling in heart failure (HF). Lidocaine and mexiletine may be applied in selected patients to suppress ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2020.173159
更新日期：2020-08-05 00:00:00
abstract：:Three important features must be considered when proposing therapeutic strategies in liver cirrhosis: inflammation, oxidative stress and fibrogenesis. Pirfenidone is a synthetic molecule which oxidative action has not been tested in cirrhosis. Cirrhosis was induced in rats by ligation of the common bile duct or carbon...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2008.06.110
更新日期：2008-10-24 00:00:00
abstract：:The involvement of brain monoamines in the mechanism of action of nefopam, a new analgesic, was investigated in rats. The study was designed to evaluate the effect of various means of impairing monoaminergic transmission on nefopam analgesia as measured with the hot plate method. Pretreatment with reserpine (2 mg/kg) ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(86)90762-4
更新日期：1986-09-09 00:00:00
abstract：:We have recently demonstrated that hyperthermia induced by 1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane (DOI) and m-chlorophenylpiperazine (m-CPP) are separately mediated by selective stimulation of 5-HT2A and 5-HT2C receptors, respectively in Wistar rats. Furthermore, hyperthermia induced by either DOI or m-CPP was ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(95)00279-t
更新日期：1995-08-25 00:00:00
abstract：:The pharmacological activity of bupropion was compared between α7 nicotinic acetylcholine receptors expressed in heterologous cells and hippocampal and dorsal raphe nucleus neurons. The inhibitory activity of bupropion was studied on GH3-α7 cells by Ca2+ influx, as well as on neurons from the dorsal raphe nucleus and ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2014.06.059
更新日期：2014-10-05 00:00:00
