Abstract：
:Using the radioactive microsphere technique in anaesthetized pigs, we studied the systemic and carotid haemodynamic effects of intracarotid infusions (0.3, 1, 3 and 10 micrograms/kg.min) of 5-methoxy-3-(1,2,3,6-tetrahydro-4-pyridinyl)-1H-indole succinate (RU 24969), a drug with high affinity for 5-HT1A and 5-HT1B recognition sites. Unlike in the rat, RU 24969 did not elicit hypotension in the pig. Instead, the two highest doses of the drug caused a slight increase in blood pressure. RU 24969 reduced common carotid artery blood flow by decreasing the non-nutrient, arteriovenous anastomotic blood flow; the nutrient, arteriolar blood flow was mildly increased. The decrease in common carotid and arteriovenous anastomotic blood flow was only slightly attenuated in animals pretreated with the 5-HT2 receptor antagonist, ketanserin (0.5 mg/kg i.a.), but was markedly reduced in animals pretreated with the 5-HT1-like and 5-HT2 receptor antagonist, methiothepin (1.0 mg/kg i.a.). However, these responses were not modified after pretreatment with the putative 5-HT1A and 5-HT1B receptor antagonist, (+/-)-pindolol (4.0 mg/kg i.v.). The slight increase in arteriolar blood flow was attenuated in the animals pretreated with either ketanserin, methiothepin or (+/-)-pindolol. It is concluded that the RU 24969-induced reduction in common carotid and arteriovenous anastomotic blood flow is mediated mainly by 5-HT1-like receptors, which do not seem to correspond to either the 5-HT1A or 5-HT1B receptor subtypes.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Bom AH,Villalón CM,Verdouw PD,Saxena PRdoi
10.1016/0014-2999(89)90432-9subject
Has Abstractpub_date
1989-11-14 00:00:00pages
87-96issue
1eissn
0014-2999issn
1879-0712pii
0014-2999(89)90432-9journal_volume
171pub_type
杂志文章abstract：:Montanine is an alkaloid isolated from Rhodophiala bifida bulb with potential anti-arthritic activity. In this context, we evaluated whether montanine has a disease modifying anti-rheumatic activity in two arthritis models and its effect in vitro on lymphocyte proliferation and on invasiveness of fibroblast-like synov...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2017.02.013
更新日期：2017-03-15 00:00:00
abstract：:There is controversy concerning the inhibitory effect of arginine-vasopressin (AVP) on human platelet adenylate cyclase activity, which putatively involves Gi as the G-protein. To clarify this point, the effects of AVP on human platelet membranes were studied by measuring the activities of the high-affinity GTPase, as...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(88)90020-9
更新日期：1988-06-10 00:00:00
abstract：:The ability of calcium entry blockers to inhibit allergic histamine release from rabbit leukocytes was studied. Bepridil, verapamil, nifedipine, diltiazem and TMB-8 produced concentration-dependent inhibition of allergic histamine release from rabbit leukocytes. The calculated IC50s (microM) were as follows: verapamil...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(85)90261-4
更新日期：1985-01-08 00:00:00
abstract：:In Krebs solution (3.36 mM Ca2+), the maximal contractile response of human ileal and urinary bladder detrusor muscle to acetylcholine (ACh) was 40-60% that to carbachol (CCh). The maximum response to ACh was reached at a bath concentration of about 1 microM and was maintained throughout a range extending to 100 micro...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(86)90698-9
更新日期：1986-04-09 00:00:00
abstract：:Mice, subjected footshock, showed a significant increase of pain threshold and motor suppression immediately after the footshock and both effects were partially antagonized by pretreatment with naloxone at high doses. The magnitude of footshock-induced analgesia, but not motor suppression, was significantly less in mo...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(83)90287-x
更新日期：1983-09-02 00:00:00
abstract：:To test the hypothesis that the flavonoid compound, fisetin, protects macrophages from lipid accumulation and senescence through regulation of casein kinase 2-interacting protein-1 (CKIP-1)/REGγ (11S regulatory particles, 28 kDa proteasome activator, proteasome activator subunit 3) signaling. RAW264.7 macrophage cells...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2019.172748
更新日期：2019-12-15 00:00:00
abstract：:The effects of capsaicin pretreatment on withdrawal responses of guinea-pig isolated ileum to [Met5]enkephalin (ME) and morphine and on the locomotor withdrawal response of guinea-pigs following a single dose of morphine, were investigated. In vitro treatment of ileum with capsaicin, 1.5 mumol/l for 1 h, did not signi...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(88)90257-9
更新日期：1988-12-06 00:00:00
abstract：:Gastrins and cholecystokinins contract the isolated taenia coli of the guinea-pig. Porcine CCK-39 produced the greatest contractile response and human gastrin-17 I and -34 the weakest. Pentagastrin had the highest affinity to the receptors and non-sulphated CCK-8 the lowest. The contractions produced by the CCK peptid...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(83)90244-3
更新日期：1983-06-03 00:00:00
abstract：:Termination of signalling by G-protein-coupled receptors requires inactivation of the G alpha-subunits of heterotrimeric G-proteins and the re-association of G alpha- and G betagamma-subunits. Inactivation of G alpha-subunits is achieved by the hydrolysis of bound GTP by an intrinsic GTPase activity, which is consider...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2008.03.047
更新日期：2008-06-10 00:00:00
abstract：:N6-2-(4-Aminophenyl)ethyl-adenosine (APNEA, a non-selective agonist of the adenosine A3 receptors), at the subprotective dose of 1 mg/kg against electroconvulsions, significantly potentiated the anticonvulsive action of phenobarbital, diphenylhydantoin and valproate against maximal electroshock, being ineffective at l...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(97)89651-3
更新日期：1997-05-30 00:00:00
abstract：:The effects of the endothelin ET(A), (BQ-123) and endothelin ET(A/B) (PD161721) receptor antagonists were investigated on ischaemia-induced arrhythmias and on the maximum following frequency. The study was carried out in Langendorff perfused rat hearts subjected to coronary artery occlusion in which the severity of ar...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(01)01396-6
更新日期：2001-11-30 00:00:00
abstract：:[Thi5,8,D-Phe7]bradykinin caused hind-paw edema and degranulation of isolated peritoneal mast cells in a dose-dependent manner. Pretreatment with diphenhydramine/methysergide or compound 48/80 completely suppressed the edematous response caused by [Thi5,8,D-Phe7]bradykinin, whereas bradykinin-induced hind-paw swelling...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(89)90836-4
更新日期：1989-02-28 00:00:00
abstract：:In pregnant rat myometrium, isoproterenol (10(-8) M) inhibited spontaneous contractions without causing hyperpolarization. Isoproterenol (10(-6) M) relaxed the depolarized muscle without affecting the membrane potential. The presence of 80 mM Na+ did not affect the degree of high-K+ depolarization. It was also without...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(79)90045-1
更新日期：1979-11-23 00:00:00
abstract：:Iron overload cardiomyopathy is the major cause of death in transfusion-dependent thalassemia (TDT) patients. Growing evidence demonstrates that combined iron chelators, or the combination of an iron chelator with antioxidant(s) are effective in diminishing myocardial iron deposition and attenuating cardiac dysfunctio...
journal_title：European journal of pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.ejphar.2015.08.017
更新日期：2015-10-15 00:00:00
abstract：:In this study, we determined the protective potential of trans resveratrol against oxygen-glucose deprivation (OGD) induced reactive oxygen species mediated apoptotic damages in PC12 cells. In vitro model of ischemic cerebral stroke was created by keeping cells in an OGD condition for 6h followed by 24h reoxygenation....
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2011.05.015
更新日期：2011-09-01 00:00:00
abstract：:The analgesic effect of cyclazocine microinjected into the diencephalon of rats was studied by using the bradykinin-induced flexor reflex test. The dorsal portion of the medial hypothalamic area was sensitive to cyclazocine with respect to the production of analgesia (ED50 2.6 micrograms/rat). Microinjections of morph...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(85)90119-0
更新日期：1985-04-23 00:00:00
abstract：:The nicotinic acetylcholine receptors in the rat stomach were characterized by means of a radioligand binding assay with (-)-[3H]nicotine as ligand. Saturation binding studies on the gastric fundus membranes revealed the presence of two binding sites with dissociation constant (KD) values of 3.1 and 289 nM, and maximu...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(88)90490-6
更新日期：1988-01-27 00:00:00
abstract：:A close relationship between the renin-angiotensin system and the pathophysiology of diabetic retinopathy has been suggested, several angiotensin II type 1 receptor (angiotensin AT1 receptor) antagonists being effective in animal models. Therefore, we examined the efficacy of an angiotensin AT1 receptor antagonist, ol...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2005.02.047
更新日期：2005-04-11 00:00:00
abstract：:We investigated the effects of 7-nitroindazole, a specific inhibitor of neuronal nitric oxide (NO) synthase, on NO concentration and on blood flow in rat hippocampus after transient forebrain ischemia which was induced by 4-vessel occlusion for 10 min. NO concentration was measured directly by an NO-selective electrod...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(99)00555-5
更新日期：1999-09-10 00:00:00
abstract：:The steady-state levels and utilization (alpha-MPT-induced disappearance) of noradrenaline (NA) and dopamine (DA) were measured in distinct mouse brain nuclei after acute morphine challenge, in mice rendered tolerant to morphine, and during the naloxone-precipitated morphine withdrawal syndrome. Mouse brain nuclei con...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(83)90132-2
更新日期：1983-09-30 00:00:00
abstract：:3-(Benzo[b]furan-5-yl)-2', 6'-dihydroxy-4'-methylpropiophenone-2'-O-(6-O-methoxycarbonyl)-bet a-D -glucopyranoside (T-1095) is a derivative of phlorizin, a potent inhibitor of Na(+)-glucose cotransporters. We determined the antidiabetic effect of T-1095 in neonatally streptozotocin-treated diabetic rats. Orally admini...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(00)00016-9
更新日期：2000-03-10 00:00:00
abstract：:Oral pretreatment with E3330, a novel quinone derivative, attenuated liver injury induced with tumor necrosis factor-alpha in galactosamine-sensitized mice. Tumor necrosis factor-alpha is known to induce inflammatory mediators such as leukotrienes and prostanoids. An in vitro study showed that E3330 inhibited the gene...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(92)90286-d
更新日期：1992-12-08 00:00:00
abstract：:The inward chloride current induced by angiotensin II (AII) in Xenopus oocytes shows strong and homologous desensitization, and was suggested to be mediated by phosphatidylinositol (PI) hydrolysis (Sakuta et al., 1991, Eur. J. Pharmacol. Mol. Pharmacol. 208, 31). As a model of agonist-induced desensitization of recept...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0922-4106(91)90049-n
更新日期：1991-09-12 00:00:00
abstract：:Earlier studies demonstrated that cytokine production is under the tonic control of noradrenaline. As the level and/or the duration of noradrenaline action is regulated by the noradrenaline transporter (NET), which is also a target of antidepressant treatment, we studied its role in the regulation of the cytokine resp...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(03)01721-7
更新日期：2003-05-23 00:00:00
abstract：:Mutations of p53 in cancer cells not only subvert its antiproliferative properties but can also promote various oncogenic responses through a gain-of-function activity. Pharmacological manipulation of the mutant p53 pathway by specific compounds could be an effective strategy for cancer therapy. We show here that gain...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2020.173584
更新日期：2020-11-15 00:00:00
abstract：:Slices of rat kidney cortex were incubated in [3H]noradrenaline, then placed in a flow cell and subjected to electrical field stimulation. At a stimulation frequency of 5 Hz, both the alpha 2-adrenoceptor antagonist idazoxan (0.1 microM) and the alpha 1-adrenoceptor antagonist prazosin (0.1 microM) significantly enhan...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(89)90026-5
更新日期：1989-10-10 00:00:00
abstract：:MK-801 (a potent non-competitive antagonist of N-methyl-D-aspartic acid-mediated events) in subcutaneous doses of 0.1 and 0.2 mg/kg increased the threshold for electroconvulsions and in doses of 0.0031 and 0.0125 mg/kg enhanced the protective activity of valproate against maximal electroshock-induced convulsions in mi...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(91)90582-b
更新日期：1991-08-06 00:00:00
abstract：:A new experimental drug pirfenidone (5-methyl-1-phenyl-2-1H-pyridine-2-one) has been reported to have beneficial effects for the treatment of certain fibrotic diseases. Here, we studied the anti-inflammatory activities of pirfenidone by investigating the mechanism of its inhibitory effect on cytokine production. In RA...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(02)01758-2
更新日期：2002-06-20 00:00:00
abstract：:Synthesized pyridine compound derivatives (SK94, SK126) from a natural lead source were administered to mice to test for possible anti-TNF alpha and anti-inflammatory activities. Lipopolysaccharide (LPS)-induced TNF alpha production was analyzed in the endothelial cells, Raw 264.7 cells, and serum of normal mice after...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2011.01.062
更新日期：2011-04-25 00:00:00
abstract：:The aim of this study was to investigate role of the N-Methyl-D-Aspartate (NMDA) receptors in the decrease of morphine analgesia in mice after nociceptive sensitization. We used a hot plate test to assess effects of morphine on pain behavior in male NMRI mice. All drugs were administered through an intraperitoneal rou...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2014.04.048
更新日期：2014-08-15 00:00:00
