Abstract:
:The biological properties of neurotensin (NT) and the chicken peptide [Lys8,Asn9]neurotensin-(8-13) (LANT-6) were compared in 3 in vitro assays: (1) competitive inhibition of [3H]NT binding to rat brain synaptic membranes, (2) relaxation of the rat ileum, and (3) contraction of the guinea-pig ileum. The data show that LANT-6 interacted with NT receptors like a weak agonist having full intrinsic activity and low affinity. LANT-6 is unlikely to represent a physiological activator of NT receptors.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Kitabgi P,Checler F,Vincent JPdoi
10.1016/0014-2999(84)90147-xsubject
Has Abstractpub_date
1984-04-06 00:00:00pages
357-60issue
4eissn
0014-2999issn
1879-0712pii
0014-2999(84)90147-Xjournal_volume
99pub_type
杂志文章abstract::The cellular localisation and distribution of mRNAs encoding beta-adrenoceptor subtypes in human lung were studied by in situ hybridisation and Northern blot analysis. The 851-bp SmaI/PvuII fragment of human beta 1-adrenoceptor cDNA, the 439-bp SmaI fragment of human beta 2-adrenoceptor cDNA and the 975-bp SmaI fragme...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(96)00104-5
更新日期:1996-04-29 00:00:00
abstract::The effects of N- and L-type voltage operated calcium channel (VOCC) antagonists were examined on the bronchoconstriction induced by vagal stimulation in artificially respired guinea-pigs. Vagal stimulation produced a reproducible and consistent bronchoconstrictor response which corresponded to an increase in pulmonar...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(92)90589-v
更新日期:1992-08-14 00:00:00
abstract::In preceding papers, we proposed that procainamide hydrochloride, a class I antiarrhythmic agent, was able to protect mice and rats from cisplatin-induced nephrotoxicity and that it could exert its action through accumulation in kidneys followed by coordination with cisplatin (or its hydrolysis metabolites) and format...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/s0014-2999(02)01537-6
更新日期:2002-05-10 00:00:00
abstract::A cDNA clone which encodes a putative kainate receptor was prepared with the polymerase chain reaction; from this, 'antisense' RNA fragments were produced and used to evaluate the distribution of mRNA for the kainate-receptor in rat brain with in situ hybridization techniques. The data demonstrate marked regional diff...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0922-4106(90)90025-s
更新日期:1990-09-18 00:00:00
abstract::Previously reported work has provided evidence that arylazido aminopropionyl ATP (ANAPP3), a P2-receptor antagonist, blocks the effects of ATP and other purine analogs, in the urinary bladder of the cat. This antagonism appeared limited to those effects mediated by P2-receptors, such as contraction of the urinary blad...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(86)90476-0
更新日期:1986-01-29 00:00:00
abstract::Treatment with soterenol (0.3-300 mug/kg, i.v.) increased the mean arterial blood pressure and decreased heart rate in rabbits. Soterenol caused a dose-dependent contraction of rabbit aorta and portal vein, guinea-pig vas deferens and cat nicitating membrane which was inhibited by phentolamine. Other beta-agonists suc...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(75)90163-6
更新日期:1975-08-01 00:00:00
abstract::The rat paw edema-inducing, acute inflammatory activity of four snake venom phospholipase A2S (PLA2) (Naja naja, Naja mocambique mocambique, Crotalus atrox and recombinant Naja naja naja) and of recombinant human type II PLA2 (rh-PLA2) found in rheumatoid synovial fluid, were compared after a bolus subplantar injectio...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(93)90818-3
更新日期:1993-04-22 00:00:00
abstract::Systemic or intracerebral administration of kainic acid in rodents induces neuronal death followed by a cascade of neuroplastic changes in the hippocampus. Kainic acid-induced neuroplasticity is evidenced by alterations in hippocampal neurogenesis, dispersion of the granule cell layer and re-organisation of mossy fibr...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2011.05.008
更新日期:2011-09-01 00:00:00
abstract::The middle ear epithelium functions to maintain a fluid-free middle ear cavity. Dysfunction of the middle ear epithelial ion and fluid transport is implicated in the pathogenesis of fluid collection in the middle ear cavity, characteristic of otitis media with effusion. The efficacy of steroid therapy for the treatmen...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2008.11.012
更新日期:2009-01-14 00:00:00
abstract::Radioligand receptor binding techniques were used to characterize the effects of different structural types of antidepressant drugs on neurotransmitter receptors. The tricyclic antidepressants more or less potently inhibited the binding to rat brain preparations of several different radiolabelled ligands [3H]WB4101, [...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(81)90172-2
更新日期:1981-03-26 00:00:00
abstract::Histamine induced a dose-dependent stimulation of 3H-catecholamine(CA) efflux (superfusion procedure) from hypothalamic, striatal, hippocampal and cortical slices. The extra-hypothalamic regions were the most sensitive to histamine. Efflux of 14C-GABA and 14C-(acetyl)choline was not affected. The effect of histamine o...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(77)90126-1
更新日期:1977-05-15 00:00:00
abstract::The [3H]nitrendipine binding activity of sarcolemmal fragments isolated from aerobically perfused or ischemic rat hearts was studied. After 90 min aerobic perfusion, two populations of binding sites were detected--high affinity sites with KD of 0.24 +/- 0.04 nM and Bmax 313 +/- 110 fmol/mg protein, and low affinity si...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(85)90587-4
更新日期:1985-09-10 00:00:00
abstract::[N-methyl-Nle 28,31)]cholecystokinin-(26-33) (SNF 8702) is a highly selective ligand for the CCKB type of receptor present in the vertebrate central nervous system. Radioligand binding data showing that SNF 8702 binding affinity is reduced by the GTP analog guanylyl-imidodiphosphate suggest that SNF 8702 is an agonist...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0922-4106(94)90079-5
更新日期:1994-10-14 00:00:00
abstract::The potencies of histamine and methacholine were significantly increased by approximately 2- and 5-fold respectively in human non-diseased isolated bronchi on removal of the epithelium. In contrast, no increases in spasmogen potency were observed following epithelium removal in bronchi obtained from a sample of asthma...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(90)90360-i
更新日期:1990-10-23 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::We investigated the effect of sevoflurane (fluoromethyl-2,2,2-trifluoro-1-(trifluoromethyl) ethylether) on intracellular calcium concentration ([Ca2+]i) and nitric oxide (NO) release from cultured porcine aortic endothelial cells using fura-2 fluorometry, and direct (ESR spectrometry with NO-trapping by 2-(4-carboxyph...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0922-4106(95)90165-5
更新日期:1995-03-15 00:00:00
abstract::It has been shown that the pancreatic beta-cell monoamines are located in the secretory granules, and that they have an inhibitory influence on insulin secretion. Monoamines are inactivated by the enzyme, monoamine oxidase. We now studied in vivo the relation between adrenergic and cholinergic stimulation, insulin sec...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(93)90063-n
更新日期:1993-03-23 00:00:00
abstract::The present study was designed to evaluate the preventive effects of p-coumaric acid on lysosomal dysfunction and myocardial infarct size in isoproterenol induced myocardial infarcted rats. Male albino Wistar rats were pretreated with p-coumaric acid (8 mg/kg body weight) daily for a period of 7 days after which isopr...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2012.11.006
更新日期:2013-01-15 00:00:00
abstract::The histamine H3 agonist, (R)-alpha-methylhistamine (alpha-MeHA, 10(-10) to 10(-5) M), caused a concentration-dependent inhibition of the sympathetic contractile response to electrical field stimulation of guinea pig isolated atria, but alpha-MeHA did not alter the basal tension or the contraction induced by exogenous...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(91)90857-m
更新日期:1991-11-12 00:00:00
abstract::Renal hemodynamics were studied using an electromagnetic perivascular flow sensor in anesthetized rats injected i.v. with vehicle, 5 or 10 mg/kg body weight (b.w.) sulindac. No hemodynamic changes occurred with vehicle (n = 6), but mean arterial pressure was significantly decreased (by 15 mmHg) with sulindac (n = 12)....
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/s0014-2999(97)00178-7
更新日期:1997-07-09 00:00:00
abstract::Transient receptor potential melastatin 2 (TRPM2) is an oxidative stress-sensitive Ca2+-permeable channel. The activation of TRPM2 by H2O2 causes cell death in various types of cells. 5-Fluorouracil (5-FU) is an important anticancer drug, but myelosuppression is one of the most frequent adverse effects. The involvemen...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2020.173671
更新日期:2021-01-15 00:00:00
abstract::In this work, the involvement of ionotropic glutamatergic receptors and nitric oxide on striatal dopamine release induced by anatoxin-a was investigated in conscious and freely-moving rats. To study the participation of glutamatergic receptors, the effects of alpha-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (A...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2006.07.044
更新日期:2006-10-24 00:00:00
abstract::To investigate the effect of a single and multiple administration of lysergic acid diethylamide (LSD) on cerebral metabolism of dopamine and serotonin, male Wistar rats were treated with low and high doses (0.1 and 2.0 mg/kg i.p.) of LSD and the levels of dopamine, 3,4-dihydroxyphenylacetic acid, homovanillic acid, 3-...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/s0014-2999(97)01025-x
更新日期:1997-07-30 00:00:00
abstract::The activity of the four glycoterpenoids: two saponins, verbascosaponin A and verbascosaponin, and two iridoids, scropolioside A and scrovalentinoside, isolated from Scrophularia auriculata ssp. pseudoauriculata, were studied in different models of acute and chronic inflammation. Both saponins significantly inhibited ...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/s0014-2999(99)00846-8
更新日期:2000-02-18 00:00:00
abstract::[3H]Rauwolscine binds with high affinity to alpha 2-adrenoceptors (Kd = 4.8 +/- 1.3 nM, Bmax = 79 +/- 26 fmol/mg protein, micromolar affinity for 5-HT) as well as to 5-HT1-like receptors (Kd = 13 +/- 2.7 nM, Bmax = 147 +/- 11.4 fmol/mg protein, nanomolar affinity for 5-HT) in human brain cortex membranes. The Ki value...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(89)90163-5
更新日期:1989-01-17 00:00:00
abstract::The contribution of tyrosine kinase activity to vasoreactivity in normotensive Wistar-Kyoto (WKY) and spontaneously hypertensive (SHR) rats was investigated on isolated aortic preparations by the use of two tyrosine kinase inhibitors: methyl-2,5-dihydroxycinnamate (30 microM) and genistein (30 microM). The pretreatmen...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/s0014-2999(99)00304-0
更新日期:1999-06-11 00:00:00
abstract::To investigate the role of ATP-sensitive K+(KATP) channels on pacemaker activity in interstitial cells of Cajal (ICC), whole-cell patch clamping, RT-PCR, and intracellular Ca2+([Ca2+]i) imaging were performed in cultured colonic ICC. Pinacidil (a K+ channel opener) hyperpolarized the membrane and inhibited the generat...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2017.05.029
更新日期:2017-08-15 00:00:00
abstract::Here we provide the first pharmacological exploration of the impact of acute central nervous system exposure to three recently developed ghrelin receptor (GHS-R1A) ligands on food intake and on the electrical activity of the target cells for ghrelin in the hypothalamus. Central (i.c.v) injection of GHS-R1A antagonists...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2009.03.066
更新日期:2009-06-10 00:00:00
abstract::Recent studies suggest that non-steroidal anti-inflammatory drugs have central sites of action which contribute to their analgesic efficacy. In the present study microinjections of the non-steroidal anti-inflammatory drug, dipyrone, were made into the medullary nucleus raphe magnus of lightly pentobarbital-anesthetize...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/s0014-2999(96)00909-0
更新日期:1996-12-27 00:00:00
abstract::Several structural analogs of mazindol were tested as inhibitors of the uptake of [3H] dopamine in rat neostriatum, of [3H] norepinephrine in rat occipital cortex and of [3H] serotonin in whole rat brain. A rather wide range of potencies was observed but a number of the drugs were even more potent than mazindol as upt...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(81)90030-3
更新日期:1981-05-08 00:00:00