RO 16-6028, a benzodiazepine receptor partial agonist, does not exhibit anticonvulsant tolerance in mice.

Abstract:

:The development of anticonvulsant tolerance with RO 16-6028, a benzodiazepine receptor partial agonist, was assessed in mice using an i.v. infusion of pentylenetetrazol as the convulsive stimulus. In contrast to other benzodiazepines tested previously in this seizure model the anticonvulsant protection afforded by RO 16-6028 did not change significantly during 10 days treatment (2 mg/kg b.i.d.). This result supports the hypothesis that partial agonists at the benzodiazepine receptor may induce less tolerance and/or dependence than full agonists.

journal_name

Eur J Pharmacol

authors

Haigh JR,Feely M

doi

10.1016/0014-2999(88)90788-1

subject

Has Abstract

pub_date

1988-03-01 00:00:00

pages

283-5

issue

2

eissn

0014-2999

issn

1879-0712

pii

0014-2999(88)90788-1

journal_volume

147

pub_type

杂志文章
  • Reversal of heparin-induced increases in aPTT in the rat by PM102, a novel heparin antagonist.

    abstract::Protamine is the only agent approved to reverse heparin-induced anticoagulation. Due to the significant adverse effects of protamine there is an important need for an alternative agent with an improved safety profile. The pharmacodynamics of PM102, a novel peptide-based heparin antagonist, was evaluated and compared t...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2010.03.016

    authors: Cushing DJ,Cooper WD,Cohen ML,McVoy JR,Sobel M,Harris RB

    更新日期:2010-06-10 00:00:00

  • Potentiation by neuropeptide Y of 5HT2A receptor-mediated contraction in porcine coronary artery.

    abstract::Potentiation by neuropeptide Y of serotonin (5-HT)-induced vasoconstriction was investigated in porcine coronary artery. 5-HT caused concentration-dependent contraction through 5-HT2A receptors. Neuropeptide Y (30 nM) significantly increased the 5HT-induced contraction by 16+/-5% in arteries with intact endothelium. R...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2006.06.036

    authors: Tsurumaki T,Nagai S,Bo X,Toyosato A,Higuchi H

    更新日期:2006-08-21 00:00:00

  • Effect of propofol on calcium homeostasis in hypoxia-reoxygenated neonatal rat cardiomyocytes.

    abstract::Intracellular Ca2+ overload induced by hypoxia-reoxygenation alters Ca2+ homeostasis, which plays an important role in myocardial cell injury. Even though propofol is known as a radical scavenger with Ca2+ channel blocking properties, little is known about cardioprotective effect associated with Ca2+ homeostasis in ca...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2008.07.027

    authors: Kim HS,Chang WC,Hwang KC,Choi IG,Park WK

    更新日期:2008-10-10 00:00:00

  • Effects of the optical isomers of verapamil on electrophysiological properties of the heart in conscious dogs.

    abstract::We compared the cumulative dose-response relations of verapamil (0.1, 0.2 and 0.4 mg kg(-1)) in different R/S enantiomer ratios (100/0, 90/10, 80/20, 50/50 and 20/80) on the electrophysiological and hemodynamic characteristics of the heart using the conscious dogs. A reduction of mean arterial pressure occurred with 2...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(98)00480-4

    authors: Takahata O,Krolikowski JG,McCallum JB,Lathrop DA,Bosnjak ZJ

    更新日期:1998-08-21 00:00:00

  • Morroniside enhances angiogenesis and improves cardiac function following acute myocardial infarction in rats.

    abstract::Angiogenesis is critical for re-establishing blood supply to the ischemic myocardium after acute myocardial infarction (AMI). This study aimed to investigate the effects of morroniside on angiogenesis after AMI and explored associated proangiogenic mechanisms. A rat model of AMI was established by ligation of the left...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2020.172954

    authors: Liu T,Sun F,Cui J,Zheng S,Li Z,Guo D,Tian X,Zhu Z,Zheng W,Wang Y,Wang W

    更新日期:2020-04-05 00:00:00

  • [3H]Batrachotoxinin A 20-alpha-benzoate binding to sodium channels in rat brain: characterization and pharmacological significance.

    abstract::Attempts were made to find whether [3H]batrachotoxinin A 20-alpha-benzoate provides a specific probe for measuring interactions of local anesthetics with the sodium channel complex. [3H]Batrachotoxinin A 20-alpha-benzoate binding, [14C]guanidine and 22Na uptake were investigated in rat brain crude synaptosomal prepara...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(86)90230-x

    authors: Pauwels PJ,Leysen JE,Laduron PM

    更新日期:1986-05-27 00:00:00

  • Chemical kindling decreases GABA-activated chloride channels of mouse brain.

    abstract::The repeated administration of N-methyl-beta-carboline-3-carboxamide (FG 7142) to mice leads to 'chemical kindling', i.e. the development of seizures in response to doses which were initially insufficient to produce convulsive activity. To determine if chemical kindling produced changes in the GABAA receptor/chloride ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(89)90658-4

    authors: Lewin E,Peris J,Bleck V,Zahniser NR,Harris RA

    更新日期:1989-01-24 00:00:00

  • Inhibition by agmatine on morphine-induced conditioned place preference in rats.

    abstract::Our previous studies demonstrated the ability of exogenous agmatine to inhibit tolerance to and physical dependence on morphine in mice, rats and monkeys. The present study further evaluated the effect of agmatine on the psychological dependence induced by morphine in conditioned place preference assay. Agmatine (0.75...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2005.03.045

    authors: Wei XL,Su RB,Lu XQ,Liu Y,Yu SZ,Yuan BL,Li J

    更新日期:2005-05-16 00:00:00

  • Negative inotropic effects of diadenosine tetraphosphate are mediated by protein kinase C and phosphodiesterases stimulation in the rat heart.

    abstract::Extracellular diadenosine polyphosphates (ApnA) are recently considered as an endogenous signaling compounds with transmitter-like activity which present in numerous tissues, including heart. It has been demonstrated previously that extracellular ApnA cause alteration of the heart functioning via purine receptors in d...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2017.12.024

    authors: Pakhomov N,Pustovit K,Potekhina V,Filatova T,Kuzmin V,Abramochkin D

    更新日期:2018-02-05 00:00:00

  • Nicotine's opioid and anti-opioid interactions: proposed role in smoking behavior.

    abstract::Nicotine produced antinociception in mice which was antagonized noncompetitively by naloxone. In addition, at significantly lower doses, nicotine noncompetitively antagonized morphine-induced antinociception. A speculative suggestion regarding the opiatergic and anti-opiatergic actions of nicotine is that it significa...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0926-6917(93)90009-f

    authors: Aceto MD,Scates SM,Ji Z,Bowman ER

    更新日期:1993-12-01 00:00:00

  • Structure-activity relationships of alpha-human atrial natriuretic peptide.

    abstract::The spasmolytic activity of synthetic alpha-human atrial natriuretic peptide (alpha-hANP) and its related peptides was determined in vitro using the chick rectum and the rat aorta. Natriuretic activity was also measured in the anesthetized rat, alpha-hANP-(7-28), with the NH2-terminal hexapeptide truncated, had greate...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(88)90632-2

    authors: Watanabe TX,Noda Y,Chino N,Nishiuchi Y,Kimura T,Sakakibara S,Imai M

    更新日期:1988-02-16 00:00:00

  • Effects of a dual L/N-type Ca(2+) channel blocker cilnidipine on neurally mediated chronotropic response in anesthetized dogs.

    abstract::We investigated the effects of an L-type and N-type Ca(2+) channel blocker, cilnidipine, on neurally mediated chronotropic responses to clarify the anti-autonomic profile of cilnidipine in anesthetized dogs. Pretreatment with cilnidipine (0.3, 1.0 and 3.0 microg/kg, i.v.), which decreased mean blood pressure by 5 to 3...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(01)00738-5

    authors: Konda T,Takahara A,Maeda K,Dohmoto H,Yoshimoto R

    更新日期:2001-02-09 00:00:00

  • Sesamin increases heme oxygenase-1 protein in RAW 264.7 macrophages through inhibiting its ubiquitination process.

    abstract::Sesamin is a major component in lignans of sesame seed oil, known to possess potent anti-oxidative capacity. In this study, the variation of heme oxygenase (HO)-1, a kind of anti-oxidative enzyme, by sesamin in murine macrophage cell line RAW 264.7 cells was investigated. Lipopolysaccharide (LPS; 10μg/ml) exposure ten...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2014.08.015

    authors: Fukunaga M,Ohnishi M,Shiratsuchi A,Kawakami T,Takahashi M,Motomura M,Egusa K,Urasaki T,Inoue A

    更新日期:2014-10-15 00:00:00

  • Inhibitory effect of anti-diabetic agents on rat organic anion transporter rOAT1.

    abstract::The interactions of sulfonylureas and a novel anti-diabetic drug, nateglinide, with rat renal organic anion transporter (rOAT1) expressed in Xenopus laevis oocytes were studied. Uptake of p-aminohippurate via rOAT1 was markedly inhibited by glibenclamide and nateglinide, and moderately by chlorpropamide and tolbutamid...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(00)00324-1

    authors: Uwai Y,Saito H,Hashimoto Y,Inui K

    更新日期:2000-06-16 00:00:00

  • Possible involvement of oxidative stress in hypoxia-induced adrenomedullin secretion in cultured rat cardiomyocytes.

    abstract::Although hypoxia induces adrenomedullin gene expression in cultured rat cardiac myocytes, it is still unknown whether oxidative stress is involved in the hypoxia-induced adrenomedullin production. We investigated whether oxidative stress might participate in hypoxia-induced adrenomedullin secretion and whether adrenom...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(01)01462-5

    authors: Yoshihara F,Horio T,Nishikimi T,Matsuo H,Kangawa K

    更新日期:2002-02-01 00:00:00

  • Mode of action of gingerols and shogaols on 5-HT3 receptors: binding studies, cation uptake by the receptor channel and contraction of isolated guinea-pig ileum.

    abstract::Ginger (rhizomes of Zingiber officinale) has been shown to exert potent anti-emetic properties, but its mode of action has not yet been elucidated. Among its active constituents, [6]-, [8]- and [10]-gingerol as well as [6]-shogaol were shown in different in vivo studies to be at least partly responsible for the drug's...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2005.10.049

    authors: Abdel-Aziz H,Windeck T,Ploch M,Verspohl EJ

    更新日期:2006-01-13 00:00:00

  • Inhibitory activity of kinetin on free radical formation of activated platelets in vitro and on thrombus formation in vivo.

    abstract::Kinetin has been shown to have anti-aging effects on several different systems, including plants and human cells. Recently, we demonstrated that kinetin markedly inhibited platelet aggregation in washed human platelets. In the present study, an electron spin resonance (ESR) method was used to further evaluate the scav...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(03)01528-0

    authors: Hsiao G,Shen MY,Lin KH,Chou CY,Tzu NH,Lin CH,Chou DS,Chen TF,Sheu JR

    更新日期:2003-04-04 00:00:00

  • Differential antagonism by conotoxin rho-TIA of contractions mediated by distinct alpha1-adrenoceptor subtypes in rat vas deferens, spleen and aorta.

    abstract::The ability of the conotoxin rho-TIA, a 19-amino acid peptide isolated from the marine snail Conus tulipa, to antagonize contractions induced by noradrenaline through activation of alpha1A-adrenoceptors in rat vas deferens, alpha1B-adrenoceptors in rat spleen and alpha1D-adrenoceptors in rat aorta, and to inhibit the ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2004.12.011

    authors: Lima V,Mueller A,Kamikihara SY,Raymundi V,Alewood D,Lewis RJ,Chen Z,Minneman KP,Pupo AS

    更新日期:2005-01-31 00:00:00

  • Expression of purinergic P2Y receptor subtypes by INS-1 insulinoma beta-cells: a molecular and binding characterization.

    abstract::Purinergic P2Y-receptor agonists amplify glucose-induced insulin secretion from pancreatic beta-cells, thus offering new opportunities for the treatment of type 2 diabetes. However, little is known about which subtypes of purinergic P2Y receptors are expressed in these cells. The INS-1 beta-cell line is used as a mode...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2007.04.012

    authors: Lugo-Garcia L,Filhol R,Lajoix AD,Gross R,Petit P,Vignon J

    更新日期:2007-07-30 00:00:00

  • Pharmacological activity of cholecystokinin analogues modified in the Met28-Gly29 region.

    abstract::Analogues of the C-terminal octapeptide of cholecystokinin (CCK) modified in the Met28-Gly29 region, were tested for their ability to interact with peripheral cholecystokinin receptors on rat pancreatic acini and to stimulate amylase secretion. These analogues were further evaluated for their ability to recognize cent...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(90)90436-a

    authors: Mendre C,Rodriguez M,Lignon MF,Galas MC,Gueudet C,Worms P,Martinez J

    更新日期:1990-09-21 00:00:00

  • Dihydrocapsaicin-induced hypothermia and substance P depletion.

    abstract::Administration of dihydrocapsaicin to rats resulted in a dose-dependent (0.5-10 mg/kg s.c.) hypothermia. Dihydrocapsaicin was approximately 65% more effective in producing hypothermia than capsaicin. Desensitization and cross-tolerance occurred to the hypothermic effects of both capsaicin and dihydrocapsaicin. Repeate...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(82)90263-1

    authors: Miller MS,Brendel K,Buck SH,Burks TF

    更新日期:1982-09-24 00:00:00

  • Indomethacin and ibuprofen inhibit the uptake of 45Ca2+ by washed human platelets through a thromboxane A2-independent mechanism.

    abstract::Indomethacin and ibuprofen inhibited adrenaline- and calcium ionophore A23187-stimulated 45Ca2+ uptake by isolated human platelets in a concentration-dependent manner. Mediation of these effects by thromboxane A2 (TXA2) inhibition was discounted since under the same experimental conditions, adrenaline did not stimulat...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(90)90351-6

    authors: Gill J,Dandona P,Jeremy JY

    更新日期:1990-10-02 00:00:00

  • Anti-tumor necrosis factor agent PEG-sTNFRI improves the growth hormone/insulin-like growth factor-I system in adjuvant-induced arthritic rats.

    abstract::Adjuvant-induced arthritis is associated with body weight loss and decreased pituitary growth hormone (GH) and hepatic insulin-like growth factor-I (IGF-I) synthesis. Cytokines as tumor necrosis factor (TNF) mediate wasting associated with chronic inflammation. The aim of this study was to analyse whether the inhibiti...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2006.02.035

    authors: Granado M,Priego T,Martín AI,Vara E,López-Calderón A,Angeles Villanúa M

    更新日期:2006-04-24 00:00:00

  • Proanaphylactic action of morphine is mediated through a central cholinergic mechanism.

    abstract::Intracerebroventricular (i.c.v.) or intravenous (i.v.) administration of morphine (10 micrograms or 25 mg/kg, respectively) increased the mortality rate in experimental anaphylaxis in mice. This effect was blocked by the opiate antagonist naltrexone administered systemically (5 mg/kg) or i.c.v. (10 micrograms). Moreov...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(83)90274-1

    authors: Amir S

    更新日期:1983-11-11 00:00:00

  • Blockade by clonidine of negative pressure breathing-induced diuresis in the dog.

    abstract::The effects of clonidine and dl-propranolol on negative pressure breathing-induced diuresis in chloralose-anaesthetized dog were studied. Clonidine (10 microgram/kg i.v.) suppressed the diuretic response, whereas dl-propranolol (1 mg/kg i.v.) was inactive. ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(81)90579-3

    authors: Montastruc P,Montastruc JL,Tran LD

    更新日期:1981-07-10 00:00:00

  • gp120 of HIV-1 induces apoptosis in rat cortical cell cultures: prevention by memantine.

    abstract::After incubation of rat cortical cell cultures with the human immunodeficiency virus type 1 (HIV-1) coat protein gp120 for 12 h, cells showed fragmentation of DNA at internucleosomal linkers, the characteristic feature of apoptosis. In a quantitative approach, it was determined that the percentage of DNA fragmentation...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0922-4106(92)90063-2

    authors: Müller WE,Schröder HC,Ushijima H,Dapper J,Bormann J

    更新日期:1992-07-01 00:00:00

  • Inhibition by histamine H1 receptor antagonists of endogenous glibenclamide-sensitive K+ channels in follicle-enclosed Xenopus oocytes.

    abstract::Effects of histamine receptor ligands on the glibenclamide-sensitive K+ currents induced by K+ channel openers, cromakalim and Y-26763, were examined in follicle-enclosed Xenopus oocytes. Histamine H1 receptor antagonists, promethazine, dimethindene and chlorpheniramine all decreased cromakalim-induced K+ currents wit...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0922-4106(94)90214-3

    authors: Sakuta H

    更新日期:1994-01-01 00:00:00

  • Vasorelaxant effect of harman.

    abstract::The in vivo cardiovascular effect and in vitro vasorelaxant effect of harman, one of harmala alkaloids isolated from Peganum harmala, were examined in this study. Harman (1-10 mg/kg, i.v.) dose-dependently produced transient hypotension and long-lasting bradycardia in pentobarbital-anesthetized rats, which were attenu...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(99)00928-0

    authors: Shi CC,Chen SY,Wang GJ,Liao JF,Chen CF

    更新日期:2000-03-03 00:00:00

  • Effects of allicin on hyperhomocysteinemia-induced experimental vascular endothelial dysfunction.

    abstract::This study was designed to investigate the effect and mechanism of allicin on hyperhomocysteinemia-induced experimental vascular endothelial dysfunction in rats. Fifty male Wistar rats were randomly divided into five groups: the normal control rats (NC), the high-methionine-diet rats (Met), the high-methionine-diet ra...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2013.05.038

    authors: Liu DS,Gao W,Liang ES,Wang SL,Lin WW,Zhang WD,Jia Q,Guo RC,Zhang JD

    更新日期:2013-08-15 00:00:00

  • Effects of systemic treatment with irbesartan and losartan on central responses to angiotensin II in conscious, normotensive rats.

    abstract::Angiotensin AT1 receptor antagonists represent a novel class of cardiovascular drugs. In conscious, normotensive rats, irbesartan ((2-n-butyl-3-[(2'-(1H-tetrazol-5-yl)-biphenyl-4-yl) methyl]-1,3-diaza-spiro[4,4]non) and losartan ((2 n-butyl-4-chloro-5-hydroxymethyl-1-[(2'-(1H-tetrazol-5-yl)biphenyl -4-yl) methyl] imid...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(98)00983-2

    authors: Culman J,von Heyer C,Piepenburg B,Rascher W,Unger T

    更新日期:1999-02-19 00:00:00