Interaction of histamine H2-receptor antagonists with GABA and benzodiazepine binding sites in the CNS.

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 was specific for imidazole-derived H2-receptor antagonists (potency: cimetidine greater than metiamide greater than tiotidine) and not observed with either several H1-receptor antagonists or histamine. These data indicate a striking similarity between the actions of cimetidine (and other imidazole-derived H2-receptor antagonists) and GABA on binding parameters at the GABA receptor complex.

journal_name

Eur J Pharmacol

authors

Lakoski JM,Aghajanian GK,Gallager DW

doi

10.1016/0014-2999(83)90011-0

subject

Has Abstract

pub_date

1983-03-25 00:00:00

pages

241-5

issue

2-3

eissn

0014-2999

issn

1879-0712

pii

0014-2999(83)90011-0

journal_volume

88

pub_type

杂志文章
  • Indirubin-3'-oxime suppresses human cholangiocarcinoma through cell-cycle arrest and apoptosis.

    abstract::Cholangiocarcinoma (CCA) is one of the most serious of all cancers and a major public health problem. CCA is an extremely invasive cancer, and the survival rate for CCA patients is only 24 months after diagnosis. Although surgery and chemotherapy can extend the survival rate to 5 years, < 20-40% of CCA patients will s...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2018.09.023

    authors: Lee MY,Li YZ,Huang KJ,Huang HC,Lin CY,Lee YR

    更新日期:2018-11-15 00:00:00

  • Effect of chronic treatment with SCH 23390 and haloperidol on spontaneous activity of dopamine neurones in substantia nigra pars compacta (SNC) and ventral tegmental area (VTA) in rats.

    abstract::The effect of chronic treatment (21 days s.c.) with SCH 23390 and haloperidol on spontaneously active DA neurones in substantia nigra pars compacta (SNC) and ventral tegmental area (VTA) was studied in rats by means of single unit recording techniques. The specific DA D-1 receptor antagonist SCH 23390 was injected twi...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(88)90238-5

    authors: Skarsfeldt T

    更新日期:1988-01-12 00:00:00

  • CysLT2 receptor activation is involved in LTC4-induced lung air-trapping in guinea pigs.

    abstract::CysLT1 receptors are known to be involved in the pathogenesis of asthma. However, the functional roles of CysLT2 receptors in this condition have not been determined. The purpose of this study is to develop an experimental model of CysLT2 receptor-mediated LTC4-induced lung air-trapping in guinea pigs and use this mod...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2016.11.036

    authors: Sekioka T,Kadode M,Yonetomi Y,Kamiya A,Fujita M,Nabe T,Kawabata K

    更新日期:2017-01-05 00:00:00

  • Responses to L-163,491, a nonpeptide angiotensin II mimic, in the pulmonary vascular bed of the cat.

    abstract::Pulmonary vascular responses to 5,7-dimethyl-2-ethyl-3-[[2'-[butyloxycarbonyl)amino-sulfonyl]-5'-(3-meth oxybenzyl)-[1,1'-biphenyl]-4-yl]methyl]-3H-imidazo[4,5-b]pyridine (L-163,491), a novel nonpeptide angiotensin agonist, and angiotensin IV, the 3-8 amino acid fragment of angiotensin, were compared with responses to...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(95)00486-6

    authors: Kaye AD,Nossaman BD,Kivlighn S,Ibrahim IN,De Witt BJ,Kadowitz PJ

    更新日期:1995-12-12 00:00:00

  • A role for cannabinoid receptors, but not endogenous opioids, in the antinociceptive activity of the CB2-selective agonist, GW405833.

    abstract::Several recent reports have demonstrated a role for selective cannabinoid CB2 receptor agonists in pain modulation, showing both analgesic and antihyperalgesic activities. While the mechanism of action is poorly understood, it has been postulated that these effects may be indirect, involving release of endogenous opio...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2005.10.043

    authors: Whiteside GT,Gottshall SL,Boulet JM,Chaffer SM,Harrison JE,Pearson MS,Turchin PI,Mark L,Garrison AE,Valenzano KJ

    更新日期:2005-12-28 00:00:00

  • Effects of tachykinins on mucus secretion in human bronchi in vitro.

    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

    authors: Rogers DF,Aursudkij B,Barnes PJ

    更新日期:1989-12-19 00:00:00

  • Neuroprotective effect of 3-morpholinosydnonimine against Zn²⁺-induced PC12 cell death.

    abstract::Excessive intracellular accumulation of zinc (Zn(2+)) is neurotoxic and contributes to a number of neuropathological conditions. Here, we investigated the protective effect of 3-morpholinosydnonimine (SIN-1) against Zn(2+)-induced neuronal cell death in differentiated PC12 cells. We found that Zn(2+)-induced PC12 cell...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2014.12.003

    authors: An JM,Moon SA,Hong SY,Kang JW,Seo JT

    更新日期:2015-02-05 00:00:00

  • Neuroprotective effects of an oxyntomodulin analogue in the MPTP mouse model of Parkinson's disease.

    abstract::Oxyntomodulin is a hormone and a growth factor. It activates two receptors, the Glucagon-like peptide 1 (GLP-1) and the glucagon receptor. GLP-1 mimetics are on the market as treatments for type 2 diabetes and are well tolerated. These drugs have shown neuroprotective properties in animal models of neurodegenerative d...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2015.08.038

    authors: Liu W,Li Y,Jalewa J,Saunders-Wood T,Li L,Hölscher C

    更新日期:2015-10-15 00:00:00

  • Cholinergic modulation of separation distress in the domestic chick.

    abstract::The effects of nicotine, carbachol, hexamethonium and scopolamine were investigated on distress vocalizations (DBs) of acutely isolated domestic chicks. Nicotine attenuated, while the antimuscarinic scopolamine increased the frequency of separation-induced DVs. Furthermore, the stress attenuating effects of nicotine w...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(81)90283-1

    authors: Sahley TL,Panksepp J,Zolovick AJ

    更新日期:1981-06-19 00:00:00

  • Insurmountable angiotensin AT1 receptor antagonists: the role of tight antagonist binding.

    abstract::Angiotensin II increased the inositol phosphates production (EC50 = 3.4+/-0.7 nM) in Chinese hamster ovary (CHO) cells expressing the cloned human angiotensin AT1 receptor (CHO-AT1 cells). Coincubation with angiotensin AT1 receptor antagonists produced parallel rightward shifts of the concentration-response curve with...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(99)00205-8

    authors: Fierens FL,Vanderheyden PM,De Backer JP,Vauquelin G

    更新日期:1999-05-14 00:00:00

  • Phosphodiesterase 4-dependent regulation of cyclic AMP levels and leukotriene B4 biosynthesis in human polymorphonuclear leukocytes.

    abstract::Several selective phosphodiesterase 4 inhibitors were found to be potent inhibitors of the N-formyl-Met-Leu-Phe (fMLP)-induced leukotriene B4 biosynthesis by human polymorphonuclear leukocytes with IC50s in the nanomolar range (0.09-26 nM). The rank order of potency was 6-(4-pyridylmethyl)-8-(3-nitrophenyl)quinoline (...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(98)00987-x

    authors: Denis D,Riendeau D

    更新日期:1999-02-19 00:00:00

  • Lipopolysaccharide-induced inhibition of gastric acid and pepsin secretion in rats.

    abstract::We used male Wistar rats to determine the effects of lipopolysaccharide (LPS) on gastric secretion. After pylorus ligation, 24-h fasted rats received i.p. injections of different doses of LPS dissolved in sterile saline. The amounts of gastric acid and pepsin secreted were determined 2, 4 or 8 h after injection. Small...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(90)90256-6

    authors: Uehara A,Okumura T,Okamura K,Takasugi Y,Namiki M

    更新日期:1990-05-31 00:00:00

  • Picrotoxin convulsions and GABA metabolism after injection of anticonvulsants in chicks.

    abstract::Two clinically effective anticonvulsants, phenobarbitone and diazepam, protected 5-day old chicks against picrotoxin convulsions without reducing brain GABA-transaminase activity or raising brain GABA concentration. Ethanolamine-O-sulphate and amino-oxyacetic acid, in doses which inhibited GABA-transminase by at least...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(76)90359-9

    authors: Horton RW,Meldrum BS,Sawaya MC,Stephenson JD

    更新日期:1976-11-01 00:00:00

  • Interaction of the neurosteroid alphaxalone with conventional antiepileptic drugs in different types of experimental seizures.

    abstract::A number of neurosteroids exert antiseizure and/or neuroprotective properties. The aim of this study was to evaluate the effect of the neurosteroid alphaxalone on the protective action of conventional antiepileptics in four seizure tests. Alphaxalone (up to 5 mg/kg) did not exert a significant action against amygdala-...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(02)01975-1

    authors: Borowicz KK,Zadrozniak M,Swiader M,Kowalska A,Kleinrok Z,Czuczwar SJ

    更新日期:2002-08-02 00:00:00

  • Effect of cyclophosphamide on gene expression of cytochromes p450 and beta-actin in the HL-60 cell line.

    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

    authors: Xie HJ,Lundgren S,Broberg U,Finnström N,Rane A,Hassan M

    更新日期:2002-08-09 00:00:00

  • A possible mechanism of choleretic action of 3-(2,4,5-triethoxybenzoyl)-propionic acid (AA-149) in dogs.

    abstract::The choleretic action of 3-(2,4,5-triethoxybenzoyl)propionic acid (AA-149) was studied in anesthetized dogs. AA-149 produced a dose-dependent increase of the bile flow with both i.v. and intrajejunal administration of doses 1 mg/kg and higher. Biliary clearance of 14C-erythritol showed that AA-149 stimulated canalicul...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(78)90050-x

    authors: Satoh H,Kanno M,Maki Y

    更新日期:1978-03-01 00:00:00

  • Mobilization of internal Ca2+ by vasoactive intestinal polypeptide in endothelial cells.

    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

    authors: Low AM,Sormaz L,Kwan CY,Daniel EE

    更新日期:1997-11-27 00:00:00

  • Endogenous nitric oxide counteracts antigen-induced bronchoconstriction.

    abstract::In anesthetized, artificially ventilated guinea pigs immunized against ovalbumin, challenge with aerosolized ovalbumin (0.1 mg) elicited a substantial and sustained increase of insufflation pressure. The inhibitor of endogenous nitric oxide (NO) synthesis, L-NAME (N omega-nitro-L-arginine methylester, 30 mg kg-1 i.v.)...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(93)90532-m

    authors: Persson MG,Friberg SG,Hedqvist P,Gustafsson LE

    更新日期:1993-11-16 00:00:00

  • Modulation of nicotine self-administration in rats by combination therapy with agents blocking alpha 3 beta 4 nicotinic receptors.

    abstract::18-Methoxycoronaridine, a novel iboga alkaloid congener that decreases drug self-administration in several animal models, may be a potential treatment for multiple forms of drug abuse. In previous work, 18-methoxycoronaridine was found to be a somewhat selective antagonist at alpha3beta4 nicotinic receptors; and low d...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(02)01944-1

    authors: Glick SD,Maisonneuve IM,Kitchen BA

    更新日期:2002-07-19 00:00:00

  • Effects of 4-aminopyridine on cat blood pressure in relation to the sympathetic nervous system.

    abstract::The pressor effect of 4-aminopyridine (4-AP) was studied in anesthetized cats and in isolated cat aortic ring preparations. A significant increase in blood pressure (38.9 +/- 11.4 mmHg) was observed following intravenous administration of 4-AP (0.3 mg/kg). The elevated blood pressure lasted for 1.3 h and returned to t...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(85)90343-7

    authors: Yen MH,Lee SH,Ho ST

    更新日期:1985-07-11 00:00:00

  • Effects of adrenoceptor antagonists on the hyperthermia and hyperglycemia induced by prostaglandin F2 alpha in rats.

    abstract::We investigated the effects of intraperitoneal administration of adrenoceptor antagonists to the hyperthermia and hyperglycemia induced by prostaglandin F2 alpha (50 micrograms) injected into the third cerebral ventricle in anesthetized rats. Phentolamine inhibited the hyperthermia and hyperglycemia induced by prostag...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(94)90043-4

    authors: Nonogaki K,Iguchi A,Sakamoto N

    更新日期:1994-09-01 00:00:00

  • Effects of oxcarbazepine and 10-hydroxycarbamazepine on action potential firing and generalized seizures.

    abstract::The anticonvulsant compound oxcarbazepine and its principal 10-monohydroxy metabolite protected potently against electroshock-induced tonic hindlimb extension. Maximal plasma concentrations depended on dose and were reached < or = 1 h after an oral dose of oxcarbazepine and < 2 h after monohydroxy derivative. In mice,...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(94)90787-0

    authors: Wamil AW,Schmutz M,Portet C,Feldmann KF,McLean MJ

    更新日期:1994-12-27 00:00:00

  • The choleretic effects of N-acetylglucosaminides, major urinary metabolites of ursodeoxycholic acid, in bile fistula rats.

    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

    authors: Iwaki T,Hirabayashi N,Miyazawa N,Takeuchi Y,Ishizaki K,Sakakura H,Kasai H,Maeda M,Araki T

    更新日期:1998-12-11 00:00:00

  • Calcium-dependent stimulation of acetylcholine release by substance P and vasoactive intestinal polypeptide.

    abstract::In the guinea-pig myenteric plexus-longitudinal muscle preparation from the small intestine, the release of acetylcholine evoked by substance P and vasoactive intestinal polypeptide was examined in vitro. Both neuropeptides stimulated efflux of [3H]acetylcholine from myenteric neurons in a calcium-dependent manner. Th...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(86)90547-9

    authors: Yau WM,Dorsett JA,Youther ML

    更新日期:1986-01-21 00:00:00

  • Biphasic effect of a kappa-opioid receptor agonist on plasma oxytocin levels in rats.

    abstract::The effect of the kappa-opioid receptor agonist, bremazocine, on plasma oxytocin levels in rats was measured by a sensitive radioimmunoassay. Initially, a decrease in plasma oxytocin levels was seen 30 min after injection. This was in accordance with the bremazocine inhibition of oxytocin release after submaximal elec...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(89)90681-x

    authors: Grell S,Fjalland B,Christensen JD

    更新日期:1989-07-04 00:00:00

  • Influence of omega-conotoxin on morphine analgesia and withdrawal syndrome in rats.

    abstract::The effect of omega-conotoxin on opiate analgesia and withdrawal syndrome was investigated in rats. omega-Conotoxin given i.c.v. and i.p. caused weak analgesia in the tail-flick test. When the toxin (20 ng/rat) was given i.c.v. immediately before morphine (1.5 micrograms/rat i.c.v.) the resultant analgesic effect was ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(92)90149-x

    authors: Basilico L,Parolaro D,Rubino T,Gori E,Giagnoni G

    更新日期:1992-07-21 00:00:00

  • Comparison of two alpha-noradrenergic agonists (clonidine and guanfacine) on norepinephrine turnover in the cortex of rats during morphine abstinence.

    abstract::The effects of the alpha-agonists clonidine and guanfacine on rat cortical norepinephrine turnover during morphine withdrawal were assessed. Cortical norepinephrine levels were measured, after administration of alpha-methyl-p-tyrosine, by fluorometric assay. Chronic treatment with morphine did not affect norepinephrin...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(81)90368-x

    authors: Zigun JR,Bannon MJ,Roth RH

    更新日期:1981-04-09 00:00:00

  • Inhibition of the vascular-endothelial growth factor-induced intracellular signaling and mitogenesis of human endothelial cells by epigallocatechin-3 gallate.

    abstract::Galloyl group-containing catechins, such as epigallocatechin-3 gallate, inhibit receptor tyrosine kinase activity of several growth factor receptors. This study investigated the effects of epigallocatechin-3 gallate, as compared to epicatechin, on vascular endothelial growth factor-induced intracellular signaling and ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2003.10.029

    authors: Neuhaus T,Pabst S,Stier S,Weber AA,Schrör K,Sachinidis A,Vetter H,Ko YD

    更新日期:2004-01-12 00:00:00

  • Claulansine F promoted the neuronal differentiation of neural stem and progenitor cells through Akt/GSK-3β/β-catenin pathway.

    abstract::The persistence of neurogenesis raises the idea that neurons produced by the resident or transplanted neural stem cells could replace the neurons lost from brain injury or neurodegenerative disease. Therefore, compounds or methods for promoting neuronal differentiation become the focus of neurodegenerative disease the...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2016.05.017

    authors: Huang JY,Ma YZ,Yuan YH,Zuo W,Chu SF,Liu H,Du GH,Zhang DM,Chen NH

    更新日期:2016-09-05 00:00:00

  • Potentiation of MK-801-induced breathing impairment by 2,3-dihydroxy-6-nitro-7-sulfamoyl-benzo(F)quinoxaline.

    abstract::The purpose of our study was to examine whether a significant interaction occurs between NMDA and non-NMDA receptor antagonists on respiratory function. For this purpose chloralose-anesthetized cats were used and respiratory minute volume (VE), tidal volume (Vt) respiratory rate (f), inspiratory and expiratory duratio...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(94)90569-x

    authors: McManigle JE,Taveira DaSilva AM,Dretchen KL,Gillis RA

    更新日期:1994-01-24 00:00:00