Physiological and pharmacological characterization of the spinal tachykinin NK2 receptor.

Abstract:

:The goal of these investigations was to study the role of tachykinin NK2 receptors in neonatal spinal cords using the selective NK2 receptor agonist [beta-Ala8]neurokinin A-(4-10) and the new NK2 receptor antagonist GR 94800. Experiments were performed with superfused hemisected rat and gerbil spinal cords. Dorsal roots were electrically stimulated and the synaptically elicited responses and the DC-potentials were recorded extracellularly from the corresponding ventral roots. [beta-Ala8]neurokinin A-(4-10) depolarized ventral roots (0.01-10 microM) and increased their spontaneous activity in a concentration-dependent manner. These effects of [beta-Ala8]neurokinin A-(4-10) were reduced by GR 94800. The action of GR 94800 was selective because the depolarizing effects of similar magnitude evoked by the NK1 receptor agonist [Sar9,Met(O2)11]substance P were not affected by GR 94800. The pA2 values of GR 94800 amounted to 6.0 +/- 0.4 in the rat and 5.4 +/- 0.3 in the gerbil. The NK2 receptor agonist was more potent in the rat than in the gerbil. The estimated EC50 (mean +/- S.E.M.) was found to be 3.9 + 6.0/-1.3 microM in the rat and 2.4 + 2.9/-1.3 microM in the gerbil spinal cord. The NK2 receptor agonist [beta-Ala8]neurokinin A-(4-10) potentiated the monosynaptic reflex evoked by dorsal root stimulation. The potentiation manifested itself as an increase in the amplitude of the early component of the response. The receptor type mediating this effect could not be elucidated. The potentiation ranged between 30 +/- 27 and 110 +/- 36% (0.3 and 10 microM), respectively.(ABSTRACT TRUNCATED AT 250 WORDS)

journal_name

Eur J Pharmacol

authors

Lepre M,Olpe HR,Evans RH,Brugger F

doi

10.1016/0014-2999(94)90053-1

subject

Has Abstract

pub_date

1994-06-02 00:00:00

pages

23-31

issue

1-2

eissn

0014-2999

issn

1879-0712

pii

0014-2999(94)90053-1

journal_volume

258

pub_type

杂志文章
  • Theophylline inhibits late asthmatic reactions induced by toluene diisocyanate in sensitised subjects.

    abstract::Toluene diisocyanate (TDI)-induced asthma is a frequent occupational airway disease. To determine whether a calibrated dosage of oral slow-release theophylline inhibits asthmatic reactions and the associated increase of airway responsiveness to methacholine induced by TDI, we examined six asthmatic subjects who develo...

    journal_title:European journal of pharmacology

    pub_type: 临床试验,杂志文章,随机对照试验

    doi:10.1016/0926-6917(92)90010-a

    authors: Crescioli S,De Marzo N,Boschetto P,Spinazzi A,Plebani M,Mapp CE,Fabbri LM,Ciaccia A

    更新日期:1992-05-01 00:00:00

  • Mechanisms of phenylalanine-induced pressor effects in conscious rats.

    abstract::Phenylalanine and tyrosine reportedly decrease blood pressure in conscious restrained rats. However, tyrosine has recently been found to increase blood pressure in anesthetized animals, questioning the generality of findings obtained in restrained animals. The present study therefore evaluated the effects of phenylala...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(89)90494-9

    authors: Yourick DL,Tessel RE

    更新日期:1989-01-31 00:00:00

  • Compared properties of central and peripheral binding sites for phencyclidine.

    abstract::Phencyclidine and its derivatives bind specifically and reversibly to rat brain and peripheral organs. Binding characteristics are different in brain, lung, kidney, heart and liver. Affinities of phencyclidines for the brain receptor but not those for peripheral organs are correlated with the pharmacological activitie...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(80)90065-5

    authors: Vincent JP,Vignon J,Kartalovski B,Lazdunski M

    更新日期:1980-11-07 00:00:00

  • Factors contributing to differences in the regulation of cGMP in isolated porcine pulmonary vessels.

    abstract::Guanosine 3',5'-cyclic monophosphate (cGMP) is an important second messenger in many biological systems including vascular smooth muscle where it mediates relaxation. Cellular levels of cGMP are regulated primarily by three enzymes; nitric oxide (NO) synthase, soluble guanylate cyclase, and cGMP-phosphodiesterase. Bas...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(98)00307-0

    authors: Bina S,Hart JL,Sei Y,Muldoon SM

    更新日期:1998-06-19 00:00:00

  • N-3 polyunsaturated fatty acids modulate B cell activity in pre-clinical models: Implications for the immune response to infections.

    abstract::B cell antigen presentation, cytokine production, and antibody production are targets of pharmacological intervention in inflammatory and infectious diseases. Here we review recent pre-clinical evidence demonstrating that pharmacologically relevant levels of n-3 polyunsaturated fatty acids (PUFA) derived from marine f...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章,评审

    doi:10.1016/j.ejphar.2015.03.100

    authors: Whelan J,Gowdy KM,Shaikh SR

    更新日期:2016-08-15 00:00:00

  • Nicorandil normalizes prolonged repolarisation in the first transgenic rabbit model with Long-QT syndrome 1 both in vitro and in vivo.

    abstract::Transgenic rabbits expressing loss-of-function pore mutants of the human gene KCNQ1 (K(v)LQT1-Y315S) have a Long QT-Syndrome 1 (LQT1) phenotype. We evaluated for the first time the effect of nicorandil, an opener of ATP-sensitive potassium channels, and of isoproterenol on cardiac action potential duration and heart r...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2010.10.016

    authors: Biermann J,Wu K,Odening KE,Asbach S,Koren G,Peng X,Zehender M,Bode C,Brunner M

    更新日期:2011-01-10 00:00:00

  • Association of microvascular leakage with induction of nitric oxide synthase: effects of nitric oxide synthase inhibitors in various organs.

    abstract::Endotoxin (Escherichia coli lipopolysaccharide 0111:B4, 3 mg/kg i.v.) induced the expression of a calcium-independent nitric oxide (NO) synthase, determined after 5 h in cardiac, hepatic, pulmonary and renal tissues, as assessed by the conversion of radiolabelled L-arginine to L-citrulline. This widespread induction o...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(95)00281-o

    authors: László F,Whittle BJ,Evans SM,Moncada S

    更新日期:1995-09-05 00:00:00

  • Anti-cancer activity of two novel heterocyclic compounds through modulation of VEGFR and miR-122 in mice bearing Ehrlich ascites carcinoma.

    abstract::Metastasis in breast cancer is a leading cause of mortality among women in many countries. This study investigated the anti-cancer role of benzoimidazoquinazoline and benzimidazotriazin; two novel compounds that were designed, synthesized, structurally elucidated, and biologically evaluated as potent anti-angiogenic a...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2020.173747

    authors: Hazem RM,Mohamed AA,Ghareb N,Mehanna ET,Mesbah NM,Abo-Elmatty DM,Elgawish MS

    更新日期:2021-02-05 00:00:00

  • Effects of N-methyl-D-aspartate antagonists on the cough reflex.

    abstract::The effects of antagonists of N-methyl-D-aspartate (NMDA) on the capsaicin-induced cough reflex in rats were studied. Intracisternal (i. cist.) injection of MK-801, a non-competitive antagonist of NMDA, significantly decreased the number of coughs in a dose-dependent manner. The competitive antagonists of NMDA, 2-DL-a...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(89)90560-8

    authors: Kamei J,Tanihara H,Igarashi H,Kasuya Y

    更新日期:1989-09-13 00:00:00

  • Dopamine D(3) receptor as a new pharmacological target for the treatment of depression.

    abstract::A substantial proportion of depressed patients do not respond to current antidepressant drug therapies. So far, antidepressant drugs have been developed based on the "monoaminergic hypothesis" of depression, which considers a synaptic deficiency in 5-hydroxytryptamine (5-HT; serotonin) or noradrenaline as main cause. ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章,评审

    doi:10.1016/j.ejphar.2013.07.022

    authors: Leggio GM,Salomone S,Bucolo C,Platania C,Micale V,Caraci F,Drago F

    更新日期:2013-11-05 00:00:00

  • Angiotensin II AT1 receptors in rat superior cervical ganglia: characterization and stimulation of phosphoinositide hydrolysis.

    abstract::Angiotensin II receptor number was higher in superior cervical ganglia of 2-week-old when compared to 8-week-old rats. In both young and adult rats, specific binding of [125I][Sar1]angiotensin II was displaced competitively by the AT1-receptor antagonist DuP 753 but not by the AT2-receptor competitor PD 123177. In gan...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0922-4106(91)90079-w

    authors: Strömberg C,Tsutsumi K,Viswanathan M,Saavedra JM

    更新日期:1991-12-12 00:00:00

  • Effects of baicalein and alpha-tocopherol on lipid peroxidation, free radical scavenging activity and 12-O-tetradecanoylphorbol acetate-induced ear edema.

    abstract::The effects of baicalein, a flavonoid, and alpha-tocopherol (vitamin E) on lipid peroxidation in rat forebrain homogenates, on free radical scavenging action against diphenyl-p-picrylhydrazyl (DPPH), and on 12-O-tetradecanoylphorbol acetate (TPA)-induced ear edema in mice were studied. Baicalein inhibited lipid peroxi...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(92)90700-e

    authors: Hara H,Sukamoto T,Ohtaka H,Abe K,Tatumi Y,Saito Y,Suzuki A,Tsukamoto G

    更新日期:1992-10-20 00:00:00

  • Ca2+ channel blockers prevent seizures induced by a class of K+ channel inhibitors.

    abstract::Intracerebroventricular injection into rats of mast-cell degranulating peptide (MCD), dendrotoxin I (DTXI) and 4-aminopyridine (4-AP), three blockers of a subclass of K+ channels, elicited epileptiform wave bursts and convulsions. Three different types of L-type Ca2+ channel inhibitors (+)PN 200-110, a 1,4-dihydropyri...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(89)90669-9

    authors: Gandolfo G,Gottesmann C,Bidard JN,Lazdunski M

    更新日期:1989-01-24 00:00:00

  • Blockade of cannabinoid CB1 receptors alters contextual learning and memory.

    abstract::The endocannabinoid system appears to have an important role in specific aspects of learning and memory, yet there has been no systematic study of the role of cannabinoid receptors in contextual fear conditioning. The present study examined the effects of cannabinoid CB(1) receptor blockade on the acquisition, consoli...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2006.04.017

    authors: Arenos JD,Musty RE,Bucci DJ

    更新日期:2006-06-13 00:00:00

  • Effects of platelet activating factor receptor antagonists on intracellular platelet activating factor function in neutrophils.

    abstract::We investigated the effects of the platelet activating factor (PAF) receptor antagonists, SM-12502 ((+)-cis-3,5-dimethyl-2-(pyridyl)- thiazolidin-4-one hydrochloride), WEB-2086 (3-(4-(2-chlorphenyl)-9-methyl-6H-thieno(3,2-f)-(1,2,4)triazolo(4, 3- a)(1,4)diazepin-2-yl)-1-(4-morpholinyl)-1-propanone) and RP-48740 (3-(3-...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0922-4106(94)90037-x

    authors: Koike H,Imanishi N,Natsume Y,Morooka S

    更新日期:1994-11-15 00:00:00

  • The effect of acute simvastatin administration on the severity of arrhythmias resulting from ischaemia and reperfusion in the canine: Is there a role for nitric oxide?

    abstract::The present study has examined the effects and the possible mechanisms of a single dose of simvastatin on the severity of arrhythmias resulting from a 25min occlusion and reperfusion of the left anterior descending coronary artery in anaesthetized (chloralose and urethane) dogs. The control animals (n=16) were given t...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2014.03.021

    authors: Kisvári G,Kovács M,Gardi J,Seprényi G,Kaszaki J,Végh Á

    更新日期:2014-06-05 00:00:00

  • Comparison of several new 5-lipoxygenase inhibitors in a rat Arthus pleurisy model.

    abstract::The 5-lipoxygenase inhibitors WY-50,295 tromethamine, A-64,077, L-663,536 and ICI-207,968 were compared in a reverse passive Arthus reaction-induced pleurisy model of eicosanoid biosynthesis in the rat. When a 1 h pretreatment schedule was employed, all four inhibitors equivalently blocked leukotriene B4 (LTB4) produc...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(91)90196-w

    authors: Berkenkopf JW,Weichman BM

    更新日期:1991-01-25 00:00:00

  • Anti-arrhythmic and electrophysiological effects of the endothelin receptor antagonists, BQ-123 and PD161721.

    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

    authors: Crockett TR,Scott GA,McGowan NW,Kane KA,Wainwright CL

    更新日期:2001-11-30 00:00:00

  • Effects of (+)-S-12967 and (-)-S-12968, two enantiomers of a new slow-acting 1,4-dihydropyridine, on rat coronary resistance arteries.

    abstract::The action of (+)-S-12967 and (-)-S-12968, two isomers of a new 1,4-dihydropyridine molecule (2-(-7-amino-2,5-dioxaheptyl)-3-ethoxycarbonyl-4-(2,3-dichlorop hen yl)-5-methoxycarbonyl-6-methyl 1,4-dihydropyridine), was studied on responses of rat isolated coronary resistance arteries (i.d. about 230 microns) to K+, Ca...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(93)90501-8

    authors: Prieto D,Mulvany MJ,Nyborg NC

    更新日期:1993-07-06 00:00:00

  • Neocuproine inhibits the decomposition of endogenous S-nitrosothiol by ultraviolet irradiation in the mouse gastric fundus.

    abstract::In the present study, we investigated whether copper ions are involved in the decomposition of endogenous S-nitrosothiols by ultraviolet (UV) light irradiation in the mouse gastric fundus. The effects of copper ions and chelators of copper(I) and copper(II), neocuproine and cuprozine, respectively, were studied on rel...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2003.11.036

    authors: Ogülener N,Ergün Y

    更新日期:2004-02-06 00:00:00

  • Kinetic studies on the interaction of nonlabeled antagonists with the angiotensin II receptor.

    abstract::Angiotensin AT1 receptor antagonists are divided into two types, surmountable and insurmountable, based on the way they inhibit angiotensin II-induced vasoconstriction. To elucidate what causes the difference, we studied how antagonists associate with and dissociate from AT1 receptor sites in rat liver membranes. Thre...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0922-4106(95)90103-5

    authors: Hara M,Kiyama R,Nakajima S,Kawabata T,Kawakami M,Ohtani K,Itazaki K,Fujishita T,Fujimoto M

    更新日期:1995-04-28 00:00:00

  • Inhibitors of arachidonate-regulated calcium channel signaling suppress triggered activity induced by the late sodium current.

    abstract::Disturbances in myocyte calcium homeostasis are hypothesized to be one cause for cardiac arrhythmia. The full development of this hypothesis requires (i) the identification of all sources of arrhythmogenic calcium and (ii) an understanding of the mechanism(s) through which calcium initiates arrhythmia. To these ends w...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2013.12.020

    authors: Wolkowicz P,Umeda PK,Sharifov OF,White CR,Huang J,Mahtani H,Urthaler F

    更新日期:2014-02-05 00:00:00

  • Role of GABA B receptors in the endomorphin-1-, but not endomorphin-2-, induced dopamine efflux in the nucleus accumbens of freely moving rats.

    abstract::In vivo microdialysis was used to study the effects of the locally applied GABA B receptor antagonist 2-hydroxysaclofen and GABA B receptor agonist baclofen on the basal dopamine efflux as well as on the endomorphin-1- and endomorphin-2-induced dopamine efflux in the nucleus accumbens of freely moving rats. 2-Hydroxys...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2007.12.008

    authors: Saigusa T,Aono Y,Mizoguchi N,Iwakami T,Takada K,Oi Y,Ueda K,Koshikawa N,Cools AR

    更新日期:2008-03-10 00:00:00

  • Ethanol differentially modulates the expression and activity of cell cycle regulatory proteins in rat aortic smooth muscle cells.

    abstract::The aim of this study was to determine the effect of ethanol on cell cycle events during the G(1) and S phases in cultured vascular smooth muscle cells (VSMC). Flow cytometric analysis for the DNA content in rat aortic VSMC indicated that following ethanol treatment, the cell population in the G(0)/G(1) phase increase...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(02)01761-2

    authors: Sayeed S,Cullen JP,Coppage M,Sitzmann JV,Redmond EM

    更新日期:2002-06-12 00:00:00

  • Pyrrolidine dithiocarbamate protects against scopolamine-induced cognitive impairment in rats.

    abstract::Alzheimer's disease (AD) is a chronic neurodegenerative disorder that leads to disturbances of cognitive functions. Although the primary cause of AD remains unclear, brain acetylcholine deficiency, oxidative stress and neuroinflammation may be considered the principal pathogenic factors. The present study was construc...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2013.11.008

    authors: Abd-El-Fattah MA,Abdelakader NF,Zaki HF

    更新日期:2014-01-15 00:00:00

  • Deltorphin II enhances extracellular levels of dopamine in the nucleus accumbens via opioid receptor-independent mechanisms.

    abstract::The effects of the delta2-opioid receptor agonist, deltorphin II, on extracellular levels of dopamine in the rat nucleus accumbens were investigated in awake animals by in vivo brain microdialysis. In agreement with previous studies, perfusion of deltorphin II (50.0 nmol) into the nucleus accumbens significantly incre...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2004.03.028

    authors: Murakawa K,Hirose N,Takada K,Suzuki T,Nagase H,Cools AR,Koshikawa N

    更新日期:2004-04-26 00:00:00

  • 12-Deoxyphorbol 13-palmitate mediated cell growth inhibition, G2-M cell cycle arrest and apoptosis in BGC823 cells.

    abstract::The highly toxic monomer 12-deoxyphorbol 13-palmitate (G) was extracted from the roots of Euphorbia fischeriana. Our experimental data confirmed studies showing that 12-deoxyphorbol 13-palmitate had certain antitumor activities. The MTT method, soft agar experiments, and nude mouse tumor experiments proved that 12-deo...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2012.11.015

    authors: Xu HY,Chen ZW,Li H,Zhou L,Liu F,Lv YY,Liu JC

    更新日期:2013-01-30 00:00:00

  • Role of nitric oxide in systemic effect of theophylline on mouse body temperature.

    abstract::In the present study, the interaction of nitric oxide synthase (NOS) inhibitors, L-NAME (N(G)-nitro-L-arginine methyl ester HCl) and L-NA (N(omega)-nitro-L-arginine), and its precursor, L-arginine (2-(S)-2-amino-5-[(aminoiminomethyl)amino] pentatonic acid), with theophylline on mouse body temperature was studied. Intr...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(02)02159-3

    authors: Zarrindast MR,Adl M,Sharifzadeh M,Bahreini T

    更新日期:2002-09-06 00:00:00

  • Ameliorating effects of 1,8-cineole on LPS-induced human umbilical vein endothelial cell injury by suppressing NF-κB signaling in vitro.

    abstract::1,8-Cineole (also known as eucalyptol) is a monoterpene that occurs naturally in many aromatic plants, 1,8-cineole has been reported to ameliorate dysfunction of endothelial cells. However, the mechanism of action of 1,8-cineole is incompletely understood. We investigated the protective effect of 1,8-cineole on lipopo...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2016.07.039

    authors: Linghu K,Lin D,Yang H,Xu Y,Zhang Y,Tao L,Chen Y,Shen X

    更新日期:2016-10-15 00:00:00

  • Time course of phorbol ester-induced contraction and protein kinase C activation in rat aorta.

    abstract::This study investigates the relationship between the rate of phorbol ester-induced contraction of intact rat aorta and protein kinase C activation, as assessed by the translocation of protein kinase C from the cytosolic to the particulate fraction. Aorta was exposed to Ca(2+)-free physiologic salt solution prior to ph...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0922-4106(95)90001-2

    authors: Bazan E,Campbell AK,Rapoport RM

    更新日期:1995-08-15 00:00:00