Non-specific activity of (+/-)-CP-96,345 in models of pain and inflammation.

Abstract:

:The non-peptide NK1 receptor antagonist, CP-96,345, and its 2R,3R enantiomer CP-96,344, which is not an NK1 receptor antagonist (IC50 > 10 microM), were evaluated for antinociceptive and anti-inflammatory activities in several classical models of pain and inflammation in the rat. Both CP-96,345 and CP-96,344 reduced carrageenin-induced paw oedema and hyperalgesia, and attenuated the second phase of formalin-induced paw licking with equal potency. These results indicate that NK1 antagonism is not responsible for the activity of (+/-)-CP-96,345 in the above animal models.

journal_name

Br J Pharmacol

authors

Nagahisa A,Asai R,Kanai Y,Murase A,Tsuchiya-Nakagaki M,Nakagaki T,Shieh TC,Taniguchi K

doi

10.1111/j.1476-5381.1992.tb12737.x

subject

Has Abstract

pub_date

1992-10-01 00:00:00

pages

273-5

issue

2

eissn

0007-1188

issn

1476-5381

journal_volume

107

pub_type

杂志文章
  • Ion channel modulation by NS 1619, the putative BKCa channel opener, in vascular smooth muscle.

    abstract::1. The effects of NS 1619, the putative BKCa channel opener, were investigated on rat intact portal veins and on single smooth muscle cells enzymatically separated from the same tissue. 2. Under whole-cell patch clamp conditions with K-rich pipettes, exposure of single cells held at -10 mV to NS 1619 (10-33 microM) in...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1994.tb17171.x

    authors: Edwards G,Niederste-Hollenberg A,Schneider J,Noack T,Weston AH

    更新日期:1994-12-01 00:00:00

  • Oxidative and non-oxidative mechanisms of neuronal cell death and apoptosis by L-3,4-dihydroxyphenylalanine (L-DOPA) and dopamine.

    abstract::1. The present study was designed to evaluate the nature of intervening agents in L-DOPA- and dopamine-induced neurotoxicity in Neuro-2A cells. 2. In the absence of cells and in conditions of light protection, at 37 degrees C, L-DOPA or dopamine (1 mM) in culture medium degraded spontaneously in a time-dependent manne...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1038/sj.bjp.0704982

    authors: Pedrosa R,Soares-da-Silva P

    更新日期:2002-12-01 00:00:00

  • Nitric oxide is not just blowing in the wind.

    abstract:LINKED ARTICLES:This article is part of a themed section on Nitric Oxide 20 Years from the 1998 Nobel Prize. To view the other articles in this section visit http://onlinelibrary.wiley.com/doi/10.1111/bph.v176.2/issuetoc. ...

    journal_title:British journal of pharmacology

    pub_type: 社论

    doi:10.1111/bph.14540

    authors: Ignarro LJ

    更新日期:2019-01-01 00:00:00

  • The role of several alpha(1)- and alpha(2)-adrenoceptor subtypes mediating vasoconstriction in the canine external carotid circulation.

    abstract::1. It has recently been shown that both alpha(1)- and alpha(2)-adrenoceptors mediate vasoconstriction in the canine external carotid circulation. The present study set out to identify the specific subtypes (alpha(1A), alpha(1B) and alpha(1D) as well as alpha(2A), alpha(2B) and alpha(2C)) mediating the above response. ...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1038/sj.bjp.0703915

    authors: Willems EW,Valdivia LF,Saxena PR,Villalón CM

    更新日期:2001-03-01 00:00:00

  • Characterization of the functional muscarinic receptors in the rat urinary bladder.

    abstract::1. Muscarinic receptors mediating contraction of the rat urinary bladder were characterized functionally in vitro by use of atropine, 4-diphenylacetoxy-N-methylpiperidine methiodide (4-DAMP methiodide), 4-diphenylacetoxy-N-(2-chloroethyl)-piperidine hydrochloride (4-DAMP mustard), hexahydro-sila-diphenidol hydrochlori...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1995.tb15065.x

    authors: Longhurst PA,Leggett RE,Briscoe JA

    更新日期:1995-10-01 00:00:00

  • Vascular actions of MDMA involve alpha1 and alpha2-adrenoceptors in the anaesthetized rat.

    abstract::We have investigated the effects of methylenedioxymethamphetamine (MDMA, 'ecstasy'), i.v., on diastolic blood pressure (DBP) in pithed and pentobarbitone anaesthetized rats. In pithed rats, the non-selective 5-HT receptor antagonist methiothepin (0.1 mg kg(-1)) and the alpha2-adrenoceptor antagonists methoxyidazoxan a...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1038/sj.bjp.0704094

    authors: McDaid J,Docherty JR

    更新日期:2001-06-01 00:00:00

  • Attenuation by chlormethiazole administration of the rise in extracellular amino acids following focal ischaemia in the cerebral cortex of the rat.

    abstract::1. In vivo microdialysis has been used to investigate the concentration of various amino acids and lactate in the extracellular fluid of the rat cortex following focal ischaemia, the probe being placed in the core of the infarct area. 2. An ischaemic infarct was produced in the cortex by use of a photochemical dye (Ro...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1994.tb13050.x

    authors: Baldwin HA,Williams JL,Snares M,Ferreira T,Cross AJ,Green AR

    更新日期:1994-05-01 00:00:00

  • Antithrombotic activity of a monoclonal antibody inducing the substrate form of plasminogen activator inhibitor type 1 in rat models of venous and arterial thrombosis.

    abstract::1. Elevated plasminogen activator inhibitor 1 (PAI-1) is a risk factor for thrombosis, and inhibitors of the interaction between PAI-1 and tissue plasminogen activator (t-PA) have antithrombotic and prothrombolytic activity in animals. We describe the antithrombotic effects in the rat of a monoclonal antibody (MA33H1)...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1038/sj.bjp.0702030

    authors: Berry CN,Lunven C,Lechaire I,Girardot C,O'Connor SE

    更新日期:1998-09-01 00:00:00

  • Effect of low-dose treatment with selegiline on dopamine transporter (DAT) expression and amphetamine-induced dopamine release in vivo.

    abstract::1. Chronic treatment with low doses of the selective monoamine oxidase (MAO) type B inhibitors selegiline [(-)-deprenyl] and rasagiline, causes elevation in extracellular level of 3,4-dihydroxyphenylethylamine (dopamine) in the rat striatum in vivo (Lamensdorf et al., 1996). The present study was carried out to determ...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1038/sj.bjp.0702389

    authors: Lamensdorf I,Porat S,Simantov R,Finberg JP

    更新日期:1999-02-01 00:00:00

  • Inhibition of neuromuscular transmission in the myenteric plexus of guinea-pig ileum by omega-conotoxins GVIA, MVIIA, MVIIC and SVIB.

    abstract::1. The effects of a number of Ca2+ channel blockers on the transmural electrical stimulation or receptor agonist-elicited contractile responses of guinea-pig ileum were compared. 2. omega-Conotoxins (MVIIA, GVIA, SVIB and MVIIC), but not omega-agatoxin IVA, completely blocked the twitch responses evoked by low frequen...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1996.tb15470.x

    authors: Hong SJ,Roan YF,Chang CC

    更新日期:1996-06-01 00:00:00

  • Gallium modulates osteoclastic bone resorption in vitro without affecting osteoblasts.

    abstract:BACKGROUND AND PURPOSE:Gallium (Ga) has been shown to be effective in the treatment of disorders associated with accelerated bone loss, including cancer-related hypercalcemia and Paget's disease. These clinical applications suggest that Ga could reduce bone resorption. However, few studies have studied the effects of G...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.2010.00665.x

    authors: Verron E,Masson M,Khoshniat S,Duplomb L,Wittrant Y,Baud'huin M,Badran Z,Bujoli B,Janvier P,Scimeca JC,Bouler JM,Guicheux J

    更新日期:2010-04-01 00:00:00

  • Clinical and preclinical evidence of somatosensory involvement in amyotrophic lateral sclerosis.

    abstract::Amyotrophic lateral sclerosis (ALS) is the most common motor neuron neurodegenerative disease. Although it has been classically considered as a disease limited to the motor system, there is increasing evidence for the involvement of other neural and non-neuronal systems. In this review, we will discuss currently exist...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章,评审

    doi:10.1111/bph.15202

    authors: Riancho J,Paz-Fajardo L,López de Munaín A

    更新日期:2020-07-16 00:00:00

  • [(3)H]-SB-269970--A selective antagonist radioligand for 5-HT(7) receptors.

    abstract::Binding of the 5-HT(7) receptor antagonist radioligand [(3)H]-SB-269970 to human 5-HT(7(a)) receptors expressed in HEK293 cell membranes (h5-HT(7(a))/293) and to guinea-pig cerebral cortex membranes, was characterized and compared with [(3)H]-5-CT binding. [(3)H]-SB-269970 (1 nM) showed full association with h5-HT(7(a...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1038/sj.bjp.0703318

    authors: Thomas DR,Atkinson PJ,Ho M,Bromidge SM,Lovell PJ,Villani AJ,Hagan JJ,Middlemiss DN,Price GW

    更新日期:2000-05-01 00:00:00

  • A comparison of the inhibitory effects of sodium nitroprusside, pinacidil and nifedipine on pressor response to NG-nitro-L-arginine.

    abstract::1. The inhibitory effects of sodium nitroprusside (SNP), a nitric oxide (NO) donor, on mean arterial pressure (MAP) responses to NG-nitro-L-arginine (L-NNA) (NO synthase inhibitor), angiotensin II (AII) and noradrenaline (NA) were compared with those of pinacidil (KATP channel opener) and nifedipine (L-type calcium an...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1993.tb12816.x

    authors: Wang YX,Zhou T,Pang CC

    更新日期:1993-02-01 00:00:00

  • Differences in the pharmacological properties of rat and chicken brain fatty acid amidohydrolase.

    abstract::The pharmacological properties of fatty acid amidohydrolase (FAAH) were investigated in brains of 35-day-old chickens, since nothing is known about the enzyme in avian species. FAAH activity towards both [(3)H]-palmitoylethanolamide (PEA) [K(M)=1.5 microM] and [(3)H]-anandamide (AEA) [K(M)=5.4 microM] was demonstrated...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1038/sj.bjp.0703569

    authors: Fowler CJ,Börjesson M,Tiger G

    更新日期:2000-10-01 00:00:00

  • Suppression of K(+)-induced hyperpolarization by phenylephrine in rat mesenteric artery: relevance to studies of endothelium-derived hyperpolarizing factor.

    abstract::In intact mesenteric arteries, increasing [K(+)]o by 5 mM hyperpolarized both endothelial and smooth muscle cells. Subsequent exposure to 10 microM phenylephrine depolarized both cell types which were then repolarized by a 5 mM increase in [K(+)]o. In endothelium-denuded vessels, increasing [K(+)]o by 5 mM hyperpolari...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1038/sj.bjp.0704256

    authors: Richards GR,Weston AH,Burnham MP,Félétou M,Vanhoutte PM,Edwards G

    更新日期:2001-09-01 00:00:00

  • The role of extracellular calcium in the contractions produced by acetylcholine in chronically denervated muscle.

    abstract::1 Acetylcholine-induced contractions of the isolated chronically denervated soleus muscle of the mouse consist of two phases, but both phases are equivalent to the contracture phase seen in vivo.2 Low [Ca(2+)](0) (0.5-1.5 mM) augmented peak tension, as well as the rate of relaxation, of the first phase, but inhibited ...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1977.tb07556.x

    authors: Hall MT,Maleque MA,Wadsworth RM

    更新日期:1977-12-01 00:00:00

  • A tachykinin antagonist inhibits gastric emptying and gastrointestinal transit in the rat.

    abstract::The effect of a substance P antagonist, [D-Pro2, D-Trp7,9]-substance P (SPA), on gastric emptying and gastrointestinal transit in the rat was studied in order to elucidate a possible physiological role of endogenous substance P and other tachykinins in gastrointestinal motility. SPA was given by intraperitoneal inject...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1986.tb11144.x

    authors: Holzer P,Holzer-Petsche U,Leander S

    更新日期:1986-11-01 00:00:00

  • The effect of indomethacin on the cardiovascular and metabolic responses to E. coli endotoxin in the cat.

    abstract::1 The response of pentobarbitone-anaesthetized cats to the intravenous administration of E. coli endotoxin (2 mg/kg) consisted of acute pulmonary vasoconstriction (3-5 min after the injection) and a secondary shock phase characterized by delayed systemic hypotension, decreased central venous pressure and cardiac outpu...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1974.tb08559.x

    authors: Parratt JR,Sturgess RM

    更新日期:1974-02-01 00:00:00

  • Age and the antihypertensive effect of aspirin in rats.

    abstract::1. We previously showed that chronic exposure to aspirin (100 mg kg-1 daily, by mouth) is effective in preventing the onset of hypertension in young (28-84 day old) spontaneously hypertensive rats (SHRs). This is contrary to what others have reported using older SHRs. 2. Renal prostaglandin F2 alpha was also reduced i...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1988.tb11585.x

    authors: Tuttle RS,Yager J,Northrup N

    更新日期:1988-07-01 00:00:00

  • An in vivo role for Rho kinase activation in the tumour vascular disrupting activity of combretastatin A-4 3-O-phosphate.

    abstract:BACKGROUND AND PURPOSE:Combretastatin A-4 3-O-phosphate (CA4P) is in clinical trial as a tumour vascular disrupting agent (VDA) but the cause of blood flow disruption is unclear. We tested the hypothesis that activation of Rho/Rho kinase (ROCK) is fundamental to the effects of this drug in vivo. EXPERIMENTAL APPROACH:...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/bph.12817

    authors: Williams LJ,Mukherjee D,Fisher M,Reyes-Aldasoro CC,Akerman S,Kanthou C,Tozer GM

    更新日期:2014-11-01 00:00:00

  • PYY-preferring receptor in the dorsal vagal complex and its involvement in PYY stimulation of gastric acid secretion in rats.

    abstract::1. Microinjection of peptide YY (PYY, 7-46 pmol) into the dorsal vagal complex (DVC) stimulated gastric acid secretion in urethane-anaesthetized rats. Using a variety of neuropeptide Y (NPY) and PYY derivatives, we characterized the pharmacological profile of the receptor mediating the acid secretory response to PYY. ...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1038/sj.bjp.0701767

    authors: Yang H,Li WP,Reeve JR Jr,Rivier J,Taché Y

    更新日期:1998-04-01 00:00:00

  • Targeting the peptidase PCSK9 to reduce cardiovascular risk: Implications for basic science and upcoming challenges.

    abstract::LDL cholesterol (LDL-C) plays a central role in the progression of atherosclerosis. Statin therapy for lowering LDL-C reduces the risk of atherosclerotic cardiovascular disease and is the recommended first-line treatment for patients with high LDL-C levels. However, some patients are unable to achieve an adequate redu...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章,评审

    doi:10.1111/bph.14851

    authors: Nishikido T,Ray KK

    更新日期:2019-08-29 00:00:00

  • High affinity binding of [3H]-tyramine in the central nervous system.

    abstract::Optimum assay conditions for the association of [3H]-para-tyramine [( 3H]-pTA) with rat brain membranes were characterized, and a saturable, reversible, drug-specific, and high affinity binding mechanism for this trace amine was revealed. The binding capacity (Bmax) for [3H]-pTA in the corpus striatum was approximatel...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1986.tb11116.x

    authors: Vaccari A

    更新日期:1986-09-01 00:00:00

  • Chloride anion concentration as a determinant of renal vascular responsiveness to vasoconstrictor agents.

    abstract::1. The role of chloride concentration in modulating vasoconstrictor responses of the rat isolated kidney, perfused with Krebs-Henseleit solution, to angiotensin II (AII), arginine vasopressin (AVP) and phenylephrine (PE) was investigated. 2. Reduction of perfusate chloride from a high (117 mM) to low (87 mM) concentra...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1993.tb13447.x

    authors: Quilley CP,Lin YS,McGiff JC

    更新日期:1993-01-01 00:00:00

  • β₁-Adrenoceptor stimulation suppresses endothelial IK(Ca)-channel hyperpolarization and associated dilatation in resistance arteries.

    abstract:BACKGROUND AND PURPOSE:In small arteries, small conductance Ca²⁺-activated K⁺ channels (SK(Ca)) and intermediate conductance Ca²⁺-activated K⁺ channels (IK(Ca)) restricted to the vascular endothelium generate hyperpolarization that underpins the NO- and PGI₂-independent, endothelium-derived hyperpolarizing factor respo...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/bph.12160

    authors: Yarova PL,Smirnov SV,Dora KA,Garland CJ

    更新日期:2013-06-01 00:00:00

  • Pulmonary metabolism of bradykinin analogues and the contribution of angiotensin converting enzyme to bradykinin inactivation in isolated lungs.

    abstract::1 The activity and pulmonary metabolism of two peptides, 7-homo Pro-bradykinin and 8-homo Phe-bradykinin were studied in isolated systems. 2 Both analogues were about 50-70 times less active than bradykinin on the guinea-pig ileum and 70-160 times less active on isolated strips of cat terminal ileum. 3 The action of b...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1977.tb06985.x

    authors: Bakhle YS

    更新日期:1977-01-01 00:00:00

  • Zolpidem and eszopiclone prime α1β2γ2 GABAA receptors for longer duration of activity.

    abstract:BACKGROUND AND PURPOSE:GABAA receptors mediate neuronal inhibition in the brain. They are the primary targets for benzodiazepines, which are widely used to treat neurological disorders including anxiety, epilepsy and insomnia. The mechanism by which benzodiazepines enhance GABAA receptor activity has been extensively s...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/bph.13142

    authors: Dixon CL,Harrison NL,Lynch JW,Keramidas A

    更新日期:2015-07-01 00:00:00

  • Predicting the emetic liability of novel chemical entities: a comparative study.

    abstract:BACKGROUND AND PURPOSE:Emesis is a multi-system reflex, which is usually investigated using in vivo models. The aim of the study is to compare the response induced by emetic compounds across species and investigate whether dogs, ferrets and rats are all similarly predictive of humans. EXPERIMENTAL APPROACH:A systemati...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章,评审

    doi:10.1111/j.1476-5381.2011.01669.x

    authors: du Sert NP,Holmes AM,Wallis R,Andrews PL

    更新日期:2012-03-01 00:00:00

  • Effects of the venom of the green mamba, Dendroaspis angusticeps on skeletal muscle and neuromuscular transmission.

    abstract::1 The venom of the green mamba, Dendroaspis angusticeps, was tested for effects on neuromuscular transmission and skeletal muscle contractility in isolated phrenic nerve-hemidiaphragm preparations of the rat and mouse, chick biventer cervicis muscle preparations and in aneural cultures of embryonic chick skeletal musc...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1979.tb08667.x

    authors: Barrett JC,Harvey AL

    更新日期:1979-10-01 00:00:00