Comparative behavioural profile of centrally administered tachykinin NK1, NK2 and NK3 receptor agonists in the guinea-pig.

Abstract:

:1. The NK1 tachykinin receptor agonists, septide, [Sar9,Met(O2)11]SP and [Pro9]SP produced locomotor hyperactivity (10-20 min) when injected intracerebroventricularly (i.c.v.) in the guinea-pig. The most potent in eliciting this hyperactivity was septide (from 0.63 to 5 micrograms), compared to [Sar9,Met(O2)11]SP, which was active at 2.5 and 5 micrograms and [Pro9]SP which induced a non-significant increase even at 10 micrograms. 2. Wet-dog shakes were elicited by septide, [Sar9,Met(O2)11]SP and [Pro9]SP injected by the i.c.v. route in the guinea-pig. [Sar9,Met(O2)11]SP, active from 0.16 to 2.5 micrograms was more potent than septide (active at 1.25 micrograms) and [Pro9]SP (active at 0.63 micrograms) in eliciting such behaviour. To a lesser extent, grooming was also observed after injection of these agonists. 3. The NK2 tachykinin receptor agonist, [Lys5,MeLeu9,Nle10]NKA(4-10), up to the dose of 10 micrograms i.c.v. had no effect in the guinea-pig. It neither modified locomotor activity nor induced a characteristic behavioural response. At higher doses (20 micrograms), some toxic effects were noted. 4. The NK3 tachykinin receptor agonist, senktide, contrasts with the NK1 receptor agonists in that it elicited only wet-dog shakes, at doses ranging from 0.32 to 1.25 micrograms. It neither modified locomotor activity (1 microgram) nor induced grooming (up to 5 micrograms) in the guinea-pig. 5. To our knowledge, these results are the first demonstration that the guinea-pig could be useful to differentiate tachykinin agonists on the basis of their behavioural profile, distinct from those obtained in mice and rats.

journal_name

Br J Pharmacol

authors

Piot O,Betschart J,Grall I,Ravard S,Garret C,Blanchard JC

doi

10.1111/j.1476-5381.1995.tb15101.x

subject

Has Abstract

pub_date

1995-11-01 00:00:00

pages

2496-502

issue

5

eissn

0007-1188

issn

1476-5381

journal_volume

116

pub_type

杂志文章
  • Potential anxiolytic- and antidepressant-like effects of salvinorin A, the main active ingredient of Salvia divinorum, in rodents.

    abstract:BACKGROUND AND PURPOSE:Drugs targeting brain kappa-opioid receptors produce profound alterations in mood. In the present study we investigated the possible anxiolytic- and antidepressant-like effects of the kappa-opioid receptor agonist salvinorin A, the main active ingredient of Salvia divinorum, in rats and mice. EX...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.2009.00230.x

    authors: Braida D,Capurro V,Zani A,Rubino T,Viganò D,Parolaro D,Sala M

    更新日期:2009-07-01 00:00:00

  • Inter-study variability of preclinical in vivo safety studies and translational exposure-QTc relationships--a PKPD meta-analysis.

    abstract:BACKGROUND AND PURPOSE:Preclinical cardiovascular safety studies (CVS) have been compared between facilities with respect to their sensitivity to detect drug-induced QTc prolongation (ΔQTc). Little is known about the consistency of quantitative ΔQTc predictions that are relevant for translation to humans. EXPERIMENTAL...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章,meta分析

    doi:10.1111/bph.13218

    authors: Gotta V,Cools F,van Ammel K,Gallacher DJ,Visser SA,Sannajust F,Morissette P,Danhof M,van der Graaf PH

    更新日期:2015-09-01 00:00:00

  • Methylene blue inhibits function of the 5-HT transporter.

    abstract:BACKGROUND AND PURPOSE:Methylene blue (MB) is commonly employed as a treatment for methaemoglobinaemia, malaria and vasoplegic shock. An increasing number of studies indicate that MB can cause 5-HT toxicity when administered with a 5-HT reuptake inhibitor. MB is a potent inhibitor of monoamine oxidases, but other targe...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.2011.01462.x

    authors: Oz M,Isaev D,Lorke DE,Hasan M,Petroianu G,Shippenberg TS

    更新日期:2012-05-01 00:00:00

  • Possible in vivo 5-HT reuptake blocking properties of 8-OH-DPAT assessed by measuring hippocampal extracellular 5-HT using microdialysis in rats.

    abstract::1. The 5-hydroxytryptamine (5-HT)1A receptor agonist, 8-hydroxy-2-(di-n-propylamino)tetralin (8-OH-DPAT), has been shown to label 5-HT reuptake sites. 2. To study the functional consequences of this property, the effects of 8-OH-DPAT were compared with those of the 5-HT reuptake inhibitors, paroxetine and clomipramine...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1996.tb15749.x

    authors: Assié MB,Koek W

    更新日期:1996-11-01 00:00:00

  • Pharmacological characterization of volume-sensitive, taurine permeable anion channels in rat supraoptic glial cells.

    abstract::To characterize the volume-sensitive, osmolyte permeable anion channels responsible for the osmodependent release of taurine from supraoptic nucleus (SON) astrocytes, we investigated the pharmacological properties of the [(3)H]-taurine efflux from acutely isolated SON. Taurine release induced by hypotonic stimulus (25...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1038/sj.bjp.0703492

    authors: Brès V,Hurbin A,Duvoid A,Orcel H,Moos FC,Rabié A,Hussy N

    更新日期:2000-08-01 00:00:00

  • The effects of formoterol on plasma exudation produced by a localized acute inflammatory response to bradykinin in the tracheal mucosa of rats in vivo.

    abstract::1. The effects of formoterol, a beta 2-adrenoceptor agonist, on plasma protein exudation and microvascular permeability induced by topical, i.e. applied onto the tracheal mucosal surface, bradykinin (10 nmol; 20 microM, 5 min, 0.1 ml min-1) were studied in a perfused segment of trachea prepared in situ in anaesthetize...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1995.tb16374.x

    authors: O'Donnell SR,Anderson GP

    更新日期:1995-09-01 00:00:00

  • The alpha7 nicotinic acetylcholine receptor as a pharmacological target for inflammation.

    abstract::The physiological regulation of the immune system encompasses comprehensive anti-inflammatory mechanisms that can be harnessed for the treatment of infectious and inflammatory disorders. Recent studies indicate that the vagal nerve, involved in control of heart rate, hormone secretion and gastrointestinal motility, is...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章,评审

    doi:10.1038/sj.bjp.0707264

    authors: de Jonge WJ,Ulloa L

    更新日期:2007-08-01 00:00:00

  • Passage of intravenously administered tubocurarine into the liquor space in man and dog.

    abstract::1. In anaesthetized patients under controlled respiration, samples of lumbar cerebrospinal fluid were withdrawn 15 and 60 min after an intravenous injection of 30 mg tubocurarine. When tested on the frog rectus muscle preparation contracted by acetylcholine, they exerted curare-like activity which corresponded to betw...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1973.tb08206.x

    authors: Devasankaraiah G,Haranath PS,Krishnamurty A

    更新日期:1973-04-01 00:00:00

  • Pharmacology of LR-B/081, a new highly potent, selective and orally active, nonpeptide angiotensin II AT1 receptor antagonist.

    abstract::1. The pharmacological profile of LR-B/081, (methyl 2-[[4-butyl-2-methyl- 6-oxo-5-[[2'-(1H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]-1(6H)- pyrimidinyl]methyl]-3-thiophenecarboxylate), a novel antagonist at the angiotensin II (AII) AT1-receptor, was studied in vitro and in vivo. 2. In rabbit aortic strips incubated w...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1995.tb13323.x

    authors: Cirillo R,Renzetti AR,Cucchi P,Guelfi M,Salimbeni A,Caliari S,Castellucci A,Evangelista S,Subissi A,Giachetti A

    更新日期:1995-03-01 00:00:00

  • On the preparation of highly purified slow reacting substance of anaphylaxis (SRS-A) from biological extracts.

    abstract::1 Very highly purified (greater than 100,000 u/mg) slow reacting substance of anaphylaxis (SRS-A) has been prepared by reversed phase high pressure liquid chromatographic (HPLC) techniques. 2 High resolution liquid chromatography suggests that SRS-A may exist in at least three distinct forms which are possible tautome...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1980.tb10696.x

    authors: Blackwell GJ,Burka JF,Flower RJ,Torkington P

    更新日期:1980-01-01 00:00:00

  • β(2)-Adrenoceptors increase translocation of GLUT4 via GPCR kinase sites in the receptor C-terminal tail.

    abstract:BACKGROUND AND PURPOSE:β-Adrenoceptor stimulation induces glucose uptake in several insulin-sensitive tissues by poorly understood mechanisms. EXPERIMENTAL APPROACH:We used a model system in CHO-K1 cells expressing the human β(2)-adrenoceptor and glucose transporter 4 (GLUT4) to investigate the signalling mechanisms i...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.2011.01647.x

    authors: Dehvari N,Hutchinson DS,Nevzorova J,Dallner OS,Sato M,Kocan M,Merlin J,Evans BA,Summers RJ,Bengtsson T

    更新日期:2012-03-01 00:00:00

  • Prominent sympathetic purinergic vasoconstriction in the rabbit splenic artery: potentiation by 2,2'-pyridylisatogen tosylate.

    abstract::1. Vasoconstrictions induced by transmural electrical field stimulation were frequency-dependent from 2 to 32 Hz in the rabbit isolated splenic artery. All contractions were abolished in the presence of tetrodotoxin 1 microM or guanethidine 100 microM. Stimulation at a frequency of more than 32 Hz induced both neuroge...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1038/sj.bjp.0700933

    authors: Ren LM,Burnstock G

    更新日期:1997-02-01 00:00:00

  • Relationship between internal Na + -K + and the accumulation of 14 C-5-hydroxytryptamine by rat platelets.

    abstract::1. 5-Hydroxytryptamine (5-HT) transport has been investigated in rat blood platelets poisoned with dinitrophenol-sodium fluoride or ouabain.2. The inhibition of transport produced by different concentrations of the metabolic inhibitors has been correlated with changes in the internal Na(+) and K(+) concentrations of t...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1971.tb07220.x

    authors: Sneddon JM

    更新日期:1971-12-01 00:00:00

  • Modulation of a recombinant invertebrate gamma-aminobutyric acid receptor-chloride channel complex by isoflurane: effects of a point mutation in the M2 domain.

    abstract::1. Inhalational anaesthetics modulate ligand-gated ion channels at clinical concentrations. In this paper we address submolecular mechanisms for gamma-aminobutyric acid (GABA) receptor modulation by isoflurane. 2. Wild-type Drosophila melanogaster homo-oligomeric GABA receptors were characterized and compared with an ...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1038/sj.bjp.0701417

    authors: Edwards MD,Lees G

    更新日期:1997-10-01 00:00:00

  • IL-13 enhances agonist-evoked calcium signals and contractile responses in airway smooth muscle.

    abstract::Growing evidence suggests that interleukin (IL)-13, a Th2-type cytokine, plays a critical role in the development of bronchial hyper-responsiveness (BHR), an essential feature of asthma, although the underlying mechanisms remain unknown. In the present study, we investigated whether IL-13 directly affects airway smoot...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1038/sj.bjp.0705558

    authors: Tliba O,Deshpande D,Chen H,Van Besien C,Kannan M,Panettieri RA Jr,Amrani Y

    更新日期:2003-12-01 00:00:00

  • Suc-[Glu9,Ala11,15]-endothelin-1 (8-21), IRL 1620, identifies two populations of ET(B) receptors in guinea-pig bronchus.

    abstract::The pharmacological properties of endothelin receptors (ETR) were investigated in guinea-pig bronchus by comparing binding and functional results. In binding assays, both the ET(B) agonists, endothelin-3 (ET-3) and N-suc-[Glu9,Ala11,15]ET-1(8-21) (IRL 1620), and the antagonist, N-cis-2,6-dimethylpiperidinocarbonyl-L-g...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1038/sj.bjp.0702672

    authors: Mazzoni MR,Breschi MC,Ceccarelli F,Lazzeri N,Giusti L,Nieri P,Lucacchini A

    更新日期:1999-07-01 00:00:00

  • The control of the contraction of myocytes from guinea-pig heart by the resting membrane potential.

    abstract::1. The influence of different holding potentials (-120 to -70 mV) on the contraction of enzymatically dispersed myocytes from guinea-pig hearts was evaluated. Contractions were elicited by repetitive depolarizations to 0 mV at 0.5 Hz. 2. While ineffective at 140 and 5 mmol l-1 [Na+]o and pipette Na+, respectively, dep...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1991.tb12492.x

    authors: Mermi J,Yajima M,Ebner F

    更新日期:1991-11-01 00:00:00

  • Effects of inflammatory agents on endothelial lysosomal fragility and their inhibition by anti-inflammatory drugs.

    abstract::1. Endothelial cells from human umbilical veins were maintained in tissue culture. The fragility of lysosomal membranes were studied by microdensitometry. 2. Histamine (50 microM to 10 mM), 4-methylhistamine (100 nM to 10 mM) and dimaprit (100 nM to 10 mM) increased lysosomal fragility. 2-Thiazolylethylamine and 2-pyr...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1981.tb09140.x

    authors: Yoffe JR

    更新日期:1981-04-01 00:00:00

  • Rho kinase inhibitors block activation of pancreatic stellate cells.

    abstract::1. In response to pancreatic injury and in cell culture, pancreatic stellate cells (PSCs) are transformed ('activated') into highly proliferative myofibroblast-like cells, which express alpha-smooth muscle actin (alpha-SMA), and produce type I collagen and other extracellular matrix components. There is accumulating e...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1038/sj.bjp.0705551

    authors: Masamune A,Kikuta K,Satoh M,Satoh K,Shimosegawa T

    更新日期:2003-12-01 00:00:00

  • Beta-adrenoceptor subtype expression and function in rat white adipocytes.

    abstract::1. The pharmacological features of rat white adipocyte beta-adrenoceptor subtypes were investigated by saturation and beta-agonist competition studies with [3H]-CGP 12177 and by lipolysis induced by beta-agonists as well as their inhibition by CGP 20712A (selective beta 1-antagonist) and ICI 118551 (selective beta 2-a...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1038/sj.bjp.0700885

    authors: Germack R,Starzec AB,Vassy R,Perret GY

    更新日期:1997-01-01 00:00:00

  • An optimized approach to study endocannabinoid signaling: evidence against constitutive activity of rat brain adenosine A1 and cannabinoid CB1 receptors.

    abstract::At nanomolar concentrations, SR141716 and AM251 act as specific and selective antagonists of the cannabinoid CB1 receptor. In the micromolar range, these compounds were shown to inhibit basal G-protein activity, and this is often interpreted to implicate constitutive activity of the CB1 receptors in native tissue. We ...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1038/sj.bjp.0705577

    authors: Savinainen JR,Saario SM,Niemi R,Järvinen T,Laitinen JT

    更新日期:2003-12-01 00:00:00

  • The effects of postligation administration of ORG 6001 and disopyramide on early ischaemia-induced arrhythmias in the anaesthetized rat.

    abstract::The effects of intravenous doses of Org 6001 and disopyramide (10 mg/kg) known to confer protection against early postligation-induced arrhythmias in the anaesthetized rat when given prophylactically, were assessed following postligation administration. When given 1 min after ligation both drugs greatly reduced the in...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1982.tb09245.x

    authors: Marshall RJ,Muir AW,Winslow E

    更新日期:1982-08-01 00:00:00

  • Electrophysiological effects of anandamide on rat myocardium.

    abstract:BACKGROUND AND PURPOSE:The endocannabinoid, anandamide, has anti-arrhythmic effects. The aim of the present study was to explore the electrophysiological effects of anandamide on rat myocardium. EXPERIMENTAL APPROACH:Evoked action potentials (APs) were recorded using intracellular recording technique in rat cardiac pa...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.2009.00518.x

    authors: Li Q,Ma HJ,Zhang H,Qi Z,Guan Y,Zhang Y

    更新日期:2009-12-01 00:00:00

  • Functional interaction between losartan and central tachykinin NK3 receptors in the conscious rat.

    abstract::1. The cardiovascular and behavioural effects elicted by the intracerebroventricular (i.c.v.) injection of substance P (SP), neurokinin A (NKA), [MePhe7]neurokinin B ([MePhe7]NKB) or angiotensin II (AII) in the conscious rat were assessed before and 5 min after i.c.v. pretreatment with antagonists selective for angiot...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1995.tb14940.x

    authors: Picard P,Chrétien L,Couture R

    更新日期:1995-04-01 00:00:00

  • Hyperhomocysteinaemia and vascular injury: advances in mechanisms and drug targets.

    abstract::Homocysteine is a sulphur-containing non-proteinogenic amino acid. Hyperhomocysteinaemia (HHcy), the pathogenic elevation of plasma homocysteine as a result of an imbalance of its metabolism, is an independent risk factor for various vascular diseases, such as atherosclerosis, hypertension, vascular calcification and ...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章,评审

    doi:10.1111/bph.13988

    authors: Fu Y,Wang X,Kong W

    更新日期:2018-04-01 00:00:00

  • Inhibition of eosinophil cyclic nucleotide PDE activity and opsonised zymosan-stimulated respiratory burst by 'type IV'-selective PDE inhibitors.

    abstract::1. The cyclic nucleotide phosphodiesterase (PDE) of guinea-pig eosinophils was partially characterized and the effects of selective inhibitors of PDE isoenzymes upon opsonized zymosan (OZ)-stimulated respiratory burst were studied. 2. PDE activity in eosinophil lysates appeared to be membrane-associated, displayed sub...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1991.tb09790.x

    authors: Dent G,Giembycz MA,Rabe KF,Barnes PJ

    更新日期:1991-06-01 00:00:00

  • Comparative study of the effect of three antibiotics on renal function.

    abstract::1. Therapeutic doses of colistin sulphomethate sodium B.P. (Colomycin), pento-N sulphomethylpolymyxin B sodium (Thiosporin) and ampicillin B.P. (Penbritin) as well as normal saline have been given to volunteers with normal kidney function.2. A blind crossover technique was used and the effects of the compounds on bloo...

    journal_title:British journal of pharmacology

    pub_type: 临床试验,杂志文章,随机对照试验

    doi:10.1111/j.1476-5381.1969.tb09545.x

    authors: Caldwell AD,Martin AJ,Trigger DJ

    更新日期:1969-09-01 00:00:00

  • S-nitrosothiols as selective antithrombotic agents - possible mechanisms.

    abstract::S-nitrosothiols have a number of potential clinical applications, among which their use as antithrombotic agents has been emphasized. This is largely because of their well-documented platelet inhibitory effects, which show a degree of platelet selectivity, although the mechanism of this remains undefined. Recent progr...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章,评审

    doi:10.1111/j.1476-5381.2010.00670.x

    authors: Gordge MP,Xiao F

    更新日期:2010-04-01 00:00:00

  • The effect of imiquimod on taste bud calcium transients and transmitter secretion.

    abstract:BACKGROUND AND PURPOSE:Imiquimod is an immunomodulator approved for the treatment of basal cell carcinoma and has adverse side effects, including taste disturbances. Paracrine transmission, representing cell-cell communication within taste buds, has the potential to shape the final signals that taste buds transmit to t...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/bph.13567

    authors: Huang AY,Wu SY

    更新日期:2016-11-01 00:00:00

  • Effects of some drugs on the responses of the rat isolated, innervated urinary bladder to indirect electrical stimulation.

    abstract::1. The effects of some drugs known to inhibit transmission in the superior cervical ganglion and at the neuromuscular junction were investigated on the cholinergic nerve-smooth muscle junction, using the rat isolated innervated urinary bladder preparation.2. HC-3 and Win 4981 inhibited the indirectly evoked contractio...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1970.tb09900.x

    authors: Dhattiwala AS,Jindal MN,Kelkar VV

    更新日期:1970-08-01 00:00:00