Assessment of the analgesic effect of centhaquin in mouse tail flick and hot-plate tests.

Abstract:

BACKGROUND:Centhaquin is a centrally acting hypotensive drug like clonidine. Clonidine also produces analgesia and hypothermia in mice and potentiates morphine analgesia. Clonidine analgesia is blocked by idazoxan and naloxone while it is potentiated by BQ123 and sulfisoxazole. This study was conducted to determine the analgesic and hypothermic properties of centhaquin, and to assess whether it potentiates morphine analgesia. Yohimbine (α(2)-adrenergic antagonist), idazoxan (imidazoline/α(2)-adrenergic antagonist), naloxone (opioid antagonist), and BQ123 and sulfisoxazole (endothelin ET(A) antagonists) were used to study the involvement of these receptors in centhaquin analgesia and hypothermia. METHODS:Analgesic (tail flick and hot-plate tests) latencies and body temperatures were measured in male Swiss Webster mice treated with vehicle plus centhaquin, antagonists plus centhaquin or centhaquin plus morphine. RESULTS:Centhaquin produced dose-dependent analgesia which was partially blocked by yohimbine, idazoxan and naloxone. BQ123 and sulfisoxazole did not affect centhaquin analgesia. Morphine analgesia was not potentiated by centhaquin. Centhaquin produced mild hypothermia which was not blocked by yohimbine, idazoxan, naloxone, BQ123 or sulfisoxazole. CONCLUSIONS:This is the first report demonstrating the analgesic activity of centhaquin. The α(2)-adrenergic, imidazoline and opioid receptors are involved in mediating centhaquin analgesia. Endothelin ET(A) receptors do not play a role in centhaquin analgesia; centhaquin does not augment morphine analgesia.

journal_name

Pharmacology

journal_title

Pharmacology

authors

Andurkar SV,Gulati A

doi

10.1159/000331880

subject

Has Abstract

pub_date

2011-01-01 00:00:00

pages

233-41

issue

5-6

eissn

0031-7012

issn

1423-0313

pii

000331880

journal_volume

88

pub_type

杂志文章
  • Resistance in malignant tumors: can resistance assays optimize cytostatic chemotherapy?

    abstract::The frequent resistance of malignant tumors to chemotherapy documents the fact that numerous patients are uselessly traumatized by highly toxic drugs. Investigations into this resistance have shown that many different mechanisms exist which can abolish the antitumor action of chemotherapeutics. So far, no safe method ...

    journal_title:Pharmacology

    pub_type: 杂志文章,评审

    doi:10.1159/000112864

    authors: Lippert TH,Ruoff HJ,Volm M

    更新日期:2008-01-01 00:00:00

  • In vitro effect of carvedilol on professional phagocytes.

    abstract:AIM:Superfluous reactive nitrogen and oxygen species generation is implicated in the damage of tissues at sites of inflammation where activated neutrophils and macrophages are involved. This study was conducted to investigate whether the beneficial effects of carvedilol involve modulation of respiratory burst, degranul...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000097818

    authors: Pecivová J,Macicková T,Lojek A,Gallova L,Cíz M,Nosál' R,Holománová D

    更新日期:2007-01-01 00:00:00

  • Clofibrate decreases jejunal cholesterol synthesis and activity of postheparin plasma lipoprotein lipase in the rat.

    abstract::Clofibrate treatment decreased drastically the activity of serum postheparin lipoprotein lipase of rats fed with fat-free test diet but had no effect on hepatic lipase. 3 weeks' treatment was followed by a significant fall in serum cholesterol caused by a marked decrease in HDL-cholesterol. Clofibrate decreased in vit...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000137813

    authors: Strandberg TE,Kuusi T,Tilvis RS,Miettinen TA

    更新日期:1983-01-01 00:00:00

  • Evaluation of antiulcer activity of delta9-tetrahydrocannabinol in the Shay rat test.

    abstract::delta9-Tetrahydrocannabinol (THC) inhibited ulcer formation in the pylorus-ligated rat (Shay rat test). However, this antiulcer activity of THC was substantially less than for the anticholinergic substance tridihexethyl chloride both in terms of degree of activity and potency. In addition, the results of the present s...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000136851

    authors: Sofia RD,Diamantis W,Harrison JE,Melton J

    更新日期:1978-01-01 00:00:00

  • Acute Treatment with T-Type Calcium Channel Enhancer SAK3 Reduces Cognitive Impairments Caused by Methimazole-Induced Hypothyroidism Via Activation of Cholinergic Signaling.

    abstract::Hypothyroidism is a common disorder that is associated with psychological disturbances such as dementia, depression, and psychomotor disorders. We recently found that chronic treatment with the T-type calcium channel enhancer SAK3 prevents the cholinergic neurodegeneration induced by a single intraperitoneal (i.p.) in...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000488083

    authors: Husain N,Yabuki Y,Shinoda Y,Fukunaga K

    更新日期:2018-01-01 00:00:00

  • Nitric oxide reduces myocardial contractility in isoproterenol-stimulated rat hearts by a mechanism independent of cyclic GMP or cyclic AMP.

    abstract::Nitric oxide has been shown to decrease myocardial contractility and O2 consumption. This study was designed to evaluate the hypothesis that nitric oxide-mediated increases in cyclic GMP require elevated cyclic AMP to produce cardiac depression. Using isolated, Langendorff-perfused rat hearts, we determined the effect...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000139529

    authors: Weiss HR,Sadoff JD,Scholz PM,Klabunde RE

    更新日期:1997-10-01 00:00:00

  • Antidiarrheal activity of wood creosote: inhibition of muscle contraction and enterotoxin-induced fluid secretion in rabbit small intestine.

    abstract::Wood creosote has long been used as an antidiarrheal agent, but its mechanism of action is not well understood. To elucidate the mechanism of its antidiarrheal activity, we have addressed questions whether it inhibits fluid secretion induced by Escherichia coli heat-stable enterotoxin (STa) in rabbit jejunum in vivo, ...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000056092

    authors: Ogata N,Shibata T

    更新日期:2001-01-01 00:00:00

  • Variation in the affinity of amitriptyline for muscarine receptor subtypes.

    abstract::The affinity of amitriptyline for muscarine M1 receptors was studied in the rat cerebral cortex and rabbit vas deferens utilizing binding studies as well as inhibition of carbachol-induced phosphoinositide hydrolysis in the cerebral cortex and blockade of the muscarinic prejunctional inhibition of sympathetic nerve st...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000139192

    authors: Choi A,Mitchelson F

    更新日期:1994-05-01 00:00:00

  • Time course of the distribution of morphine in brain regions, spinal cord and serum following intravenous injection to rats of differing ages.

    abstract::Previously it was demonstrated that intravenously administered morphine produced greater analgesic but lower hyperthermic responses to morphine in 24-week-old rats in comparison to 8-week-old rats. The differential pharmacological responses to morphine could not solely be attributed to the pharmacokinetic parameters, ...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000139073

    authors: Bhargava HN,Villar VM,Rahmani NH,Larsen AK

    更新日期:1993-07-01 00:00:00

  • Stimulation of glucose release of the rat kidney in vivo by epinephrine and isoprenaline.

    abstract::In anesthetized rats the glucose release of the kidneys was estimated from the glucose concentrations in the arterial and renal venous plasma, urinary glucose excretion and the total renal plasma flow. Net renal glucose release was found in control experiments. The glucose release of the kidneys decreased with rising ...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000136914

    authors: Greven J,van Eys B,Jacobs W

    更新日期:1975-01-01 00:00:00

  • Inhibition of the histamine-stimulated adenylate cyclase activity of guinea pig gastric cells by the H2-receptor antagonists cimetidine, oxmetidine and SKF 93479.

    abstract::The effect of cimetidine and two new histamine H2-receptor antagonists, oxmetidine and SKF 93479, on histamine-stimulated adenylate cyclase activity was studied in guinea pig gastric mucosal cells. Histamine stimulated the enzyme activity in concentration-dependent fashion. The concentration-response curve of histamin...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000137973

    authors: Cheret AM,Scarpignato C,Lewin MJ,Bertaccini G

    更新日期:1984-01-01 00:00:00

  • Characterization of Ascaris-induced biphasic skin allergic reaction model in mice: possible roles of mast cells in early-phase and CD4-positive T cells in late-phase reactions.

    abstract::We established an Ascaris-induced biphasic skin allergic reaction in mice. In the early-phase reaction (EPR), mast cell degranulation was observed, and tranilast inhibited ear edema. In mast-cell-deficient mice (WBB6F(1)-W/W(V) mice), ear edema in the EPR disappeared, whereas that in the late-phase reaction (LPR) rema...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000056117

    authors: Sengoku T,Sato S,Sakuma S,Ogawa T,Ohkubo Y,Goto T

    更新日期:2001-01-01 00:00:00

  • Stability of chloramphenicol metabolites in human blood and liver as determined by high-performance liquid chromatography.

    abstract::The pathogenesis of aplastic anemia from chloramphenicol (CAP) remains uncertain. Recent observations suggest that metabolites of CAP generated by intestinal bacteria may play an important role in mediating hematotoxicity from the drug. Thus, it is possible that once in circulation and after passage through the liver,...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000138394

    authors: Abou-Khalil WH,Yunis AA,Abou-Khalil S

    更新日期:1988-01-01 00:00:00

  • Effects of Polybrominated Diphenyl Ethers on Rat and Human 11β-Hydroxysteroid Dehydrogenase 1 and 2 Activities.

    abstract::Polybrominated diphenyl ethers (PBDEs) are a class of brominated flame retardants. PBDEs have been widely used in textiles, flexible polyurethane foams, electronic components, electrical components, and plastics. 11β-Hydroxysteroid dehydrogenases, isoform 1 (HSD11B1) and isoform 2 (HSD11B2), have been demonstrated to ...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000445213

    authors: Chen X,Dong Y,Cao S,Li X,Wang Z,Chen R,Ge RS

    更新日期:2016-01-01 00:00:00

  • Tetanic Facilitation of Neuromuscular Transmission by Adenosine A2A and Muscarinic M1 Receptors is Dependent on the Uptake of Choline via High-Affinity Transporters.

    abstract:BACKGROUND/AIMS:In this study, we evaluated the functional impact of facilitatory presynaptic adenosine A2A and muscarinic M1 receptors in the recovery of neuromuscular tetanic depression caused by the blockage of high-affinity choline transporter (HChT) by hemicholinium-3 (HC-3), a condition that mimics a myasthenia-l...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000494058

    authors: Castellão-Santana LM,Yumi Abiko P,Ambiel CR,Peixoto AR,Noronha-Matos JB,Correia-de-Sá P,Alves-Do-Prado W

    更新日期:2019-01-01 00:00:00

  • Reversion of multidrug resistance in a chemoresistant human breast cancer cell line by β-elemene.

    abstract:BACKGROUND:Multidrug resistance (MDR) presents a problem in cancer chemotherapy, and developing new agents to overcome MDR is important. This study intends to investigate the reversal effect of -elemene on MDR in human breast carcinoma MCF-7 and doxorubicin-resistant MCF-7 cells. METHODS:MTT cytotoxicity assays, flow ...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000337178

    authors: Xu HB,Li L,Fu J,Mao XP,Xu LZ

    更新日期:2012-01-01 00:00:00

  • Intraspecific aggressiveness after lesions of midbrain raphe nuclei in rats.

    abstract::Serotonin-depleting lesions of midbrain raphe (extensive lesions located within dorsal and partly median raphe muclei) induced intraspecific agressiveness in grouped Wistar male rats but failed to increase mouse-killing behaviour. Rats which had lesions in the lateral midbrain did not display intraspecific aggression ...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000136887

    authors: Kostowski W,Cxlonkowski A,Markowdka L,Markiewicz L

    更新日期:1975-01-01 00:00:00

  • Transcytosis of lipid microspheres by human endothelial cells.

    abstract::Human endothelial cells were cultivated on microporous membranes mimicking the luminal and basal spaces of blood vessels. When fluorescence-labeled lipid microspheres (LM) were added to the upper chambers of the model cultures, confluent monolayers of endothelial cells transported considerable levels of fluorescence t...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000139413

    authors: Takahashi K,Suzuki K,Ichiki Y,Fukushima T,Nakamura H,Sawasaki Y

    更新日期:1996-07-01 00:00:00

  • Anticonvulsant effect of morphine and morphine-like analgesics in Mongolian gerbils.

    abstract::The effect of morphine, fentanyl, pethidine and pentazocine was studied in gerbils against air blast-induced seizures. Major, generalized seizures were suppressed by morphine (ED50 = 4.0 mg/kg s.c.), fentanyl (ED50 = 64 micrograms/kg s.c.), and pethidine (ED50 = 2.4 mg/kg s.c.), but not by pentazocine. The anticonvuls...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000138189

    authors: Frey HH

    更新日期:1986-01-01 00:00:00

  • Evidence for a mitochondrial impact of trimetazidine during cold ischemia and reperfusion.

    abstract::In organ transplantation, ischemia-reperfusion injury (IRI) has been implicated in delayed graft function (DGF) as well as in short- and long-term complications. Using an autotransplant pig kidney model, changes in renal function and morphology were determined after different periods of cold ischemia in kidneys preser...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000076259

    authors: Baumert H,Faure JP,Zhang K,Petit I,Goujon JM,Dutheil D,Favreau F,Barrière M,Tillement JP,Mauco G,Papadopoulos V,Hauet T

    更新日期:2004-05-01 00:00:00

  • Sennosides and aloin do not promote dimethylhydrazine-induced colorectal tumors in mice.

    abstract::In a model of dimethylhydrazine-induced colorectal tumors in male mice aloin- or sennoside-enriched diets (0.03%) did not promote incidence and growth of adenomas and carcinomas after 20 weeks. Furthermore, in anthranoid-fed mice no significant changes in serum electrolytes as well as parameters of hepato- and nephrot...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000139859

    authors: Siegers CP,Siemers J,Baretton G

    更新日期:1993-10-01 00:00:00

  • Effects of acetaldehyde on action potentials and Ca2+ currents in single atrial myocytes from the bullfrog.

    abstract:AIM:The purpose of the present study was to examine the effects of acetaldehyde on the contractile force and membrane potentials and currents in the bullfrog heart. METHODS:Contractile force was recorded using right atrial tissues, and membrane potentials and currents were measured by using whole cell patch clamp meth...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000342388

    authors: Chen FS,Satoh Y,Ide Y,Sugano T,Iimura M,Momose Y,Tsuchida K,Tagami M

    更新日期:2012-01-01 00:00:00

  • Endothelial dysfunction, macrophage infiltration and NADPH oxidase-dependent superoxide production were attenuated by erythropoietin in streptozotocin-induced diabetic rat aorta.

    abstract::Erythropoietin (EPO) has been used for the management of renal anemia. Recent studies suggest the pleiotropic properties of EPO in various tissues such as brain, kidney and vasculature. Diabetes mellitus is a major risk for development of vascular impairment. The aim of the present study was to investigate the hypothe...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000343963

    authors: Wang J,Toba H,Morita Y,Nakashima K,Noda K,Tian W,Kobara M,Nakata T

    更新日期:2013-01-01 00:00:00

  • Pharmacokinetics of macitentan in caucasian and Japanese subjects: the influence of ethnicity and sex.

    abstract:BACKGROUND/AIMS:Macitentan is a novel dual endothelin receptor antagonist with sustained receptor binding in clinical development for pulmonary arterial hypertension. The present study compared the pharmacokinetics and safety of macitentan in healthy Caucasian and Japanese subjects and explored the potential sex differ...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000351704

    authors: Bruderer S,Marjason J,Sidharta PN,Dingemanse J

    更新日期:2013-01-01 00:00:00

  • Effects induced by Tityus serrulatus scorpion venom and its toxins TsTX-I and TsTX-V on the rat isolated retractor penis muscle.

    abstract::The aims of the present study were to investigate the pharmacological effects induced by Tityus serrulatus venom (TsV) and its fractions and to compare with the effects induced by pure alpha (TsTX-V) and beta (TsTX-I) toxins isolated from TsV on rat retractor penis muscle (RPM). TsV, fractions X, XI, XIIa, XIIb (0.01-...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000082804

    authors: Bomfim JH,de Godoy MA,Giglio JR,de Oliveira AM,Arantes EC

    更新日期:2005-03-01 00:00:00

  • Cimetidine, ranitidine and mifentidine in specific gastric and duodenal ulcer models.

    abstract::The protective effect of cimetidine, ranitidine and a newer H2-receptor antagonist, mifentidine (proposed INN), on models of gastric and duodenal damage, caused by activation of H2 receptors, was studied. Gastric erosions were induced in rats by intravenous dimaprit (100 mg/kg) while duodenal damage was investigated i...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000138049

    authors: Del Soldato P,Ghiorzi A,Cereda E,Donetti A

    更新日期:1985-01-01 00:00:00

  • Pharmacological characterization of M-II, the major human metabolite of ramelteon.

    abstract::The duration of action of melatonin may be important for improvements in sleep efficiency in insomniacs. Ramelteon, a selective melatonin agonist, is primarily metabolized to the active metabolite M-II, which has a longer half-life and greater systemic exposure than ramelteon. Hence, M-II may contribute significantly ...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000362459

    authors: Nishiyama K,Nishikawa H,Kato K,Miyamoto M,Tsukamoto T,Hirai K

    更新日期:2014-01-01 00:00:00

  • Functional evidence for the presence of beta 3-adrenoceptors in the guinea pig common bile duct and colon.

    abstract::To determine the existence of beta 3-adrenoceptors in functional assays in isolated preparations for which data are lacking, we compared the effects of SR 58611A, a selective beta 3-adrenoceptor agonist, and isoprenaline in the guinea pig common bile duct, distal colon and urinary bladder. SR 58611A and isoprenaline r...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000139338

    authors: De Ponti F,Gibelli G,Crema F,Lecchini S

    更新日期:1995-11-01 00:00:00

  • Adrenergic activity of ortho-, meta-, and para-octopamine.

    abstract::DL-o-, and p-octopamine were tested for beta- and alpha-adrenergic activity in rats. When compared to DL-isoproterenol, a beta-adrenergic agonist, all three isomers failed to show significant beta-adrenergic activity as assessed by intiation of thirst and by increase in tail skin temperature. All three isomers increas...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000137250

    authors: Fregly MJ,Kelleher DL,Williams CM

    更新日期:1979-01-01 00:00:00

  • Paeoniflorin on Rat Myocardial Ischemia Reperfusion Injury of Protection and Mechanism Research.

    abstract:OBJECTIVE:To study the myocardial benefit effect and mechanism of paeoniflorin on myocardial ischemia reperfusion injury (MIRI) in rats. METHODS:Hundred SD rats were randomly divided into 5 groups: sham group, model group, Paeoniflorin (15 mg/kg) group, Paeoniflorin (30 mg/kg) group, and Paeoniflorin (60 mg/kg) group....

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000503583

    authors: Wu F,Ye B,Wu X,Lin X,Li Y,Wu Y,Tong L

    更新日期:2020-01-01 00:00:00