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


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.






Andurkar SV,Gulati A




Has Abstract


2011-01-01 00:00:00














  • Mechanism of the antihypertensive effect of FCE 22716, a new ergoline derivative, in the spontaneously hypertensive rat.

    abstract::Both acute and chronic oral administration (1-20 mg/kg) of FCE 22716, a new ergoline derivative, resulted in a dose-related fall of arterial blood pressure lasting for more than 6 h. Tachycardia was observed only at high dosages. Yohimbine, propranolol and indometacin did not modify its antihypertensive effect; on the...


    pub_type: 杂志文章


    authors: Salvati P,Bondiolotti GP,Caccia C,Vaghi F,Bianchi G

    更新日期:1989-01-01 00:00:00

  • Development of an intravenous desferrioxamine mesylate treatment protocol for swine: monitoring of desferrioxamine and metabolites by high-performance liquid chromatography.

    abstract::Desferrioxamine (DFO) metabolism and its pharmacokinetics were studied in a swine model using high-performance liquid chromatography. DFO and three iron-binding metabolites occurred in plasma. Interindividual differences in pharmacokinetics and metabolism were observed. Urine analysis in 4 pigs showed three iron-bindi...


    pub_type: 杂志文章


    authors: Fisher EA,McLachlan DR,Kruck TP,Mustard RA

    更新日期:1990-01-01 00:00:00

  • Contractility of diabetic human corpus cavernosum smooth muscle in response to serotonin mediated via Rho-kinase.

    abstract:BACKGROUND/AIMS:Serotonin (5-hydroxytryptamine, 5-HT)-induced contraction and the involvement of RhoA/Rho-kinase pathway in the 5-HT-induced contraction was investigated isometrically in vitro in both diabetic and nondiabetic human corpus cavernosum (HCC) tissues. METHODS:HCC tissues were obtained from 12 patients. Th...


    pub_type: 杂志文章


    authors: Murat N,Soner BC,Demir O,Esen A,Gidener S

    更新日期:2009-01-01 00:00:00

  • Effects of mitemcinal (GM-611), an acid-resistant nonpeptide motilin receptor agonist, on the gastrointestinal contractile activity in conscious dogs.

    abstract::The effects of mitemcinal (GM-611) on the gastrointestinal contractile activity were investigated using chronically implanted force transducers in conscious dogs and were compared with the effects of porcine motilin (pMTL), EM-523 and EM-574. In the interdigestive state, intravenous and oral administration of mitemcin...


    pub_type: 杂志文章


    authors: Ozaki K,Yogo K,Sudo H,Onoma M,Kamei K,Akima M,Koga H,Itoh Z,Omura S,Takanashi H

    更新日期:2007-01-01 00:00:00

  • Melatonin Induces Osteoblastic Differentiation of Mesenchymal Stem Cells and Promotes Fracture Healing in a Rat Model of Femoral Fracture via Neuropeptide Y/Neuropeptide Y Receptor Y1 Signaling.

    abstract::The function of melatonin (MLT) in promoting fracture healing has been demonstrated in previous studies. However, the molecular mechanism underlying therapeutic effects of MLT is not entirely clear. In this study, mesenchymal stem cells (MSCs) were isolated from rat bone marrow and identified by flow cytometry. We fou...


    pub_type: 杂志文章


    authors: Dong P,Gu X,Zhu G,Li M,Ma B,Zi Y

    更新日期:2018-01-01 00:00:00

  • Enhanced pressor responses to angiotensin II caused by excessive sodium loading in the pithed rat.

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    pub_type: 杂志文章


    authors: Knape JT,van Zwieten PA

    更新日期:1988-01-01 00:00:00

  • A randomised, two-period, cross-over, open-label study to evaluate the pharmacokinetic profiles of single doses of two different flurbiprofen 8.75-mg lozenges in healthy volunteers.

    abstract:AIMS:To compare the bioavailability of a new oromucosal formulation of flurbiprofen 8.75-mg lozenges, developed by Alfa Wassermann S.p.A. (test drug) to that of marketed flurbiprofen 8.75-mg lozenges (Benactiv Gola®, reference drug). METHODS:This was an open, randomised, two-period, crossover, pharmacokinetic (PK) stu...


    pub_type: 杂志文章,随机对照试验


    authors: Matzneller P,Burian A,Martin W,Annoni O,Lauro V,Tacchi R,Brunner M,Zeitlinger M

    更新日期:2012-01-01 00:00:00

  • Brain receptors and zopiclone.

    abstract::Zopiclone (ZPC; RP 27,267), which is chemically unrelated to benzodiazepines (BZD), was found to have a similar pharmacological profile and to possess in man hypnotic activity similar to that of some BZD such as nitrazepam. It was, therefore, interesting to study the interaction of ZPC with rat brain receptors and spe...


    pub_type: 杂志文章


    authors: Blanchard JC,Boireau A,Julou L

    更新日期:1983-01-01 00:00:00

  • Single nucleotide polymorphisms of the pregnane x receptor gene in Han Chinese and a comparison with other ethnic populations.

    abstract::The pregnane X receptor (PXR/NR1I2) gene is a master regulator for a number of cytochrome P450s (CYPs) and drug transporters. This study aimed to detect the single nucleotide polymorphisms (SNPs) of the PXR gene in Han Chinese (n = 186) and to compare the frequencies of polymorphisms of the PXR gene with those in Cauc...


    pub_type: 杂志文章


    authors: Wang XD,Deng XY,Chen J,Li JL,Chen X,Zhao LZ,Lu Y,Chowbay B,Su QB,Huang M,Zhou SF

    更新日期:2008-01-01 00:00:00

  • Cardiovascular effects of dihydroergotamine during epidural anaesthesia in dogs.

    abstract::The haemodynamic changes during epidural anaesthesia and following the administration of dihydroergotamine (DHE; 10 micrograms/kg i.v.) were studied in 7 dogs (epidural group). Epidural anaesthesia was associated with reductions in mean arterial, mean pulmonary arterial and mean right atrial pressures. Femoral flow wa...


    pub_type: 杂志文章


    authors: Zimpfer M,Schwarz M,Stanek B,Raberger G

    更新日期:1981-01-01 00:00:00

  • Transport of model compounds across the peritoneal membrane in the rat.

    abstract::The absorption into the systemic circulation of compounds administered intraperitoneally in large volumes was investigated in the rat. The influence on absorption of molecular weight, lipid-water partition coefficient (K), and dissociation constant (pKa) was studied. Nine neutral compounds ranging in molecular weight ...


    pub_type: 杂志文章


    authors: Torres IJ,Litterst CL,Guarino AM

    更新日期:1978-01-01 00:00:00

  • Substance P--structure-activity studies and the development of antagonists.

    abstract::Various attempts to developing antagonists for substance P (SP) and related peptides, based on our past experience with angiotensin, kinins, and neurotensin, were unsuccessful. The particular features of SP, namely the high activity of C-terminal partial sequences in some pharmacological tests were used to develop one...


    pub_type: 杂志文章,评审


    authors: Regoli D,Escher E,Mizrahi J

    更新日期:1984-01-01 00:00:00

  • Evidence that adrenergic and cholinergic but not capsaicin-sensitive nerves are involved in the nerve-mediated contraction of the guinea pig seminal vesicle.

    abstract:BACKGROUND/AIMS:The neurotransmitters participating in the nerve-mediated contraction of the guinea pig seminal vesicle (GPSV) have not been firmly established. There is debate as to the mediating role of norepinephrine and acetylcholine. METHODS:We have used longitudinally and circularly oriented strips of GPSV and a...


    pub_type: 杂志文章


    authors: Benko R,Szombati V,Bartho L

    更新日期:2013-01-01 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...


    pub_type: 杂志文章


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

    更新日期:2018-01-01 00:00:00

  • N-tosyl-L-phenylalanyl-chloromethyl ketone eliminates the increase in caspase-3 and bcl-2 caused by brain injury in the newborn rat.

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    pub_type: 杂志文章


    authors: Feng Y,LeBlanc MH

    更新日期:2002-11-01 00:00:00

  • Inhibitory effect of TRK-530 on inflammatory cytokines in bone marrow of rats with adjuvant arthritis.

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    pub_type: 杂志文章


    authors: Tanahashi M,Koike J,Kawabe N,Nakadate-Matsushita T

    更新日期:1998-05-01 00:00:00

  • Effect of Angiotensin-(1-7) on Aortic Response, TNF-α, IL-1β and Receptor for Advanced Glycation Endproduct in Rat's Adjuvant-Induced Arthritis.

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    pub_type: 杂志文章


    authors: Açikalin Ö,Bölükbaşi Hatip FF,Tan RF,Hatip-Al-Khatib I

    更新日期:2016-01-01 00:00:00

  • Study of the vasodilating activity of salbutamol on dog coronary arteries. Unexpected effects of methylene blue.

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    pub_type: 杂志文章


    authors: Bernard F,Jouquey S,Hamon G

    更新日期:1991-01-01 00:00:00

  • Analysis of the effects of halothane on Gi-coupled muscarinic M2 receptor signaling in Xenopus oocytes using a chimeric G alpha protein.

    abstract::Metabotropic G protein-coupled receptors have recently been recognized as targets for anesthetics and analgesics. In particular, G(q)-coupled receptors such as muscarinic M(1) receptors (M(1)R) and 5-hydroxytryptamine (5-HT) type 2A receptors have been reported to be targets for anesthetics. Much less is known, howeve...


    pub_type: 杂志文章


    authors: Minami K,Uezono Y,Shiraishi M,Okamoto T,Ogata J,Horishita T,Taniyama K,Shigematsu A

    更新日期:2004-11-01 00:00:00

  • Changes of superoxide dismutase in cultured rat aortic smooth muscle cells (A7r5) by an incubation of vitamin E.

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    pub_type: 杂志文章


    authors: Huang W,Chan P,Chen Y,Chen C,Liao S,Chin W,Cheng J

    更新日期:1999-11-01 00:00:00

  • Effects of selective and nonselective alpha-1-adrenoceptor antagonists on intraurethral and arterial pressures in intact conscious dogs.

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    pub_type: 杂志文章


    authors: Brune ME,Katwala SP,Milicic I,Buckner SA,Ireland LM,Kerwin JF Jr,Hancock AA

    更新日期:1996-12-01 00:00:00

  • Sucralfate and gastric bicarbonate.

    abstract::The effect of sucralfate treatment (3 g daily for 6 weeks) on gastric HCO3- secretion was investigated in 15 duodenal ulcer patients. After treatment a highly significant (p less than 0.01) increase in gastric bicarbonate output was found. It is suggested that the mode of action of sucralfate includes stimulation of g...


    pub_type: 杂志文章


    authors: Guslandi M

    更新日期:1985-01-01 00:00:00

  • Studies on accumulation of (14C)-mescaline in brain homogenates: effects of psychotropic and other agents.

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    pub_type: 杂志文章


    authors: Shah NS,Gulati OD

    更新日期:1975-01-01 00:00:00

  • Ameliorative Effect of Hochu-ekki-to on Natural Skin Aging.

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    pub_type: 杂志文章


    authors: Orita K,Yamate Y,Kobayashi H,Hiramoto K

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    pub_type: 杂志文章


    authors: Sund RB,Junker T,Malterud KE

    更新日期:1993-10-01 00:00:00

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    pub_type: 杂志文章


    authors: Rumsey RD,Squires PE,Read NW

    更新日期:1993-10-01 00:00:00

  • Fisher Discrimination of Metabolic Changes in Rats Treated with Aspirin and Ibuprofen.

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    pub_type: 杂志文章


    authors: Zhang J,Song H,Jiang S,Chen Z,Tong S,Lin F,Wen C,Zhang X,Hu L

    更新日期:2017-01-01 00:00:00

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    pub_type: 杂志文章


    authors: Markov AK,Farias LA,Bennett WS,Subramony C,Mihas AA

    更新日期:1991-01-01 00:00:00

  • Pitavastatin inhibits upregulation of intermediate conductance calcium-activated potassium channels and coronary arteriolar remodeling induced by long-term blockade of nitric oxide synthesis.

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    pub_type: 杂志文章


    authors: Terata Y,Saito T,Fujiwara Y,Hasegawa H,Miura H,Watanabe H,Chiba Y,Kibira S,Miura M

    更新日期:2003-08-01 00:00:00

  • N-acetylcysteine: potential for AIDS therapy.

    abstract::The observations that people infected with HIV suffer not only from an inflammatory stress but also from depleted glutathione levels have led to a general hypothesis that these two are causally related, and that treatment of AIDS should include thiol-replenishment therapy. In particular, inflammatory stimulations are ...


    pub_type: 杂志文章,评审


    authors: Roederer M,Staal FJ,Ela SW,Herzenberg LA,Herzenberg LA

    更新日期:1993-01-01 00:00:00