Kinetics, distribution, and biotransformation of the chemical HI-6 in the rat, dog, and rhesus monkey.

Abstract:

:Disposition of the bis-pyridinium mono-oxime, HI-6, following intramuscular injection in rats (200 mg/kg bw), beagle dogs (10 and 50 mg/kg bw), and rhesus monkeys (50 mg/kg bw) revealed that the oxime was absorbed rapidly and completely from the site of injection, was distributed rapidly in the tissues, and that tissue concentrations decreased below the limits of detection by 4 h after treatment. No overt signs of toxicity were observed in any species at the concentrations given. Tissue analysis for HI-6 and degradation products was conducted by extraction followed by ion-pair, reverse phase, HPLC chromatography. The estimated plasma half-life values were 20, 40-55, and 25-30 min for rats, dogs, and monkeys, respectively. HI-6 and the degradation products were excreted via the urine. A marked species difference in disposition was observed in that HI-6 selectively accumulated in the diaphragmatic muscle of the rat to a level 10- to 20-fold higher than the level in blood plasma, whereas in the dog and monkey, diaphragmatic concentrations were comparable with those in the plasma. Three degradation products of HI-6 were detected in the plasma of the three species. One excreted product formed spontaneously since it was also detected in buffered solutions used for abiotic stability studies. The second product, the picolinic acid analog of HI-6, appeared to be metabolically formed in vivo. A third product remains unidentified.

authors

Ecobichon DJ,Comeau AM,O'Neil WM,Marshall WD

doi

10.1139/y90-089

subject

Has Abstract

pub_date

1990-05-01 00:00:00

pages

614-21

issue

5

eissn

0008-4212

issn

1205-7541

journal_volume

68

pub_type

杂志文章
  • Prior glucose deprivation increases the first phase of glucose-induced insulin response: possible involvement of endogenous ATP and (or) ADP.

    abstract::A possible implication of endogenously released ATP and (or) ADP in insulin response to glucose stimulation was investigated in the isolated rat pancreas. The first phase of insulin response to the same glucose concentration (8.3 mM) was much higher in pancreas previously perfused in the absence of glucose than in pan...

    journal_title:Canadian journal of physiology and pharmacology

    pub_type: 杂志文章

    doi:10.1139/y93-086

    authors: Chapal J,Bertrand G,Hillaire-Buys D,Gross R,Loubatières-Mariani MM

    更新日期:1993-08-01 00:00:00

  • Studies on transhepatic insulin absorption.

    abstract::The intraperitoneal administration of insulin has been recommended because it was found to effectively control the plasma glucose level. Several authors have suggested that intraperitoneal insulin administration may be more "physiological" and therefore preferable because the insulin is absorbed into the portal venous...

    journal_title:Canadian journal of physiology and pharmacology

    pub_type: 杂志文章

    doi:10.1139/y86-036

    authors: Zingg W,Rappaport AM,Leibel BS

    更新日期:1986-03-01 00:00:00

  • Atrial natriuretic factor and urinary kallikrein in the rat: antagonistic factors?

    abstract::The rat atrium contains a potent natriuretic factor which appears to inhibit the sodium reabsorption in the collecting tubules of the kidneys. We examined the effects of the injection of partially purified atrial natriuretic factor (ANF) and synthetic ANF (8-33) into rats with simultaneous infusions of dextrose or apr...

    journal_title:Canadian journal of physiology and pharmacology

    pub_type: 杂志文章

    doi:10.1139/y84-105

    authors: Thibault G,Garcia R,Cantin M,Genest J

    更新日期:1984-06-01 00:00:00

  • Association of the positive inotropic action of ouabain with a second species of digitalis receptors.

    abstract::Studies were conducted to determine whether Na-K ATPase or a second species of digitalis receptors in canine cardiac sarcolemma membrane preparations is associated with the positive inotropic action of nontoxic concentrations of ouabain. [3H]ouabain association and dissociation experiments using highly enriched sarcol...

    journal_title:Canadian journal of physiology and pharmacology

    pub_type: 杂志文章

    doi:10.1139/y85-083

    authors: Kurobane I,Nandi DL,Okita GT

    更新日期:1985-05-01 00:00:00

  • Enhancement of hybrid-fiber types in rat soleus muscle after clenbuterol administration during hindlimb unloading.

    abstract::Our objective was to determine the effects of a clenbuterol (CB) treatment orally administered (2 mg per kg) to rats submitted to 14 days of hindlimb unloading (HU). The morphological and the contractile properties as well as the myosin heavy chain isoforms contained in each fiber type were determined in whole soleus ...

    journal_title:Canadian journal of physiology and pharmacology

    pub_type: 杂志文章

    doi:10.1139/y04-034

    authors: Picquet F,De-Doncker L,Falempin M

    更新日期:2004-05-01 00:00:00

  • Relaxant effect of atorvastatin on isolated rat gastric fundus strips: implications for Ca2+-signalling mechanisms.

    abstract::Statins are determined to have various pleiotropic effects apart from their lipid-lowering properties. Herein, we investigated the direct effects of atorvastatin on gastric smooth muscle tone. Atorvastatin effectively relaxed isolated rat gastric fundus strips precontracted with acetylcholine, potassium chloride, and ...

    journal_title:Canadian journal of physiology and pharmacology

    pub_type: 杂志文章

    doi:10.1139/cjpp-2018-0723

    authors: Kaleli-Durman D,Alp-Yıldırım Fİ,Özdemir O,Uydeş-Doğan BS

    更新日期:2019-05-01 00:00:00

  • Vascular, renal, and endocrine responses to low-dose atrial natriuretic peptide in the fluid-balanced New Zealand genetically hypertensive rats with and without endogenous arginine vasopressin.

    abstract::In hypertension, the relationship between atrial natriuretic peptide (ANP) and vasopressin (AVP) is not yet clear, although their renal actions are effectively autoregulation. To examine the possible interaction further, the responses to ANP infusion (75 ng x min (-1), i.v.) have been investigated in both hypertensive...

    journal_title:Canadian journal of physiology and pharmacology

    pub_type: 杂志文章

    doi:

    authors: Abu-Amarah I,Balment RJ

    更新日期:1999-02-01 00:00:00

  • Tranilast ameliorates cyclophosphamide-induced lung injury and nephrotoxicity.

    abstract::The world-wide increase in cancer incidence imposes a corresponding significant increase in the use of chemotherapeutic agents. Nephrotoxicity is a side effect frequently encountered with cyclophosphamide (CP), which is also well-known to cause acute and chronic lung toxicities. The current study focuses on the evalua...

    journal_title:Canadian journal of physiology and pharmacology

    pub_type: 杂志文章

    doi:10.1139/cjpp-2015-0070

    authors: Said E,Elkashef WF,Abdelaziz RR

    更新日期:2016-04-01 00:00:00

  • Preservation of ischemic myocardial tissue with an antagonist of vasoconstrictor eicosanoids.

    abstract::A new antagonist of the vasoconstrictor eicosanoids, L-640,035, was studied in a standardized model of myocardial ischemia (MI) in anesthetized cats. This eicosanoid antagonist was not found to exert any overt hemodynamic action in cats subjected to a sham myocardial ischemia protocol. However, the antagonist markedly...

    journal_title:Canadian journal of physiology and pharmacology

    pub_type: 杂志文章

    doi:10.1139/y84-246

    authors: Lefer AM,Burke SE,Lepran I

    更新日期:1984-12-01 00:00:00

  • Rate of fatigue during repeated submaximal contractions of human quadriceps muscle.

    abstract::Our purpose was to determine the effect of eight different combinations of contraction intensity, duration, and rest on the rate of fatigue in vastus lateralis muscle. A single combination consisted of contractions at 30 or 70% maximal voluntary contraction (MVC), held for 3 or 7 s with 3- or 7-s rest intervals. Contr...

    journal_title:Canadian journal of physiology and pharmacology

    pub_type: 杂志文章

    doi:10.1139/y91-211

    authors: Dolmage T,Cafarelli E

    更新日期:1991-10-01 00:00:00

  • Blood pressure control and erythrocytosis in rats: theory and observations.

    abstract::We compared some of our latest experiments on blood pressure control and erythrocytosis in spontaneously hypertensive rats with Gaar's computer-simulated studies, which suggest that erythrocytosis is a key to understanding the hemodynamic changes in hypertension. We tested two of Gaar's several predictions: (i) periph...

    journal_title:Canadian journal of physiology and pharmacology

    pub_type: 杂志文章

    doi:10.1139/y94-096

    authors: Gould AB,Goodman S,Swartz C

    更新日期:1994-06-01 00:00:00

  • Effect of chronic sulfonylurea treatment on the myocardium of insulin-dependent diabetic rats.

    abstract::Adult rats treated with high doses of streptozocin became progressively more hyperglycemic during the first month of the diabetic condition. Treatment of these rats with the sulfonylurea glyburide halted, and in some cases, reversed this process in a high percentage of the diabetics. Associated with the glyburide-medi...

    journal_title:Canadian journal of physiology and pharmacology

    pub_type: 杂志文章

    doi:10.1139/y88-242

    authors: Mozaffari MS,Wilson GL,Schaffer SW

    更新日期:1988-12-01 00:00:00

  • Hepoxilin A, hydroxyepoxide metabolite of arachidonic acid, stimulates transport of 45Ca across the guinea pig visceral yolk sac.

    abstract::The effect of hepoxilin A, a newly isolated hydroxyepoxide metabolite of arachidonic acid, on calcium transport across the visceral yolk sac membrane of the guinea pig was investigated in vitro in Ussing chambers. While 1-14C-labelled hepoxilin A itself was not transported across the membrane, it increased the rate of...

    journal_title:Canadian journal of physiology and pharmacology

    pub_type: 杂志文章

    doi:10.1139/y84-243

    authors: Derewlany LO,Pace-Asciak CR,Radde IC

    更新日期:1984-12-01 00:00:00

  • PTP1B and TC-PTP: novel roles in immune-cell signaling.

    abstract::It has recently been demonstrated that the protein tyrosine phosphatase (PTP) PTP1B and the T-cell PTP (TC-PTP) target several substrates involved in immune cell signaling. Recent data have furthered the view of these 2 PTP members as key regulators of the immune response. This review will focus on the substrate speci...

    journal_title:Canadian journal of physiology and pharmacology

    pub_type: 杂志文章,评审

    doi:10.1139/y06-012

    authors: Simoncic PD,McGlade CJ,Tremblay ML

    更新日期:2006-07-01 00:00:00

  • Comparative effects of tamoxifen and angiotensin II type-1 receptor antagonist therapy on the hemodynamic profile of the ovariectomized female rat.

    abstract::Hormonal replacement therapy (HRT) has failed to provide a cardioprotective action in postmenopausal women, and thus alternative pharmacological approaches are required. The present study examined the therapeutic potential of the partial estrogen receptor agonist tamoxifen and the angiotensin II type-1 receptor antago...

    journal_title:Canadian journal of physiology and pharmacology

    pub_type: 杂志文章

    doi:10.1139/y03-086

    authors: Pham-Dang ML,Clement R,Mercier I,Calderone A

    更新日期:2003-09-01 00:00:00

  • Vanadium exposure enhances lipid peroxidation in the kidney of rats and mice.

    abstract::Vanadium (V) as sodium orthovanadate induces an increase in lipid peroxidation in the kidneys after a single subcutaneous or intraperitoneal injection to rats or mice. The rate of malondialdehyde (MDA) formation, an index of lipid peroxidation, by kidney homogenates increased by more than 100% 1 h after injection. Chr...

    journal_title:Canadian journal of physiology and pharmacology

    pub_type: 杂志文章

    doi:10.1139/y85-037

    authors: Donaldson J,Hemming R,LaBella F

    更新日期:1985-03-01 00:00:00

  • Electromechanical characterization of the effects of racemic sotalol and its optical isomers on isolated canine ventricular trabecular muscles and Purkinje strands.

    abstract::In both isolated canine ventricular trabecular muscle and Purkinje strand preparations, dl-sotalol and its two optical isomers d- and l-sotalol produced a concentration-dependent increase in action potential duration while other transmembrane electrical characteristics were not significantly affected. The magnitude of...

    journal_title:Canadian journal of physiology and pharmacology

    pub_type: 杂志文章

    doi:10.1139/y85-248

    authors: Lathrop DA

    更新日期:1985-12-01 00:00:00

  • Mechanical factors regulating gastric emptying examined by the effects of exogenous cholecystokinin and secretin on canine gastroduodenal motility.

    abstract::The aim of this study was to elucidate the variables of gastroduodenal motility determining gastric emptying. For this purpose the effects of exogenous cholecystokinin, secretin, and gastric inhibitory polypeptide on motility and gastric emptying were studied during a meal. Motility was measured with extraluminal stra...

    journal_title:Canadian journal of physiology and pharmacology

    pub_type: 杂志文章

    doi:10.1139/y87-050

    authors: Keinke O,Ehrlein HJ,Wulschke S

    更新日期:1987-03-01 00:00:00

  • The interactive effects of fatigue and pH on the ionic conductance of frog sartorius muscle fibers.

    abstract::The effects of fatigue on the membrane conductance of frog sartorius muscle at the resting potential and during an action potential were studied. When muscles were exposed to an extracellular pH of 8.0 the membrane conductance at the resting potential increased during fatigue by about 20% and returned to prefatigue le...

    journal_title:Canadian journal of physiology and pharmacology

    pub_type: 杂志文章

    doi:10.1139/y85-237

    authors: Renaud JM,Mainwood GW

    更新日期:1985-11-01 00:00:00

  • Systemic site of action for pressor effect of angiotensin II injected into the fourth cerebral ventricle of rats?

    abstract::Angiotensin II (ANG II) causes a systemic pressor effect when injected into the cerebral ventricles. In the rat fourth ventricle, the effective doses for the ANG II pressor effect are over 100 times larger than in the systemic circulation. Considering the discrepancy of doses, the possibility that ANG II may reach the...

    journal_title:Canadian journal of physiology and pharmacology

    pub_type: 杂志文章

    doi:10.1139/y02-062

    authors: Pesquero JB,Fior-Chadi DR,Yu YG,Merjan AJ,Lindsey CJ,Paiva AC

    更新日期:2002-05-01 00:00:00

  • Vital marker for muscle nuclei in myoblast transfer.

    abstract::A new method is developed using Fluoro-Gold (FG) as a vital stain to label the nuclei of donor myoblasts in myoblast transfer studies. In vitro incubation with 0.01% FG for 16 h resulted in 100% nuclei labelling. Intensive fluorescence persisted following 9 days of subculture, when the human myoblasts were injected in...

    journal_title:Canadian journal of physiology and pharmacology

    pub_type: 杂志文章

    doi:10.1139/y91-008

    authors: Fang QW,Chen M,Li HJ,Goodwin TG,Law PK

    更新日期:1991-01-01 00:00:00

  • Hesperidin protects against cyclophosphamide-induced hepatotoxicity by upregulation of PPARγ and abrogation of oxidative stress and inflammation.

    abstract::The most important reason for the non-approval and withdrawal of drugs by the Food and Drug Administration is hepatotoxicity. Therefore, this study was undertaken to evaluate the protective effects of hesperidin against cyclophosphamide (CYP)-induced hepatotoxicity in Wistar rats. The rats received a single intraperit...

    journal_title:Canadian journal of physiology and pharmacology

    pub_type: 杂志文章

    doi:10.1139/cjpp-2014-0204

    authors: Mahmoud AM

    更新日期:2014-09-01 00:00:00

  • Geraniol promotes functional recovery and attenuates neuropathic pain in rats with spinal cord injury.

    abstract::Geraniol, a plant-derived monoterpene, has been extensively studied and showed a wide variety of beneficial effects. The aim of this study was to investigate the therapeutic effect of geraniol on functional recovery and neuropathic pain in rats with spinal cord injury (SCI). Rats received a clip-compression SCI and we...

    journal_title:Canadian journal of physiology and pharmacology

    pub_type: 杂志文章

    doi:10.1139/cjpp-2016-0528

    authors: Lv Y,Zhang L,Li N,Mai N,Zhang Y,Pan S

    更新日期:2017-12-01 00:00:00

  • Differential participation of protein kinase C and Rho kinase in alpha 1-adrenoceptor mediated contraction in rat arteries.

    abstract::The major functional alpha1-adrenoceptor in the rat aorta is of the alpha1Dsubtype and that in the caudal artery is of the alpha1A subtype. In the present study, the participation of protein kinase C (PKC) and Rho kinase (RhoK) in contractile responses to stimulation of the alpha1-adrenoceptors in these two arteries w...

    journal_title:Canadian journal of physiology and pharmacology

    pub_type: 杂志文章

    doi:10.1139/y04-086

    authors: Mueed I,Bains P,Zhang L,Macleod KM

    更新日期:2004-10-01 00:00:00

  • Myocardial and vascular lesions in the LA/N-corpulent rat.

    abstract::The LA/N-corpulent (LA/N-cp) rat is a normotensive strain derived from Koltesky's original mutant strain of the spontaneously hypertensive rat (SHR). When homozygous for the cp gene (cp/cp), the rats are hyperphagous, hyperlipidemic, hyperinsulinemic, and obese. The rats have been shown, by scanning electron microscop...

    journal_title:Canadian journal of physiology and pharmacology

    pub_type: 杂志文章

    doi:10.1139/y86-215

    authors: Russell JC,Amy RM

    更新日期:1986-10-01 00:00:00

  • Effect of taurine deficiency on tissue taurine concentrations and pregnancy outcome in the rat.

    abstract::Taurine status and pregnancy outcome were assessed in rats fed low dietary taurine and varying doses of guanidinoethyl sulfonate (GES), a structural analogue of taurine. Female Sprague-Dawley rats (225-270 g) were mated overnight and assigned to one of four groups from day 0 to 20 of gestation. Taurine-deficient anima...

    journal_title:Canadian journal of physiology and pharmacology

    pub_type: 杂志文章

    doi:10.1139/y95-161

    authors: Gottschall-Pass KT,Gorecki DK,Paterson PG

    更新日期:1995-08-01 00:00:00

  • Effects of medial prefrontal cortex stimulation on the spontaneous activity of the ventral pallidal neurons in the rat.

    abstract::The neural connections from the medial prefrontal cortex to the ventral pallidum were investigated in urethane-anesthetized rats. Extracellular recordings were made from 124 spontaneously firing neurons in the ventral pallidum while the medial prefrontal cortex was electrically stimulated. The most frequent response t...

    journal_title:Canadian journal of physiology and pharmacology

    pub_type: 杂志文章

    doi:10.1139/y93-053

    authors: Delgado-Martínez AD,Vives F

    更新日期:1993-05-01 00:00:00

  • In vivo interactions between prejunctional alpha 2- and beta 2-adrenoceptors at the level of the adrenal medulla.

    abstract::The combined effect of a beta 2-antagonist and an alpha 2-agonist on the release of adrenal catecholamines was studied in the anaesthetized and vagotomized dog. The electrical stimulation of the splanchnic nerve (5-V pulses of 2 ms duration for 3 min at a frequency of 3 Hz) produced a significant rise in adrenal catec...

    journal_title:Canadian journal of physiology and pharmacology

    pub_type: 杂志文章

    doi:10.1139/y88-219

    authors: Foucart S,de Champlain J,Nadeau R

    更新日期:1988-10-01 00:00:00

  • Chronic glucose-lowering effects of rosiglitazone and bis(ethylmaltolato)oxovanadium(IV) in ZDF rats.

    abstract::The aim of this study was to determine if there was a synergistic or additive effect of a thiazolidinedione derivative (rosiglitazone (ROS)) and a vanadium compound (bis(ethylmaltolato)oxovanadium(IV) (BEOV)) on plasma glucose and insulin levels following chronic oral administration to Zucker diabetic fatty (ZDF) rats...

    journal_title:Canadian journal of physiology and pharmacology

    pub_type: 杂志文章

    doi:10.1139/y03-094

    authors: Yuen VG,Bhanot S,Battell ML,Orvig C,McNeill JH

    更新日期:2003-11-01 00:00:00

  • Receptors for angiotensin: a critical analysis.

    abstract::Angiotensin exerts numerous contractile and secretory effects by activating specific receptors. Recent pharmacological findings obtained with this peptide in various laboratories are analyzed, using the order of potency of agonists and the affinity of competitive antagonists as criteria for the classification of recep...

    journal_title:Canadian journal of physiology and pharmacology

    pub_type: 杂志文章,评审

    doi:10.1139/y79-020

    authors: Regoli D

    更新日期:1979-02-01 00:00:00