Dissociation constants (KA) and relative efficacies of sympathomimetic amines in isolated atria during hypothermia-induced supersensitivity.

Abstract:

:Hypothermia increases the sensitivity of isolated cardiac muscle to stimulation by beta-adrenoceptor agonists. The purpose of this study was to determine pharmacologically whether this supersensitivity is associated with a change in the affinity of agonists for the receptor. The positive inotropic and chronotropic responses of guinea-pig paced left and spontaneously beating right atria were recorded. Cumulative dose--response curves to noradrenaline (or adrenaline) were compared with isoproterenol in each tissue. At 38 degrees C, the rate curves were to the left of the tension curves, with lower mean effective concentration (EC50) values. However, this difference was less for noradrenaline and adrenaline which were therefore tension selective relative to isoproterenol. Lowering the temperature to 25 degrees C induced supersensitivity, all dose--response curves being displaced to the left. In the presence of carbachol the curves were shifted to the right with depression of the maxima. Dissociation constants (KA) were calculated from plots of reciprocals of equiactive concentrations obtained before and in the presence of carbachol. KA values for rate and tension responses of each agonist were identical at 38 degrees C, indicating that the rate selectivity was not due to affinity differences. The efficacies (er) of noradrenaline and adrenaline were greater than isoproterenol for tension, but smaller for rate responses, which may explain their relative tension selectivity. At 25 degrees C, the KA values of all agonists were reduced approximately 10-fold. Hypothermia-induced supersensitivity is therefore associated with an increase in affinity for the cardiac beta-adrenoceptor.

authors

Broadley KJ,McNeill JH

doi

10.1139/y83-088

subject

Has Abstract

pub_date

1983-06-01 00:00:00

pages

572-80

issue

6

eissn

0008-4212

issn

1205-7541

journal_volume

61

pub_type

杂志文章
  • Bradykinin B2 receptor antagonists: development and applications.

    abstract::Most physiological and pathophysiological responses to bradykinin are mediated by G-protein-coupled receptors designated B2 receptors. Discovery of antagonists for these receptors has brought about a revolution in research in the kinin field. The chemistry and development of antagonists for B2 kinin receptors are disc...

    journal_title:Canadian journal of physiology and pharmacology

    pub_type: 杂志文章,评审

    doi:10.1139/y95-106

    authors: Stewart JM

    更新日期:1995-07-01 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

  • Intracerebroventricular infusion of angiotensin AT2 receptor agonist novokinin aggravates some diabetes-mellitus-induced alterations in Wistar rats.

    abstract::Cumulative data suggest the significant role of the renin-angiotensin system in the development of the pathological consequences of diabetes mellitus (DM). Newly synthesized AT2 receptor agonists gained importance as a target for creating new antihypertensives. The aim of the present work was to study the effects of p...

    journal_title:Canadian journal of physiology and pharmacology

    pub_type: 杂志文章

    doi:10.1139/cjpp-2017-0428

    authors: Pechlivanova D,Petrov K,Grozdanov P,Nenchovska Z,Tchekalarova J,Stoynev A

    更新日期:2018-05-01 00:00:00

  • The soluble guanylyl cyclase inhibitor 1H-[1,2,4]oxadiazolo[4,3-alpha]quinoxalin-1-one (ODQ) inhibits relaxation of rabbit aortic rings induced by carbon monoxide, nitric oxide, and glyceryl trinitrate.

    abstract::Carbon monoxide (CO), a vasodilator, has been implicated as an activator of soluble guanylyl cyclase (sGC) to effect smooth muscle relaxation; however, this idea has not received universal support. The purpose of this study was to examine the effects of the sGC inhibitor 1H-[1,2,4]oxadiazolo[4,3-alpha]quinoxalin-1-one...

    journal_title:Canadian journal of physiology and pharmacology

    pub_type: 杂志文章

    doi:

    authors: Hussain AS,Marks GS,Brien JF,Nakatsu K

    更新日期:1997-08-01 00:00:00

  • A dual mechanism for the anticonvulsant action of aminooxyacetic acid.

    abstract::The intramuscular injection of aminooxyacetic acid (AOAA) into mice elevated the concentration of gamma-aminobutyric acid (GABA) in the brain, inhibited glutamic acid decarboxylase activity and delayed the onset of isonicotinic acid hydrazide induced seizures. Analyses of these results and of those obtained previously...

    journal_title:Canadian journal of physiology and pharmacology

    pub_type: 杂志文章

    doi:10.1139/y76-074

    authors: Wood JD,Peesker SJ

    更新日期:1976-08-01 00:00:00

  • Involvement of insulin-like growth factor 1 receptor transactivation in endothelin-1-induced signaling in vascular smooth muscle cells.

    abstract::Endothelin-1 (ET-1) is a potent vasoactive peptide that exerts hypertrophic, migratory, and mitogenic effects in vascular smooth muscle cells. ET-1-induced activation of several signaling events has been shown to mediate the cellular effects of ET-1. In the past several years, transactivation of growth factor receptor...

    journal_title:Canadian journal of physiology and pharmacology

    pub_type: 杂志文章,评审

    doi:10.1139/y10-030

    authors: Bouallegue A,Vardatsikos G,Srivastava AK

    更新日期:2010-05-01 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

  • Increase in ventricular fibrillation threshold following blockade of atrioventricular conduction.

    abstract::The threshold for electrically induced ventricular fibrillation was determined in anesthetized open-chest dogs, before and after blockade of atrioventricular (A-V) conduction. Without exception, the threshold was significantly elevated after creation of the block. The precise mechanism of this effect is not known at t...

    journal_title:Canadian journal of physiology and pharmacology

    pub_type: 杂志文章

    doi:10.1139/y83-160

    authors: Reynolds AK,Dresel PE

    更新日期:1983-09-01 00:00:00

  • Reciprocal regulation of cholesterol and beta amyloid at the subcellular level in Alzheimer's disease.

    abstract::Since the discovery that apolipoprotein E, a cholesterol transport protein, is a major risk factor for Alzheimer's disease (AD) development, there has been a remarkable interest in understanding the many facets of the relationship between cholesterol and AD. Several lines of evidence have demonstrated the importance o...

    journal_title:Canadian journal of physiology and pharmacology

    pub_type: 杂志文章,评审

    doi:10.1139/y2012-076

    authors: Posse de Chaves E

    更新日期:2012-06-01 00:00:00

  • YC-1 enhances the responsiveness of tolerant vascular smooth muscle to glyceryl trinitrate.

    abstract::A major limitation of the use of organic nitrates in cardiovascular medicine is the development of tolerance, which has been attributed, in part, to a decrease in their metabolic activation in the vascular smooth muscle cell. Recently, 3-(5'-hydroxymethyl-2'-furyl)-1-benzylindazole (YC-1) was shown to potentiate vascu...

    journal_title:Canadian journal of physiology and pharmacology

    pub_type: 杂志文章

    doi:

    authors: O'Reilly DA,McLaughlin BE,Marks GS,Brien JF,Nakatsu K

    更新日期:2001-01-01 00:00:00

  • Role of the Na+-H+ exchanger (NHE1) in heart muscle function during transient acidosis. A study in papillary muscles from rat and guinea pig hearts.

    abstract::The sodium-hydrogen exchanger (NHE) helps the cell to recover from intracellular acidosis. In this study, we have investigated the effect of HOE 642 (a specific NHE1 blocker) on papillary muscles from rats and guinea pigs during transient acidosis and PKC activation by recording developed force (DF), action potential ...

    journal_title:Canadian journal of physiology and pharmacology

    pub_type: 杂志文章

    doi:10.1139/y03-091

    authors: Sundset R,Bertelsen G,Ytrehus K

    更新日期:2003-10-01 00:00:00

  • NMDA receptors in the dorsal hippocampal area are involved in tramadol state-dependent memory of passive avoidance learning in mice.

    abstract::The precise neurobiological mechanisms of tramadol abuse underlying the cognitive function are still unknown. The aim of the present study was to examine the possible effects of intra-CA1 injections of N-methyl-d-aspartate (NMDA), a glutamate NMDA receptor (NMDAR) agonist, and d,l-2-amino-5-phosphonopentanoic acid (DL...

    journal_title:Canadian journal of physiology and pharmacology

    pub_type: 杂志文章

    doi:10.1139/cjpp-2017-0228

    authors: Jafari-Sabet M,Mofidi H,Attarian-Khosroshahi MS

    更新日期:2018-01-01 00:00:00

  • Synthetic nitrovasodilators are effective, in vitro, in relaxing penile tissue from impotent men: the findings and their implications.

    abstract::Normal penile erectile function is dependent on arterial adequacy, appropriate venous occlusion, neurohumoral factors, and finally the relaxation of penile cavernous trabecular smooth muscle. The present experiments were designed to test whether compounds related to endothelium-derived relaxing factor have a role in p...

    journal_title:Canadian journal of physiology and pharmacology

    pub_type: 杂志文章

    doi:10.1139/y89-014

    authors: Heaton JP

    更新日期:1989-01-01 00:00:00

  • Impact of enalapril therapy on in vitro coronary artery responsiveness in pacing-induced heart failure.

    abstract::In vitro coronary artery responsiveness to angiotensin I, angiotensin II, noradrenaline, phenylephrine, BHT 920, and potassium chloride together with functional relaxation to acetylcholine was investigated in dogs with pacing-induced heart failure treated with enalapril (oral administration of 10 mg.day-1) for a mean ...

    journal_title:Canadian journal of physiology and pharmacology

    pub_type: 杂志文章

    doi:10.1139/y92-199

    authors: Forster C,Larosa G,Armstrong PW

    更新日期:1992-10-01 00:00:00

  • Exposure to ionizing radiation alters vasoreactivity in rat jejunum ex vivo.

    abstract::The effect of ionizing radiation on jejunal blood flow was investigated in rats receiving whole-body exposure to 10 Gy gamma-radiation. Irradiation resulted in increased myeloperoxidase activity, indicative of neutrophil infiltration, and prostaglandin E2 synthesis by 2 h post-irradiation, but had no effect on leukotr...

    journal_title:Canadian journal of physiology and pharmacology

    pub_type: 杂志文章

    doi:10.1139/y95-090

    authors: MacNaughton WK,Prud'homme-Lalonde L

    更新日期:1995-06-01 00:00:00

  • Subcellular calcium transport during contractile failure and recovery in heart perfused with Na-free medium.

    abstract::Perfusion of isolated rat hearts with Na-free medium resulted in an immediate increase in contractile force followed by a decline and complete loss of contractile force within 25 s. The recovery of the contractile force upon reperfusion was only partial if the duration of Na-free perfusions was 10 min or longer. Ca bi...

    journal_title:Canadian journal of physiology and pharmacology

    pub_type: 杂志文章

    doi:10.1139/y80-218

    authors: Dhalla NS,Lee SL,Singal PK,Yates JC,Panagia V

    更新日期:1980-12-01 00:00:00

  • Improved carbohydrate tolerance in fibre-fed rats: studies of the chronic effect.

    abstract::The effect of chronic consumption of diets containing either different sources of dietary fibre (8% guar, 8% pectin, or 8% multifibre) or low carbohydrate upon carbohydrate tolerance was examined in rats. Weight gain was significantly lower throughout the entire 28-day study period with the guar group and after 20 day...

    journal_title:Canadian journal of physiology and pharmacology

    pub_type: 杂志文章

    doi:10.1139/y82-107

    authors: Track NS,Cannon MM,Flenniken A,Katamay S,Woods EF

    更新日期:1982-06-01 00:00:00

  • Tyrosine kinase inhibitors and the contractile action of G-protein-linked vascular agonists.

    abstract::In a porcine coronary artery helical strip preparation, the tyrosine kinase inhibitors genistein and tyrphostin (AG82) attenuated the contractile actions of angiotensin II, arginine vasopressin, epidermal growth factor--urogastrone, noradrenaline, and prostaglandin F2 alpha, under conditions where contractions due to ...

    journal_title:Canadian journal of physiology and pharmacology

    pub_type: 杂志文章

    doi:10.1139/y94-150

    authors: Laniyonu AA,Saifeddine M,Yang SG,Hollenberg MD

    更新日期:1994-09-01 00:00:00

  • B2 receptor activation reduces Erk1 and Erk2 phosphorylation induced by insulin-like growth factor-1, platelet-derived growth factor-BB, and high glucose in rat isolated glomeruli.

    abstract::Several experimental data document an activation of the mitogen-activated protein kinases Erk1 and Erk2 by bradykinin (BK), an agonist of the kinin B2 receptor (B2R). In contrast, other reports showed an inhibitory modulation of mitogenesis by BK. Therefore, we explored in the isolated glomeruli the effect of B2R acti...

    journal_title:Canadian journal of physiology and pharmacology

    pub_type: 杂志文章

    doi:10.1139/y02-033

    authors: Cellier E,Duchêne J,Pécher C,Alric C,Bascands JL,Schanstra JP,Girolami JP

    更新日期:2002-04-01 00:00:00

  • Cyclocarya paliurus prevents high fat diet induced hyperlipidemia and obesity in Sprague-Dawley rats.

    abstract::Cyclocarya paliurus (CP; qing qian liu), which is used as an herbal tea in China, has been confirmed to have therapeutic effects on hyperlipidemia and obesity, and therefore it is widely consumed to prevent metabolic diseases such as hyperlipidemia and diabetes. In this study, we investigated the preventive effects of...

    journal_title:Canadian journal of physiology and pharmacology

    pub_type: 杂志文章

    doi:10.1139/cjpp-2014-0477

    authors: Yao X,Lin Z,Jiang C,Gao M,Wang Q,Yao N,Ma Y,Li Y,Fang S,Shang X,Ni Y,Zhang J,Yin Z

    更新日期:2015-08-01 00:00:00

  • Neuropeptide Y: a new mediator linking sympathetic nerves, blood vessels and immune system?

    abstract::Neuropeptide Y (NPY(1-36)), a sympathetic cotransmitter and neurohormone, has pleiotropic activities ranging from the control of obesity to anxiolysis and cardiovascular function. Its actions are mediated by multiple Gi/o-coupled receptors (Y1-Y5) and modulated by dipeptidyl peptidase IV (DPPIV/cd26), which inactivate...

    journal_title:Canadian journal of physiology and pharmacology

    pub_type: 杂志文章,评审

    doi:10.1139/y03-006

    authors: Zukowska Z,Pons J,Lee EW,Li L

    更新日期:2003-02-01 00:00:00

  • The endothelium: influencing vascular smooth muscle in many ways.

    abstract::The endothelium, although only a single layer of cells lining the vascular and lymphatic systems, contributes in multiple ways to vascular homeostasis. Subsequent to the 1980 report by Robert Furchgott and John Zawadzki, there has been a phenomenal increase in our knowledge concerning the signalling molecules and path...

    journal_title:Canadian journal of physiology and pharmacology

    pub_type: 杂志文章,评审

    doi:10.1139/y2012-073

    authors: Triggle CR,Samuel SM,Ravishankar S,Marei I,Arunachalam G,Ding H

    更新日期:2012-06-01 00:00:00

  • Voltage-dependent inactivation of the potassium current of embryonic chick hepatocytes.

    abstract::The whole-cell patch electrode voltage clamp technique was used to study the inactivation properties of the delayed rectifying potassium current of single cultured embryonic chick hepatocytes at 20 degrees C. The potassium current activates maximally within 250-500 ms of membrane depolarization, after which it decays ...

    journal_title:Canadian journal of physiology and pharmacology

    pub_type: 杂志文章

    doi:10.1139/y91-110

    authors: Hill CE,Shrier A

    更新日期:1991-06-01 00:00:00

  • Validation of a single-compartment approach to the calculation of secretion rates of ACTH.

    abstract::A single-compartment model used in this laboratory for continuously calculating ACTH secretion rates from measured plasma ACTH concentrations has been tested for its ability to follow changing rates of ACTH entry (rapid departure from steady state). ACTH was infused at known moderately high but physiological rates int...

    journal_title:Canadian journal of physiology and pharmacology

    pub_type: 杂志文章

    doi:10.1139/y78-061

    authors: Cowan JS

    更新日期:1978-06-01 00:00:00

  • Evidence that the hypothermic response of mice to delta-9-tetrahydrocannabinol is not mediated by changes in thermogenesis in brown adipose tissue.

    abstract::Delta 9-Tetrahydrocannabinol (20 mg/kg i.p.) and propranolol (20 and 50 mg/kg i.p.) produced marked falls in the rectal temperatures of mice kept at an ambient temperature of 22 degrees C. Propranolol (50 mg/kg i.p.) also decreased the thermogenic activity of brown fat, as measured by a decrease in the level of [3H]GD...

    journal_title:Canadian journal of physiology and pharmacology

    pub_type: 杂志文章

    doi:10.1139/y91-114

    authors: Pertwee RG,Nash K,Trayhurn P

    更新日期:1991-06-01 00:00:00

  • Myocardial energetics and blood flow in acute rapid ventricular pacing.

    abstract::The mechanism whereby chronic rapid ventricular pacing induces severe heart failure is unclear, but the phenomenon is associated with a reduction in left ventricular ATP levels. Accordingly, the current study was undertaken to evaluate the acute effects of rapid ventricular pacing on hemodynamics, left ventricular ade...

    journal_title:Canadian journal of physiology and pharmacology

    pub_type: 杂志文章

    doi:10.1139/y94-002

    authors: Simmons WW,Moe GW,Grima EA,Howard RJ,Armstrong PW

    更新日期:1994-01-01 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

  • A comparison of the dipsogenic responses of male and female rats to a variety of stimuli.

    abstract::Female rats subjected to 48 h of water deprivation drank more than similarly deprived males. There was no sexual difference in the dipsogenic responses to intracellular dehydration produced by intravenous hypertonic NaCl but females drank considerably more than males in response to the extracellular stimuli of hyperon...

    journal_title:Canadian journal of physiology and pharmacology

    pub_type: 杂志文章

    doi:10.1139/y80-179

    authors: Kaufman S

    更新日期:1980-10-01 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

  • Digoxin-amiodarone interaction: in vivo and in vitro studies in rats.

    abstract::Amiodarone is a new antiarrhythmic drug, commonly coadministered with digoxin in various cardiac disorders. Amiodarone caused a 10-fold increase of serum digoxin in rats, when the two drugs were simultaneously administered. Amiodarone significantly reduced digoxin uptake by renal cortical slices in the rat, and failed...

    journal_title:Canadian journal of physiology and pharmacology

    pub_type: 杂志文章

    doi:10.1139/y83-212

    authors: Koren G,Soldin S,Macleod SM

    更新日期:1983-12-01 00:00:00