Vasorelaxant effects of the potassium channel opener SR on the isolated human saphenous vein and rat aorta

Similar documents
Effect of ryanodine on sinus node recovery time determined in vitro

The effect of L-arginine on guinea-pig and rabbit airway smooth muscle function in vitro

Atropine and ODQ antagonize tetanic fade induced by L-arginine in cats

Differential effects of isoproterenol on the activity of angiotensin-converting enzyme in the rat heart and aorta

Abstract. J.F. Cunha 1, F.D. Campestrini 1, J.B. Calixto 2, A. Scremin 1 and N. Paulino 1

E ects of KRN2391 on ionic currents in rabbit femoral arterial myocytes

Temporal Relation of ATP-Sensitive Potassium- Channel Activation and Contractility Before Cardioplegia

INVOLVEMENT OF K+ CHANNELS IN THE RELAXANT RESPONSES TO VARIOUS AGONISTS IN ESTROGEN PRIMED RAT UTERUS

Ischaemic Preconditioning prevents the differentiation induced by ischaemia/reperfusion injury of rat cardiac fibroblast to myofibroblast

Effect of chronic oral administration of a low dose of captopril on sodium appetite of hypothyroid rats. Influence of aldosterone treatment

Abstract. A.N.C. Santana 1, E.M. Trindade-Filho 2, R.B. Cunha 3, M.V. Sousa 3, E.A. Cavalheiro 2 and K.M. Carvalho 1

Role of bradykinin in postprandial hypotension in humans

Zinc and water intake in rats: investigation of adrenergic and opiatergic central mechanisms

Standardization of a fluorimetric assay for the determination of tissue angiotensin-converting enzyme activity in rats

Cross-talk between Two Partners Regulates the Gating of the K ATP Channel Pore

Central lead administration inhibits water intake and sodium appetite in rats

Staircase in mammalian muscle without light chain phosphorylation

Reactivity of the isolated perfused rat tail vascular bed

gravid rat myometrial activity

Axotomy increases NADPH-diaphorase activity in the dorsal root ganglia and lumbar spinal cord of the turtle Trachemys dorbigni

The negative inotropic effect of nicorandil is independent of cyclic GMP changes: a comparison with pinacidil and cromakalim in canine atrial muscle

We also tested the hypothesis that the inhibitory effects of etomidate and ketamine involved a decrease in

Contributions of K ATP and K Ca channels to cerebral arteriolar dilation to hypercapnia in neonatal brain

11/10/2014. Muscular pump Two atria Two ventricles. In mediastinum of thoracic cavity 2/3 of heart's mass lies left of midline of sternum

Calcium handling by vascular myocytes in hypertension

Pulmonary circulation. Lung Blood supply : lungs have a unique blood supply system :

Examination Period 3: 2016/17

Differential responses to endothelial dependent relaxation of the thoracic and abdominal aorta from male Sprague-Dawley rats

10/23/2017. Muscular pump Two atria Two ventricles. In mediastinum of thoracic cavity 2/3 of heart's mass lies left of midline of sternum

Abstract. R. Roesler 1, J. Quevedo 1, C. Rodrigues 1, M. Madruga 1, M.R.M. Vianna 1 and M.B.C. Ferreira 2

Anatomy and Physiology, Spring 2015 Exam II: Form A April 9, Name Student Number

Inhibition of ATP-sensitive potassium channels attenuates propofol-induced vasorelaxation

Access to the published version may require journal subscription. Published with permission from: Elsevier.

The Mammalian Circulatory System

Supplemental Figure I

Relaxant Effects of Matrine on Aortic Smooth Muscles of Guinea Pigs 1

Mr. Epithelium s Anatomy and Physiology Test SSSS

Centro de Engenharia Biomédica and 2

Lab 16. The Cardiovascular System Heart and Blood Vessels. Laboratory Objectives

Previous experimental evidence indicates that some cardiovascular

Evidence for a Role of Cyclic AMP and Endothelium in Rat Aortic Relaxation

Aprikalim Reduces the Na -Ca 2 Exchange Outward Current Enhanced by Hyperkalemia in Rat Ventricular Myocytes

New Treatment Modalities for Benign Prostatic Hyperplasia. Seung-June Oh, MD Department of Urology, Seoul National University Hospital

Gracious R. Ross and Chandra Yallampalli. Department of Obstetrics and Gynecology, University of Texas Medical Branch, Galveston, Texas

produce smooth muscle contraction. technique in single smooth muscle cells isolated from the rabbit portal vein.

Differences in cardiac atrial and ventricular ion channels

Relaxation responses of aortic rings from salt-loaded high calcium fed rats to potassium chloride, calcium chloride and magnesium sulphate

In vivo and in vitro effect of imipramine and fluoxetine on Na +,K + -ATPase activity in synaptic plasma membranes from the cerebral cortex of rats

The Heart. Happy Friday! #takeoutyournotes #testnotgradedyet

Sulfur dioxide relaxes rat aorta by endothelium-dependent and. -independent mechanisms

Chapter 11. The Cardiovascular System. Clicker Questions Pearson Education, Inc.

Cardiovascular Physiology. Heart Physiology. Introduction. The heart. Electrophysiology of the heart

Evaluation of Relaxant Effect of Levcromakalim on Oxytocin Induced Contraction of Isolated Rat Uterus

Cardiovascular Physiology

Effects of adrenalectomy and adrenal enucleation on liquid gastric emptying in rats

Antihypertensive Agents Part-2. Assistant Prof. Dr. Najlaa Saadi PhD Pharmacology Faculty of Pharmacy University of Philadelphia

Summary of PhD thesis. Attila Kun

Hawthorn Extract - Viable Treatment for Cardiovascular Disease or Unscrupulous Herbal Supplement?

CONTRIBUTION OF POTASSIUM CHANNELS TO MYOGENIC RESPONSE IN SKELETAL MUSCLE ARTERIOLES: EFFECTS OF AGE AND FIBER TYPE. A Thesis SE JEONG KIM

Mechanisms of Vasodilation of Cerebral Vessels Induced by the Potassium Channel Opener Nicorandil in Canine In Vivo Experiments

Mapping cancer, cardiovascular and malaria research in Brazil

Endothelium-Dependent Responses in Small Human Mesenteric Arteries

Research Pulmonary vasoconstrictor action of KCNQ potassium channel blockers Shreena Joshi 1,2, Prabhu Balan 1 and Alison M Gurney* 1,2

Lesson 10 Circulatory System (Nelson p.88-93)

Studies on the effects of viprostol in isolated small blood vessels and thoracic aorta of the rat

Catecholamine-induced vasoconstriction is sensitive to carbonic anhydrase I activation

cast specimens Showing the branches of arteries, with the skull reserved. C005 Head veins and skull

2) Put these in order: I repolarization II- depolarization of action potential III- rest IV- depolarization to threshold

A high-fructose diet induces changes in pp185 phosphorylation in muscle and liver of rats

single-channel events was very similar to that of the whole-cell, delayed rectifier (Kotlikoff, 1990).

Angina Pectoris Dr. Shariq Syed

1. Which of the following blood vessels has a thin elastic layer? A. Aorta. B. Pulmonary artery. C. Posterior vena cava. D. Mesenteric capillary.

DOI: /AVB N UDK 619:

S. Houjou*, K. Iizuka*, K, Dobashi*, T. Nakazawa**

The Heart. Size, Form, and Location of the Heart. 1. Blunt, rounded point; most inferior part of the heart.

Inhibition of vascular K ATP channels by U-37883A: a comparison with cardiac and skeletal muscle

Pharmacological and histopathological study of cyclophosphamide-induced hemorrhagic cystitis - comparison of the effects of dexamethasone and Mesna

Collin County Community College

PKC, Ca 2+, and Myogenic Constriction

PHYSIOLOGY MeQ'S (Morgan) All the following statements related to blood volume are correct except for: 5 A. Blood volume is about 5 litres. B.

The effect of acidosis on the ECG of the rat heart

Blood flows away from the heart in arteries, to the capillaries and back to the heart in the veins

Structure and organization of blood vessels

Alteration of binding sites for [ 3 H]P1075 and [ 3 H]glibenclamide in renovascular hypertensive rat aorta 1

Cardiovascular System. I. Structures of the heart A. : Pericardium sack that surrounds the heart

RV dysfunction and failure PATHOPHYSIOLOGY. Adam Torbicki MD, Dept Chest Medicine Institute of Tuberculosis and Lung Diseases Warszawa, Poland

Blood Vessels and Our Pulse

This lab activity is aligned with Visible Body s A&P app. Learn more at visiblebody.com/professors

Circulatory Systems. All cells need to take in nutrients and expel metabolic wastes.

Chapter 14. The Cardiovascular System

Abstract. Introduction. M.O. Lásaro 1, A.M.B. Alves 1,2, H.C.R. Guillobel 3, D.F. Almeida 1 and L.C.S. Ferreira 1

Abstract. S.L.D. Dalle Lucca 1, J.J. Dalle Lucca 1, A.C.R. Borges 1, S.S.M. Ihara 2 and T.B. Paiva 1

38 Noble ] mm. Acta Physiologica Sinica Tsinghua Tongfang Optical Disc Co., Ltd. All rights reserved. ; icv M ; icv H 1 (250 , NT

Coronary Circulation Under normal conditions cardiac muscle metabolism is almost exclusively aerobic depending on oxidative phosorylation to

Chapter 12. Capillaries. Circulation. The circulatory system connects with all body tissues

Pharmacological characterization of the sulphonylurea receptor in rat isolated aorta

Drug Treatment of Ischemic Heart Disease

A&P 2 CANALE T H E U R I N A R Y S Y S T E M

Effects of ouabain on vascular reactivity

Transcription:

Brazilian Vasorelaxant Journal effects of Medical of SR 4763 and Biological Research (2) 33: 961-966 ISSN -879X 961 Vasorelaxant effects of the potassium channel opener SR 4763 on the isolated human saphenous vein and rat aorta D.N. Criddle 1 and R.S. de Moura 2 1 Departamento de Ciências Fisiológicas, Centro de Ciências da Saúde, Universidade Estadual do Ceará, Fortaleza, CE, Brasil 2 Departamento de Farmacologia, Instituto de Biologia, Centro Biomédico, Universidade do Estado do Rio de Janeiro, Rio de Janeiro, RJ, Brasil Correspondence D.N. Criddle Departamento de Ciências Fisiológicas Centro de Ciências da Saúde Universidade Estadual do Ceará Av. Paranjana, 17 674- Fortaleza, CE Brasil Fax: +55-85-299-27 E-mail: criddle@uece.br Research supported by CNPq, FAPERJ and FUNCAP. Received July 28, 1999 Accepted May 3, 2 Abstract Key words SR 4763 K + -channel Human saphenous vein K ATP Rat aorta Levcromakalim Glibenclamide Introduction

962 D.N. Criddle and R.S. de Moura Material and Methods Preparation of blood vessels Organ chamber experiments Experimental protocols Drugs Statistical analysis

Vasorelaxant effects of SR 4763 963 Results Relaxant effects of SR 4763 on KCl- and noradrenaline-induced contraction of the human saphenous vein Relaxant effects of SR 4763 on KCl- and noradrenaline-induced contraction of the rat aorta 2 4 6 8 2 4 6 8 A B Figure 1 - Relaxant effects of SR 4763 on human saphenous vein precontracted with 2 mm KCl (A) and 1 µm noradrenaline (B) in the presence (filled circles) and absence (open circles) of 3 µm glibenclamide. Data are reported as means ± SEM (N = 6-11). Table 1 - IC 5 values for SR 4763-induced relaxation of human saphenous vein and rat aorta. Values are reported as means, with 95% confidence limits and number of observations in parentheses. *P<.1 for control vs glibenclamide (glib) (Student t-test). DR A = + glib IC 5 /control IC 5. Spasmogen Human saphenous vein Rat thoracic aorta Control IC 5 + glib IC 5 DR A Control IC 5 + glib IC 5 DR A KCl (2 mm) 8.1 nm.412 µm 5.9 3.86 nm.219 µm 56.7 (7.48-8.72) (11) (.272-.552) (9)* (2.7-5.55) (8) (.151-.287) (8)* Noradrenaline 3.2 nm - 8.82 nm - (1 µm) (2.64-34.) (6) (7.5-1.14) (8)

964 D.N. Criddle and R.S. de Moura Figure 2 - Relaxant effects of SR 4763 on rat aorta precontracted with 2 mm KCl (A) and 1 µm noradrenaline (B) in the presence (filled circles) and absence (open circles) of 3 µm glibenclamide. Data are reported as means ± SEM (N = 8). Discussion 2 4 6 8 2 4 6 8 A B

Vasorelaxant effects of SR 4763 965 Acknowledgments References 1. Lacour C, Canals F, Galindo G & Gaultier P (1991). Hypotensive effects of a novel potassium channel opener, SR 4763, in rats. Fundamental and Clinical Pharmacology, 5: 829 (Abstract). 2. Dorman BH, Hebbar L, Zellner JL, New RB, Houck WV, Acsell J, Nettles C, Hendrick JW, Sampson AP, Mukherjee R & Spinale FG (1998). ATP-sensitive potassium channel activation before cardioplegia. Effects on ventricular and myocyte function. Circulation, 98: II-176-II-183. 3. Guiraudou P, Rizzoli G, Gavraud R, Nisato D & Gaultier P (1991). New potassium channel opener, SR 4763, effects on rat portal vein and on isolated perfused guinea pig heart. Fundamental and Clinical Pharmacology, 5: 829 (Abstract). 4. Cristophe B, Chatelain P & Manning AS (1992). SR 4763, a new K + channel opener: effect on 86 Rb efflux from rat aorta. British Journal of Pharmacology, 16: 34P (Abstract). 5. Martin CAE, Naline E & Advenier C (1991). Comparison of the effects of SR 4763 and cromakalim on airway smooth muscle. Fundamental and Clinical Pharmacology, 5: 836 (Abstract). 6. Kajioka S, Oike M & Kitamura K (199). Nicorandil opens a calcium-dependent potassium channel in smooth muscle cells of the rat portal vein. Journal of Pharmacology and Experimental Therapeutics, 254: 95-913. 7. Noack Th, Deitmer P, Edwards G & Weston AH (1992). Characterization of potassium currents modulated by BRL 38227 in rat portal vein. British Journal of Pharmacology, 16: 717-726. 8. Beech DJ, Zhang H, Nakao K & Bolton TB (1993). Single channel and whole-cell currents evoked by levcromakalim in smooth muscle cells from rabbit portal vein. British Journal of Pharmacology, 11: 583-59. 9. Criddle DN, Greenwood IA & Weston AH (1994). Levcromakalim-induced modulation of membrane potassium currents, intracellular Ca 2+ and mechanical activity in rat mesenteric artery. Naunyn-Schmiedeberg s Archives of Pharmacology, 349: 422-43. 1. Gaultier P & Bertrand JP (1991). Study of a new potassium channel opener, SR 4763, on action potential and contraction of guinea pig papillary muscle. Fundamental and Clinical Pharmacology, 5: 828 (Abstract). 11. Criddle DN, Jazbik W & Soares de Moura R (1995). Differential vasorelaxant effects of levcromakalim and P16 in the isolated KCl- and RbCl-precontracted human saphenous vein: possible involvement of intracellular calcium stores. European Journal of Pharmacology, 286: 123-13. 12. Criddle DN, Soares De Moura R, Domingos LR & De Lima Maia E (1995). Vasorelaxant effects of SR 4763 in human saphenous vein and rat aorta. British Journal of Pharmacology, 117: 263P (Abstract). 13. Cook NS, Weir SW & Danzeisen MC (1988). Anti-vasoconstrictor effects of the K + channel opener cromakalim on the rabbit aorta - comparison with the Ca 2+ -antagonist isradipine. British Journal of Pharmacology, 95: 741-752. 14. Masuzawa K, Asano M, Matsuda T, Imaizumi Y & Watanabe M (199). Comparison of effects of cromakalim and pinacidil on mechanical activity and 86 Rb + efflux in dog coronary arteries. Journal of Pharmacology and Experimental Therapeutics, 253: 586-593. 15. Masuzawa K, Asano M, Matsuda T, Imaizumi Y & Watanabe M (199). Possible involvement of ATP-sensitive K + channels in the relaxant response of dog middle cerebral artery to cromakalim. Journal of Pharmacology and Experimental Therapeutics, 255: 818-825. 16. Forestier C, Depresle Y & Vivaudou M (1993). Intracellular protons control the affinity of skeletal muscle ATP-sensitive K + channels for potassium-channel-openers. FEBS Letters, 325: 276-28. 17. Forestier C, Pierrard J & Vivaudou M (1996). Mechanism of action of K channel openers on skeletal muscle KATP chan-

966 D.N. Criddle and R.S. de Moura nels. Interactions with nucleotides and protons. Journal of General Physiology, 17: 489-52. 18. Tourneur Y, Marion A & Gaultier P (1994). SR 4763, a potent channel opener, activates K ATP and a time-dependent current likely due to potassium accumulation. Journal of Membrane Biology, 142: 337-347. 19. Edwards G, Henshaw M, Miller M & Weston AH (1991). Comparison of the effects of several potassium-channel openers on rat bladder and rat portal vein in vitro. British Journal of Pharmacology, 12: 679-686. 2. Greenwood IA & Weston AH (1993). Effects of Rb on responses to potassium channel openers in rat isolated aorta. British Journal of Pharmacology, 19: 925-932. 21. Gonçalves de Mello R, Soares de Moura R & Damião R (1994). Actions of SR 4763 in human isolated detrusor. Canadian Journal of Physiology and Pharmacology, 72 (Suppl 1): P21-1.25 (Abstract).