Effects of the calmodulin inhibitor, trifluoperazine, on membrane potentials and slow action potentials of cultured heart cells.

Abstract:

:The effects of an inhibitor of calmodulin, trifluoperazine (TFP), were determined on the electrical activity of cultured cell reaggregates derived from chick embryonic hearts (15-day-old). The cells exhibited naturally occurring slowly rising action potentials (APs) having a maximum rate of rise (+Vmax) of less than 35 V/s. After superfusion with 100 microM TFP, the maximal diastolic potential (MDP) decreased, within 30 min, from -66.0 to -55.5 mV. The frequency of discharge decreased, and there was also a decrease in AP amplitude and in +Vmax (from 10.0 to 4.9 V/s). By 90 min, all spontaneous activity had stopped, and the resting potential was about -10 mV. Input resistance increased, consistent with a decrease in K+ conductance. Hyperpolarization by current pulses did not allow the production of APs upon electrical stimulation, suggesting that the TFP blocks slow inward current (Isi). No recovery occurred upon washout (up to 48 h). Higher concentrations of TFP (200-500 microM), or injection of the inhibitor intracellularly be means of phosphatidylcholine liposomes, accelerated the time course of the blockade (e.g. within 15 min). In fresh (non-cultured) chick ventricle with fast-rising APs, TFP (400 microM) caused excitation-contraction uncoupling within 10 min, presumably by blocking the slow Ca2+ channels; the the fast APs were depressed (+Vmax) within 45 min, before any depolarization occurred. The cells became completely depolarized (Em congruent to -4 mV) by 195 min; hyperpolarization by current pulses did not allow the production of APs, suggesting that the fast Na+ channels were blocked.(ABSTRACT TRUNCATED AT 250 WORDS)

journal_name

Eur J Pharmacol

authors

Bkaily G,Sperelakis N,Eldefrawi M

doi

10.1016/0014-2999(84)90645-9

subject

Has Abstract

pub_date

1984-10-01 00:00:00

pages

23-31

issue

1-2

eissn

0014-2999

issn

1879-0712

pii

0014-2999(84)90645-9

journal_volume

105

pub_type

杂志文章
  • Dopamine-induced homologous and heterologous desensitizations of adenylate cyclase-coupled receptors on striatal neurons.

    abstract::Striatal neurons in primary culture express a wide variety of adenylate cyclase-coupled receptors, and particularly dopamine (DA) D1 receptors, which are known to induce an increase in cyclic AMP production. To study desensitization of those receptor-mediated responses, neurons were incubated in the presence of satura...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0922-4106(90)90121-d

    authors: Chneiweiss H,Glowinski J,Premont J

    更新日期:1990-10-30 00:00:00

  • Ginsenoside Rg(3) decelerates hERG K(+) channel deactivation through Ser631 residue interaction.

    abstract::The human ether-a-go-go-related gene (hERG) cardiac K(+) channels are one of the representative pharmacological targets for development of drugs against cardiovascular diseases such as arrhythmia. Panax ginseng has been known to have cardio-protective effects. However, little is known about the molecular mechanisms of...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2011.05.006

    authors: Choi SH,Shin TJ,Hwang SH,Lee BH,Kang J,Kim HJ,Jo SH,Choe H,Nah SY

    更新日期:2011-08-01 00:00:00

  • Oxymatrine attenuates hepatic steatosis in non-alcoholic fatty liver disease rats fed with high fructose diet through inhibition of sterol regulatory element binding transcription factor 1 (Srebf1) and activation of peroxisome proliferator activated recep

    abstract::The aim of this study was to examine the therapeutic effect of oxymatrine, a monomer isolated from the medicinal plant Sophora flavescens Ait, on the hepatic lipid metabolism in non-alcoholic fatty liver (NAFLD) rats and to explore the potential mechanism. Rats were fed with high fructose diet for 8 weeks to establish...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2013.06.013

    authors: Shi LJ,Shi L,Song GY,Zhang HF,Hu ZJ,Wang C,Zhang DH

    更新日期:2013-08-15 00:00:00

  • Des-aspartate-angiotensin I causes specific release of PGE2 and PGI2 in HUVEC via the angiotensin AT1 receptor and biased agonism.

    abstract::DAA-I (des-aspartate-angiotensin I), an endogenous angiotensin, had been shown earlier to ameliorate animal models of cardiovascular diseases via the angiotensin AT1 receptor and prostaglandins. The present study investigated further the action of DAA-I on the release of PGE2, PGI2, PGF2α and TXA2 in HUVEC. 10(-11)-10...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2015.10.051

    authors: Wen Q,Lee KO,Sim SZ,Xu XG,Sim MK

    更新日期:2015-12-05 00:00:00

  • Factors contributing to differences in the regulation of cGMP in isolated porcine pulmonary vessels.

    abstract::Guanosine 3',5'-cyclic monophosphate (cGMP) is an important second messenger in many biological systems including vascular smooth muscle where it mediates relaxation. Cellular levels of cGMP are regulated primarily by three enzymes; nitric oxide (NO) synthase, soluble guanylate cyclase, and cGMP-phosphodiesterase. Bas...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(98)00307-0

    authors: Bina S,Hart JL,Sei Y,Muldoon SM

    更新日期:1998-06-19 00:00:00

  • New hyperprolactinemia and anovulation model in common marmoset (Callithrix jacchus) and effect of cabergoline.

    abstract::We aimed to develop an anovulation model, using sulpiride-induced hyperprolactinemia in common marmosets. The serum prolactin level gradually increased during the twice-daily administration of sulpiride and reached a plateau after 4 days. Sulpiride produced as big a response at 10 mg kg(-1) as at 50 mg kg(-1). In this...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(98)00940-6

    authors: Moro M,Inada Y,Kojima M,Miyata H,Komatsu H,Torii R

    更新日期:1999-02-26 00:00:00

  • Antagonism of beta-adrenoceptor-mediated relaxations of human bronchial smooth muscle by carbachol.

    abstract::Activation of muscarinic M2 receptors has been suggested to account, in part, for the reduced relaxant potency of beta-adrenoceptor agonists in canine and guinea-pig tracheal smooth muscle pre-contracted with muscarinic agonists as compared to histamine. The aim of the present study was to determine whether the potenc...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(95)00048-p

    authors: Watson N,Magnussen H,Rabe KF

    更新日期:1995-03-14 00:00:00

  • Individual differences in the sensitivity of cold allodynia to phentolamine in neuropathic rats.

    abstract::In neuropathic rats sensitive to phentolamine (alpha-adrenoreceptor antagonist, 2 mg/kg, i.p.), prazosin (alpha1-adrenoreceptor antagonist, 0.5 mg/kg, i.p.) significantly attenuated cold allodynia whereas yohimbine (alpha2-adrenoreceptor antagonist, 0.5 mg/kg, i.p.) had no significant effect. In neuropathic rats insen...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2005.08.030

    authors: Kim SK,Min BI,Kim JH,Hwang BG,Yoo GY,Park DS,Na HS

    更新日期:2005-10-31 00:00:00

  • Brain phospholipase C, diacylglycerol lipase and monoacylglycerol lipase are involved in (±)-epibatidine-induced activation of central adrenomedullary outflow in rats.

    abstract::We previously reported that intracerebroventricularly (i.c.v.) administered (±)-epibatidine (a potent agonist of nicotinic acetylcholine receptors) (1, 5 and 10 nmol/animal) dose-dependently elevated plasma levels of noradrenaline and adrenaline and that this response was reduced by i.c.v. administered indomethacin (c...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2012.07.017

    authors: Shimizu T,Tanaka K,Nakamura K,Taniuchi K,Yokotani K

    更新日期:2012-09-15 00:00:00

  • Efficacy of testosterone combined with a PDE5 inhibitor and testosterone combined with a serotonin (1A) receptor agonist in women with SSRI-induced sexual dysfunction. A preliminary study.

    abstract::Selective serotonin reuptake inhibitors (SSRIs) are known to cause sexual dysfunction, such as decreased sexual motivation, desire, arousal, and orgasm difficulties. These SSRI-induced sexual complaints have a high prevalence rate, while there is no approved pharmacological treatment for SSRI-induced sexual dysfunctio...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章,随机对照试验

    doi:10.1016/j.ejphar.2014.10.061

    authors: van Rooij K,Poels S,Worst P,Bloemers J,Koppeschaar H,Goldstein A,Olivier B,Tuiten A

    更新日期:2015-04-15 00:00:00

  • The bradykinin B2 receptor antagonist Icatibant (HOE 140) corrects avid Na+ retention in rats with CCl4-induced liver cirrhosis: possible role of enhanced microvascular leakage.

    abstract::Avid Na+ retention is a hallmark of liver cirrhosis. The aim of this study was to investigate whether and how bradykinin is involved in Na+ retention in rats with CCl4-induced liver cirrhosis. To this end the bradykinin B2 receptor antagonist Icatibant (HOE 140) was used. On one hand, bradykinin has a renal natriureti...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(97)01281-8

    authors: Wirth KJ,Bickel M,Hropot M,Günzler V,Heitsch H,Ruppert D,Schölkens BA

    更新日期:1997-10-15 00:00:00

  • Compound action potential inhibition produced by various antidepressants in the frog sciatic nerve.

    abstract::Although an inhibition of action potential conduction in nerve fibers possibly contributes to at least a part of antinociception produced by analgesics and the adjuvants, it has not been fully examined yet how the conduction inhibition differs in extent among their drugs. We investigated the effects of various antidep...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2017.11.047

    authors: Hirao R,Fujita T,Sakai A,Kumamoto E

    更新日期:2018-01-15 00:00:00

  • Coptisine ameliorates DSS-induced ulcerative colitis via improving intestinal barrier dysfunction and suppressing inflammatory response.

    abstract::Ulcerative colitis (UC), as an autoimmune disease, has been troubling human health for many years. Up to now, the available treatments remain unsatisfactory. Rhizoma Coptidis has been widely applied to treat gastrointestinal diseases in China for a long time, and coptisine (COP) is identified as one of its major activ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2021.173912

    authors: Wang Y,Liu J,Huang Z,Li Y,Liang Y,Luo C,Ni C,Xie J,Su Z,Chen J,Li C

    更新日期:2021-01-25 00:00:00

  • Pharmacological nature of nicotine-induced contraction in the rat basilar artery: involvement of arachidonic acid metabolites.

    abstract::The pharmacological nature of nicotine-induced contraction in the rat basilar artery is poorly understood. The purpose of this study was to investigate the endothelium dependency and involvement of arachidonic acid metabolites in nicotine-induced contraction in the rat basilar artery. The rat basilar artery was remove...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2007.08.011

    authors: Ji X,Nishihashi T,Trandafir CC,Wang A,Shimizu Y,Kurahashi K

    更新日期:2007-12-22 00:00:00

  • Differentiation of group 2 and group 3 metabotropic glutamate receptor cAMP responses in the rat hippocampus.

    abstract::The effects of group 2- versus group 3-selective metabotropic glutamate (mGlu) receptor agonists were examined against forskolin (10 microM)-, vasoactive intestinal peptide (VIP; 1 microM)- and 5'-N-ethylcarboxamidoadenosine (NECA; 10 microM)-stimulated cAMP accumulations in adult rat hippocampal slices (in the presen...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(95)00747-4

    authors: Wright RA,Schoepp DD

    更新日期:1996-02-22 00:00:00

  • Effects of central administration of tachykinin receptor agonists and antagonists on plus-maze behavior in mice.

    abstract::This study assessed the effects of intracerebroventricular administration of selective agonists and antagonists for tachykinin NK1 and NK2 receptors on performance of mice in the elevated plus-maze, an ethological model of anxiety. Mice were treated with either vehicle (5 microliters) or 1, 10, 100 or 500 pmol of subs...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(96)00390-1

    authors: Teixeira RM,Santos AR,Ribeiro SJ,Calixto JB,Rae GA,De Lima TC

    更新日期:1996-09-05 00:00:00

  • Triphasic vascular responses to bradykinin in the mesenteric resistance artery of the rat.

    abstract::The vascular effects of bradykinin were studied in rat perfused mesenteric vascular beds with active tone. Bolus injections of bradykinin (1-1000 pmol) but not des-Arg(9)-bradykinin (bradykinin B(1) receptor agonist) induced triphasic vascular responses: the initial sharp vasodilation followed by transient vasoconstri...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(01)01513-8

    authors: Nawa H,Kawasaki H,Nakatsuma A,Isobe S,Kurosaki Y

    更新日期:2001-12-14 00:00:00

  • Comparative effects of high and low-dose simvastatin on prostate epithelial cells: the role of LDL.

    abstract::Epidemiological studies have linked statin use with a decreased risk of advanced prostate cancer and an improved recurrence-free survival after radical therapy. It is unclear, however, whether statins could have direct effects against prostate cancer in a clinical setting, as their growth-inhibiting effects on prostat...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2011.10.022

    authors: Murtola TJ,Syvälä H,Pennanen P,Bläuer M,Solakivi T,Ylikomi T,Tammela TL

    更新日期:2011-12-30 00:00:00

  • Identification of a domain affecting agonist potency of meta-chlorophenylbiguanide in 5-HT3 receptors.

    abstract::The pharmacological properties of rat and human 5-HT3 receptors expressed in Xenopus oocytes were assessed using a two-electrode voltage clamp technique. Meta-chlorophenylbiguanide (mCPBG), a 5-HT3 receptor-selective agonist, elicited typical current responses in both rat and human 5-HT3 receptor-expressing oocytes. H...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(99)00058-8

    authors: Mochizuki S,Miyake A,Furuichi K

    更新日期:1999-03-12 00:00:00

  • Heterologous desensitization and reduced G protein ADP-ribosylation following exposure to alpha 2-adrenoceptor and muscarinic receptor agonists.

    abstract::We investigated the acute and chronic effects of alpha 2-adrenoceptor and muscarinic receptor agonists on dihydropyridine-sensitive voltage-dependent Ca2+ channels in spinal cord-dorsal root ganglion cocultures. Clonidine and oxotremorine inhibited the voltage-dependent Ca2+ influx (42 +/- 2% and 35 +/- 6% with 100 mi...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0922-4106(93)90060-m

    authors: Nah SY,Attali B,Vogel Z

    更新日期:1993-01-04 00:00:00

  • Vasorelaxant effects of benzodiazepines, non-benzodiazepine sedative-hypnotics, and tandospirone on isolated rat arteries.

    abstract::Benzodiazepines (BDZs) and non-BDZ sedative-hypnotics are effective for the management of chronic insomnia; however, they are associated with adverse effects such as headache, dizziness, and palpitations. Furthermore, long-term use of these medications is associated with decreased blood pressure (BP) or depressed baro...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2020.173744

    authors: Kagota S,Morikawa K,Ishida H,Chimoto J,Maruyama-Fumoto K,Yamada S,Shinozuka K

    更新日期:2021-02-05 00:00:00

  • Reduced contractile function after balloon denudation of rat carotid arteries.

    abstract::In rat carotid arteries isolated 2 weeks after balloon denudation, a significant neointima developed with little change in medial size. Associated with this neointimal hyperplasia was a marked decrease in contraction to various agents including angiotensins I and II, big endothelin-1, endothelin-1, norepinephrine, phe...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(94)90610-6

    authors: Antonaccio MJ,Normandin D,Ferrer P

    更新日期:1994-04-11 00:00:00

  • Conditioned taste aversion: modulation by 5-HT receptor activity and corticosterone.

    abstract::Two experiments were designed to elucidate the involvement of the hypothalamic-pituitary-adrenal axis and the 5-hydroxytryptamine (5-HT) system in the acquisition of lithium chloride-conditioned taste aversion. In Experiment 1, rats were administered either vehicle or 50 mg/kg nefazodone daily for 4 weeks. Rats were t...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(03)01790-4

    authors: Gorzalka B,Hanson L,Harrington J,Killam S,Campbell-Meiklejohn D

    更新日期:2003-06-20 00:00:00

  • Resveratrol modifies risk factors for coronary artery disease in swine with metabolic syndrome and myocardial ischemia.

    abstract::Resveratrol has been purported to modify risk factors for obesity and cardiovascular disease. We sought to examine the effects of resveratrol in a porcine model of metabolic syndrome and chronic myocardial ischemia. Yorkshire swine were fed either a normal diet (control), a high cholesterol diet (HCD), or a high chole...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2011.04.059

    authors: Robich MP,Osipov RM,Chu LM,Han Y,Feng J,Nezafat R,Clements RT,Manning WJ,Sellke FW

    更新日期:2011-08-16 00:00:00

  • Partial agonist activity of celiprolol, a cardioselective beta-antagonist.

    abstract::The beta-antagonistic effects of celiprolol were assessed in isolated guinea-pig preparations. The pA2 values obtained were 7.84 +/- 0.07, 7.79 +/- 0.06 and 6.45 +/- 0.11 against the positive chronotropic and inotropic effects in the atria and relaxant effects in the trachea induced by isoproterenol, respectively, ind...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(91)90115-7

    authors: Ochi S,Nakazawa M,Kimura T,Nakagawa Y,Imai S

    更新日期:1991-02-26 00:00:00

  • Effects of nicotine on K+ channel currents in vascular smooth muscle cells from rat tail arteries.

    abstract::Intake of nicotine has been related in many cases to acute or chronic hypertension. Using the patch-clamp technique the effect of nicotine on voltage-dependent K+ channel currents in rat tail artery smooth muscle cells was studied. Nicotine at concentrations of 1-100 microM or 0.3-3 mM increased or decreased, respecti...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(98)00833-4

    authors: Tang G,Hanna ST,Wang R

    更新日期:1999-01-08 00:00:00

  • Inhibition of enkephalin metabolism by, and antinociceptive activity of, bestatin, an aminopeptidase inhibitor.

    abstract::In the presence of thiorphan an 'enkephalinase' inhibitor, bestatin an aminopeptidase inhibitor of bacterial origin potently inhibited the hydrolysis of [3H][Leu5]enkephalin by slices from rat striatum with an IC50 value of about 0.2 microM whereas puromycin was approximately 1000 times less potent on this preparation...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(83)90181-4

    authors: Chaillet P,Marçais-Collado H,Costentin J,Yi CC,De La Baume S,Schwartz JC

    更新日期:1983-01-21 00:00:00

  • Effects of carbamazepine and valproic acid on brain immunoreactive somatostatin and gamma-aminobutyric acid in amygdaloid-kindled rats.

    abstract::Somatostatin and gamma-aminobutyric acid (GABA) concentrations were evaluated in the brain of kindled rats treated chronically with carbamazepine and valproic acid. Kindled seizures were almost completely blocked by treatment with carbamazepine, whereas the effect of valproic acid was partial, suppressing only general...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(86)90024-5

    authors: Higuchi T,Yamazaki O,Takazawa A,Kato N,Watanabe N,Minatogawa Y,Yamazaki J,Ohshima H,Nagaki S,Igarashi Y

    更新日期:1986-06-17 00:00:00

  • Inhibitory effect of sevoflurane on nitric oxide release from cultured endothelial cells.

    abstract::We investigated the effect of sevoflurane (fluoromethyl-2,2,2-trifluoro-1-(trifluoromethyl) ethylether) on intracellular calcium concentration ([Ca2+]i) and nitric oxide (NO) release from cultured porcine aortic endothelial cells using fura-2 fluorometry, and direct (ESR spectrometry with NO-trapping by 2-(4-carboxyph...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0922-4106(95)90165-5

    authors: Az-ma T,Fujii K,Yuge O

    更新日期:1995-03-15 00:00:00

  • Serotonin-stimulated increase in cytosolic Ca(2+) in cultured rat heart endothelial cells.

    abstract::This study was designed to investigate the effects of serotonin on changes in intracellular Ca(2+) concentration ([Ca(2+)](i)) in cultured rat heart endothelial cells. Serotonin stimulated a biphasic change in cytosolic Ca(2+) of rat heart endothelial cells: an initial transient increase, which primarily reflects the ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(99)00672-x

    authors: Lee HZ,Wu CH

    更新日期:1999-11-12 00:00:00