Opposite effects of Bay k 8644 and nicardipine on the inhibitory effect of Ca2+ on rat myometrium.

Abstract:

:The effect of Ca2+ on the oxytocin-induced, sustained contraction of rat uterine muscle in Ca-free medium after prolonged incubation with 3 mM EGTA (Ca-free contraction) was investigated. A micromolar concentration of Ca2+ caused phasic contraction followed by relaxation while a submicromolar concentration caused relaxation only. Cumulative addition of Ca2+ (10(-8)-3 X 10(-6) M) caused dose-dependent relaxation (Ca reversal). This relaxation was inhibited by nicardipine and enhanced by Bay k 8644, and the effects of these two drugs were potentiated in 45.6 mM K+ medium. It is concluded that the inhibitory effect of Ca2+ on Ca-free contraction is caused by the influx of a minute amount of Ca2+. Thus, Ca2+ has dual actions in the cell: activation at concentrations higher than 10(-6) M, and inhibition alone at concentrations lower than 10(-7) M.

journal_name

Eur J Pharmacol

authors

Matsuo K,Uchida MK

doi

10.1016/0014-2999(87)90286-x

subject

Has Abstract

pub_date

1987-08-21 00:00:00

pages

295-301

issue

3

eissn

0014-2999

issn

1879-0712

pii

0014-2999(87)90286-X

journal_volume

140

pub_type

杂志文章
  • Antiulcer and gastric secretory activity of N-phthaloyl gamma-aminobutyric acid.

    abstract::N-Phthaloyl gamma-aminobutyric acid, a new gamma-aminobutyric acid derivative synthesized in this laboratory, has been found to possess anticonvulsant, antinociceptive and antistress activities. Effects of this derivative on gastric lesions induced by aspirin and ethanol were studied in rats. N-Phthaloyl gamma-aminobu...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(92)90298-i

    authors: Banerji S,Habibuddin M,Pal SP

    更新日期:1992-08-25 00:00:00

  • Neuroprotective effects of thymoquinone against transient forebrain ischemia in the rat hippocampus.

    abstract::Increasing evidence demonstrates that oxidative stress plays an important role in brain injury in experimental models of brain ischemia. Thymoquinone, the main constituents of the volatile oil from Negella sativa seeds, is reported to possess strong antioxidant properties. Hence, the present study was undertaken to ev...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2006.05.046

    authors: Al-Majed AA,Al-Omar FA,Nagi MN

    更新日期:2006-08-14 00:00:00

  • Pannexin-1 channels do not regulate α1-adrenoceptor-mediated vasoconstriction in resistance arteries.

    abstract::Recent reports have provided evidence for a new concept that in small resistance arteries α1D-adrenoceptor-mediated contraction is intimately linked to pannexin-1 (Px1) hemichannels that open to allow the release of ATP, from the smooth muscle effector cell, that acts back on P2Y purinoceptors to cause contraction. Th...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2015.01.024

    authors: Angus JA,Betrie AH,Wright CE

    更新日期:2015-03-05 00:00:00

  • Muscarinic receptor subtypes in the human colon: lack of evidence for atypical subtypes.

    abstract::Characteristics of muscarinic receptors were investigated in circular muscle from normal human colon. In saturation studies (n=18), binding of [3H]quinuclidinyl benzylate (QNB) was of high affinity (K(d) 87.3 pM) and capacity (B(max) 362+/-27 fmol/mg protein), with no differences between ascending and sigmoid colon. K...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2003.10.008

    authors: Mansfield KJ,Mitchelson FJ,Moore KH,Burcher E

    更新日期:2003-12-15 00:00:00

  • Cocaine N-demethylation and the metabolism-related hepatotoxicity can be prevented by cytochrome P450 3A inhibitors.

    abstract::Cocaine is eliminated and detoxified principally through the metabolism of nonspecific plasma and tissue esterases. Microsomal oxidative metabolism is of importance in cocaine N-demethylation, this being a principal pathway of cocaine bioactivation and hepatotoxicity. The contribution of different cytochrome P450 (CYP...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0926-6917(94)90078-7

    authors: Pellinen P,Honkakoski P,Stenbäck F,Niemitz M,Alhava E,Pelkonen O,Lang MA,Pasanen M

    更新日期:1994-01-03 00:00:00

  • Insulin-induced relaxation of rat mesenteric artery is mediated by Ca(2+)-activated K(+) channels.

    abstract::We tested the hypothesis that relaxation of the rat mesenteric artery in response to insulin is mediated by K(+) channels. Two concentrations of insulin (10 and 100 mU/ml) induced relaxation of the artery by 6+/-1%, 24+/-3% (mean+/-S.E.M.). Denudation of the endothelium or precontraction by KCl (30 mM), clotrimazole (...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(00)00892-x

    authors: Iida S,Taguchi H,Watanabe N,Kushiro T,Kanmatsuse K

    更新日期:2001-01-05 00:00:00

  • Pharmacological and pharmacokinetic study of olmesartan medoxomil in animal diabetic retinopathy models.

    abstract::A close relationship between the renin-angiotensin system and the pathophysiology of diabetic retinopathy has been suggested, several angiotensin II type 1 receptor (angiotensin AT1 receptor) antagonists being effective in animal models. Therefore, we examined the efficacy of an angiotensin AT1 receptor antagonist, ol...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2005.02.047

    authors: Nakamura H,Inoue T,Arakawa N,Shimizu Y,Yoshigae Y,Fujimori I,Shimakawa E,Toyoshi T,Yokoyama T

    更新日期:2005-04-11 00:00:00

  • Terfenadine induces thymocyte apoptosis via mitochondrial pathway.

    abstract::The treatment of rat thymocytes with 10 microM terfenadine resulted in a significant increase in DNA fragmentation. The DNA fragmentation induced by terfenadine was dependent on its concentration and incubation time. In terfenadine-treated cells, the translocation of phosphatidylserine from the inside of plasma membra...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2004.05.048

    authors: Enomoto R,Komai T,Yoshida Y,Sugahara C,Kawaguchi E,Okazaki K,Kinoshita H,Komatsu H,Konishi Y,Lee E

    更新日期:2004-08-02 00:00:00

  • Antitussive action of nociceptin in the cat.

    abstract::Experiments were conducted to determine the influence of the specific ORL1 receptor agonist, nociceptin, on the cough reflex in the cat. Cats were anesthetized and allowed to breathe spontaneously. Cough was elicited by mechanical stimulation of the intrathoracic airway. Intravenous administration of nociceptin (0.001...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(01)01244-4

    authors: Bolser DC,McLeod RL,Tulshian DB,Hey JA

    更新日期:2001-10-26 00:00:00

  • Epidermal growth factor-induced rapid relaxation of the isolated rabbit mesenteric artery.

    abstract::Epidermal growth factor (EGF) (10-100 ng ml-1) induced a rapidly developing relaxation of precontracted rabbit mesenteric artery rings within 30 min of exposure. Indomethacin or protein synthesis inhibitors prevented or acutely reversed the effect of EGF on the preparation and an erbstatin analogue significantly reduc...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(94)90164-3

    authors: Petitclerc E,Poubelle PE,Marceau F

    更新日期:1994-06-23 00:00:00

  • Antipyretic activity of cinnamyl derivatives and related compounds in influenza virus-infected mice.

    abstract::Kakkon-to is composed of seven medicinal herbs and exhibited novel antipyretic activity by suppressing interleukin-1alpha production responsive to interferon in a murine intranasal influenza virus infection model. Using this model, antipyretic compounds with such novel biological activities were characterized from the...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(98)00121-6

    authors: Kurokawa M,Kumeda CA,Yamamura J,Kamiyama T,Shiraki K

    更新日期:1998-05-01 00:00:00

  • Hydrogen peroxide and antioxidizing enzymes involved in modulation of transient facilitatory effects of nicotine on neurogenic contractile responses in rat gastric fundus.

    abstract::Nicotine acts as an agonist of nicotinic acetylcholine receptors. Nicotinic acetylcholine receptors play a role in the modulation of neurotransmitter release in both the central and the peripheral nervous system. Moderate reactive oxygen species levels modulate the regulation of physiological functions e.g. neurotrans...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2008.03.029

    authors: Ozger Ilhan S,Sarioglu Y,Vural IM,Dileköz E,Oztürk GS,Ercan ZS

    更新日期:2008-06-10 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

  • A novel purine analogue bearing nitrate ester prevents platelet activation by ROCK activity inhibition.

    abstract::Natural purines like ATP, ADP and adenosine have crucial roles in platelet physiology. This knowledge has been significant in drug development and today ADP receptor antagonists are widely used for prevention of thrombotic events following myocardial infarction and ischaemic stroke. Recent studies have shown that a pu...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2019.172428

    authors: Kardeby C,Paramel GV,Pournara D,Fotopoulou T,Sirsjö A,Koufaki M,Fransén K,Grenegård M

    更新日期:2019-08-15 00:00:00

  • Ligand affinities at recombinant N-methyl-D-aspartate receptors depend on subunit composition.

    abstract::The ligand preferences of recombinant NR1 homomeric and NR1-NR2 heteromeric NMDA receptors were examined by homogenate binding assay. The binding affinities for most ligands were similar to those reported for native NMDA receptors. The order of affinity for [3H]glutamate was NR1-NR2B > NR1-NR2A approximately NR1-NR2D ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0922-4106(94)90058-2

    authors: Laurie DJ,Seeburg PH

    更新日期:1994-08-16 00:00:00

  • Tempol, an antioxidant, restores endothelium-derived hyperpolarizing factor-mediated vasodilation during hypertension.

    abstract::Acetylcholine releases a non-prostanoid endothelium-derived hyperpolarizing factor (EDHF) and nitric oxide from physiological salt solution perfused rat mesenteric arteries. This study reports an impairment in EDHF-mediated vasodilation in deoxycorticosterone acetate (DOCA)-salt hypertensive versus control normotensiv...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2003.09.005

    authors: Adeagbo AS,Joshua IG,Falkner C,Matheson PJ

    更新日期:2003-11-14 00:00:00

  • Long-term benzodiazepine treatment reduces neuronal responsiveness to cholecystokinin: an electrophysiological study in the rat.

    abstract::Acute benzodiazepine administration has been reported to antagonize the effect of cholecystokinin both in the periphery and in the central nervous system. A two-week treatment with either diazepam (5 mg/kg per day) or flurazepam (15 mg/kg per day) markedly reduced the excitatory effect of microiontophoretically applie...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(88)90703-0

    authors: Bouthillier A,De Montigny C

    更新日期:1988-06-22 00:00:00

  • Effects of allicin on hyperhomocysteinemia-induced experimental vascular endothelial dysfunction.

    abstract::This study was designed to investigate the effect and mechanism of allicin on hyperhomocysteinemia-induced experimental vascular endothelial dysfunction in rats. Fifty male Wistar rats were randomly divided into five groups: the normal control rats (NC), the high-methionine-diet rats (Met), the high-methionine-diet ra...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2013.05.038

    authors: Liu DS,Gao W,Liang ES,Wang SL,Lin WW,Zhang WD,Jia Q,Guo RC,Zhang JD

    更新日期:2013-08-15 00:00:00

  • Pharmacokinetic-pharmacodynamic influence of N-palmitoylethanolamine, arachidonyl-2'-chloroethylamide and WIN 55,212-2 on the anticonvulsant activity of antiepileptic drugs against audiogenic seizures in DBA/2 mice.

    abstract::We evaluated the effects of ACEA (selective cannabinoid (CB)1 receptor agonist), WIN 55,212-2 mesylate (WIN; non-selective CB1 and CB2 receptor agonist) and N-palmitoylethanolamine (PEA; an endogenous fatty acid of ethanolamide) in DBA/2 mice, a genetic model of reflex audiogenic epilepsy. PEA, ACEA or WIN intraperito...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2016.09.029

    authors: Citraro R,Russo E,Leo A,Russo R,Avagliano C,Navarra M,Calignano A,De Sarro G

    更新日期:2016-11-15 00:00:00

  • CNS site of antiarrhythmic action of diphenylhydantoin (DPH) in the cat.

    abstract::Diphenylhydantoin (DPH) is known to be a potent anticonvulsant agent, useful in treating and preventing grand mal seizures. More recently, DPH was reported also to be a potent antiarrhythmic agent acting by means of a depressant action on the heart. The present experiments demonstrated that DPH has also a potent antia...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(75)90078-3

    authors: Lisander B,Jaju B,Wang SC

    更新日期:1975-03-01 00:00:00

  • The effect of intracisternally administered bombesin on cysteamine-induced duodenal ulcers in rats.

    abstract::Cysteamine (420 mg/kg s.c.) increased gastric acid secretion in rats 3-6 h post-injection; duodenal pH fell from 6.0 +/- 0.2 (S.E.M.) at 0 time to 2.2 +/- 0.3 at 12 h. A high (60-80%) incidence of duodenal ulcerations was observed 18 h after cysteamine injection. Intracisternal (i.c.) administration of bombesin (1 mic...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(82)90203-5

    authors: Hernandez DE,Adcock JW,Nemeroff CB,Prange AJ Jr

    更新日期:1982-10-22 00:00:00

  • In vivo and in vitro study of the influence of the anticholinesterase drug galantamine on motor and evacuative functions of rat gastrointestinal tract.

    abstract::Galantamine is efficacious for vascular dementia and Alzheimer's disease. Its application leads to some negative gastrointestinal side effects. The present study observes galantamine-induced influence on gastrointestinal motility of rats and its effects on isolated gastrointestinal smooth muscles. The gastrointestinal...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2004.07.054

    authors: Turiiski VI,Krustev AD,Sirakov VN,Getova DP

    更新日期:2004-09-13 00:00:00

  • Vincamine and vincanol are potent blockers of voltage-gated Na+ channels.

    abstract::The effects of three vinca derivatives on [3H]batrachotoxin binding in rat cortical synaptosomes, on the inhibition of whole-cell Na+ currents evoked in voltage-clamped cortical neurones of the rat, on the protection against veratridine-induced cell death in cortical cultures and on the maximal electroshock-induced se...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(96)00542-0

    authors: Erdo SA,Molnár P,Lakics V,Bence JZ,Tömösközi Z

    更新日期:1996-10-24 00:00:00

  • Interactions between gallamine and muscarinic receptors: allosterism and subpopulation specificity are separate phenomena.

    abstract::The quaternary antagonist gallamine discriminates subpopulations of muscarinic receptors in the forebrain and brainstem of the rat and also modulates the binding of other muscarinic ligands via an allosteric mechanism in both brain regions. The calcium channel antagonist verapamil exhibits a similar allosteric effect ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(87)90006-9

    authors: Ellis J,Seidenberg M

    更新日期:1987-11-24 00:00:00

  • Melanin potentiates gentamicin-induced inhibition of collagen biosynthesis in human skin fibroblasts.

    abstract::One of the recognized side effects of gentamicin is ototoxicity. The mechanism underlying the organ specificity of this side effect of gentamicin has not been fully established. In view of the fact that a number of pharmacologic agents are known to form complexes with melanin and melanin is an abundant constituent of ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(02)01793-4

    authors: Wrześniok D,Buszman E,Karna E,Nawrat P,Palka J

    更新日期:2002-06-20 00:00:00

  • Small interfering RNA-mediated knockdown of NF-κBp65 attenuates neuropathic pain following peripheral nerve injury in rats.

    abstract::Recent reports show that the nuclear factor-κB (NF-κB) can control numerous genes encoding inflammatory and nociceptive mediators and play an important role in the development of central pain sensitization. The aim of the present study is to assess the role of NF-κB signal pathway and its downstream pro-inflammatory c...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2012.02.017

    authors: Sun T,Luo J,Jia M,Li H,Li K,Fu Z

    更新日期:2012-05-05 00:00:00

  • Sphingosine-1-phosphate induced contraction of bladder smooth muscle.

    abstract::Sphingosine-1-phosphate (S1P) is a bioactive sphingolipid that contracts most smooth muscles. Although S1P has been shown to contract bladder smooth muscle, the mechanism(s) by which S1P initiates contraction has not been extensively investigated. The goal of this study was to determine if S1P-induced force generation...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2013.10.004

    authors: Kendig DM,Matsumoto AK,Moreland RS

    更新日期:2013-11-15 00:00:00

  • Effects of lithium ex vivo on the GTP-mediated inhibition of calcium-stimulated adenylate cyclase activity in rat brain.

    abstract::The aim of this study was to investigate the effects of chronic lithium treatment on calcium (Ca2+)-stimulated adenylate cyclase activity in rat striatum and hippocampus, and to elucidate the effect of lithium treatment on the neurotransmitter/GTP-mediated inhibition of Ca2+-stimulated enzyme activity in the two brain...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(89)90796-6

    authors: Mørk A,Geisler A

    更新日期:1989-09-22 00:00:00

  • Anti-tumor necrosis factor agent PEG-sTNFRI improves the growth hormone/insulin-like growth factor-I system in adjuvant-induced arthritic rats.

    abstract::Adjuvant-induced arthritis is associated with body weight loss and decreased pituitary growth hormone (GH) and hepatic insulin-like growth factor-I (IGF-I) synthesis. Cytokines as tumor necrosis factor (TNF) mediate wasting associated with chronic inflammation. The aim of this study was to analyse whether the inhibiti...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2006.02.035

    authors: Granado M,Priego T,Martín AI,Vara E,López-Calderón A,Angeles Villanúa M

    更新日期:2006-04-24 00:00:00

  • Regional in vivo binding of the substituted benzamide [3H]eticlopride in the rat brain: evidence for selective labelling of dopamine receptors.

    abstract::The novel substituted benzamide eticlopride, (S)-(-)-5-chloro-3-ethyl-N-[(1-ethyl-2-pyrrolidinyl)methyl]-6-methoxy salicylamide hydrochloride (A38503; FLB 131), was radiolabelled to high specific activity and used for in vivo receptor binding studies in the rat brain. Intravenous injections of [3H]eticlopride resulted...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(86)90543-1

    authors: Köhler C,Hall H,Gawell L

    更新日期:1986-01-21 00:00:00