Block of rat brain recombinant SK channels by tricyclic antidepressants and related compounds.

Abstract:

:SK channels are small conductance, Ca(2+)-activated K(+) channels that underlie neuronal slow afterhyperpolarization and mediate spike frequency adaptation. Using the patch clamp technique, we tested the effects of eight clinically relevant psychoactive compounds structurally related to the tricyclic antidepressants, on SK2 subtype channels cloned from rat brain and functionally expressed in the human embryonic kidney cell line, HEK293. Amitriptyline, carbamazepine, chlorpromazine, cyproheptadine, imipramine, tacrine and trifluperazine blocked SK2 channel currents with micromolar affinity. The block was reversible and concentration-dependent. The potency differed according to chemical structure. In contrast, the cognitive enhancer linopirdine was ineffective at blocking these channels. Our results point to a distinct pharmacological profile for SK channels.

journal_name

Eur J Pharmacol

authors

Dreixler JC,Bian J,Cao Y,Roberts MT,Roizen JD,Houamed KM

doi

10.1016/s0014-2999(00)00401-5

keywords:

subject

Has Abstract

pub_date

2000-07-28 00:00:00

pages

1-7

issue

1

eissn

0014-2999

issn

1879-0712

pii

S0014299900004015

journal_volume

401

pub_type

杂志文章
  • Personality and polymorphisms of genes involved in aminergic neurotransmission.

    abstract::Genetic factors significantly contribute to the determination of human personality traits assessed by self-report questionnaires. However, only in the past few years have common genetic polymorphisms especially the dopamine D4 receptor and the serotonin transporter promoter region been associated with specific persona...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章,评审

    doi:10.1016/s0014-2999(00)00852-9

    authors: Ebstein RP,Benjamin J,Belmaker RH

    更新日期:2000-12-27 00:00:00

  • Endogenous nitric oxide counteracts antigen-induced bronchoconstriction.

    abstract::In anesthetized, artificially ventilated guinea pigs immunized against ovalbumin, challenge with aerosolized ovalbumin (0.1 mg) elicited a substantial and sustained increase of insufflation pressure. The inhibitor of endogenous nitric oxide (NO) synthesis, L-NAME (N omega-nitro-L-arginine methylester, 30 mg kg-1 i.v.)...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(93)90532-m

    authors: Persson MG,Friberg SG,Hedqvist P,Gustafsson LE

    更新日期:1993-11-16 00:00:00

  • pH dependency of the binding of [3H]BAY U 3405 and various non-labelled ligands to the thromboxane A2/prostaglandin H2 receptor of human platelet membranes.

    abstract::[3H]BAY U 3405 was used to characterize the effect of acidic and alkaline pH values on the binding of the thromboxane A2/prostaglandin H2 (TXA2/PGH2) receptor of human platelet membranes. The specific binding of [3H]BAY U 3405 largely increased upon acidification up to pH 5.8. Saturation binding studies revealed an in...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0922-4106(92)90176-v

    authors: Theis JG,Dellweg H,Perzborn E,Gross R

    更新日期:1992-06-05 00:00:00

  • In vitro inhibition of allergic histamine release by calcium antagonists.

    abstract::The ability of calcium entry blockers to inhibit allergic histamine release from rabbit leukocytes was studied. Bepridil, verapamil, nifedipine, diltiazem and TMB-8 produced concentration-dependent inhibition of allergic histamine release from rabbit leukocytes. The calculated IC50s (microM) were as follows: verapamil...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(85)90261-4

    authors: Chand N,Pillar J,Diamantis W,Sofia RD

    更新日期:1985-01-08 00:00:00

  • SCH-23390 antagonism of a D-2 dopamine agonist depends upon catecholaminergic neurons.

    abstract::SCH-23390, a selective D-1 dopamine antagonist, was found to antagonize the locomotor stimulation induced by LY-171555, an action similar to that for haloperidol in control animals. However, this action of SCH-23390 was prevented in rats treated with 6-hydroxydopamine (6-OHDA) or with reserpine plus alpha-methyl-tyros...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(85)90349-8

    authors: Breese GR,Mueller RA

    更新日期:1985-07-11 00:00:00

  • Clozapine-induced Fos-protein expression in rat forebrain regions: differential effects of adrenalectomy and corticosterone supplement.

    abstract::Unlike classical antipsychotic drugs, clozapine activates the hypothalamo-pituitary-adrenal axis and induces a specific regional pattern of Fos-protein expression in the rat forebrain. Whether corticosterone plays a role in the clozapine-induced Fos response is the subject of this study. Some rats were adrenalectomize...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(01)00870-6

    authors: Sebens JB,Middelveld RJ,Koch T,Ter Horst GJ,Korf J

    更新日期:2001-04-06 00:00:00

  • Contraction velocity analysis of norepinephrine and angiotensin-II activation of vascular smooth muscle.

    abstract::The contractile response of vascular smooth muscle is known to consist of fast and slow components of contraction. We investigated the effect of norepinephrine and angiotensin-II on these functional properties of vascular smooth muscle in a quantitative fashion by analyzing the velocity of isometric tension developmen...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(80)90274-5

    authors: Watkins RW,Davidson IW

    更新日期:1980-03-21 00:00:00

  • Lipopolysaccharide-induced inhibition of gastric acid and pepsin secretion in rats.

    abstract::We used male Wistar rats to determine the effects of lipopolysaccharide (LPS) on gastric secretion. After pylorus ligation, 24-h fasted rats received i.p. injections of different doses of LPS dissolved in sterile saline. The amounts of gastric acid and pepsin secreted were determined 2, 4 or 8 h after injection. Small...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(90)90256-6

    authors: Uehara A,Okumura T,Okamura K,Takasugi Y,Namiki M

    更新日期:1990-05-31 00:00:00

  • Deltorphin II enhances extracellular levels of dopamine in the nucleus accumbens via opioid receptor-independent mechanisms.

    abstract::The effects of the delta2-opioid receptor agonist, deltorphin II, on extracellular levels of dopamine in the rat nucleus accumbens were investigated in awake animals by in vivo brain microdialysis. In agreement with previous studies, perfusion of deltorphin II (50.0 nmol) into the nucleus accumbens significantly incre...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2004.03.028

    authors: Murakawa K,Hirose N,Takada K,Suzuki T,Nagase H,Cools AR,Koshikawa N

    更新日期:2004-04-26 00:00:00

  • The effect of an iron (III) chelator, silybin, on the proliferation and cell cycle of Jurkat cells: a comparison with desferrioxamine.

    abstract::Silybin is a flavonoid with antioxidant and free radical scavenging abilities. Silybin also acts as an iron chelator by binding Fe (III). The present study was undertaken to assess the biological effects of silybin on T leukemia cells in the presence or absence of iron and compare its effects with a well-known iron ch...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2008.03.059

    authors: Gharagozloo M,Khoshdel Z,Amirghofran Z

    更新日期:2008-07-28 00:00:00

  • Long-term blockade of the expression of cocaine sensitization by ondansetron, a 5-HT(3) receptor antagonist.

    abstract::Intermittent cocaine administration induces sensitization (reverse tolerance) to its behavioral effects. The mechanism(s) mediating sensitization is not clear, however, previous research has implicated 5-HT(3) receptors in the expression of sensitization. The present experiment evaluated the ability of the 5-HT(3) rec...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(99)00926-7

    authors: King GR,Xiong Z,Douglass S,Ellinwood EH

    更新日期:2000-04-07 00:00:00

  • Coagulation factor Xa induces an inflammatory signalling by activation of protease-activated receptors in human atrial tissue.

    abstract::Activated factor X (FXa) is an important player in the coagulation cascade responsible for thrombin generation, which is activated during atrial fibrillation. Increasing evidence suggests that FXa influences cell signalling in various cell types by activating protease-activated receptors (PARs). It is so far not known...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2013.09.006

    authors: Bukowska A,Zacharias I,Weinert S,Skopp K,Hartmann C,Huth C,Goette A

    更新日期:2013-10-15 00:00:00

  • Pilocarpine vs. lithium-pilocarpine for induction of status epilepticus in mice: development of spontaneous seizures, behavioral alterations and neuronal damage.

    abstract::In recent years, the pilocarpine model of temporal lobe epilepsy has become the most popular and widely used rodent model of this common and difficult-to-treat type of epilepsy. In this model, the cholinomimetic convulsant pilocarpine is used to induce a status epilepticus, which is followed by hippocampal damage and ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2009.07.020

    authors: Müller CJ,Bankstahl M,Gröticke I,Löscher W

    更新日期:2009-10-01 00:00:00

  • Identification of [3H]P1075 binding sites and P1075-activated K+ currents in ovine choroid plexus cells.

    abstract::This study examined the pharmacological characteristics of binding sites for the potent K+ channel opener [3H]P1075, as well as the functional effects of P1075 on ionic currents and membrane potential, in ovine choroid plexus (OCP) cells. [3H]P1075 bound to OCP cells with a Kd of 26 +/- 4 nM and a Bmax of 10400 +/- 48...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(97)01617-8

    authors: Dickinson KE,Baska RA,Cohen RB,Bryson CC,Smith MA,Schroeder K,Lodge NJ

    更新日期:1998-03-12 00:00:00

  • Interaction of topiramate with conventional antiepileptic drugs in mice.

    abstract::Topiramate [2,3:4, 5-bis-O-(1-methyl-ethylidene-)-beta-D-fructopyranose sulfamate], administered intraperitoneally (i.p.) up to 5 mg/kg, did not influence the threshold for electroconvulsions. In doses of 10-30 mg/kg, topiramate significantly raised the threshold. This novel antiepileptic drug, in subprotective doses,...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(00)00365-4

    authors: Swiader M,Kotowski J,Gasior M,Kleinrok Z,Czuczwar SJ

    更新日期:2000-06-30 00:00:00

  • Central inhibitory effects on feeding induced by the adipo-myokine irisin.

    abstract::Irisin, the soluble secreted form of fibronectin type III domain containing 5 (FNDC5)-cleaved product, is a recently identified adipo-myokine that has been indicated as a possible link between physical exercise and energetic homeostasis. The co-localization of irisin with neuropeptide Y in hypothalamic sections of par...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2016.09.011

    authors: Ferrante C,Orlando G,Recinella L,Leone S,Chiavaroli A,Di Nisio C,Shohreh R,Manippa F,Ricciuti A,Vacca M,Brunetti L

    更新日期:2016-11-15 00:00:00

  • Effects of SQ 27,427, a thromboxane A2 receptor antagonist, in the human platelet and isolated smooth muscle.

    abstract::The TxA2 receptor antagonist properties of SQ 27,427 [a cyclohexylcarbinol-7-oxabicyclo(2.2.1)heptenoic acid analog] were studied in vitro both in the human platelet and various isolated smooth muscle preparations. SQ 27,427 was found to be a potent inhibitor of human platelet aggregation induced by arachidonic acid, ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(84)90183-3

    authors: Harris DN,Greenberg R,Phillips MB,Michel IM,Goldenberg HJ,Haslanger MF,Steinbacher TE

    更新日期:1984-08-03 00:00:00

  • The glucagon-like peptide 1 receptor agonist exendin-4 improves reference memory performance and decreases immobility in the forced swim test.

    abstract::We have earlier shown that the glucagon-like peptide 1 receptor agonist exendin-4 stimulates neurogenesis in the subventricular zone and excerts anti-parkinsonian behavior. The aim of this study was to assess the effects of exendin-4 treatment on hippocampus-associated cognitive and mood-related behavior in adult rode...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2010.10.008

    authors: Isacson R,Nielsen E,Dannaeus K,Bertilsson G,Patrone C,Zachrisson O,Wikström L

    更新日期:2011-01-10 00:00:00

  • Trichloroethanol inhibits ATP-induced membrane currents in cultured HEK 293-hP2X3 cells.

    abstract::Membrane currents in response to the application of alpha, beta-methylene ATP (alpha,beta-meATP) were recorded by the whole-cell patch-clamp technique in human embryonic kidney 293 cells transfected with the human P2X3 receptor (HEK 293-hP2X3 cells). Trichloroethanol, the biologically active metabolite of chloral hydr...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(00)00833-5

    authors: Köles L,Wirkner K,Fürst S,Wnendt S,Illes P

    更新日期:2000-12-15 00:00:00

  • Allosteric modulation of nicotinic acetylcholine receptors as a treatment strategy for Alzheimer's disease.

    abstract::The basic symptoms of Alzheimer's dementia, i.e., a loss in cognitive function, are due to impaired nicotinic cholinergic neurotransmission. To compensate for this impairment by drug treatment, blockers of the acetylcholine-degrading enzyme acetylcholinesterase are applied, even though this approach obviously is prone...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(00)00093-5

    authors: Maelicke A,Albuquerque EX

    更新日期:2000-03-30 00:00:00

  • Goniothalamin induces cell cycle-specific apoptosis by modulating the redox status in MDA-MB-231 cells.

    abstract::Goniothalamin, a natural occurring styryl-lactone, is a novel compound with putative anticancer activities. In the present study, the mechanism of action of goniothalamin was further investigated in human breast cancer MDA-MB-231 cells. Goniothalamin treatment of cells significantly induced cell cycle arrest at G(2)/M...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2005.08.047

    authors: Chen WY,Wu CC,Lan YH,Chang FR,Teng CM,Wu YC

    更新日期:2005-10-17 00:00:00

  • The antinociceptive effect of Delta9-tetrahydrocannabinol in the arthritic rat involves the CB(2) cannabinoid receptor.

    abstract::Cannabinoid CB(2) receptors have been implicated in antinociception in animal models of both acute and chronic pain. We evaluated the role both cannabinoid CB(1) and CB(2) receptors in mechanonociception in non-arthritic and arthritic rats. The antinociceptive effect of Delta(9)-tetrahydrocannabinol (Delta(9)THC) was ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2007.05.024

    authors: Cox ML,Haller VL,Welch SP

    更新日期:2007-09-10 00:00:00

  • MK-801 powerfully protects against N-methyl aspartate neurotoxicity.

    abstract::Using the ex vivo chick embryo retina to study the efficacy of antagonists in blocking the excitotoxic effects of excitatory amino acid agonists, we previously identified phencyclidine as the most powerful known anti-excitotoxin. Here we show that MK-801 is 5 times more powerful than phencyclidine as an anti-excitotox...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(87)90552-8

    authors: Olney J,Price M,Salles KS,Labruyere J,Frierdich G

    更新日期:1987-09-23 00:00:00

  • Differential relaxant effects of isoproterenol on methacholine- versus leukotriene D4-induced contraction in the guinea-pig trachea.

    abstract::The ability of isoproterenol to relax guinea-pig trachea was examined in tissues precontracted with three concentrations of methacholine or three corresponding equieffective concentrations of leukotriene D4. Although increasing the concentration of either contractile agent progressively shifted isoproterenol concentra...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(84)90580-6

    authors: Torphy TJ

    更新日期:1984-07-20 00:00:00

  • Characterisation of [3H]gabapentin binding to a novel site in rat brain: homogenate binding studies.

    abstract::The binding characteristics of [3H]gabapentin, the radiolabelled analogue of the novel anticonvulsant gabapentin (1-(aminomethyl)cyclohexaneacetic acid) were studied using purified synaptic plasma membranes prepared from rat cerebral cortex. In 10 mM HEPES buffer [3H]gabapentin bound to a single population of sites wi...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0922-4106(93)90155-3

    authors: Suman-Chauhan N,Webdale L,Hill DR,Woodruff GN

    更新日期:1993-02-15 00:00:00

  • A pharmacological comparison of the cloned frog and human mu opioid receptors reveals differences in opioid affinity and function.

    abstract::This study presents a direct comparison of the ligand binding and signaling profiles of a mammalian and non-mammalian mu opioid receptor. Opioid ligand binding and agonist potencies were determined for an amphibian (Rana pipiens) mu opioid receptor (rpMOR) and the human mu opioid receptor (hMOR) in transfected, intact...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2008.09.043

    authors: Brasel CM,Sawyer GW,Stevens CW

    更新日期:2008-12-03 00:00:00

  • Reversal by [D-Ala2,D-Leu5]enkephalin of the dopamine transporter loss caused by methamphetamine.

    abstract::A single administration of 40 mg/kg (i.p.) of methamphetamine caused a loss of dopamine transporter in the striatum of albino Swiss (CD-1) mouse for at least 3 weeks. The administration of a single dose of [D-Ala2,D-Leu5]enkephalin (DADLE) (18 mg/kg, i.p.), given at day 14 after the administration of methamphetamine, ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(99)00240-x

    authors: Tsao LI,Cadet JL,Su TP

    更新日期:1999-05-21 00:00:00

  • LK 204-545, a highly selective beta1-adrenoceptor antagonist at human beta-adrenoceptors.

    abstract::LK 204-545 ((+/-)-1-(2-(3-(2-cyano-4-(2-cyclopropyl-methoxy-ethoxy)phenoxy)-2-hydro xy-propyl-amino)-ethyl)-3-(4-hydrxy-phenyl) urea), an antagonist that possesses high beta1-/beta2-selectivity in the rat, and a range of cardio-selective and non-selective beta-adrenoceptor antagonists were examined to compare their ra...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(99)00019-9

    authors: Louis SN,Nero TL,Iakovidis D,Jackman GP,Louis WJ

    更新日期:1999-02-19 00:00:00

  • Oral clonidine inhibits visceral pain-related viscerosomatic and cardiovascular responses to colorectal distension in rats.

    abstract::The alpha(2)-adrenoceptor agonist, clonidine, modulates colorectal sensorimotor functions in humans and, given intrathecally, has analgesic effects in the colorectal distension (CRD) model in rats. We tested the effects of systemic clonidine on the visceral pain-related viscerosomatic and autonomic cardiovascular resp...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2008.06.056

    authors: Brusberg M,Ravnefjord A,Lindgreen M,Larsson H,Lindström E,Martinez V

    更新日期:2008-09-04 00:00:00

  • Parental morphine exposure affects repetitive grooming actions and marble burying behavior in the offspring: Potential relevance for obsessive-compulsive like behavior.

    abstract::Family, adoption and twin studies have highlighted the significant role of heritable influences on individual differences in opioid addiction. Meanwhile, obsessive-compulsive disorder (OCD) is a disorder wherein the individual experiences recurring thoughts that cause irrational fears and anxiety. In the present study...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2019.172757

    authors: Rohbani K,Sabzevari S,Sadat-Shirazi MS,Nouri Zadeh-Tehrani S,Ashabi G,Khalifeh S,Ale-Ebrahim M,Zarrindast MR

    更新日期:2019-12-15 00:00:00