Effects of ginsenosides, active components of ginseng, on nicotinic acetylcholine receptors expressed in Xenopus oocytes.

Abstract:

:We investigated the effects of ginsenosides, the active ingredient of ginseng, on neuronal or muscle-type nicotinic acetylcholine receptor channel activity expressed in Xenopus oocytes after injection of cRNA encoding bovine neuronal alpha3beta4, alpha7 or human muscle alphabetadeltavarepsilon subunits. Treatment with acetylcholine elicited an inward peak current (I(ACh)) in oocytes expressing nicotinic acetylcholine receptor subtypes. Cotreatment with ginsenoside Rg2 and acetylcholine inhibited I(ACh) in oocytes expressing with alpha3beta4 or alphabetadeltavarepsilon but not in oocytes expressing alpha7 nicotinic acetylcholine receptors. The inhibition of I(ACh) by ginsenoside Rg2 was reversible and dose-dependent. The half-inhibitory concentrations (IC50) of ginsenoside Rg2 were 60.2+/-14.1 and 15.7+/-3.5 microM in oocytes expressing alpha3beta4 and alphabetadeltavarepsilon nicotinic acetylcholine receptors, respectively. The inhibition of I(ACh) by ginsenoside Rg2 was voltage-independent and noncompetitive. Other ginsenosides besides ginsenoside Rg2 also inhibited I(ACh) in oocytes expressing alpha3beta4 or alphabetadeltavarepsilon nicotinic acetylcholine receptors. The order of potency for the inhibition of I(ACh) was ginsenoside Rg2>Rf>Re>Rg1>Rc>Rb2>Rb1 in oocytes expressing alpha3beta4 nicotinic acetylcholine receptors and was ginsenoside Rg2>Rf>Rg1>Re>Rb1>Rc>Rb2 in oocytes expressing alphabetadeltavarepsilon nicotinic acetylcholine receptors. These results indicate that ginsenosides might regulate nicotinic acetylcholine receptors in a differential manner and this regulation might be one of the pharmacological actions of Panax ginseng.

journal_name

Eur J Pharmacol

authors

Choi S,Jung SY,Lee JH,Sala F,Criado M,Mulet J,Valor LM,Sala S,Engel AG,Nah SY

doi

10.1016/s0014-2999(02)01508-x

keywords:

subject

Has Abstract

pub_date

2002-05-03 00:00:00

pages

37-45

issue

1-2

eissn

0014-2999

issn

1879-0712

pii

S001429990201508X

journal_volume

442

pub_type

杂志文章
  • Conditioned place preference studies with atomoxetine in an animal model of ADHD: effects of previous atomoxetine treatment.

    abstract::To investigate the putative rewarding effects of atomoxetine, a non-stimulant medication for Attention-deficit/hyperactivity disorder (ADHD), we conducted conditioned place preference (CPP) tests in an animal model of ADHD, the spontaneously hypertensive rat (SHR). The effects of drug pre-exposure were also evaluated,...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2011.05.057

    authors: dela Peña IC,Ahn HS,Ryu JH,Shin CY,Park IH,Cheong JH

    更新日期:2011-09-30 00:00:00

  • Platycodin D-induced apoptosis through nuclear factor-kappaB activation in immortalized keratinocytes.

    abstract::Platycodi Radix is the root of Platycodon grandiflorum and it is widely used in the traditional Oriental medicine as an expectorant for pulmonary diseases and a remedy for respiratory disorders. Platycodin D is the major constituent of triterpene saponins in the root. This study investigates apoptosis by platycodin D ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2006.03.012

    authors: Ahn KS,Hahn BS,Kwack K,Lee EB,Kim YS

    更新日期:2006-05-10 00:00:00

  • Protein kinase A-dependent coupling of mouse prostacyclin receptors to Gi is cell-type dependent.

    abstract::The ability of the prostacyclin (IP) receptor agonist cicaprost to activate Gs-, Gq/11- and Gi-mediated cell signalling pathways has been examined in Chinese hamster ovary (CHO) cells and human embryonic kidney 293 (HEK 293) cells expressing the cloned human (hIP) or mouse (mIP) prostacyclin receptor, and compared wit...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(03)02006-5

    authors: Chow KB,Jones RL,Wise H

    更新日期:2003-08-01 00:00:00

  • Galanin decreases the activity of locus coeruleus neurons in vitro.

    abstract::A brain slice preparation was used to examine the effects of galanin on the spontaneous firing rate of locus coeruleus noradrenergic neurons. Galanin (10(-9)-10(-7) M), added to the bath, inhibited the firing of 14 out of 19 neurons in a concentration-dependent manner. The observed effect was quite variable, ranging f...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(89)90481-0

    authors: Seutin V,Verbanck P,Massotte L,Dresse A

    更新日期:1989-05-19 00:00:00

  • Decreased beta-adrenoceptor-mediated vasodilation in aorta from aged rats: possible involvement of a stimulatory GTP-binding protein.

    abstract::KCl-contracted aortic rings from 18-month-old rats, in contrast with those from 2-month-old rats, showed a substantial reduction in the relaxant effects of the non-selective beta-adrenoceptor agonist, isoproterenol, and of the selective beta 2-adrenoceptor agonist, clenbuterol, without changes in the relaxant actions ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(91)90618-z

    authors: Kazanietz MG,Enero MA

    更新日期:1991-06-06 00:00:00

  • Wy-48,252 (1,1,1-trifluoro-N-[3-(2-quinolinylmethoxy)phenyl]membrane sulfonamide), an orally active leukotriene antagonist: effects on arachidonic acid metabolism in various inflammatory cells.

    abstract::The LTD4 antagonist, Wy-48,252 (1,1,1-trifluoro-N-[3-(2-quinolinylmethoxy)phenyl]methanesulfonamide), was assessed for its ability to modulate arachidonic acid metabolism in several inflammatory cells. In A23187-stimulated rat neutrophils, Wy-48,252 effectively inhibited the conversion of exogenous [14C]arachidonic ac...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(88)90462-1

    authors: Chang J,Borgeat P,Schleimer RP,Musser JH,Marshall LA,Hand JM

    更新日期:1988-03-22 00:00:00

  • Effects of oxcarbazepine and 10-hydroxycarbamazepine on action potential firing and generalized seizures.

    abstract::The anticonvulsant compound oxcarbazepine and its principal 10-monohydroxy metabolite protected potently against electroshock-induced tonic hindlimb extension. Maximal plasma concentrations depended on dose and were reached < or = 1 h after an oral dose of oxcarbazepine and < 2 h after monohydroxy derivative. In mice,...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(94)90787-0

    authors: Wamil AW,Schmutz M,Portet C,Feldmann KF,McLean MJ

    更新日期:1994-12-27 00:00:00

  • Clozapine potently stimulates mesocortical dopamine neurons.

    abstract::The effects of clozapine on dopamine neurons projecting to the medial-prefrontal cortex, nuclei accumbens and caudatus were compared. Clozapine (1.25 mg/kg i.v.) maximally stimulated the firing rate and burst activity of dopamine neurons projecting to the medialprefrontal cortex. Much higher doses (5 and 10 mg/kg i.v....

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(98)00934-0

    authors: Melis M,Diana M,Gessa GL

    更新日期:1999-02-05 00:00:00

  • Gene expression, localization, and pharmacological characterization of endothelin receptors in diabetic rat bladder dome.

    abstract::As there are significant amounts of functional endothelin receptors in the mammalian urinary tract, we examined the effect of experimental diabetes on the expression of endothelin receptors and their mRNAs in the rat bladder dome. The density of endothelin receptors in the rat bladder dome was higher (8 and 16 weeks f...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(99)00753-0

    authors: Saito M,Wada Y,Ikeda K,Wang Z,Smith SD,Foster HE,Nishi K,Weiss RM,Latifpour J

    更新日期:2000-01-17 00:00:00

  • Tricyclic antidepressants activate the pituitary-adrenal axis in the rat. Tolerance to repeated drug administration.

    abstract::The effects of acute chronic administration of tricyclic antidepressants on the pituitary-adrenal axis were studied in adult male rats. Acute administration of desipramine, imipramine and chlorimipramine activated the pituitary-adrenal axis. The effect of imipramine was found to be of short duration with a significant...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(87)90812-0

    authors: Armario A,García-Marquez C

    更新日期:1987-08-11 00:00:00

  • (-)-Trans-epsilon-viniferin, a polyphenol present in wines, is an inhibitor of noradrenaline and 5-hydroxytryptamine uptake and of monoamine oxidase activity.

    abstract::(-)-Trans-epsilon-viniferin (epsilon-viniferin, 5-200 microM), a dimer of resveratrol, concentration-dependently inhibited the uptake of [3H]noradrenaline and [3H]5-HT by synaptosomes from rat brain (being slightly but significantly more selective against [3H]noradrenaline) and the uptake of [3H]5-HT by human platelet...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2006.06.005

    authors: Yáñez M,Fraiz N,Cano E,Orallo F

    更新日期:2006-08-07 00:00:00

  • Negative inotropic effects of diadenosine tetraphosphate are mediated by protein kinase C and phosphodiesterases stimulation in the rat heart.

    abstract::Extracellular diadenosine polyphosphates (ApnA) are recently considered as an endogenous signaling compounds with transmitter-like activity which present in numerous tissues, including heart. It has been demonstrated previously that extracellular ApnA cause alteration of the heart functioning via purine receptors in d...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2017.12.024

    authors: Pakhomov N,Pustovit K,Potekhina V,Filatova T,Kuzmin V,Abramochkin D

    更新日期:2018-02-05 00:00:00

  • Factors affecting the transition of acute kidney injury to chronic kidney disease: Potential mechanisms and future perspectives.

    abstract::Acute kidney injury (AKI) is defined as a rapid loss of kidney function characterised by inflammation and cell death, ultimately leading to further functional and structural renal alterations. Based on experimental and epidemiological pieces of evidence, AKI may progress to chronic kidney disease (CKD) even after a re...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章,评审

    doi:10.1016/j.ejphar.2019.172711

    authors: Ogbadu J,Singh G,Aggarwal D

    更新日期:2019-12-15 00:00:00

  • The effect of acute simvastatin administration on the severity of arrhythmias resulting from ischaemia and reperfusion in the canine: Is there a role for nitric oxide?

    abstract::The present study has examined the effects and the possible mechanisms of a single dose of simvastatin on the severity of arrhythmias resulting from a 25min occlusion and reperfusion of the left anterior descending coronary artery in anaesthetized (chloralose and urethane) dogs. The control animals (n=16) were given t...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2014.03.021

    authors: Kisvári G,Kovács M,Gardi J,Seprényi G,Kaszaki J,Végh Á

    更新日期:2014-06-05 00:00:00

  • Carvedilol treatment ameliorates acute coxsackievirus B3-induced myocarditis associated with oxidative stress reduction.

    abstract::Oxidative stress has been implicated in the pathogenesis of acute myocarditis. The imbalance between the occurrence of reactive oxygen species and the cellular antioxidant defense mechanism plays a key role in myocardial injury of viral myocarditis. Carvedilol, a nonselective beta-adrenoceptor antagonist with addition...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2010.04.037

    authors: Li YC,Ge LS,Yang PL,Tang JF,Lin JF,Chen P,Guan XQ

    更新日期:2010-08-25 00:00:00

  • Inhibitors of 1,2-diacylglycerol kinase potentiate the TRH-induced stimulation of Ca2+-activated K+ current.

    abstract::Transient activation of the outward K+ current caused by a rise in the cytosolic free Ca2+ concentration, [Ca2+]i was the predominant change in plasma membrane ion flux during the first phase of thyrotropin-releasing hormone (TRH) action on pituitary cells. Following the intracellular application of inhibitors of 1,2-...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0922-4106(89)90046-1

    authors: Mollard P,Vacher P,Dufy B,Winiger BP,Schlegel W

    更新日期:1989-03-07 00:00:00

  • Interaction of histamine H2-receptor antagonists with GABA and benzodiazepine binding sites in the CNS.

    abstract::The histamine H2-receptor antagonist cimetidine potently inhibited [3H]muscimol and enhanced [3H]flunitrazepam binding in membranes prepared from several brain regions in the rat, including the dorsal raphe nucleus. As further examined in cortical membranes, this effect on both GABA and benzodiazepine binding sites wa...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(83)90011-0

    authors: Lakoski JM,Aghajanian GK,Gallager DW

    更新日期:1983-03-25 00:00:00

  • Neuropeptide modulation of muscarinic receptors and function in cerebral cortex of young and senescent rats.

    abstract::The possible influence of several neuropeptides on muscarinic receptor binding and function in fronto-parietal cortex of young and senescent Fischer 344 rats was examined. Low concentrations (100 nM) of cholecystokinin, neurotensin and vasoactive intestinal polypeptide (VIP), added in vitro, enhanced carbachol-stimula...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0922-4106(92)90095-d

    authors: Pedigo NW Jr,Rice MA

    更新日期:1992-02-13 00:00:00

  • Anti-thrombin action of low-dose acetylsalicylic acid.

    abstract::It is known that low-dose aspirin is effective in coronary artery therapy, although it has not yet been clarified how it exerts its action. Here, we report that treatment of coronary artery patients with 100 mg/day of aspirin does not attenuate thrombin generation, but reduces free thrombin by favouring the formation ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(02)02925-4

    authors: Di Micco B,Colonna G,Di Micco P,Di Micco G,Russo BM,Macalello MA,Ragone R

    更新日期:2003-01-26 00:00:00

  • Mediation of dopamine D1 and D2 receptors in the effects of GBR 12909 on latent learning and locomotor activity in mice.

    abstract::We investigated the involvement of dopamine D1 and D2 receptor subtypes in the effects of GBR 12909, a selective dopamine uptake inhibitor, on latent learning in the performance of a water-finding task and on locomotor activity in mice. GBR 12909 (10 and 20 mg/kg) impaired latent learning, and this effect was countera...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(93)90949-i

    authors: Ichihara K,Nabeshima T,Kameyama T

    更新日期:1993-04-06 00:00:00

  • Cannabinoid precipitated withdrawal by the selective cannabinoid receptor antagonist, SR 141716A.

    abstract::Precipitated withdrawal in rats chronically exposed to delta 9-tetrahydrocannabinol, the major psychoactive principle of the marijuana plant, was unequivocally demonstrated for the first time using a selective antagonist, SR 141716A (N-(piperidin-1-yl)-5-(4-chlorophenyl)-1(2,4- dichloro-phenyl)-4-methyl-1H-pyrazole ca...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(95)00447-s

    authors: Aceto MD,Scates SM,Lowe JA,Martin BR

    更新日期:1995-08-25 00:00:00

  • Antipsychotic-induced suppression of locomotion in juvenile, adolescent and adult rats.

    abstract::Schizophrenia is a serious psychiatric disorder that is most frequently treated with the administration of antipsychotics. Although onset of schizophrenia typically occurs in late adolescence, the majority of preclinical research on the behavioral effects of antipsychotics and their mechanism(s) of action has been con...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2007.09.010

    authors: Wiley JL

    更新日期:2008-01-14 00:00:00

  • Role of brain arachidonic acid cascade on central CRF1 receptor-mediated activation of sympatho-adrenomedullary outflow in rats.

    abstract::The present experiments were designed to characterize the mechanisms involved in the corticotropin releasing factor (CRF)-induced activation of central sympatho-adrenomedullary outflow in rats. Intracerebroventricularly (i.c.v.) administered CRF and urocortin (0.5, 1.5 and 3.0 nmol/animal) effectively and dose-depende...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(01)00987-6

    authors: Yokotani K,Murakami Y,Okada S,Hirata M

    更新日期:2001-05-11 00:00:00

  • Adenosine A(2A) receptor dynamics studied with the novel fluorescent agonist Alexa488-APEC.

    abstract::G protein-coupled receptors, such as the adenosine A(2A) receptor, are dynamic proteins, which undergo agonist-dependent redistribution from the cell surface to intracellular membranous compartments, such as endosomes. In order to study the kinetics of adenosine A(2A) receptor redistribution in living cells, we synthe...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2008.05.036

    authors: Brand F,Klutz AM,Jacobson KA,Fredholm BB,Schulte G

    更新日期:2008-08-20 00:00:00

  • Differential antinociceptive effects induced by intrathecally administered endomorphin-1 and endomorphin-2 in the mouse.

    abstract::Two highly selective mu-opioid receptor agonists, endomorphin-1 and endomorphin-2, have been identified and postulated to be endogenous ligands for mu-opioid receptors. Intrathecal (i.t.) administration of endomorphin-1 and endomorphin-2 at doses from 0.039 to 5 nmol dose-dependently produced antinociception with the ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(01)01238-9

    authors: Sakurada S,Hayashi T,Yuhki M,Orito T,Zadina JE,Kastin AJ,Fujimura T,Murayama K,Sakurada C,Sakurada T,Narita M,Suzuki T,Tan-no K,Tseng LF

    更新日期:2001-09-21 00:00:00

  • Mixed type inhibition of [D-Ala2, D-Leu5]enkephalin binding to mu-opiate binding sites by mu-, but not by kappa-opiate ligands.

    abstract::The interaction of the delta-opiate agonist [D-Ala2,D]Leu5]enkephalin (DADL) with the mu-opiate ligands dihydromorphine (DHM) and naloxone and the kappa-opiate ligand ethylketocyclazocine (EK) was studied in rat diencephalic membranes which contain mainly mu-opiate binding sites. Saturation binding experiments perform...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(82)90145-5

    authors: Pfeiffer A,Herz A

    更新日期:1982-02-05 00:00:00

  • The CRF1 receptor antagonist, R121919, attenuates the severity of precipitated morphine withdrawal.

    abstract::Corticotropin-releasing factor (CRF) regulates the hypothalamic-pituitary-adrenal axis, coordinates the mammalian stress response, and acting primarily via the CRF(1) receptor, has been strongly implicated in the pathophysiology of depression and anxiety. Furthermore, the behavioral and autonomic activation that occur...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2007.05.041

    authors: Skelton KH,Oren D,Gutman DA,Easterling K,Holtzman SG,Nemeroff CB,Owens MJ

    更新日期:2007-09-24 00:00:00

  • Galanin stimulates growth hormone (GH) secretion via GH-releasing factor (GRF) in conscious rats.

    abstract::The possibility of a role of hypothalamic growth hormone (GH)-releasing factor (GRF) in GH secretion induced by centrally administered galanin was investigated in freely moving male rats. Intracerebroventricular (i.c.v.) injection of synthetic galanin (0.4 or 2 micrograms/rat) elicited a dose-related increase in plasm...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(87)90316-5

    authors: Murakami Y,Kato Y,Koshiyama H,Inoue T,Yanaihara N,Imura H

    更新日期:1987-04-29 00:00:00

  • Glibenclamide blocks the relaxant action of pinacidil and cromakalim in airway smooth muscle.

    abstract::Concentration-relaxation curves for pinacidil and cromakalim were obtained in isolated guinea-pig tracheas contracted by histamine. Pinacidil produced complete relaxation with an EC50 value of 2.8 microM. The antidiabetic sulfonylurea, glibenclamide (0.1, 1, 10 microM), caused concentration-dependent rightward shifts ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(90)90312-t

    authors: Nielsen-Kudsk JE,Bang L,Brønsgaard AM

    更新日期:1990-05-16 00:00:00

  • The in vivo pharmacological profile of eletriptan (UK-116,044): a potent and novel 5-HT(1B/1D) receptor agonist.

    abstract::The anti-migraine drug, eletriptan [(R)-3-(1-methyl-2-pyrrolidinylmethyl)-5-[2-(phenylsulphonyl )ethyl]-1 H-indole; UK-116,044], is a novel 5-HT(1B/1D) receptor agonist. In this paper, the regional vasoconstrictor profile of eletriptan, in comparison with sumatriptan, was examined in the anaesthetised dog. The inhibit...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(00)00240-5

    authors: Gupta P,Butler P,Shepperson NB,McHarg A

    更新日期:2000-06-09 00:00:00