The discovery and status of sibutramine as an anti-obesity drug.

Abstract:

:Sibutramine is a serotonin-norepinephrine reuptake inhibitor indicated for the management of obesity in conjunction with a reduced calorie diet. Though sibutramine was originally evaluated for possible use as an antidepressant, its research development was eventually redirected to evaluate it as an anorexiant. The pharmacological mechanisms by which sibutramine exerts its weight loss effect are likely due to a combination of reduced appetite, feelings of satiety, and possibly the induction of thermogenesis. Its efficacy for inducing an initial weight-loss and the subsequent maintenance of the weight-loss is well proven in short- and long-term clinical trials of up to 2 years duration. In general, sibutramine has been well tolerated. Increases in blood pressure and heart rate are possible adverse effects that require regular monitoring. Sibutramine is one of the few established and well-proven agents for obesity available for use today and should be considered effective in the management of patients requiring pharmacotherapy as part of the multi-modal approach to weight-loss.

journal_name

Eur J Pharmacol

authors

Luque CA,Rey JA

doi

10.1016/s0014-2999(02)01423-1

keywords:

subject

Has Abstract

pub_date

2002-04-12 00:00:00

pages

119-28

issue

2-3

eissn

0014-2999

issn

1879-0712

pii

S0014299902014231

journal_volume

440

pub_type

杂志文章,评审
  • Curcumin ameliorates scopolamine-induced mice memory retrieval deficit and restores hippocampal p-Akt and p-GSK-3β.

    abstract::The loss of cholinergic neurons has been a major issue in researches on Alzheimer's disease (AD) for about 40 years. Therefore, the scopolamine model of amnesia has been widely used in AD researches. Recently, it was reported that the early stage amnesia of AD is related to memory retrieval deficit. Curcumin, as the m...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2018.10.012

    authors: SoukhakLari R,Moezi L,Pirsalami F,Ashjazadeh N,Moosavi M

    更新日期:2018-12-15 00:00:00

  • Vasodilator profile of synthetic atrial natriuretic factor.

    abstract::The vasodilator profile of synthetic atrial natriuretic factor (ANF) was characterized using isolated vascular preparations. Nanomolar concentrations of ANF relaxed rabbit aortic rings contracted by serotonin, histamine, methoxamine or angiotensin II. The synthetic peptide was most effective (IC50 = 1.3 X 10(-10) M) i...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(84)90353-4

    authors: Winquist RJ,Faison EP,Nutt RF

    更新日期:1984-06-15 00:00:00

  • Effect of N,N-dimethyl-p-methoxyphenylethylamine on blood pressure and brain catecholamines in DOCA-saline hypertensive rats.

    abstract::Intraperitoneal and intraventricular injections of N,N-dimethyl-p-methoxyphenyl ethylamine (PMPEA) decreased blood pressure in conscious DOCA-saline hypertensive rats. Bilateral injection of this agent into the nucleus tractus solitarii (NTS) of anaesthetized normotensive rats also caused a decrease in blood pressure....

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(82)90472-1

    authors: Shalita B,Versteeg DH,De Jong W

    更新日期:1982-11-19 00:00:00

  • Melatonin as a protective agent in cardiac ischemia-reperfusion injury: Vision/Illusion?

    abstract::Melatonin, an emphatic endogenous molecule exerts protective effects either via activation of G-protein coupled receptors (Melatonin receptors, MTR 1-3), tumor necrosis factor receptor (TNFR), toll like receptors (TLRS), nuclear receptors (NRS) or by directly scavenging the free radicals. MTRs are extensively expresse...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章,评审

    doi:10.1016/j.ejphar.2020.173506

    authors: Randhawa PK,Gupta MK

    更新日期:2020-10-15 00:00:00

  • Effect of pretreatment with bronchodilator drugs on in vitro responsiveness of guinea pig lung adenylate cyclase.

    abstract::Pretreatment of guinea pigs with 5 microgram/kg isoprenaline or 10 microgram/kg salbutamol s.c. thrice daily for 7 days reduced the responsiveness of lung slice and tracheal ring adenylate cyclase to isoprenaline, but not to prostaglandin E1. Pretreatment of guinea pigs with isoprenaline also reduced the sensitivity o...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(78)90406-5

    authors: Elfellah MS,Turnbull MJ

    更新日期:1978-10-01 00:00:00

  • Cardioprotective signalling: Past, present and future.

    abstract::A few decades ago, cardiac muscle was discovered to possess signalling pathways that, when activated, protect the myocardium against the damage induced by ischaemia-reperfusion. The ability of cardiac muscle to protect itself against injury has been termed 'cardioprotection'. Many compounds and procedures can trigger ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章,评审

    doi:10.1016/j.ejphar.2018.06.029

    authors: Jovanović A

    更新日期:2018-08-15 00:00:00

  • Further evaluation of the selectivity of a novel antihypertensive agent, SGB-1534, for peripheral alpha 1-adrenoceptors in the spinally anesthetized dog.

    abstract::Experiments were designed to examine some characteristics of an orally active antihypertensive agent, SGB-1534 on alpha-adrenoceptors in spinally anesthetized dogs. In the saphenous arterial bed perfused by a constant pump volume, saphenous nerve stimulation and bolus applications of norepinephrine and phenylephrine i...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(86)90579-0

    authors: Imagawa J,Sakai K

    更新日期:1986-11-19 00:00:00

  • An outline for the pharmacological effect of icariin in the nervous system.

    abstract::Icariin is a major active component of the traditional herb Epimedium, also known as Horny Goat Weed. It has been extensively studied throughout the past several years and is known to exert anti-oxidative, anti-neuroinflammatory, and anti-apoptotic effects. It is now being considered as a potential therapeutic agent f...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章,评审

    doi:10.1016/j.ejphar.2018.10.006

    authors: Jin J,Wang H,Hua X,Chen D,Huang C,Chen Z

    更新日期:2019-01-05 00:00:00

  • Differential effects of systemic and intraseptal administration of the acetylcholinesterase inhibitor tacrine on the recovery of spatial behavior in an animal model of diencephalic amnesia.

    abstract::Several lines of evidence suggest that acetylcholinesterase inhibitors (AChE) have their cognitive enhancing effects by stimulating cholinergic receptors within the medial septum. However, intraseptal administration of cholinergic enhancing drugs produce mixed results that appear to depend on both the integrity of the...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2009.12.005

    authors: Roland JJ,Levinson M,Vetreno RP,Savage LM

    更新日期:2010-03-10 00:00:00

  • Therapeutic potential of cannabidiol against ischemia/reperfusion liver injury in rats.

    abstract::The therapeutic potential of cannabidiol, the major non-psychotropic Cannabis constituent, was investigated in rats exposed to ischemia/reperfusion liver injury. Ischemia was induced by clamping the pedicle of the left hepatic lobe for 30 min, and cannabidiol (5mg/kg, i.v.) was given 1h following the procedure and eve...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2011.08.048

    authors: Fouad AA,Jresat I

    更新日期:2011-11-16 00:00:00

  • Effects of ageing and adrenergic stimulation on alpha 1- and beta-adrenoceptors and phospholipid fatty acids in rat heart.

    abstract::The purpose of this study was to examine the influence of ageing on the alterations in binding characteristics of adrenoceptors and membrane phospholipid fatty acids in rat heart following repeated administration of epinephrine. The maximal number of binding sites (Bmax) and dissociation constant (Kd) of [3H]prazosin ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0922-4106(95)90150-7

    authors: Benediktsdóttir VE,Skúladóttir GV,Gudbjarnason S

    更新日期:1995-05-26 00:00:00

  • CysLT2 receptor activation is involved in LTC4-induced lung air-trapping in guinea pigs.

    abstract::CysLT1 receptors are known to be involved in the pathogenesis of asthma. However, the functional roles of CysLT2 receptors in this condition have not been determined. The purpose of this study is to develop an experimental model of CysLT2 receptor-mediated LTC4-induced lung air-trapping in guinea pigs and use this mod...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2016.11.036

    authors: Sekioka T,Kadode M,Yonetomi Y,Kamiya A,Fujita M,Nabe T,Kawabata K

    更新日期:2017-01-05 00:00:00

  • Inhibition of soluble epoxide hydrolase attenuates airway remodeling in a chronic asthma model.

    abstract::Airway remodeling in asthma is difficult to treat because of its complex pathophysiology that involves proinflammatory cytokines, as well as the arachidonic acid cytochrome P-450 (CYP) pathway; however, it has received little attention. In this study, we assessed the efficacy of a soluble epoxide hydrolase (sEH) on ai...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2019.172874

    authors: Jiang JX,Guan Y,Shen HJ,Jia YL,Shen J,Zhang LH,Liu Q,Zhu YL,Xie QM

    更新日期:2020-02-05 00:00:00

  • Blockade of endothelin ET(A), but not thromboxane, receptors offsets the cyclosporine-evoked hypertension and interrelated baroreflex and vascular dysfunctions.

    abstract::The impairment of arterial baroreceptor and vasodilator functions are two major contributors to the hypertensive action of cyclosporine (CSA). In this study, in vivo and in vitro pharmacological studies were performed to investigate whether these effects of CSA are differentially modulated by endothelin and thromboxan...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2014.01.034

    authors: Nasser SA,Elmallah AI,Sabra R,Khedr MM,El-Din MM,El-Mas MM

    更新日期:2014-03-15 00:00:00

  • Differences between rats and mice in MDMA (methylenedioxymethylamphetamine) neurotoxicity.

    abstract::In both rats and mice a single large dose of methylenedioxymethylamphetamine (MDMA; 25 mg/kg i.p.) caused a fall 3 h after injection in the content of 5-hydroxytryptamine (5-HT) and 5-hydroxyindoleacetic acid (5-HIAA) in cortex, a fall in noradrenaline in hippocampus and cerebellum, and a rise in dopamine (DA) but fal...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(88)90717-0

    authors: Logan BJ,Laverty R,Sanderson WD,Yee YB

    更新日期:1988-08-02 00:00:00

  • Block of the transient inward current by R56865 in guinea-pig ventricular myocytes.

    abstract::Single myocytes isolated from the guinea-pig ventricle were used under voltage-clamp conditions to study the activity of a newly developed drug, R56865, a benzothiazolamine derivative, against digitalis toxicity. Multicellular Purkinje preparations were used in some experiments. The drug blocked the transient inward c...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(91)90407-h

    authors: Leyssens A,Carmeliet E

    更新日期:1991-04-10 00:00:00

  • Differential changes of myocardial beta-adrenoceptor subtypes and G-proteins in dogs with right-sided congestive heart failure.

    abstract::We have shown previously in dogs with right heart failure that the reduction of myocardial beta-adrenoceptor density occurs only in the failing right ventricle, while cardiac inotropic responses to beta-adrenergic stimulation are reduced in both the right and left ventricles. The purpose of the present study was to de...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(96)00340-8

    authors: Lai LP,Suematsu M,Elam H,Liang CS

    更新日期:1996-08-08 00:00:00

  • Ipratropium bromide potentiates bronchoconstriction induced by vagal nerve stimulation in the guinea-pig.

    abstract::In anaesthetised guinea-pigs, bronchoconstriction induced by vagal nerve stimulation was potentiated by low doses of the antimuscarinic bronchodilator drug, ipratropium (0.01-1.0 microgram/kg); the maximum effect was obtained with 1.0 microgram/kg which doubled the bronchoconstriction. When the dose was increased abov...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(87)90251-2

    authors: Fryer AD,Maclagan J

    更新日期:1987-07-09 00:00:00

  • The role of atrial natriuretic peptide in the diuretic effect of Ca2+ entry blockers.

    abstract::The effect of three calcium entry blockers--verapamil, nifedipine and felodipine--on diuresis, natriuresis, the renin-aldosterone axis, and atrial natriuretic peptide (ANP) levels was studied in 30 previously untreated patients with mild to moderate essential hypertension. All three blockers produced significant antih...

    journal_title:European journal of pharmacology

    pub_type: 临床试验,杂志文章,随机对照试验

    doi:10.1016/0014-2999(93)90356-m

    authors: Shamiss A,Peleg E,Rosenthal T,Ezra D

    更新日期:1993-03-16 00:00:00

  • Reversal of heparin-induced increases in aPTT in the rat by PM102, a novel heparin antagonist.

    abstract::Protamine is the only agent approved to reverse heparin-induced anticoagulation. Due to the significant adverse effects of protamine there is an important need for an alternative agent with an improved safety profile. The pharmacodynamics of PM102, a novel peptide-based heparin antagonist, was evaluated and compared t...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2010.03.016

    authors: Cushing DJ,Cooper WD,Cohen ML,McVoy JR,Sobel M,Harris RB

    更新日期:2010-06-10 00:00:00

  • Effects of gentamicin on catecholamine levels in the striatum, hypothalamus, adrenal gland and vas deferens.

    abstract::The effects of gentamicin, an aminoglycoside antibiotic, on changes in the catecholamine levels in the rat striatum, hypothalamus, adrenal medulla and vas deferens were studied. When rats were i.v. injected with gentamicin (1.0 mg/kg), the catecholamine content of all tissues increased 2-4 h after injection. The incre...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(92)90656-o

    authors: Mikami M,Tachikawa E,Kashimoto T

    更新日期:1992-01-07 00:00:00

  • Sensitivity of histamine H3 receptor agonist-stimulated [35S]GTP gamma[S] binding to pertussis toxin.

    abstract::The effect of histamine H3 receptor-selective ligands on [35S]guanosine 5'-o-(gamma-thio)triphosphate ([35S]GTP gamma[S]) binding has been examined in rat cerebral cortical membranes. R alpha-Methylhistamine and N alpha-methylhistamine produced a concentration-dependent stimulation of [35S]GTP gamma[S] binding which w...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(95)00800-4

    authors: Clark EA,Hill SJ

    更新日期:1996-01-25 00:00:00

  • Hydroxytyrosol enhances cisplatin-induced ototoxicity: Possible relation to the alteration in the activity of JNK and AIF pathways.

    abstract::Hydroxytyrosol (HT), a polyphenol widely contained as an ester in olive fruits and olive leaves, exhibits a broad spectrum of effectiveness. The present study was designed to investigate the effect of HT alone as well as in the combination with cisplatin on the House Ear Institute-Organ of Corti 1 cells (HEI-OC1) and ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2020.173338

    authors: Zhang W,Man R,Yu X,Yang H,Yang Q,Li J

    更新日期:2020-11-15 00:00:00

  • Stereotyped behavior correlates better than ataxia with phencyclidine-receptor interactions.

    abstract::The interaction of phencyclidine, dexoxadrol, their analogs and stereoisomers with phencyclidine receptors was compared to their ability to induce stereotyped behavior and ataxia after i.c.v. administration to rats. The order of potency for binding to phencyclidine receptors revealed that among the stereoisomers of ph...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(86)90386-9

    authors: Contreras PC,Rice KC,Jacobson AE,O'Donohue TL

    更新日期:1986-02-11 00:00:00

  • PPADS, a P2X receptor antagonist, as a novel inhibitor of the reverse mode of the Na⁺/Ca²⁺ exchanger in guinea pig airway smooth muscle.

    abstract::The Na(+)/Ca(2+)exchanger (NCX) principal function is taking 1 Ca(2+) out of the cytoplasm and introducing 3 Na(+). The increase of cytoplasmic Na(+) concentration induces the NCX reverse mode (NCX(REV)), favoring Ca(2+) influx. NCX(REV) can be inhibited by: KB-R7943 a non-specific compound that blocks voltage-depende...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2011.11.018

    authors: Flores-Soto E,Reyes-García J,Sommer B,Chavez J,Barajas-López C,Montaño LM

    更新日期:2012-01-15 00:00:00

  • Inhaled formoterol inhibits histamine-induced airflow obstruction and airway microvascular leakage.

    abstract::We studied the effects of inhaled formoterol (0.75 mg/ml, 60 breaths = 26 micrograms), a long-acting beta 2-adrenoceptor agonist, or of the more short-acting drug, salbutamol (25 mg/ml, 60 breaths = 875 micrograms), on acute airflow obstruction and airway microvascular leakage (MVL) induced by inhaled histamine in ane...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(91)90197-x

    authors: Tokuyama K,Lötvall JO,Löfdahl CG,Barnes PJ,Chung KF

    更新日期:1991-01-25 00:00:00

  • Anti-cancer activity of two novel heterocyclic compounds through modulation of VEGFR and miR-122 in mice bearing Ehrlich ascites carcinoma.

    abstract::Metastasis in breast cancer is a leading cause of mortality among women in many countries. This study investigated the anti-cancer role of benzoimidazoquinazoline and benzimidazotriazin; two novel compounds that were designed, synthesized, structurally elucidated, and biologically evaluated as potent anti-angiogenic a...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2020.173747

    authors: Hazem RM,Mohamed AA,Ghareb N,Mehanna ET,Mesbah NM,Abo-Elmatty DM,Elgawish MS

    更新日期:2021-02-05 00:00:00

  • Selected nucleos(t)ide-based prescribed drugs and their multi-target activity.

    abstract::Nucleos(t)ide analogues play pivotal roles as antiviral, cytotoxic or immunosuppressive agents. Here, we review recent reports of nucleoside analogues that exhibit broad-spectrum activity towards multiple life-threatening RNA and DNA viruses. We also present a discussion about nucleoside antimetabolites-approved antin...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章,评审

    doi:10.1016/j.ejphar.2019.172747

    authors: Pastuch-Gawołek G,Gillner D,Król E,Walczak K,Wandzik I

    更新日期:2019-12-15 00:00:00

  • Levetiracetam effect and electrophysiological mechanism of action in rats with cobalt-induced chronic epilepsy.

    abstract::Levetiracetam was initially developed as a nootropic drug, although since 2002 it has been used as anticonvulsant for the treatment of partial and generalized epilepsy syndromes. The purpose of the research was to investigate anti-paroxysmal activity of levetiracetam (LEV) on the model of cobalt-induced chronic epilep...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2019.04.041

    authors: Litvinova Svetlana A,Voroninа Tatyana A,Nerobkova Lubov N,Kutepova Inga S,Avakyan Georgii G,Avakyan Gagik N

    更新日期:2019-07-05 00:00:00

  • Current advances in stem cell-based therapies for hair regeneration.

    abstract::Alopecia is resulted from various factors that can decrease the regeneration capability of hair follicles and affect hair cycles. This process can be devastating physically and psychologically. Nevertheless, the available treatment strategies are limited, and the therapeutic outcomes are not satisfactory. According to...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章,评审

    doi:10.1016/j.ejphar.2020.173197

    authors: Yuan AR,Bian Q,Gao JQ

    更新日期:2020-08-15 00:00:00