The non-psychoactive cannabis constituent cannabidiol is an orally effective therapeutic agent in rat chronic inflammatory and neuropathic pain.

Abstract:

:Cannabidiol, the major psycho-inactive component of cannabis, has substantial anti-inflammatory and immunomodulatory effects. This study investigated its therapeutic potential on neuropathic (sciatic nerve chronic constriction) and inflammatory pain (complete Freund's adjuvant intraplantar injection) in rats. In both models, daily oral treatment with cannabidiol (2.5-20 mg/kg to neuropathic and 20 mg/kg to adjuvant-injected rats) from day 7 to day 14 after the injury, or intraplantar injection, reduced hyperalgesia to thermal and mechanical stimuli. In the neuropathic animals, the anti-hyperalgesic effect of cannabidiol (20 mg/kg) was prevented by the vanilloid antagonist capsazepine (10 mg/kg, i.p.), but not by cannabinoid receptor antagonists. Cannabidiol's activity was associated with a reduction in the content of several mediators, such as prostaglandin E(2) (PGE(2)), lipid peroxide and nitric oxide (NO), and in the over-activity of glutathione-related enzymes. Cannabidiol only reduced the over-expression of constitutive endothelial NO synthase (NOS), without significantly affecting the inducible form (iNOS) in inflamed paw tissues. Cannabidiol had no effect on neuronal and iNOS isoforms in injured sciatic nerve. The compound's efficacy on neuropathic pain was not accompanied by any reduction in nuclear factor-kappaB (NF-kappaB) activation and tumor necrosis factor alpha (TNFalpha) content. The results indicate a potential for therapeutic use of cannabidiol in chronic painful states.

journal_name

Eur J Pharmacol

authors

Costa B,Trovato AE,Comelli F,Giagnoni G,Colleoni M

doi

10.1016/j.ejphar.2006.11.006

subject

Has Abstract

pub_date

2007-02-05 00:00:00

pages

75-83

issue

1-3

eissn

0014-2999

issn

1879-0712

pii

S0014-2999(06)01257-X

journal_volume

556

pub_type

杂志文章
  • Characterization of the intrinsic activity for a novel class of cannabinoid receptor ligands: Indole quinuclidine analogs.

    abstract::Our laboratory recently reported that a group of novel indole quinuclidine analogs bind with nanomolar affinity to cannabinoid type-1 and type-2 receptors. This study characterized the intrinsic activity of these compounds by determining whether they exhibit agonist, antagonist, or inverse agonist activity at cannabin...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2014.05.007

    authors: Franks LN,Ford BM,Madadi NR,Penthala NR,Crooks PA,Prather PL

    更新日期:2014-08-15 00:00:00

  • Species-specific binding of transformed Ah receptor to a dioxin responsive transcriptional enhancer.

    abstract::The Ah receptor (AhR) mediates many, if not all, of the toxic and biological effects of 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD, dioxin) and related halogenated aromatic hydrocarbons. Although wide variations in species sensitivity to these compounds have been observed, numerous biochemical and physiochemical charac...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0926-6917(92)90016-6

    authors: Bank PA,Yao EF,Phelps CL,Harper PA,Denison MS

    更新日期:1992-09-01 00:00:00

  • Tonic GABA-ergic modulation of striatal dopamine release studied by in vivo microdialysis in the freely moving rat.

    abstract::GABAA and GABAB receptor agonists and antagonists were administered locally in the striatum of intact and kainic acid lesioned rats. (+/-)-Baclofen, a GABAB receptor agonist, significantly decreased the level of extracellular dopamine in the striatum of intact rats. (+/-)-Phaclofen, a GABAB receptor antagonist, increa...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(95)00369-v

    authors: Smolders I,De Klippel N,Sarre S,Ebinger G,Michotte Y

    更新日期:1995-09-15 00:00:00

  • Solubilization and characterization of the kappa-opioid receptor type from guinea-pig cerebellum.

    abstract::The kappa-opioid receptor (kappa Op) from guinea-pig cerebellum membranes has been solubilized in an active form and in good yield (30-40%) with digitonin in 10 mM Tes-KOH buffer, pH 7.4. [3H]Bremazocine (KD = 1.1 nM in the soluble extract) was used to monitor the binding and hydrodynamic characteristics of the digito...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(88)90755-8

    authors: Francés B,Moisand C,Meunier JC

    更新日期:1988-05-20 00:00:00

  • Medical ozone promotes Nrf2 phosphorylation reducing oxidative stress and pro-inflammatory cytokines in multiple sclerosis patients.

    abstract::Oxidative stress and inflammation play key roles in the pathogenesis of Multiple sclerosis (MS). Different drugs have been used in the clinical practice, however, there is not a completely effective treatment. Due to its potential therapeutic action, medical ozone represents a promising approach for neurodegenerative ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2017.06.017

    authors: Delgado-Roche L,Riera-Romo M,Mesta F,Hernández-Matos Y,Barrios JM,Martínez-Sánchez G,Al-Dalaien SM

    更新日期:2017-09-15 00:00:00

  • Antinociceptive effect of a kappa-opioid receptor agonist that minimally crosses the blood-brain barrier (ICI 204448) in a rat model of mononeuropathy.

    abstract::The antinociceptive effect of intraplantar (i.pl.) ICI 204448 ((R,S)-N-[2-(N-methyl-3,4-dichloro-phenylacetamido)-2-(3-carbox yph enyl)- ethyl]pyrrolidine hydrochloride)) (20, 30, 40 and 50 micrograms), a kappa-opioid receptor agonist which has limited access to the central nervous system, was studied in a well-establ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(95)00122-2

    authors: Keïta H,Kayser V,Guilbaud G

    更新日期:1995-04-24 00:00:00

  • Differential effects of sulfonylurea derivatives on vascular ATP-sensitive potassium channels.

    abstract::Sulfonylurea drugs exert their insulinotropic action by inhibiting ATP-sensitive potassium channels in the pancreas. However, these channels are also expressed in myocardial and vascular smooth muscle, implicating possible detrimental cardiovascular effects. Aim of the present study was to investigate the inhibitory p...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2012.02.006

    authors: Engbersen R,Masereeuw R,van Gestel MA,Siero HL,Moons MM,Smits P,Russel FG

    更新日期:2012-04-15 00:00:00

  • Histamine release induced by neurotensin from rat peritoneal mast cells.

    abstract::Neurotensin induced the release of histamine from both purified and non-purified rat peritoneal mast cells by a non-cytotoxic mechanism. It was effective at a concentration as low as 10(-8) M. The dose-response curve for the neurotensin effect was triphasic: and initial gentle rise, a plateau (2.5 X 10(-7) -2.5 X 10(-...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(81)90494-5

    authors: Kurose M,Saeki K

    更新日期:1981-12-03 00:00:00

  • Pharmacological evidence for selective inhibition of gastric acid secretion by telenzepine, a new antimuscarinic drug.

    abstract::The new antisecretory drug, telenzepine (4,9-dihydro-3-methyl-4-[(4-methyl-1-piperazinyl)acetyl]-10H-thieno-[3,4 - b][1,5]benzodiazepin-10-one), was investigated for its inhibition of functionally intact muscarinic receptors involved in gastric acid secretion in rabbit fundic glands, perfused mouse stomach in vitro, p...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(85)90498-4

    authors: Eltze M,Gönne S,Riedel R,Schlotke B,Schudt C,Simon WA

    更新日期:1985-06-07 00:00:00

  • Differential effects of agents acting at various sites of the NMDA receptor complex in a place preference conditioning model.

    abstract::A conditioned place preference paradigm was used to assess the potential rewarding properties of the uncompetitive NMDA receptor antagonist, MK-801 (dizolcipine), the two competitive NMDA receptor antagonists, CGP 37849 (DL-(E)-2-amino-4-methyl-5-phosphono-3-pentonoic acid) and its (R)-enantiomer CGP 40116, as well as...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(96)00747-9

    authors: Papp M,Moryl E,Maccecchini ML

    更新日期:1996-12-19 00:00:00

  • Effects of second-generation histamine H1 receptor antagonists on the sleep-wakefulness cycle in rats.

    abstract::The present study was performed to examine the sedative effects of second-generation histamine H(1) receptor antagonist using power spectrum analysis in the rat. Similar to ketotifen, olopatadine caused a decrease in sleep latency at a dose of 50 mg/kg, while epinastine and cetirizine showed no significant effect even...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2004.05.010

    authors: Shigemoto Y,Shinomiya K,Mio M,Azuma N,Kamei C

    更新日期:2004-06-28 00:00:00

  • Influence of sub-chronic selective 11β-hydroxysteroid dehydrogenase 1 inhibition on the hypothalamic-pituitary-adrenal axis in female cynomolgus monkeys.

    abstract::Inhibition of local cortisol regeneration from circulating cortisone by blocking 11β-hydroxysteroid dehydrogenase 1 (11β-HSD1) has been shown to ameliorate the risk factors associated with the metabolic syndrome. Chronic modulation of glucocorticoid homeostasis may result in hypothalamic-pituitary-adrenal (HPA) axis s...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2016.07.004

    authors: Hamilton BS,Schoelch C,Schuler-Metz A,Krosky P,Lala DS,Claremon DA,McGeehan GM

    更新日期:2016-10-15 00:00:00

  • Detailed investigation of anticancer activity of sulfamoyl benz(sulfon)amides and 1H-pyrazol-4-yl benzamides: An experimental and computational study.

    abstract::Cancer is the second leading cause of mortality worldwide. Therapeutic approach to cancer is a multi-faceted one, whereby many cellular/enzymatic pathways have been discovered as important drug targets for the treatment of cancer. A major disadvantage of most of the currently available anticancer drugs is their non-se...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2018.05.011

    authors: Iqbal J,Ejaz SA,Saeed A,Al-Rashida M

    更新日期:2018-08-05 00:00:00

  • [D-Met2,Pro5]enkephalinamide activates cardioinhibitory efferents in anaesthetized dogs.

    abstract::[D-Met2,Pro5]enkephalinamide (DMPEA) strongly activated cardioinhibitory vagal efferents and elicited bradycardia when perfused through the cerebroventricular system of anaesthetized dogs. These effects were concentration-dependent but plateaued at an intraventricular concentration of 200 micrograms/ml. At this maxima...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(85)90216-x

    authors: Inoue K,Nashan B,Arndt JO

    更新日期:1985-04-02 00:00:00

  • Immunopharmacology: anti-inflammatory therapy targeting transcription factors.

    abstract::Immunopharmacology is one of the most dynamic areas in pharmacology encompassing classical immunosuppressive drugs which reveal completely new clues concerning their mode of action as well as novel molecular biology approaches for treating inflammatory and autoimmune diseases, infections and cancer. This article focus...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章,评审

    doi:10.1016/s0014-2999(99)00361-1

    authors: Pfeilschifter J,Mühl H

    更新日期:1999-06-30 00:00:00

  • Cordycepin protects against cerebral ischemia/reperfusion injury in vivo and in vitro.

    abstract::Cordycepin, (3'-deoxyadenosine), a bioactive compound of Cordyceps militaris, has been shown to exhibit many pharmacological actions, such as anti-inflammatory, antioxidative and anticancer activities. Little is known about the neuroprotective action of cordycepin as well as its molecular mechanisms. In this study, co...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2011.04.052

    authors: Cheng Z,He W,Zhou X,Lv Q,Xu X,Yang S,Zhao C,Guo L

    更新日期:2011-08-16 00:00:00

  • Relations between muscimol, quinuclidinyl benzilate and nicotine binding sites in brain after very long treatment with ethanol in rats.

    abstract::Rats were treated with ethanol in the drinking fluid 2 X 1 h daily for 83 weeks. [3H]Muscimol, [3H]quinuclidinyl benzilate ( [3H]QNB) and [3H]nicotine binding was measured in selected brain areas 7, 14 and 21 days after withdrawal of ethanol. A significant increase (P less than 0.05) when compared to controls was foun...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(85)90704-6

    authors: Nordberg A,Wahlström G,Eriksson B

    更新日期:1985-09-24 00:00:00

  • Stimulation of kappa-opioid receptor reduces isoprenaline-induced cardiac hypertrophy and fibrosis.

    abstract::The aim of the present study was to determine whether U50,488H (a selective kappa-opioid receptor agonist) inhibits cardiac hypertrophy and fibrosis induced by beta-adrenoceptor stimulation in a rat model. Cardiac hypertrophy and fibrosis were developed by intraperitoneal administration of isoprenaline (ip. 3.0 mg/kg/...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2009.01.050

    authors: Yin W,Zhang P,Huang JH,Zhang QY,Fan R,Li J,Zhou JJ,Hu YZ,Guo HT,Zhang SM,Wang YM,Kaye AD,Gu CH,Liu JC,Cheng L,Cui Q,Yi DH,Pei JM

    更新日期:2009-04-01 00:00:00

  • Biological evaluation of novel Pt(II) and Pd(II) complexes with pyrazole-containing ligands.

    abstract::The new platinum (II) and palladium (II) complexes (2-4) with ligands 5-(2-hydroxyphenyl)-1,3-dimethyl-4-(dimethoxy)phosphonyl-1H]-pyrazole (1a) and 5-(2-hydroxyphenyl)-1,3-dimethyl-4-methoxycarbonyl-1H]-2-pyrazole (1b) were screened in a search for novel anticancer agents. Thus, alkylating activity, cytotoxicity, abi...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2004.08.053

    authors: Budzisz E,Krajewska U,Rozalski M,Szulawska A,Czyz M,Nawrot B

    更新日期:2004-10-11 00:00:00

  • Low nanomolar thapsigargin inhibits the replication of vascular smooth muscle cells through reversible endoplasmic reticular stress.

    abstract::Thapsigargin (TG), an inhibitor of Ca(2+) ATPase pumps in the endoplasmic reticulum (ER), inhibits replication of human vascular smooth muscle cell (hVSMC) at low nM concentrations. TG blocks replication of other cell types through promotion of ER stress (ERS). In order to determine whether ERS may mediate the cytosta...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2013.05.036

    authors: Shukla N,Wan S,Angelini GD,Jeremy JY

    更新日期:2013-08-15 00:00:00

  • The quinoxalinediones antagonise the visual firing of sustained retinal ganglion cells.

    abstract::The non N-methyl-D-aspartate (NMDA) receptor antagonists dinitroquinoxaline-2,3-dione (DNQX) and 6-cyano-7-nitroquinoxaline-2,3-dione (CNQX), both inhibit the visually driven response of sustained ganglion cells in the cat retina in vivo. In contrast to these findings, the potent NMDA receptor antagonist 3-[+/- )-2-ca...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(89)90483-4

    authors: Kay CD,Ikeda H

    更新日期:1989-05-19 00:00:00

  • Increase of glucocorticoids is not required for the acquisition, but hinders the extinction, of lithium-induced conditioned taste aversion.

    abstract::Lithium chloride at doses sufficient to induce conditioned taste aversion (CTA) causes c-Fos expression in the paraventricular nucleus and increases the plasma level of corticosterone with activation of the hypothalamic-pituitary-adrenal axis. This study was conducted to define the role of glucocorticoid in the acquis...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2014.02.017

    authors: Kim KN,Kim BT,Kim YS,Lee JH,Jahng JW

    更新日期:2014-05-05 00:00:00

  • Anticonvulsant action and biochemical effects in DBA/2 mice of CPP (3-((+/-)-2-carboxypiperazin-4-yl)-propyl-1-phosphonate), a novel N-methyl-D-aspartate antagonist.

    abstract::CPP has a potent anticonvulsant effect against sound-induced seizures in audiogenic DBA/2 mice. Pretreatment with CPP (0.01-10 nmol i.c.v., 45 min) protects against successive phases of sound-induced seizures in a dose-dependent fashion (ED50, tonic phase, 0.023 nmol; clonic phase, 0.039 nmol; wild running, 0.17 nmol)...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(87)90501-2

    authors: Chapman AG,Meldrum BS,Nanji N,Watkins JC

    更新日期:1987-07-02 00:00:00

  • Effects of serotonin 5-HT1B receptor ligands on the cocaine- and food-maintained self-administration in rats.

    abstract::In order to substantiate the concept that cocaine behavioral effects may be influenced by serotonin (5-HT)1B receptors, male Wistar rats were trained to self-administer cocaine intravenously (0.5 mg/kg/injection), and were systemically pretreated with the selective 5-HT1B receptor antagonist N-[3-[3-(dimethylamine)eth...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2006.12.012

    authors: Przegaliński E,Gołda A,Frankowska M,Zaniewska M,Filip M

    更新日期:2007-03-22 00:00:00

  • Identification of novel pyrazoloquinazolinecarboxilate analogues to inhibit nerve growth factor in vitro.

    abstract::Nerve growth factor (NGF) is known to regulate the development and survival of select populations of neurons via its binding/activation of the TrkA and p75(NTR) receptors. However, in some physiological circumstances NGF dysregulation can result in debilitating pathologies, including diabetic neuropathies, interstitia...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2013.03.029

    authors: Eibl JK,Strasser BC,Ross GM

    更新日期:2013-05-15 00:00:00

  • The potassium channel opener CGS7184 activates Ca²⁺ release from the endoplasmic reticulum.

    abstract::CGS7184 (ethyl 1-[[(4-chlorophenyl)amino]oxo]-2-hydroxy-6-trifluoromethyl-1H-indole-3-carboxylate) is a synthetic large-conductance Ca(2+)-activated potassium (BK(Ca)) channel opener. The existing literature suggests that potassium channels are involved in cardioprotection, particularly during ischemia-reperfusion eve...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2012.06.029

    authors: Wrzosek A,Tomaskova Z,Ondrias K,Lukasiak A,Szewczyk A

    更新日期:2012-09-05 00:00:00

  • Pericardial mesothelial cells produce endothelin-1 and possess functional endothelin ETB receptors.

    abstract::We investigated the endothelin production and endothelin receptor activity of pericardial mesothelial cells obtained from spontaneously hypertensive rats (SHR) and Wistar-Kyoto (WKY) rats. The pericardial mesothelial cells were maintained in vitro and the production of endothelin-1 by these cells was evaluated by usin...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(98)00110-1

    authors: Kuwahara M,Kuwahara M

    更新日期:1998-04-24 00:00:00

  • Inhibition by histamine H1 receptor antagonists of endogenous glibenclamide-sensitive K+ channels in follicle-enclosed Xenopus oocytes.

    abstract::Effects of histamine receptor ligands on the glibenclamide-sensitive K+ currents induced by K+ channel openers, cromakalim and Y-26763, were examined in follicle-enclosed Xenopus oocytes. Histamine H1 receptor antagonists, promethazine, dimethindene and chlorpheniramine all decreased cromakalim-induced K+ currents wit...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0922-4106(94)90214-3

    authors: Sakuta H

    更新日期:1994-01-01 00:00:00

  • Cooperative effect of angiotensin AT(1) and endothelin ET(A) receptor antagonism limits the brain damage after ischemic stroke in rat.

    abstract::Cerebral ischemia results in enhanced expression of smooth muscle cell endothelin and angiotensin receptors in cerebral arteries. We hypothesise that this phenomenon may be detrimental and that acute treatment with a combined non-hypotensive dose of the angiotensin AT(1) receptor inhibitor candesartan and the endothel...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2007.05.049

    authors: Stenman E,Jamali R,Henriksson M,Maddahi A,Edvinsson L

    更新日期:2007-09-10 00:00:00

  • The aetiology of gastric ulceration induced by electrical vagal stimulation in rats.

    abstract::Histamine and serotonin levels in gastric secretion and the effects of pharmacological antagonists were studied in rats in which stomach ulceration was induced by electrical vagal stimulation. Electrical vagal stimulation (2 and 5 V) produced a graded increase in haemorrhagic glandular mucosal ulcers. NaHCO3 perfusion...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(85)90213-4

    authors: Cho CH,Hung KM,Ogle CW

    更新日期:1985-04-02 00:00:00