The Inhibitory Effect of S-777469, a Cannabinoid Type 2 Receptor Agonist, on Skin Inflammation in Mice.

Abstract:

:We investigated the effects of S-777469 (1-[[6-Ethyl-1-[4-fluorobenzyl]-5-methyl-2-oxo-1, 2-dihydropyridine-3-carbonyl]amino]-cyclohexanecarboxylic acid), a novel cannabinoid type 2 receptor (CB2) agonist, on 1-fluoro-2,4-dinitrobenzene (DNFB)-induced ear inflammation and mite antigen-induced dermatitis in mice. The oral administration of S-777469 significantly suppressed DNFB-induced ear swelling in a dose-dependent manner. In addition, S-777469 significantly alleviated mite antigen-induced atopic dermatitis-like skin lesions in NC/Nga mice. A histological analysis revealed that S-777469 significantly reduced the epidermal thickness and the number of mast cells infiltrating skin lesions. We demonstrated that S-777469 inhibited mite antigen-induced eosinophil accumulation in skin lesions and an endogenous CB2 ligand, 2-arachidonoylglycerol (2-AG)-induced eosinophil migration in vitro. Moreover, we confirmed that 2-AG levels significantly increased in skin lesions of mite antigen-induced dermatitis model. Together, these results suggest that S-777469 inhibits skin inflammation in mice by blocking the activities of 2-AG.

journal_name

Pharmacology

journal_title

Pharmacology

authors

Haruna T,Soga M,Morioka Y,Imura K,Furue Y,Yamamoto M,Hayakawa J,Deguchi M,Arimura A,Yasui K

doi

10.1159/000455916

subject

Has Abstract

pub_date

2017-01-01 00:00:00

pages

259-267

issue

5-6

eissn

0031-7012

issn

1423-0313

pii

000455916

journal_volume

99

pub_type

杂志文章
  • Actions of mibefradil, efonidipine and nifedipine block of recombinant T- and L-type Ca channels with distinct inhibitory mechanisms.

    abstract::We compared detailed efficacy of efonidipine and nifedipine, dihydropyridine analogues, and mibefradil using recombinant T- and L-type Ca2+ channels expressed separately in mammalian cells. All these Ca2+ channel antagonists blocked T-type Ca2+ channel currents (I(Ca(T))) with distinct blocking manners: I(Ca(T)) was b...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000094900

    authors: Lee TS,Kaku T,Takebayashi S,Uchino T,Miyamoto S,Hadama T,Perez-Reyes E,Ono K

    更新日期:2006-01-01 00:00:00

  • Indirect comparison of once daily insulin detemir and glargine in reducing weight gain and hypoglycaemic episodes when administered in addition to conventional oral anti-diabetic therapy in patients with type-2 diabetes.

    abstract:AIMS:Basal insulin administered to type-2 diabetic patients with poor glycaemic control when managed with oral anti-diabetics (OADs) alone can lead to an increased risk of weight gain and hypoglycaemia. In the absence of head-to-head trials, an indirect comparison of the once-daily insulin detemir with insulin glargine...

    journal_title:Pharmacology

    pub_type: 杂志文章,meta分析

    doi:10.1159/000149569

    authors: Fakhoury W,Lockhart I,Kotchie RW,Aagren M,LeReun C

    更新日期:2008-01-01 00:00:00

  • Effect of cromakalim and pinacidil on 86Rb efflux from guinea pig urinary bladder smooth muscle.

    abstract::86Rb efflux assay was used to investigate the effect of cromakalim, pinacidil and P1075 in guinea pig urinary bladder strips. The type of K channel opened by cromakalim and pinacidil was determined using specific K channel blockers through 86Rb efflux assay in detrusor strips. Cromakalim, pinacidil and P1075 all three...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000139230

    authors: Trivedi S,Stetz S,Levin R,Li J,Kau S

    更新日期:1994-09-01 00:00:00

  • Is [3H]-tiotidine a specific ligand for the H2-receptor?

    abstract::The H2-antagonist tiotidine inhibited the H2-receptor-mediated, histamine-induced increase in cyclic AMP in dispersed mucosal cells from guinea pig stomach (Ki, 4 X 10(-8) M). The radiolabeled [3H]-tiotidine bound specifically and reversibly to the same cells with a half-maximal binding occurring at 5 X 10(-7) M tioti...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000138176

    authors: Batzri S,Harmon JW

    更新日期:1986-01-01 00:00:00

  • On the heterogeneity of mast cells.

    abstract::Mast cells from different locations are shown to vary in their histochemical, ultrastructural, cytochemical and functional properties. The clinical consequences of this heterogeneity and possible reasons for its origin are discussed. ...

    journal_title:Pharmacology

    pub_type: 杂志文章,评审

    doi:10.1159/000138153

    authors: Pearce FL

    更新日期:1986-01-01 00:00:00

  • Action of cytidine diphosphocholine on functional and hemodynamic effects of cerebral ischemia in cats.

    abstract::The depression of evoked cortical potentials caused by brief periods of cerebral ischemia is attenuated by prior intracarotid injection of cytidoline (2, 4 or 8 mg/kg). Studies performed in hypercapnic cats suggest that the protection afforded by cytidoline is of metabolic rather than hemodynamic origin. The participa...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000136830

    authors: Boismare F,Le Poncin M,Lefrançois J,Lecordier JC

    更新日期:1978-01-01 00:00:00

  • Inhibition of muscimol on morphine-induced hyperactivity, reverse tolerance and postsynaptic dopamine receptor supersensitivity.

    abstract::This study was performed to investigate the effect of muscimol on morphine-induced hyperactivity, reverse tolerance and postsynaptic dopamine receptor supersensitivity in mice. A single administration of morphine induced hyperactivity as measured in mice, and the morphine-induced hyperactivity was inhibited dose-depen...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000064345

    authors: Yoon IS,Kim HS,Hong JT,Lee MK,Oh KW

    更新日期:2002-08-01 00:00:00

  • Pharmacokinetics of macitentan in caucasian and Japanese subjects: the influence of ethnicity and sex.

    abstract:BACKGROUND/AIMS:Macitentan is a novel dual endothelin receptor antagonist with sustained receptor binding in clinical development for pulmonary arterial hypertension. The present study compared the pharmacokinetics and safety of macitentan in healthy Caucasian and Japanese subjects and explored the potential sex differ...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000351704

    authors: Bruderer S,Marjason J,Sidharta PN,Dingemanse J

    更新日期:2013-01-01 00:00:00

  • The Efficacy of Rituximab Combined with 131I for Ophthalmic Outcomes of Graves' Ophthalmopathy Patients.

    abstract:PURPOSE:The purpose of this study is to examine the effectiveness of introducing both rituximab (RTX) and 131I for active Graves' ophthalmopathy (GO) with hyperthyroidism. METHODS:In total, 217 patients suffering from active GO with hyperthyroidism were included in this research. All subjects were randomly assigned to...

    journal_title:Pharmacology

    pub_type: 杂志文章,随机对照试验

    doi:10.1159/000453618

    authors: Li J,Xiao Z,Hu X,Li Y,Zhang X,Zhang S,Gong W,Zhao J,Ye X

    更新日期:2017-01-01 00:00:00

  • Prevention of galactosamine-induced hepatotoxicity in rats with fructose-1,6-diphosphate.

    abstract::Galactosamine (GalN) administration produces hepatitis-like liver injury in animals. The hepatotoxicity of GalN is attenuated by several interventions, including activation of the reticuloendothelial system (RES). Fructose-1,6-diphosphate (FDP) administration significantly increases the phagocytic activity of the RES ...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000138861

    authors: Markov AK,Farias LA,Bennett WS,Subramony C,Mihas AA

    更新日期:1991-01-01 00:00:00

  • Attitudes and opinion about adverse drug events of women living in a city of south Italy.

    abstract:BACKGROUND/AIM:Perception of risk of adverse drug events (ADEs) is different between health and nonhealth professionals, but these differences have not been investigated sufficiently in the general population. Women are more affected by ADEs. With the aim to investigate ADE risk perception in a sample of nonhealth prof...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000346737

    authors: Salvo F,Miroddi M,Alibrandi A,Calapai F,Cafeo V,Mancari F,Gangemi S,Caputi AP,Calapai G

    更新日期:2013-01-01 00:00:00

  • Effects of mitemcinal (GM-611), an acid-resistant nonpeptide motilin receptor agonist, on the gastrointestinal contractile activity in conscious dogs.

    abstract::The effects of mitemcinal (GM-611) on the gastrointestinal contractile activity were investigated using chronically implanted force transducers in conscious dogs and were compared with the effects of porcine motilin (pMTL), EM-523 and EM-574. In the interdigestive state, intravenous and oral administration of mitemcin...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000101537

    authors: Ozaki K,Yogo K,Sudo H,Onoma M,Kamei K,Akima M,Koga H,Itoh Z,Omura S,Takanashi H

    更新日期:2007-01-01 00:00:00

  • Overexpression of Orphan Receptor GPR61 Increases cAMP Levels upon Forskolin Stimulation in HEK293 Cells: in vitro and in silico Validation of 5-(Nonyloxy)Tryptamine as a Low-Affinity Inverse Agonist.

    abstract::GPR61 is an orphan receptor that belongs to Class A of G-protein-coupled receptors. It has been reported that GPR61 has a constitutive activity and couples to Gαs. In the present study, we characterized GPR61 function and ligand binding by experimental and molecular docking studies. We demonstrated that heterologous e...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000501926

    authors: Kozielewicz P,Grafton G,Sajkowska-Kozielewicz JJ,Barnes NM

    更新日期:2019-01-01 00:00:00

  • Cardiovascular effects of alloxan diabetes in normotensive and spontaneously hypertensive rats.

    abstract::The diabetogenic effects of alloxan (50 mg/kg i.v.) were recorded for 6 weeks in normotensive (WKY) and spontaneously hypertensive (SHR) rats. While systolic blood pressure increased in diabetic WKY, SHR exhibited a reduction in systolic blood pressure over the 6-week period. Heart rate of treated SHR, but not WKY, wa...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000137367

    authors: Cavaliere TA,Taylor DG,Kerwin LJ,Antonaccio MJ

    更新日期:1980-01-01 00:00:00

  • ICI 198615 is an antagonist of leukotriene C4, leukotriene D4 and leukotriene E4 vasopressor responses in the conscious rat.

    abstract::The purpose of these studies was to evaluate the effects of the peptidoleukotriene (LT) receptor antagonist, ICI 198615, on the vasopressor responses produced by LTC4, LTD4 and LTE4. Conscious, normotensive rats were prepared with arterial and venous catheters for measurement of changes in arterial blood pressure and ...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000138699

    authors: Smith EF 3rd,Slivjak MJ

    更新日期:1990-01-01 00:00:00

  • Evaluation of pharmacological profile of meloxicam as an anti-inflammatory agent, with particular reference to its relative selectivity for cyclooxygenase-2 over cyclooxygenase-1.

    abstract::We studied the anti-inflammatory activity of meloxicam on rat carrageenin-induced pleurisy and its toxicity for rat gastric mucosa, relative to its in vitro inhibitory potency against partially purified cyclooxygenase (COX)-1 and COX-2 preparations in order to clarify the pharmacological profile of the compound as an ...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000139511

    authors: Ogino K,Hatanaka K,Kawamura M,Katori M,Harada Y

    更新日期:1997-07-01 00:00:00

  • Antipyretic and analgesic effects of zaltoprofen for the treatment of acute upper respiratory tract infection: verification of a noninferiority hypothesis using loxoprofen sodium.

    abstract::A multicenter, placebo-controlled, double-dummy, randomized, parallel-group, double-blind study was conducted to verify the hypothesis of noninferiority for single-dose administration of zaltoprofen 160 mg, a nonsteroidal anti-inflammatory drug, compared with loxoprofen sodium 60 mg (loxoprofen), in terms of antipyret...

    journal_title:Pharmacology

    pub_type: 杂志文章,多中心研究,随机对照试验

    doi:10.1159/000324532

    authors: Azuma A,Kudoh S,Nakashima M,Nagatake T

    更新日期:2011-01-01 00:00:00

  • Does nitrous oxide induce release of brain opioid peptides?

    abstract::Increased concentrations of immunoreactive methionine-enkephalin but not leucine-enkephalin were measured in fractions of cerebrospinal fluid perfusate collected from ventricular-cisternally perfused, urethane-anesthetized rats exposed to a mixture of 75% nitrous oxide/25% oxygen for 60 min. These findings suggest tha...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000138056

    authors: Quock RM,Kouchich FJ,Tseng LF

    更新日期:1985-01-01 00:00:00

  • Transport of model compounds across the peritoneal membrane in the rat.

    abstract::The absorption into the systemic circulation of compounds administered intraperitoneally in large volumes was investigated in the rat. The influence on absorption of molecular weight, lipid-water partition coefficient (K), and dissociation constant (pKa) was studied. Nine neutral compounds ranging in molecular weight ...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000136874

    authors: Torres IJ,Litterst CL,Guarino AM

    更新日期:1978-01-01 00:00:00

  • Antihypertensive effect of 5-HT1A agonist buspirone and 5-HT2B antagonists in experimentally induced hypertension in rats.

    abstract::We investigated the antihypertensive effect of 5-HT1A agonist (buspirone) and 5-HT2B antagonists (SB204741 and SB200646) in deoxycorticosterone acetate (DOCA)-salt-induced hypertensive rats. Experiments were divided into two sets: in the first set, sham-operated control and DOCA-treated hypertensive rats received busp...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000082114

    authors: Shingala JR,Balaraman R

    更新日期:2005-03-01 00:00:00

  • Differential induction of sister chromatid exchange by chemical carcinogens in lymphocytes cultured from patients with solid tumors.

    abstract::Three carcinogens with different requirements for activation were used to generate sister chromatid exchange (SCE) in cultured lymphocytes from 22 untreated patients with solid tumors. These data were compared to SCEs produced by incubating lymphocytes, from 44 normal persons, with the same carcinogens. In vitro treat...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000137578

    authors: Wiencke JK,Vosika J,Johnson P,Wang N,Garry VF

    更新日期:1982-01-01 00:00:00

  • Euodia daniellii Hemsl. (Bee-Bee Tree) Oil Attenuates Palmitate-Induced Lipid Accumulation and Apoptosis in Hepatocytes.

    abstract::Hepatic lipid accumulation and apoptosis is elevated in patients with non-alcoholic steatohepatitis and is closely associated with severity. Saturated fatty acid palmitate stimulates lipid accumulation and apoptosis in hepatocytes. In the present study, we examined bee-bee tree oil (BO)-mediated protective effects on ...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000487892

    authors: Jung TW,Kim SY,Kim DS,Shin EC,Park YB,Lee KT

    更新日期:2018-01-01 00:00:00

  • The synthetic PPARgamma agonist troglitazone inhibits IL-5-induced CD69 upregulation and eosinophil-derived neurotoxin release from eosinophils.

    abstract::Peroxisome proliferator-activated receptor-gamma (PPARgamma) is a nuclear receptor that regulates lipid metabolism. Recently, PPARgamma was reported to be a negative regulator in the immune system. Eosinophils also express PPARgamma, however, the role of PPARgamma in eosinophil functions is not well understood. Surfac...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000085034

    authors: Matsuwaki Y,Ueki S,Adachi T,Oyamada H,Kamada Y,Yamaguchi K,Kanda A,Hamada K,Kayaba H,Chihara J

    更新日期:2005-07-01 00:00:00

  • In vitro effect of carvedilol on professional phagocytes.

    abstract:AIM:Superfluous reactive nitrogen and oxygen species generation is implicated in the damage of tissues at sites of inflammation where activated neutrophils and macrophages are involved. This study was conducted to investigate whether the beneficial effects of carvedilol involve modulation of respiratory burst, degranul...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000097818

    authors: Pecivová J,Macicková T,Lojek A,Gallova L,Cíz M,Nosál' R,Holománová D

    更新日期:2007-01-01 00:00:00

  • Stereoselective glucuronidation of carvedilol in human liver and intestinal microsomes.

    abstract:BACKGROUND AND PURPOSE:Carvedilol is used clinically as a β-adrenoceptor antagonist for the treatment of chronic heart failure and is primarily metabolized into glucuronides by UDP-glucuronosyltransferase (UGT). In this study, the stereoselective glucuronidation of carvedilol by the human liver and intestinal microsome...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000340020

    authors: Hanioka N,Tanaka S,Moriguchi Y,Narimatsu S

    更新日期:2012-01-01 00:00:00

  • Inhibition of prostaglandin biosynthesis in human endotoxin-stimulated peripheral blood monocytes: effects of caffeine.

    abstract::There is an ongoing debate about possible advantages of the coadministration of caffeine with cyclooxygenase (COX) inhibitors in the treatment of pain. There are results suggesting interference by caffeine with COX expression and activity in rat immune cells. In the present study, we have used, therefore, human endoto...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000067742

    authors: Ulcar R,Schuligoi R,Heinemann A,Santner B,Amann R

    更新日期:2003-02-01 00:00:00

  • Involvement of the nitric oxide/cyclic guanylate monophosphate pathway in the pilocarpine-induced seizure model in mice.

    abstract::The present study was designed to investigate the involvement of the nitric oxide (NO)/cyclic guanylate monophosphate pathway in pilocarpine-induced seizures in mice. Male Swiss mice (26-32 g) were used as the in vivo model. The following pharmacological tools were utilized: the non-selective NO synthase (NOS) inhibit...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000346268

    authors: Vasconcelos Rios ER,Moura Rocha NF,Rodrigues Carvalho AM,Freire Vasconcelos L,Leite Dias M,de Carvalho Lima CN,Soares Lopes K,Cavalcante Melo FH,de França Fonteles MM

    更新日期:2013-01-01 00:00:00

  • Effect of mannitol on Helicobacter pylori-induced cyclooxygenase-2 expression in gastric epithelial AGS cells.

    abstract::Oxygen radicals have been considered to be important regulatory molecules in Helicobacter pylori-induced gastric ulceration and carcinogenesis. H. pylori-induced inflammation has been shown to be associated with cyclooxygenase-2 (COX-2) expression in experimental animals and human patients. This study aimed to determi...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000065532

    authors: Kim H,Seo JY,Kim KH

    更新日期:2002-12-01 00:00:00

  • Central effect of dibutyryl cyclic AMP on the temperature in the conscious rabbit.

    abstract::In the rabbit, intracerebroventricular administration of dibutyryl cyclic AMP (DBC) produces fever which is selectively antagonised by phenoxybenzamine. This indicates the involvement of central alpha-adrenoceptors in DBC-induced fever. The decrease in DBC hyperthermia after 6-hydroxydopamine (6-OH-DA) supports the vi...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000137385

    authors: Kandasamy SB

    更新日期:1980-01-01 00:00:00

  • Effect of promethazine on human polymorphonuclear chemiluminescence.

    abstract::The effect of promethazine on the metabolic responsiveness of human polymorphonuclear leukocytes to opsonized zymosan was evaluated by chemiluminescence (CL) assay under the following situations: (1) preincubation of granulocytes with promethazine; (2) simultaneous addition of zymosan and promethazine, and (3) additio...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000136787

    authors: Trush MA,Van Dyke K

    更新日期:1978-01-01 00:00:00