abstract：BACKGROUND AND PURPOSE:This study examined the antinociceptive effects of sinomenine in a rat model of postoperative pain. EXPERIMENTAL APPROACH:Male and female rats were subjected to a surgical incision in the right hind paw, and the von Frey filament test was used to measure mechanical hypersensitivity after drug or...

journal_title：British journal of pharmacology

authors： Zhu Q,Sun Y,Mao L,Liu C,Jiang B,Zhang W,Li JX

更新日期：2016-05-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Palmitoylethanolamide (PEA) is an endogenous congener of anandamide and potentiates its actions at cannabinoid CB1 and CB2 receptors, and at transient receptor potential vanilloid type-1 (TRPV1) channels. The other endocannabinoid, 2-arachidonoylglycerol (2-AG), was recently suggested to act as a...

journal_title：British journal of pharmacology

authors： Petrosino S,Schiano Moriello A,Cerrato S,Fusco M,Puigdemont A,De Petrocellis L,Di Marzo V

更新日期：2016-04-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Biased GPCR ligands are able to engage with their target receptor in a manner that preferentially activates distinct downstream signalling and offers potential for next generation therapeutics. However, accurate quantification of ligand bias in vitro is complex, and current best practice is not a...

journal_title：British journal of pharmacology

authors： Winpenny D,Clark M,Cawkill D

更新日期：2016-04-01 00:00:00

abstract：UNLABELLED:Increasing evidence suggests that an overactive endocannabinoid system (ECS) may contribute to the development of diabetes by promoting energy intake and storage, impairing both glucose and lipid metabolism, by exerting pro-apoptotic effects in pancreatic beta cells and by facilitating inflammation in pancre...

journal_title：British journal of pharmacology

authors： Gruden G,Barutta F,Kunos G,Pacher P

更新日期：2016-04-01 00:00:00

abstract：BACKGROUND AND PURPOSE:The Rho GTPase, Rac1, is involved in the pathogenesis of neuropathic pain induced by malformation of dendritic spines in the spinal dorsal horn (sDH) neurons. In the present study, the contribution of spinal Rac1 to peripheral inflammatory pain was studied. EXPERIMENTAL APPROACH:Effects of s.c. ...

journal_title：British journal of pharmacology

authors： Wang Y,Lu YF,Li CL,Sun W,Li Z,Wang RR,He T,Yang F,Yang Y,Wang XL,Guan SM,Chen J

更新日期：2016-03-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Angiotensin II (AngII) induces migration and growth of vascular smooth muscle cell (VSMC), which is responsible for vascular remodelling in some cardiovascular diseases. Ang II also activates a Cl(-) current, but the underlying mechanism is not clear. EXPERIMENTAL APPROACH:The A10 cell line and ...

journal_title：British journal of pharmacology

authors： Ma MM,Lin CX,Liu CZ,Gao M,Sun L,Tang YB,Zhou JG,Wang GL,Guan YY

更新日期：2016-02-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Sepsis is a systemic inflammatory response accompanied by excessive production of inflammatory cytokines and cardiovascular dysfunction. Importantly, macrophage-derived pro-inflammatory agents play a key role in cardiovascular impairment in sepsis. Here we have investigated the effects of trimeta...

journal_title：British journal of pharmacology

authors： Chen J,Lai J,Yang L,Ruan G,Chaugai S,Ning Q,Chen C,Wang DW

更新日期：2016-02-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Inflammasomes are multimeric complexes that facilitate caspase-1-mediated processing of the pro-inflammatory cytokines IL-1β and IL-18. Clinical hypertension is associated with renal inflammation and elevated circulating levels of IL-1β and IL-18. Therefore, we investigated whether hypertension i...

journal_title：British journal of pharmacology

authors： Krishnan SM,Dowling JK,Ling YH,Diep H,Chan CT,Ferens D,Kett MM,Pinar A,Samuel CS,Vinh A,Arumugam TV,Hewitson TD,Kemp-Harper BK,Robertson AA,Cooper MA,Latz E,Mansell A,Sobey CG,Drummond GR

更新日期：2016-02-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Endothelin-1 (ET-1) is increased in patients with sickle cell disease and may contribute to the development of sickle cell nephropathy. The current study was designed to determine whether ET-1 acting via the ETA receptor contributes to renal injury in a mouse model of sickle cell disease. EXPERI...

journal_title：British journal of pharmacology

authors： Heimlich JB,Speed JS,O'Connor PM,Pollock JS,Townes TM,Meiler SE,Kutlar A,Pollock DM

更新日期：2016-01-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Tumour cell migration and adhesion constitute essential features of metastasis. G-protein coupled receptor 55 (GPR55), a lysophospholipid receptor, has been shown to play an important role in carcinogenesis. Here, we investigated the involvement of GPR55 in migration and metastasis of colon cance...

journal_title：British journal of pharmacology

authors： Kargl J,Andersen L,Hasenöhrl C,Feuersinger D,Stančić A,Fauland A,Magnes C,El-Heliebi A,Lax S,Uranitsch S,Haybaeck J,Heinemann A,Schicho R

更新日期：2016-01-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Although botulinum toxin type A (BoNT/A) is approved for chronic migraine treatment, its mechanism of action is still unknown. Dural neurogenic inflammation (DNI) commonly used to investigate migraine pathophysiology can be evoked by trigeminal pain. Here, we investigated the reactivity of crania...

journal_title：British journal of pharmacology

authors： Lacković Z,Filipović B,Matak I,Helyes Z

更新日期：2016-01-01 00:00:00

abstract：BACKGROUND AND PURPOSE:N-arachidonyl dopamine (NADA) has been identified as a putative endocannabinoid, but there is little information about which signalling pathways it activates. The purpose of this study was to identify the signalling pathways activated by NADA in vitro. EXPERIMENTAL APPROACH:Human or rat cannabin...

journal_title：British journal of pharmacology

authors： Redmond WJ,Cawston EE,Grimsey NL,Stuart J,Edington AR,Glass M,Connor M

更新日期：2016-01-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Small conductance calcium-activated potassium (KCa 2.x) channels have a widely accepted canonical function in regulating cellular excitability. In this study, we address a potential non-canonical function of KCa 2.x channels in breast cancer cell survival, using in vitro models. EXPERIMENTAL APP...

journal_title：British journal of pharmacology

authors： Abdulkareem ZA,Gee JM,Cox CD,Wann KT

更新日期：2016-01-01 00:00:00

abstract：:Class A1 scavenger receptors (SR-A1) are membrane glycoproteins that can form homotrimers. This receptor was originally defined by its ability to mediate the accumulation of lipids in macrophages. Subsequent studies reveal that SR-A1 plays critical roles in innate immunity, cell apoptosis and proliferation. This revie...

journal_title：British journal of pharmacology

authors： Ben J,Zhu X,Zhang H,Chen Q

更新日期：2015-12-01 00:00:00

abstract：:The Concise Guide to PHARMACOLOGY 2015/16 provides concise overviews of the key properties of over 1750 human drug targets with their pharmacology, plus links to an open access knowledgebase of drug targets and their ligands (www.guidetopharmacology.org), which provides more detailed views of target and ligand propert...

journal_title：British journal of pharmacology

authors： Alexander SP,Peters JA,Kelly E,Marrion N,Benson HE,Faccenda E,Pawson AJ,Sharman JL,Southan C,Davies JA,CGTP Collaborators.

更新日期：2015-12-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Sphingosine 1-phosphate (S1P), an important inflammatory mediator, has been shown to regulate COX-2 production and promote various cellular responses such as cell migration. Mevastatin, an inhibitor of 3-hydroxy-3-methylglutaryl-CoA reductase (HMG-CoA), effectively inhibits inflammatory responses...

journal_title：British journal of pharmacology

authors： Hsu CK,Lin CC,Hsiao LD,Yang CM

更新日期：2015-11-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Cholecystokinin (CCK) is secreted by intestinal I cells and regulates important metabolic functions. In pancreatic islets, CCK controls beta cell functions primarily through CCK1 receptors, but the signalling pathways downstream of these receptors in pancreatic beta cells are not well defined. E...

journal_title：British journal of pharmacology

authors： Ning SL,Zheng WS,Su J,Liang N,Li H,Zhang DL,Liu CH,Dong JH,Zhang ZK,Cui M,Hu QX,Chen CC,Liu CH,Wang C,Pang Q,Chen YX,Yu X,Sun JP

更新日期：2015-11-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Cannabidiol has been reported to act as an antagonist at cannabinoid CB1 receptors. We hypothesized that cannabidiol would inhibit cannabinoid agonist activity through negative allosteric modulation of CB1 receptors. EXPERIMENTAL APPROACH:Internalization of CB1 receptors, arrestin2 recruitment, ...

journal_title：British journal of pharmacology

authors： Laprairie RB,Bagher AM,Kelly ME,Denovan-Wright EM

更新日期：2015-10-01 00:00:00

abstract：BACKGROUND AND PURPOSE:11β-hydroxysteroid dehydrogenase type I (11β-HSD1), a target for Type 2 diabetes mellitus, converts inactive glucocorticoids into bioactive forms, increasing tissue concentrations. We have compared the pharmacokinetic-pharmacodynamic (PK/PD) relationship of target inhibition after acute and repea...

journal_title：British journal of pharmacology

authors： Morentin Gutierrez P,Gyte A,deSchoolmeester J,Ceuppens P,Swales J,Stacey C,Eriksson JW,Sjöstrand M,Nilsson C,Leighton B

更新日期：2015-10-01 00:00:00

abstract：BACKGROUND AND PURPOSE:An influx drug/proton antiporter of unknown structure has been functionally demonstrated at the blood-brain barrier. This transporter, which handles some psychoactive drugs like diphenhydramine, clonidine, oxycodone, nicotine and cocaine, could represent a new pharmacological target in drug addic...

journal_title：British journal of pharmacology

authors： Chapy H,Goracci L,Vayer P,Parmentier Y,Carrupt PA,Declèves X,Scherrmann JM,Cisternino S,Cruciani G

更新日期：2015-10-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Disruptions of executive function, including attentional deficits, are a hallmark of a number of diseases. ACh in the prefrontal cortex regulates attentive behaviour; however, the role of α7 nicotinic ACh receptor (α7nAChR) in attention is contentious. EXPERIMENTAL APPROACH:In order to probe att...

journal_title：British journal of pharmacology

authors： Kolisnyk B,Al-Onaizi MA,Prado VF,Prado MA

更新日期：2015-10-01 00:00:00

abstract：:Cyclic adenosine monophosphate (cAMP) is one of the second messengers critically involved in the molecular mechanisms underlying memory formation. In the CNS, the availability of cAMP is tightly controlled by phosphodiesterase 4 (PDE4), a family of enzymes that degrades the cyclic nucleotide to inactive AMP. Among the...

journal_title：British journal of pharmacology

authors： Ricciarelli R,Fedele E

更新日期：2015-10-01 00:00:00

abstract：BACKGROUND AND PURPOSE:As the pathogenesis of postoperative ileus (POI) involves inflammation and oxidative stress, comparable to ischaemia/reperfusion injury which can be ameliorated with nitrite, we investigated whether nitrite can protect against POI and explored the mechanisms involved. EXPERIMENTAL APPROACH:We us...

journal_title：British journal of pharmacology

authors： Cosyns SM,Shiva S,Lefebvre RA

更新日期：2015-10-01 00:00:00

abstract：:[This retracts the article on p. 3702 in vol. 171, PMID: 24758388.]. ...

journal_title：British journal of pharmacology

authors：

更新日期：2015-09-01 00:00:00

abstract：BACKGROUND AND PURPOSE:The Munich Wistar Frömter (MWF) rat strain represents an experimental model to study cardiovascular alterations under conditions of progressive albuminuria. The aim of this study was to evaluate the association between genetic predisposition to albuminuria and the development of arterial stiffnes...

journal_title：British journal of pharmacology

authors： Gil-Ortega M,García-Prieto CF,Ruiz-Hurtado G,Steireif C,González MC,Schulz A,Kreutz R,Fernández-Alfonso MS,Arribas S,Somoza B

更新日期：2015-09-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Preclinical cardiovascular safety studies (CVS) have been compared between facilities with respect to their sensitivity to detect drug-induced QTc prolongation (ΔQTc). Little is known about the consistency of quantitative ΔQTc predictions that are relevant for translation to humans. EXPERIMENTAL...

journal_title：British journal of pharmacology

authors： Gotta V,Cools F,van Ammel K,Gallacher DJ,Visser SA,Sannajust F,Morissette P,Danhof M,van der Graaf PH

更新日期：2015-09-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Pulmonary vascular dysfunction is a key event in acute lung injury. We recently demonstrated that PGE2 , via activation of E-prostanoid (EP)4 receptors, strongly enhances microvascular barrier function in vitro. The aim of this study was to investigate the beneficial effects of concomitant EP4 re...

journal_title：British journal of pharmacology

authors： Konya V,Maric J,Jandl K,Luschnig P,Aringer I,Lanz I,Platzer W,Theiler A,Bärnthaler T,Frei R,Marsche G,Marsh LM,Olschewski A,Lippe IT,Heinemann A,Schuligoi R

更新日期：2015-09-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Angiotensin AT1 receptor antagonists induce weight loss; however, the mechanism underlying this phenomenon is unknown. The Mas receptor agonist angiotensin-(1-7) is a metabolite of angiotensin I and of angiotensin II . As an agonist of Mas receptors, angiotensin-(1-7) has beneficial cardiovascula...

journal_title：British journal of pharmacology

authors： Schuchard J,Winkler M,Stölting I,Schuster F,Vogt FM,Barkhausen J,Thorns C,Santos RA,Bader M,Raasch W

更新日期：2015-08-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Lung cancer is one of the leading causes of cancer death worldwide. Despite advances in therapy, conventional therapy is still the main treatment and has a high risk of chemotherapy resistance. Caspase-8 is involved in cell death and is a recognized marker for poor patient prognosis. EXPERIMENTA...

journal_title：British journal of pharmacology

authors： Terlizzi M,Di Crescenzo VG,Perillo G,Galderisi A,Pinto A,Sorrentino R

更新日期：2015-08-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Pelitinib is a potent irreversible EGFR TK inhibitor currently in clinical trials for the treatment of lung cancer. Hyperthermia has been applied concomitantly with chemotherapy and radiotherapy to enhance treatment outcome. In this study, we investigated the ability of the combination of pelitin...

journal_title：British journal of pharmacology

authors： To KK,Poon DC,Wei Y,Wang F,Lin G,Fu L

更新日期：2015-08-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Highly vascularized ovarian carcinoma secretes the putative endocannabinoid and GPR55 agonist, L-α-lysophosphatidylinositol (LPI), into the circulation. We aimed to assess the involvement of this agonist and its receptor in ovarian cancer angiogenesis. EXPERIMENTAL APPROACH:Secretion of LPI by t...

journal_title：British journal of pharmacology

authors： Hofmann NA,Yang J,Trauger SA,Nakayama H,Huang L,Strunk D,Moses MA,Klagsbrun M,Bischoff J,Graier WF

更新日期：2015-08-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Interstitial lung disease accounts for a group of chronic and progressive disorders associated with severe pulmonary vascular remodelling, peripheral vascular rarefaction and fibrosis, thus limiting lung function. We have previously shown that Akt is necessary for myofibroblast differentiation, a...

journal_title：British journal of pharmacology

authors： Abdalla M,Sabbineni H,Prakash R,Ergul A,Fagan SC,Somanath PR

更新日期：2015-08-01 00:00:00

abstract：:The processes underpinning post-developmental neurogenesis in the mammalian brain continue to be defined. Such processes involve the proliferation of neural stem cells and neural progenitor cells (NPCs), neuronal migration, differentiation and integration into a network of functional synapses within the brain. Both in...

journal_title：British journal of pharmacology

authors： Prenderville JA,Kelly ÁM,Downer EJ

更新日期：2015-08-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Increased level of very low-density lipoprotein (VLDL) is a key feature of the metabolic syndrome and is associated with cardiovascular diseases. PPAR-δ agonists play a protective role in lipid metabolism and vascular function. In this study, we aimed to investigate the role of PPAR-δ in the upta...

journal_title：British journal of pharmacology

authors： Fang X,Fang L,Liu A,Wang X,Zhao B,Wang N

更新日期：2015-08-01 00:00:00

abstract：BACKGROUND AND PURPOSE:GABAA receptors mediate neuronal inhibition in the brain. They are the primary targets for benzodiazepines, which are widely used to treat neurological disorders including anxiety, epilepsy and insomnia. The mechanism by which benzodiazepines enhance GABAA receptor activity has been extensively s...

journal_title：British journal of pharmacology

authors： Dixon CL,Harrison NL,Lynch JW,Keramidas A

更新日期：2015-07-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Using an innovative chemical approach, peptide welding technology (PWT), a tetrabranched derivative of nociceptin/orphanin FQ (N/OFQ) has been generated and pharmacologically characterized. Both in vitro and in vivo PWT2-N/OFQ displayed the same pharmacological profile to the natural ligand. It w...

journal_title：British journal of pharmacology

authors： Rizzi A,Sukhtankar DD,Ding H,Hayashida K,Ruzza C,Guerrini R,Calò G,Ko MC

更新日期：2015-07-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Nociceptin/orphanin FQ (N/OFQ) peptide (NOP) receptor agonists display a promising analgesic profile in preclinical studies. However, supraspinal N/OFQ produced hyperalgesia in rodents and such effects have not been addressed in primates. Thus, the aim of this study was to investigate the effects...

journal_title：British journal of pharmacology

authors： Ding H,Hayashida K,Suto T,Sukhtankar DD,Kimura M,Mendenhall V,Ko MC

更新日期：2015-07-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Benzofurans are newly used psychoactive substances, but their pharmacology is unknown. The aim of the present study was to pharmacologically characterize benzofurans in vitro. EXPERIMENTAL APPROACH:We assessed the effects of the benzofurans 5-APB, 5-APDB, 6-APB, 6-APDB, 4-APB, 7-APB, 5-EAPB and ...

journal_title：British journal of pharmacology

authors： Rickli A,Kopf S,Hoener MC,Liechti ME

更新日期：2015-07-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Dehydrodiconiferyl alcohol (DHCA), a lignan compound isolated from Cucurbita moschata, has previously been shown to contain anti-adipogenic and antilipogenic effects on 3T3-L1 cells and mouse embryonic fibroblasts. As some of phytochemicals derived from natural plants show anti-inflammatory or an...

journal_title：British journal of pharmacology

authors： Lee J,Choi J,Kim S

更新日期：2015-07-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Hydrogen sulphide reduces uterine contractility and is of potential interest as a treatment for uterine disorders. The aim of this study was to explore the mechanism of sodium sulphide (Na2 S)-induced relaxation of rat uterus, investigate the importance of redox effects and ion channel-mediated m...

journal_title：British journal of pharmacology

authors： Mijušković A,Kokić AN,Dušić ZO,Slavić M,Spasić MB,Blagojević D

更新日期：2015-07-01 00:00:00