abstract：:The Concise Guide to PHARMACOLOGY 2017/18 provides concise overviews of the key properties of nearly 1800 human drug targets with an emphasis on selective pharmacology (where available), plus links to an open access knowledgebase of drug targets and their ligands (www.guidetopharmacology.org), which provides more deta...

journal_title：British journal of pharmacology

authors： Alexander SP,Christopoulos A,Davenport AP,Kelly E,Marrion NV,Peters JA,Faccenda E,Harding SD,Pawson AJ,Sharman JL,Southan C,Davies JA,CGTP Collaborators.

更新日期：2017-12-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Heat-sensitive transient receptor potential vanilloid (TRPV) channels are expressed in various epithelial tissues regulating, among else, barrier functions. Their expression is well established in the distal nephron; however, we have no data about their presence in podocytes. As podocytes are ind...

journal_title：British journal of pharmacology

authors： Ambrus L,Kelemen B,Szabó T,Bíró T,Tóth BI

更新日期：2017-12-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Bortezomib (Velcade®) is a breakthrough treatment for multiple myeloma, significantly improving patient survival. However, its use is limited by painful neuropathy often resulting in dose reduction/cessation of first-line treatment due to lack of treatment. The aim of this study was to characteri...

journal_title：British journal of pharmacology

authors： Duggett NA,Flatters SJL

更新日期：2017-12-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Gain of function mutations in TRPC6 channels can cause autosomal dominant forms of focal segmental glomerulosclerosis (FSGS). Validated inhibitors of TRPC6 channels that are biologically active on FSGS-related TRPC6 mutants are eagerly sought. EXPERIMENTAL APPROACH:We synthesized new TRPC6-inhib...

journal_title：British journal of pharmacology

authors： Urban N,Neuser S,Hentschel A,Köhling S,Rademann J,Schaefer M

更新日期：2017-11-01 00:00:00

abstract：BACKGROUND AND PURPOSE:The development of subtype-selective ligands to inhibit voltage-sensitive sodium channels (VSSCs) has been attempted with the aim of developing therapeutic compounds. Tetrodotoxin (TTX) is a toxin from pufferfish that strongly inhibits VSSCs. Many TTX analogues have been identified from marine an...

journal_title：British journal of pharmacology

authors： Tsukamoto T,Chiba Y,Wakamori M,Yamada T,Tsunogae S,Cho Y,Sakakibara R,Imazu T,Tokoro S,Satake Y,Adachi M,Nishikawa T,Yotsu-Yamashita M,Konoki K

更新日期：2017-11-01 00:00:00

abstract：:Perivascular adipose tissue (PVAT) is now recognized as an active player in vascular homeostasis. The expansion of PVAT in obesity and its possible role in vascular dysfunction have attracted much interest. In terms of the regulation of vascular tone and blood pressure, PVAT has been shown to release vasoactive mediat...

journal_title：British journal of pharmacology

authors： Ramirez JG,O'Malley EJ,Ho WSV

更新日期：2017-10-01 00:00:00

abstract：:Heart disease is a major cause of morbidity and mortality throughout the world. Some cardiovascular conditions can be modulated by lifestyle factors such as increased exercise or a healthier diet, but many require surgical or pharmacological interventions for their management. More targeted and less invasive therapies...

journal_title：British journal of pharmacology

authors： Rietdorf K,MacQueen H

更新日期：2017-10-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Chronic stress impairs GABAA (GABA type A) receptor-mediated inhibition in the hypothalamic paraventricular nucleus (PVN). It is not clear whether GABAB receptor function is also altered. We hypothesize that chronic stress alters GABAB receptor function in PVN corticotrophin-releasing hormone (CR...

journal_title：British journal of pharmacology

authors： Gao Y,Zhou JJ,Zhu Y,Wang L,Kosten TA,Zhang X,Li DP

更新日期：2017-09-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Psychological stress exacerbates symptoms of urinary bladder dysfunction; however, the underlying brain mechanisms are unclear. We have demonstrated that centrally administered bombesin, a stress-related neuropeptide, facilitates the rat micturition reflex. Brain bombesin-like peptides modulate t...

journal_title：British journal of pharmacology

authors： Shimizu T,Shimizu S,Wada N,Takai S,Shimizu N,Higashi Y,Kadekawa K,Majima T,Saito M,Yoshimura N

更新日期：2017-09-01 00:00:00

abstract：BACKGROUND AND PURPOSE:The psychostimulant cocaine induces complex molecular, cellular and behavioural responses as a consequence of inhibiting presynaptic dopamine, noradrenaline and 5-HT transporters. To elucidate 5-HT transporter (SERT)-specific contributions to cocaine action, we evaluated cocaine effects in the SE...

journal_title：British journal of pharmacology

authors： Simmler LD,Anacker AMJ,Levin MH,Vaswani NM,Gresch PJ,Nackenoff AG,Anastasio NC,Stutz SJ,Cunningham KA,Wang J,Zhang B,Henry LK,Stewart A,Veenstra-VanderWeele J,Blakely RD

更新日期：2017-08-01 00:00:00

abstract：BACKGROUND AND PURPOSE:The ω-3 polyunsaturated fatty acids (PUFAs) mediate protective effects on several metabolic disorders. However, the functions of their metabolites in the early stage of nonalcoholic fatty liver disease (NAFLD) are largely unknown. EXPERIMENTAL APPROACH:Mice were fed a control diet, high-fat diet...

journal_title：British journal of pharmacology

authors： Wang C,Liu W,Yao L,Zhang X,Zhang X,Ye C,Jiang H,He J,Zhu Y,Ai D

更新日期：2017-07-01 00:00:00

abstract：:Multiple sclerosis (MS) is a chronic inflammatory disease of the CNS, and one of the most common causes of disability in young adults. Over the last decade, new disease-modifying therapies have emerged, including monoclonal antibodies (mAbs) that provide highly targeted therapies with greater efficacy than platform th...

journal_title：British journal of pharmacology

authors： Nguyen AL,Gresle M,Marshall T,Butzkueven H,Field J

更新日期：2017-07-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Fatty acid amide hydrolase (FAAH) inhibitors are postulated to possess anti-hypertensive potential, because their acute injection decreases BP in spontaneously hypertensive rats (SHR), partly through normalization of cardiac contractile function. Here, we examined whether the potential hypotensiv...

journal_title：British journal of pharmacology

authors： Pędzińska-Betiuk A,Weresa J,Toczek M,Baranowska-Kuczko M,Kasacka I,Harasim-Symbor E,Malinowska B

更新日期：2017-07-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Cloxyquin (5-cloroquinolin-8-ol) has been described as an activator of TRESK (K2P 18.1, TWIK-related spinal cord K+ channel) background potassium channel. We have examined the specificity of the drug by testing several K2P channels. We have investigated the mechanism of cloxyquin-mediated TRESK a...

journal_title：British journal of pharmacology

authors： Lengyel M,Dobolyi A,Czirják G,Enyedi P

更新日期：2017-07-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Chromosomal instability is not only a hallmark of cancer but also an attractive therapeutic target. A diverse set of mitotic kinases maintains chromosomal stability. One of these is monopolar spindle 1 (Mps1, also known as TTK), which is essential for chromosome alignment and for the spindle asse...

journal_title：British journal of pharmacology

authors： Choi M,Min YH,Pyo J,Lee CW,Jang CY,Kim JE

更新日期：2017-06-01 00:00:00

abstract：:The NADPH oxidase (NOX) family of enzymes produces ROS as their sole function and is becoming recognized as key modulators of signal transduction pathways with a physiological role under acute stress and a pathological role after excessive activation under chronic stress. The seven isoforms differ in their regulation,...

journal_title：British journal of pharmacology

authors： Teixeira G,Szyndralewiez C,Molango S,Carnesecchi S,Heitz F,Wiesel P,Wood JM

更新日期：2017-06-01 00:00:00

abstract：:Tannins are a heterogeneous group of high MW, water-soluble, polyphenolic compounds, naturally present in cereals, leguminous seeds and, predominantly, in many fruits and vegetables, where they provide protection against a wide range of biotic and abiotic stressors. Tannins exert several pharmacological effects, inclu...

journal_title：British journal of pharmacology

authors： Smeriglio A,Barreca D,Bellocco E,Trombetta D

更新日期：2017-06-01 00:00:00

abstract：:Phytoestrogens are plant-derived dietary compounds with structural similarity to 17-β-oestradiol (E2), the primary female sex hormone. This structural similarity to E2 enables phytoestrogens to cause (anti)oestrogenic effects by binding to the oestrogen receptors. The aim of the present review is to present a state-of...

journal_title：British journal of pharmacology

authors： Rietjens IMCM,Louisse J,Beekmann K

更新日期：2017-06-01 00:00:00

abstract：BACKGROUND AND PURPOSE:A body of evidence suggests activation of metabotropic glutamate 2/3 (mGlu2/3 ) receptors would be an effective analgesic in chronic pain conditions. Thus, the analgesic properties of a novel mGlu2/3 receptor agonist prodrug were investigated. EXPERIMENTAL APPROACH:After oral absorption, the pro...

journal_title：British journal of pharmacology

authors： Johnson MP,Muhlhauser MA,Nisenbaum ES,Simmons RM,Forster BM,Knopp KL,Yang L,Morrow D,Li DL,Kennedy JD,Swanson S,Monn JA

更新日期：2017-05-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Toll-like receptor 4 (TLR4) plays a key role in the induction of inflammatory responses both in peripheral organs and the CNS. Curcumin exerts anti-inflammatory functions by interfering with LPS-induced dimerization of TLR4-myeloid differentiation protein-2 (MD-2) complex and suppressing pro-infl...

journal_title：British journal of pharmacology

authors： Zusso M,Mercanti G,Belluti F,Di Martino RMC,Pagetta A,Marinelli C,Brun P,Ragazzi E,Lo R,Stifani S,Giusti P,Moro S

更新日期：2017-05-01 00:00:00

abstract：LINKED ARTICLES:This article is part of a themed section on Recent Progress in the Understanding of Relaxin Family Peptides and their Receptors. To view the other articles in this section visit http://onlinelibrary.wiley.com/doi/10.1111/bph.v174.10/issuetoc. ...

journal_title：British journal of pharmacology

authors： Summers RJ

更新日期：2017-05-01 00:00:00

abstract：:Relaxin is a small heterodimeric peptide hormone of the insulin/relaxin superfamily produced mainly in female and male reproductive organs. It has potent antifibrotic, vasodilatory and angiogenic effects and regulates the normal function of various physiological systems. Preclinical studies and recent clinical trials ...

journal_title：British journal of pharmacology

authors： Agoulnik AI,Agoulnik IU,Hu X,Marugan J

更新日期：2017-05-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Iridoid glycosides containing the double bond scaffold of cyclopentapyran are reversible and orthosteric agonists of glucagon-like peptide-1 (GLP-1) receptors and exert anti-nociceptive and neuroprotective actions. Morroniside, derived from the medicinal herb Cornus officinalis, is an atypical se...

journal_title：British journal of pharmacology

authors： Xu M,Wu HY,Liu H,Gong N,Wang YR,Wang YX

更新日期：2017-04-01 00:00:00

abstract：:Pulmonary hypertension (PH) is defined by elevated mean pulmonary artery pressure following the pathological remodelling of small pulmonary arteries. An increase in right ventricular (RV) afterload results in RV hypertrophy and RV failure. The pathophysiology of PH, and RV remodelling in particular, is not well unders...

journal_title：British journal of pharmacology

authors： Maarman GJ,Schulz R,Sliwa K,Schermuly RT,Lecour S

更新日期：2017-04-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Prefrontal dopamine release by the combined activation of 5-HT1A and sigma-1 (σ1 ) receptors is enhanced by the GABAA receptor antagonist picrotoxin in mice. Here, we examined whether this neurochemical event was accompanied by behavioural changes. EXPERIMENTAL APPROACH:Male mice were treated wi...

journal_title：British journal of pharmacology

authors： Hasebe S,Ago Y,Watabe Y,Oka S,Hiramatsu N,Tanaka T,Umehara C,Hashimoto H,Takuma K,Matsuda T

更新日期：2017-02-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Human lung fibroblasts (HLF) express high levels of the LPA1 receptor, a GPCR that responds to the endogenous lipid mediator, lysophosphatidic acid (LPA). Several molecular species or analogues of LPA exist and have been detected in biological fluids such as serum and plasma. The most widely expr...

journal_title：British journal of pharmacology

authors： Sattikar A,Dowling MR,Rosethorne EM

更新日期：2017-02-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Peptides from venomous animals have long been important for understanding pain mechanisms and for the discovery of pain treatments. Here, we hypothesized that Phα1β, a peptide from the venom of the armed spider Phoneutria nigriventer, produces analgesia by blocking the TRPA1 channel. EXPERIMENTA...

journal_title：British journal of pharmacology

authors： Tonello R,Fusi C,Materazzi S,Marone IM,De Logu F,Benemei S,Gonçalves MC,Coppi E,Castro-Junior CJ,Gomez MV,Geppetti P,Ferreira J,Nassini R

更新日期：2017-01-01 00:00:00

abstract：:In moderate-to-severe asthma, adding an inhaled long-acting β2 -adenoceptor agonist (LABA) to an inhaled corticosteroid (ICS) provides better disease control than simply increasing the dose of ICS. Acting on the glucocorticoid receptor (GR, gene NR3C1), ICSs promote anti-inflammatory/anti-asthma gene expression. In vi...

journal_title：British journal of pharmacology

authors： Newton R,Giembycz MA

更新日期：2016-12-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Oxaliplatin is a platinum-based chemotherapeutic drug used as a first-line therapy for colorectal cancer. However, its use is associated with severe gastrointestinal side-effects resulting in dose limitations and/or cessation of treatment. In this study, we tested whether oxidative stress, caused...

journal_title：British journal of pharmacology

authors： McQuade RM,Carbone SE,Stojanovska V,Rahman A,Gwynne RM,Robinson AM,Goodman CA,Bornstein JC,Nurgali K

更新日期：2016-12-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Pancreatic cancer is a solid tumour that is often fatal. Hence, there is an urgent need to identify new drug targets for this disease. Highly proliferating cancer cells have an increased demand for nutrients and, therefore, need to up-regulate selective amino acid transporters. Here, we investiga...

journal_title：British journal of pharmacology

authors： Coothankandaswamy V,Cao S,Xu Y,Prasad PD,Singh PK,Reynolds CP,Yang S,Ogura J,Ganapathy V,Bhutia YD

更新日期：2016-12-01 00:00:00

abstract：:The endoplasmic reticulum (ER) is an important intracellular membranous organelle. Previous studies have demonstrated that the ER is responsible for protein folding and trafficking, lipid synthesis and the maintenance of calcium homeostasis. Interestingly, the morphology and structure of the ER were recently found to ...

journal_title：British journal of pharmacology

authors： Hu W,Ma Z,Di S,Jiang S,Li Y,Fan C,Yang Y,Wang D

更新日期：2016-12-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Adenosine A2A receptor stimulation promotes the synthesis of collagen type I and type III (Col1 and Col3), mediators of fibrosis and scarring. The A2A receptor modulates collagen balance via cAMP/PKA/p38-MAPK/Akt pathways. Wnt signalling is important in fibrosis and the cAMP and Wnt pathways conv...

journal_title：British journal of pharmacology

authors： Shaikh G,Zhang J,Perez-Aso M,Mediero A,Cronstein B

更新日期：2016-12-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Imiquimod is an immunomodulator approved for the treatment of basal cell carcinoma and has adverse side effects, including taste disturbances. Paracrine transmission, representing cell-cell communication within taste buds, has the potential to shape the final signals that taste buds transmit to t...

journal_title：British journal of pharmacology

authors： Huang AY,Wu SY

更新日期：2016-11-01 00:00:00

abstract：:Ligands targeting GPCRs can be categorized according to their intrinsic efficacy to trigger a specific, receptor-mediated response. A ligand endowed with the same level of efficacy as the endogenous agonist can be classified as a full agonist, whereas a compound that displays greater efficacy, that is, higher receptor...

journal_title：British journal of pharmacology

authors： Schrage R,De Min A,Hochheiser K,Kostenis E,Mohr K

更新日期：2016-10-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Agmatine, a putative neurotransmitter, plays a vital role in learning and memory. Although it is considered an endogenous ligand of imidazoline receptors, agmatine exhibits high affinity for α-adrenoceptors, NOS and NMDA receptors. These substrates within the locus coeruleus (LC) are critically i...

journal_title：British journal of pharmacology

authors： Shelkar GP,Gakare SG,Chakraborty S,Dravid SM,Ugale RR

更新日期：2016-09-01 00:00:00

abstract：:Melatonin receptors are seven transmembrane-spanning proteins belonging to the GPCR superfamily. In mammals, two melatonin receptor subtypes exist - MT1 and MT2 - encoded by the MTNR1A and MTNR1B genes respectively. The current review provides an update on melatonin receptors by the corresponding subcommittee of the I...

journal_title：British journal of pharmacology

authors： Jockers R,Delagrange P,Dubocovich ML,Markus RP,Renault N,Tosini G,Cecon E,Zlotos DP

更新日期：2016-09-01 00:00:00

abstract：UNLABELLED:Alzheimer's disease (AD) is accepted nowadays as a complex neurodegenerative disorder with multifaceted cerebral pathologies, including extracellular deposition of amyloid β peptide-containing plaques, intracellular neurofibrillary tangles, progressive loss of cholinergic neurons, metal dyshomeostasis, mitoc...

journal_title：British journal of pharmacology

authors： Weinreb O,Amit T,Bar-Am O,Youdim MB

更新日期：2016-07-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Previous findings suggest that the growth and differentiation factor midkine (Mdk) is a negative regulator of osteoblast activity and bone formation, thereby raising the possibility that a specific Mdk antagonist might improve bone formation during fracture healing. EXPERIMENTAL APPROACH:In the ...

journal_title：British journal of pharmacology

authors： Haffner-Luntzer M,Heilmann A,Rapp AE,Roessler R,Schinke T,Amling M,Ignatius A,Liedert A

更新日期：2016-07-01 00:00:00

abstract：BACKGROUND AND PURPOSE:5-HT (serotonin) regulates various physiological functions, both directly and via enteric neurons. The present study investigated the role of endogenous 5-HT and 5-HT3 receptors in the pathogenic mechanisms involved in colonic inflammation, especially in relation to substance P (SP) and the neuro...

journal_title：British journal of pharmacology

authors： Utsumi D,Matsumoto K,Amagase K,Horie S,Kato S

更新日期：2016-06-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Avoiding danger and finding food are closely related behaviours that are essential for surviving in a natural environment. Growing evidence supports an important role of gut-brain peptides in modulating energy homeostasis and emotional-affective behaviour. For instance, postprandial release of pa...

journal_title：British journal of pharmacology

authors： Verma D,Hörmer B,Bellmann-Sickert K,Thieme V,Beck-Sickinger AG,Herzog H,Sperk G,Tasan RO

更新日期：2016-06-01 00:00:00