abstract：BACKGROUND AND PURPOSE:Patients with diabetes mellitus are reported to show a raised prevalence of mental disorders, which may be reflected in impaired social interaction. However, the mechanisms underlying such impairment in diabetes are unknown. EXPERIMENTAL APPROACH:The present study investigated whether social int...

journal_title：British journal of pharmacology

authors： Ueda D,Yonemochi N,Kamata T,Shibasaki M,Kamei J,Waddington JL,Ikeda H

更新日期：2021-02-01 00:00:00

abstract：BACKGROUND AND PURPOSE:In cardiac myocytes, cAMP produced by both β1 and β2 -adrenergic receptors (ARs) results in an increase in L-type Ca2+ channel activity and myocyte contraction. However, only cAMP produced by β1 ARs is able to enhance myocyte relaxation through phospholamban-dependent regulation of the sarco/endo...

journal_title：British journal of pharmacology

authors： Rudokas MW,Post JP,Sataray-Rodriguez A,Sherpa RT,Moshal KS,Agarwal SR,Harvey RD

更新日期：2021-01-21 00:00:00

abstract：BACKGROUND AND PURPOSE:Inflammation associated with the tumour microenvironment (TME) plays a critical role in the cancer development, and immunotherapeutic strategies that aim to modulate the immune response in cancer have been crucial. In this study, a Methotrexate-loaded (MTX) poly (lactic-co-glycolic acid)-based (P...

journal_title：British journal of pharmacology

authors： Cavalcante RS,Ishikawa U,Silva ES,Silva Júnior AA,Araújo AA,Cruz LJ,Chan AB,Araújo Júnior RF

更新日期：2021-01-12 00:00:00

abstract：:Recent genome-wide analyses of rare and common sequence variations have brought greater clarity to the genetic architecture of pulmonary arterial hypertension and implicated novel genes in disease development. Transcriptional signatures have been reported in whole lung tissue, pulmonary vascular cells and peripheral c...

journal_title：British journal of pharmacology

authors： Harbaum L,Rhodes CJ,Otero-Núñez P,Wharton J,Wilkins MR

更新日期：2021-01-01 00:00:00

abstract：:Idiopathic pulmonary fibrosis (IPF) is a fatal lung disease where the additional presence of pulmonary hypertension (PH) reduces survival. In particular, the presence of coexistent pulmonary vascular disease in patients with advanced lung parenchymal disease results in worse outcomes than either diagnosis alone. This ...

journal_title：British journal of pharmacology

authors： Rajagopal K,Bryant AJ,Sahay S,Wareing N,Zhou Y,Pandit LM,Karmouty-Quintana H

更新日期：2021-01-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Subset of macrophages within the atheroma plaque displays a high glucose uptake activity. Nevertheless, the molecular mechanisms and the pathophysiological significance of this high glucose need remain unclear. While the role for hypoxia and hypoxia inducible factor 1α has been demonstrated, the ...

journal_title：British journal of pharmacology

authors： Ménégaut L,Jalil A,Pilot T,van Dongen K,Crespy V,Steinmetz E,Pais de Barros JP,Geissler A,Le Goff W,Venteclef N,Lagrost L,Gautier T,Thomas C,Masson D

更新日期：2020-12-29 00:00:00

abstract：BACKGROUND AND PURPOSE:Gut microbiota plays an important role in type 2 diabetes mellitus (T2DM) progression. From our previous work N-(4-Hydroxyphenethyl)-3-mercapto-2-methylpropanamide (HMPA) is a potential T2DM drug. We evaluated the effect of HMPA on gut microbiota and studied the molecular mechanism underlying HMP...

journal_title：British journal of pharmacology

authors： Liu H,Qin Y,Li K,Li M,Yang J,Tao H,Tang Y,Yang L,Chen S,Liu Y,Yang C,Gao W,Sun T

更新日期：2020-12-07 00:00:00

abstract：BACKGROUND AND PURPOSE:Rho kinase (ROCK) activation is involved in neuroinflammatory processes leading to progression of neurodegenerative diseases such as Parkinson's disease. Furthermore, ROCK plays a major role in angiogenesis. Neuroinflammation and angiogenesis are mechanisms involved in developing l-DOPA-induced d...

journal_title：British journal of pharmacology

authors： Lopez-Lopez A,Labandeira CM,Labandeira-Garcia JL,Muñoz A

更新日期：2020-12-01 00:00:00

abstract：:Temperature-sensitive transient receptor potential vanilloid ion channel subtypes 1-4 (thermoTRPV1-thermoTRPV4) play important roles in a wide range of physiological processes, including temperature sensing and body temperature regulation, inflammation, pain, itch, maintenance of skin, bone and hair, along with osmoti...

journal_title：British journal of pharmacology

authors： Zubcevic L

更新日期：2020-11-06 00:00:00

abstract：:Prostate cancer is the second most common malignancy in men and androgen deprivation therapy is the first-line therapy. However, most cases will eventually develop castration-resistant prostate cancer after androgen deprivation therapy treatment. Enzalutamide is a second-generation androgen receptor antagonist approve...

journal_title：British journal of pharmacology

authors： Wang Y,Chen J,Wu Z,Ding W,Gao S,Gao Y,Xu C

更新日期：2020-11-05 00:00:00

abstract：:The complement system plays a major role in threat recognition and in orchestrating responses to microbial intruders and accumulating debris. This immune surveillance is largely driven by lectins that sense carbohydrate signatures on foreign, diseased and healthy host cells and act as complement activators, regulators...

journal_title：British journal of pharmacology

authors： Hevey R,Pouw RB,Harris C,Ricklin D

更新日期：2020-11-03 00:00:00

abstract：:In the last 20 years, the global regulatory frameworks for drug assessment have been managing the challenges posed by using cellular products as new therapeutic tools. Currently, they are defined as "Advanced Therapy Medicinal Products", comprising a large group of cellular types that either alone or in combination wi...

journal_title：British journal of pharmacology

authors： Ciccocioppo R,Comoli P,Astori G,Del Bufalo F,Prapa M,Dominici M,Locatelli F

更新日期：2020-11-03 00:00:00

abstract：BACKGROUND AND PURPOSE:Resurgence in the use of chloroquine as a potential treatment for COVID-19 has seen recent cases of fatal toxicity due to unintentional overdoses. Protocols for the management of poisoning recommend diazepam, although there are uncertainties in its pharmacology and efficacy in this context. The a...

journal_title：British journal of pharmacology

authors： Hughes DA

更新日期：2020-11-01 00:00:00

abstract：:Since December 2019 SARS-Cov-2 was found responsible for the disease COVID-19, which has spread worldwide. No specific therapies/vaccines are yet available for the treatment of COVID-19. Drug repositioning may offer a strategy and a number of drugs have been repurposed, including lopinavir/ritonavir, remdesivir, favip...

journal_title：British journal of pharmacology

authors： Scavone C,Brusco S,Bertini M,Sportiello L,Rafaniello C,Zoccoli A,Berrino L,Racagni G,Rossi F,Capuano A

更新日期：2020-11-01 00:00:00

abstract：:Liver X receptors (LXRs) are members of the nuclear receptor superfamily that are canonically activated by oxidized derivatives of cholesterol. Since the mid-90s, numerous groups have identified LXRs as endocrine receptors that are involved in the regulation of various physiological functions. As a result, when their ...

journal_title：British journal of pharmacology

authors： Buñay J,Fouache A,Trousson A,de Joussineau C,Bouchareb E,Zhu Z,Kocer A,Morel L,Baron S,Lobaccaro JA

更新日期：2020-10-20 00:00:00

abstract：BACKGROUND AND PURPOSE:Tooth eruption is a complicated process regulated by the dental follicles (DF). Our recent study discovered that tooth eruption was inhibited upon injection of bleomycin into DF. However, the mechanisms were unknown. EXPERIMENTAL APPROACH:Human dental follicle cells (hDFCs) were treated by bleom...

journal_title：British journal of pharmacology

authors： Li ZZ,Wang HT,Lee GY,Yang Y,Zou YP,Wang B,Gong CJ,Cai Y,Ren JG,Zhao JH

更新日期：2020-10-17 00:00:00

abstract：BACKGROUND AND PURPOSE:Airway hyperresponsiveness (AHR) is a central abnormality in asthma. IL-5 may modulate AHR in animal models of asthma, but the available data is inconsistent on the impact of targeting IL-5 pathway against AHR. The difference between targeting IL-5 or the IL-5 receptor, α subunit (IL-5Rα) in modu...

journal_title：British journal of pharmacology

authors： Calzetta L,Ritondo BL,Matera MG,Facciolo F,Rogliani P

更新日期：2020-10-01 00:00:00

abstract：:Amyotrophic lateral sclerosis (ALS) is an adult onset disorder characterized by progressive neuromuscular junction (NMJ) dismantling and degeneration of motor neurons leading to atrophy and paralysis of voluntary muscles responsible for motion and breathing. Except for a minority of patients harbouring genetic mutatio...

journal_title：British journal of pharmacology

authors： Manzano R,Toivonen JM,Moreno-Martínez L,de la Torre M,Moreno-García L,López-Royo T,Molina N,Zaragoza P,Calvo AC,Osta R

更新日期：2020-09-28 00:00:00

abstract：:The POZ domain Krüppel-like zinc finger transcription repressor (POK family) contains many important molecules, including RP58, Bcl6 and PLZF. They function as transcription repressors via chromatin remodelling and histone deacetylation and are known to be involved in the development and tumourigenesis of various orga...

journal_title：British journal of pharmacology

authors： Okado H

更新日期：2020-09-22 00:00:00

abstract：:Alcohol-use disorders are chronically relapsing conditions characterized by cycles of use, abstinence and relapse. The ventral pallidum (VP) is a key node in the neural circuits controlling relapse to alcohol seeking and a key target of pharmacotherapies for relapse prevention. There has been a significant increase in...

journal_title：British journal of pharmacology

authors： Prasad AA,McNally GP

更新日期：2020-09-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Concatenation of Cys-loop receptor subunits is a commonly used technique to ensure experimental control of receptor assembly. However, we recently demonstrated that widely used constructs did not lead to the expression of uniform pools of ternary and more complex receptors. The aim was therefore ...

journal_title：British journal of pharmacology

authors： Liao VWY,Kusay AS,Balle T,Ahring PK

更新日期：2020-09-01 00:00:00

abstract：:Despite the importance of members of the GPCR superfamily as targets of a broad range of effective medicines many GPCRs remain poorly characterised. GPR84 is an example. Expression of GPR84 is strongly up regulated in immune cells in a range of pro-inflammatory settings and clinical trials to treat idiopathic pulmonar...

journal_title：British journal of pharmacology

authors： Marsango S,Barki N,Jenkins L,Tobin AB,Milligan G

更新日期：2020-09-01 00:00:00

abstract：:Cholesterol and oxysterol sulfates are important regulators of lipid metabolism, inflammation, cell apoptosis, and cell survival. Among the sulfate-based lipids, cholesterol sulfate (CS) is the most studied lipid both quantitatively and functionally. Despite the importance, very few studies have analysed and linked th...

journal_title：British journal of pharmacology

authors： Sanchez LD,Pontini L,Marinozzi M,Sanchez-Aranguren LC,Reis A,Dias IHK

更新日期：2020-08-06 00:00:00

abstract：BACKGROUND AND PURPOSE:Non-alcoholic fatty liver disease (NAFLD) is considered to be one of the most common chronic liver diseases across worldwide. Astaxanthin (Ax) is a carotenoid, and beneficial effects of astaxanthin, including anti-oxidative, anti-inflammatory, and anti-tumour activity, have been identified. The p...

journal_title：British journal of pharmacology

authors： Wu L,Mo W,Feng J,Li J,Yu Q,Li S,Zhang J,Chen K,Ji J,Dai W,Wu J,Xu X,Mao Y,Guo C

更新日期：2020-08-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Pulmonary arterial hypertension (PAH, type 1 pulmonary hypertension) has a 3-year survival of ~50% and is in need of new, effective therapies. In PAH, remodelling of the pulmonary artery (PA) increases pulmonary vascular resistance and can result in right heart dysfunction and failure. Genetic mu...

journal_title：British journal of pharmacology

authors： Gorr MW,Sriram K,Muthusamy A,Insel PA

更新日期：2020-08-01 00:00:00

abstract：BACKGROUND AND PURPOSE:A fluorinated derivative (2F-MT-45) of the synthetic μ-opioid receptor agonist MT-45 (1-cyclohexyl-4-(1,2-diphenylethyl)piperazine) was recently identified in a seized illicit tablet. While MT-45 is a Class A drug, banned in a number of countries, nothing is known about the pharmacology of 2F-MT-...

journal_title：British journal of pharmacology

authors： Baptista-Hon DT,Smith M,Singleton S,Antonides LH,Nic Daeid N,McKenzie C,Hales TG

更新日期：2020-08-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Anxiety disorder is a common mental health disorder. However, there are few safe and fast-acting anxiolytic drugs available that can treat anxiety disorder. We previously demonstrated that the interaction of neuronal NOS (nNOS) with its carboxy-terminal PDZ ligand (CAPON) is involved in regulatin...

journal_title：British journal of pharmacology

authors： Zhu LJ,Shi HJ,Chang L,Zhang CC,Si M,Li N,Zhu DY

更新日期：2020-08-01 00:00:00

abstract：BACKGROUND AND PURPOSE:2-Hydroxypropyl-β-cyclodextrin (HPCD) is an FDA approved vehicle for drug delivery and an efficient cholesterol-lowering agent. HPCD was proposed to lower tissue cholesterol via multiple mechanisms including those mediated by oxysterols. CYP27A1 and CYP46A1 are the major oxysterol-producing enzym...

journal_title：British journal of pharmacology

authors： El-Darzi N,Mast N,Petrov AM,Pikuleva IA

更新日期：2020-07-22 00:00:00

abstract：:Amyotrophic lateral sclerosis (ALS) is the most common motor neuron neurodegenerative disease. Although it has been classically considered as a disease limited to the motor system, there is increasing evidence for the involvement of other neural and non-neuronal systems. In this review, we will discuss currently exist...

journal_title：British journal of pharmacology

authors： Riancho J,Paz-Fajardo L,López de Munaín A

更新日期：2020-07-16 00:00:00

abstract：BACKGROUND AND PURPOSE:As a hallmark of glioblastoma multiforme (GBM), CD44 plays a crucial role in promoting glioblastoma stem cell (GSC) stemness phenotypes and multiple drug resistance. The therapeutic potential of CD44 has been validated by the clinical successes of several CD44 inhibitors, including antibodies and...

journal_title：British journal of pharmacology

authors： Wang C,Wang Z,Chen C,Fu X,Wang J,Fei X,Yan X,Xu R

更新日期：2020-07-01 00:00:00

abstract：BACKGROUND AND PURPOSE:The synthetic compound efsevin was recently identified to suppress arrhythmogenesis in models of cardiac arrhythmia, making it a promising candidate for antiarrhythmic therapy. Its activity was shown to be dependent on the voltage-dependent anion channel 2 (VDAC2) in the outer mitochondrial membr...

journal_title：British journal of pharmacology

authors： Wilting F,Kopp R,Gurnev PA,Schedel A,Dupper NJ,Kwon O,Nicke A,Gudermann T,Schredelseker J

更新日期：2020-07-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Mast cells are important in allergic reactions. Here, we assessed the anti-allergic effects of the anti-cancer drug tozasertib specifically regarding regulatory effects on mast cell activation. EXPERIMENTAL APPROACH:Tozasertib effects on mast cell degranulation were determined by measuring β-hex...

journal_title：British journal of pharmacology

authors： Zhang LN,Ji K,Sun YT,Hou YB,Chen JJ

更新日期：2020-06-01 00:00:00

abstract：:Following the discovery of the involvement of the ribonucleoprotein TDP-43 in amyotrophic lateral sclerosis (ALS) and frontotemporal lobar degeneration (FTLD), a major research focus has been to develop treatments that can prevent or alleviate these disease conditions. One pharmacological approach has been to use TDP-...

journal_title：British journal of pharmacology

authors： Buratti E

更新日期：2020-05-29 00:00:00

abstract：:Chemotherapy-induced immune-suppression is a common, but potential detrimental, adverse reaction in patients undergoing treatment for cancer and strategies with capacity to boost the immune cell populations are needed. Physical exercise training is a potent regulator of immune cell viability and function and may serve...

journal_title：British journal of pharmacology

authors： Schauer T,Hojman P,Gehl J,Christensen JF

更新日期：2020-05-25 00:00:00

abstract：BACKGROUND AND PURPOSE:The free fatty acid receptor 1 (FFAR1) plays an important role in glucose-stimulated insulin secretion making it an attractive anti-diabetic target. This study characterizes the pharmacological profile of HWL-088 (2-(2-fluoro-4-((2'-methyl-[1,1'- biphenyl]-3-yl)methoxy)phenoxy)acetic acid), a nov...

journal_title：British journal of pharmacology

authors： Chen Y,Ren Q,Zhou Z,Deng L,Hu L,Zhang L,Li Z

更新日期：2020-05-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Pemphigus and pemphigoid diseases are characterized and caused predominantly by IgG autoantibodies targeting structural proteins of the skin. Their current treatment relies on general and prolonged immunosuppression that causes severe adverse events, including death. Hence, novel safe and more ef...

journal_title：British journal of pharmacology

authors： Kasprick A,Hofrichter M,Smith B,Ward P,Bieber K,Shock A,Ludwig RJ,Schmidt E

更新日期：2020-05-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Memantine and marijuana smoking have been found to inhibit tremor in parkinsonian patients, although the observed effects were relatively weak. The tremorolytic effects of combinations of memantine and cannabinoids have not been studied. Here, we have evaluated the anti-tremor activity of memanti...

journal_title：British journal of pharmacology

authors： Ionov ID,Pushinskaya II,Frenkel DD,Gorev NP,Shpilevaya LA

更新日期：2020-04-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Pancreatic islet transplantation is a promising therapeutic approach for Type 1 diabetes. A major prerequisite for the survival of grafted islets is a rapid revascularization after transplantation. Erythropoietin (EPO), the primary regulator of erythropoiesis, has been shown to promote angiogenes...

journal_title：British journal of pharmacology

authors： Menger MM,Nalbach L,Roma LP,Körbel C,Wrublewsky S,Glanemann M,Laschke MW,Menger MD,Ampofo E

更新日期：2020-04-01 00:00:00

abstract：BACKGROUND AND PURPOSE:We previously demonstrated that paracetamol has to be metabolised in the brain by fatty acid amide hydrolase enzyme into AM404 (N-(4-hydroxyphenyl)-5Z,8Z,11Z,14Z-eicosatetraenamide) to activate CB1 receptors and TRPV1 channels, which mediate its analgesic effect. However, the brain mechanisms sup...

journal_title：British journal of pharmacology

authors： Barrière DA,Boumezbeur F,Dalmann R,Cadeddu R,Richard D,Pinguet J,Daulhac L,Sarret P,Whittingstall K,Keller M,Mériaux S,Eschalier A,Mallet C

更新日期：2020-04-01 00:00:00

abstract：:In the mammalian CNS, glutamate is the major excitatory neurotransmitter. Ionotropic glutamate receptors (iGluRs) are responsible for the glutamate-mediated postsynaptic excitation of neurons. Regulation of glutamatergic synapses is critical for higher brain functions including neural communication, memory formation, ...

journal_title：British journal of pharmacology

authors： Hayashi T

更新日期：2020-03-11 00:00:00