Mechanisms of enzalutamide resistance in castration-resistant prostate cancer and therapeutic strategies to overcome it.

abstract：:1 Pinacidil relaxes blood vessels through opening the K(ATP) channels with a resultant membrane hyperpolarization and inhibition of Ca(2+) influx. The aim of this study was to examine the mechanisms thereby pinacidil induces K(+) channel-independent relaxation in isolated endothelium-denuded rat mesenteric artery. 2 P...

journal_title：British journal of pharmacology

authors： Tsang SY,Yao X,Wong CM,Au CL,Chen ZY,Huang Y

更新日期：2003-02-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Recent studies suggest that the effects of cyclooxygenase-2 (COX-2) inhibition are mediated by cannabinoid receptor activation. However, some non-steroidal anti-inflammatory drugs inhibit the enzyme fatty acid amide hydrolase, which regulates levels of some endocannabinoids. Whether COX-2 directl...

journal_title：British journal of pharmacology

authors： Staniaszek LE,Norris LM,Kendall DA,Barrett DA,Chapman V

更新日期：2010-06-01 00:00:00

abstract：:1. We have examined the mechanisms of local oedema formation in the passive cutaneous anaphylactic (PCA) reaction in the rabbit. 2. IgE-containing antiserum was injected i.d. and allowed to sensitize skin sites for periods up to 240 h. Antigen (bovine gamma globulin) was injected i.d. or i.v. and local oedema formatio...

journal_title：British journal of pharmacology

authors： Hellewell PG,Jose PJ,Williams TJ

更新日期：1992-12-01 00:00:00

abstract：:1. Glycine responses were studied under voltage clamp in Xenopus oocytes injected with cDNA encoding mammalian glycine receptor subunits and in rat medullary neurones. Bath application of glycine gave strychnine-sensitive currents which reversed close to the expected equilibrium potentials for chloride ions. The peak ...

journal_title：British journal of pharmacology

authors： Downie DL,Hall AC,Lieb WR,Franks NP

更新日期：1996-06-01 00:00:00

abstract：:1. The present study characterized highly effective agonists from different classes of compounds for the neuronal octopamine receptor (OAR3) of the migratory locust (Locusta migratoria L.). Biogenic amines and phenyliminoimidazolidines (PIIs) were employed for the study of structure-activity relationships. 2. The high...

journal_title：British journal of pharmacology

authors： Roeder T

更新日期：1995-01-01 00:00:00

abstract：:1. The effects of 3 competitive N-methyl-D-aspartate (NMDA) receptor antagonists, LY274614, LY233536 and LY235723, on the micturition reflex and external urethral sphincter EMG activity, were examined either under isovolumetric conditions or during continuous filling cystometry in urethane-anaesthetized (1.2 g kg-1, s...

journal_title：British journal of pharmacology

authors： Yoshiyama M,Roppolo JR,Thor KB,de Groat WC

更新日期：1993-09-01 00:00:00

abstract：:1. Various neurotransmitters in the brain regulate gastric acid secretion. Previously, we reported that the central injection of kappa-opioid receptor agonists stimulated this secretion in rats. Although the existence of kappa(1)-kappa(3)-opioid receptor subtypes has been proposed, the character is not defined. We inv...

journal_title：British journal of pharmacology

authors： Minowa S,Ishihara S,Tsuchiya S,Horie S,Watanabe K,Murayama T

更新日期：2003-03-01 00:00:00

abstract：:1. The action of the non-steroidal anti-inflammatory drugs (NSAID), sodium salicylate, aspirin, phenylbutazone and indomethacin was investigated on the migration of human polymorphonuclear cells (PMNs) and lymphocytes, using the system of migration of leucocytes from glass capillary tubes. 2. All NSAID produced a dose...

journal_title：British journal of pharmacology

authors： Brown KA,Collins AJ

更新日期：1978-11-01 00:00:00

abstract：:The dependence of neurotransmitter secretion on external calcium ions during development of opiate tolerance in the mouse vas deferens was studied. The writhing response of mice to an i.p. injection of acetylcholine was inhibited by morphine. Reversal of this antinociceptive effect of morphine during chronic treatment...

journal_title：British journal of pharmacology

authors： Einstein R,Lavidis NA

更新日期：1984-12-01 00:00:00

abstract：:1. We have studied whether a nucleotide receptor mediates the effects of extracellular ATP and UTP on phosphatidylcholine metabolism in rat cultured glomerular mesangial cells. 2. ATP and UTP stimulated a biphasic 1,2-diacylglycerol (DAG) formation in [3H]-arachidonic acid-labelled mesangial cells. In contrast, in cel...

journal_title：British journal of pharmacology

authors： Pfeilschifter J,Merriweather C

更新日期：1993-10-01 00:00:00

abstract：:1. Intracellular recordings were made from neurones in vitro in the rat substantia nigra zona compacta and ventral tegmental area; the neurones had the characteristic properties of dopamine-containing cells, and fired action potentials spontaneously. 2. Cocaine (1-10 microM) inhibited spontaneous firing, hyperpolarize...

journal_title：British journal of pharmacology

authors： Lacey MG,Mercuri NB,North RA

更新日期：1990-04-01 00:00:00

abstract：BACKGROUND AND PURPOSE:8-Nitroguanosine 3',5'-cyclic monophosphate (8-nitro-cGMP), formed nitric oxide (NO)-dependently, is a physiological second messenger, yet little is known about its role in the pathophysiology of vascular diseases. To study the pharmacological activity of 8-nitro-cGMP in diabetic mice, we compare...

journal_title：British journal of pharmacology

authors： Tokutomi Y,Kataoka K,Yamamoto E,Nakamura T,Fukuda M,Nako H,Toyama K,Dong YF,Ahmed KA,Sawa T,Akaike T,Kim-Mitsuyama S

更新日期：2011-04-01 00:00:00

abstract：BACKGROUND AND PURPOSE:AZ11645373 and N-{2-methyl-5-[(1R, 5S)-9-oxa-3,7-diazabicyclo[3.3.1]non-3-ylcarbonyl]phenyl}-2-tricyclo[3.3.1.13,7]dec-1-ylacetamide hydrochloride (compound-22) are recently described P2X(7) receptor antagonists. In this study we have further characterized these compounds to determine their mecha...

journal_title：British journal of pharmacology

authors： Michel AD,Ng SW,Roman S,Clay WC,Dean DK,Walter DS

更新日期：2009-04-01 00:00:00

abstract：:The N6-2'-O-dibutyryl derivative of adenosine 3',5'-monophosphate (db cyclic AMP) and related compounds have been micro-injected into the preoptic/anterior hypothalamic nuclei (PO/AH) of the unanaesthetized, restrained rabbit and the effects on deep body temperature observed. Db cyclic AMP (100-400 micrograms) produce...

journal_title：British journal of pharmacology

authors： Dascombe MJ

更新日期：1984-04-01 00:00:00

abstract：:Multidrug transporters play a dual role in haematopoietic cells, mediating the efflux of xenobiotics and regulating cell migration. For several reasons including the lack of specific antibodies, reports of multidrug transporter distribution on lymphocytes conflict. Murine B cells have been reported to completely lack ...

journal_title：British journal of pharmacology

authors： Elliott JI,Raguz S,Higgins CF

更新日期：2004-12-01 00:00:00

abstract：:The effects of the angiotensin-converting-enzyme inhibitor (ACEI) ramiprilat, the angiotensin II type 1 receptor antagonist (AT(1)A) candesartan, and the combination of both drugs on infarct size (IS) resulting from regional myocardial ischaemia were studied in pigs. Both ACEI and AT(1)A reduce myocardial IS by a brad...

journal_title：British journal of pharmacology

authors： Weidenbach R,Schulz R,Gres P,Behrends M,Post H,Heusch G

更新日期：2000-09-01 00:00:00

abstract：:1. Chronic treatment with a combined ETA/ETB endothelin receptor antagonist has been shown to reduce blood pressure in experimental rat models of hypertension in which endothelin-1 gene overexpression occurs in the walls of blood vessels, particularly small, resistance-sized arteries, but not in those genetic or exper...

journal_title：British journal of pharmacology

authors： Schiffrin EL,Turgeon A,Deng LY

更新日期：1997-07-01 00:00:00

abstract：:1. The effects of ryanodine on changes in cytoplasmic Ca2+ level ([Ca2+]i) and muscle tension induced by maximum concentrations of phenylephrine (Phe; 1 microM), prostaglandin F2 alpha (PGF2 alpha, 10 microM), caffeine (Caf, 30 mM) and isoprenaline (Iso, 1 microM) were examined in rat aortic strips using fura-2. 2. In...

journal_title：British journal of pharmacology

authors： Hisayama T,Takayanagi I,Okamoto Y

更新日期：1990-08-01 00:00:00

abstract：:1. The pharmacokinetic interaction between phenylbutazone and sulphadoxine has been studied in live sheep.2. Intravenous injection of phenylbutazone causes a rapid fall in the concentration of total sulphadoxine together with a simultaneous rise in the concentration of free sulphadoxine in plasma. Both processes are c...

journal_title：British journal of pharmacology

authors： McQueen EG,Wardell WM

更新日期：1971-10-01 00:00:00

abstract：:1 The actions of 5-methoxytryptamine (5-MeOT), N,N-dimethyltryptamine (DMT), 5-hydroxy-N,N-dimethyltryptamine (bufotenine, 5-HODMT) and 5-methoxy-N,N-dimethyltryptamine (5-MeODMT), and their interactions with 5-hydroxytryptamine (5-HT), acetylcholine, (-)-noradrenaline, and glutamate were studied by microiontophoresis...

journal_title：British journal of pharmacology

authors： Bradley PB,Briggs I

更新日期：1974-03-01 00:00:00

abstract：:1. A quaternary derivative of (-)-hyoscyamine, phenthonium (Phen) induced a concentration-dependent increase in the rate of spontaneous quantal release of acetylcholine (ACh) at the mammalian neuromuscular junction, as shown by intracellular recordings of the miniature endplate potentials (m.e.p.ps) in rat diaphragm m...

journal_title：British journal of pharmacology

authors： Fann ML,Souccar C,Lapa AJ

更新日期：1990-07-01 00:00:00

abstract：:In the clinic, low efficacy positive GABAA modulators might be preferred to high efficacy positive modulators insofar as low efficacy modulators might have comparatively less abuse and dependence liability. Drug discrimination was used to examine the behavioral effects of L-838,417 and bretazenil, two low efficacy pos...

journal_title：British journal of pharmacology

authors： McMahon LR,France CP

更新日期：2006-02-01 00:00:00

abstract：:Previous studies have provided evidence for the presence on B cell membrane of adenosine receptors (P1-purinoceptors) of the A1-subtype which inhibit insulin secretion. In this work we have investigated the implication of a guanosine triphosphate (GTP) binding protein (G protein) in the A1 purinoceptor-induced inhibit...

journal_title：British journal of pharmacology

authors： Hillaire-Buys D,Gross R,Loubatières-Mariani MM,Ribes G

更新日期：1989-01-01 00:00:00

abstract：:1. We have investigated the effects of a standardised mixture of hydroxyethylrutosides (HR, Venoruton), a mixture of five of its main components (M) and each of the five components separately (7-mono-HR, 7,4'-di-HR, 7,3',4'-tri-HR, 5,7,3',4'-tetra-HR and 7,3'4'-tri HQ) upon the permeability of single perfused capillar...

journal_title：British journal of pharmacology

authors： Kendall S,Towart R,Michel CC

更新日期：1993-09-01 00:00:00

abstract：:1. Electroconvulsive treatment (ECT) of rabbits produced ocular inflammation consisting of conjunctival hyperaemia, miosis and protein extravasation into the aqueous humour, reflected by the so-called aqueous flare response (AFR): the maximal reduction in pupil size was 3.8 +/- 0.1 mm (s.e. of mean, n = 16) while the ...

journal_title：British journal of pharmacology

authors： Wang ZY,Waldeck K,Grundemar L,Håkanson R

更新日期：1997-04-01 00:00:00

abstract：:1. This study was undertaken to evaluate in vivo the influence of amiodarone on the effects of triiodothyronine (T3) in brown adipose tissue (BAT) which are independent of thyroid hormone synthesis and of the conversion of thyroxine (T4) to T3. Thyroidectomized rats were given a replacement dose of T3 (0.5 mg kg(-1) p...

journal_title：British journal of pharmacology

authors： Adli H,Bazin R,Perret GY

更新日期：1999-03-01 00:00:00

abstract：:1. Diadenosine tetraphosphate (Ap4A) a dinucleotide stored and released from rat brain synaptic terminals presents two types of affinity binding sites in synaptosomes. When [3H]-Ap4A was used for binding studies a Kd value of 0.10 +/- 0.014 nM and a Bmax value of 16.6 +/- 1.2 fmol mg-1 protein were obtained for the hi...

journal_title：British journal of pharmacology

authors： Pintor J,Díaz-Rey MA,Miras-Portugal MT

更新日期：1993-04-01 00:00:00

abstract：:1. We studied the effects of intracerebroventricular (i.c.v.) administration of prostanoid EP receptor ligands on vagally stimulated gastric acid secretion in rats anaesthetized with urethane. 2. Administration of misoprostol (EP3/EP2 receptor agonist) and sulprostone (EP3/EP1 receptor agonist) reduced vagally mediate...

journal_title：British journal of pharmacology

authors： Yokotani K,Okuma Y,Osumi Y

更新日期：1996-02-01 00:00:00

abstract：:1. Capsaicin, the irritant principle of hot peppers, is a vanilloid agonist known to activate the transient receptor potential channel vanilloid subfamily member 1 (VR1), recently reported to be involved in neurodegeneration. The present study investigated the role of VR1 in a model of global cerebral ischemia in gerb...

journal_title：British journal of pharmacology

authors： Pegorini S,Braida D,Verzoni C,Guerini-Rocco C,Consalez GG,Croci L,Sala M

更新日期：2005-03-01 00:00:00

abstract：:1. A number of superoxide dismutase (SOD) mimetics were examined both biochemically for their ability to inhibit the superoxide-catalyzed reduction of cytochrome c and nitro blue tetrazolium, and functionally for their ability to mimic authentic Cu/Zn SOD in restoring nitrergic neurotransmission in bovine retractor pe...

journal_title：British journal of pharmacology

authors： Mok JS,Paisley K,Martin W

更新日期：1998-05-01 00:00:00