Phenylglycine derivatives as antagonists of group III metabotropic glutamate receptors expressed on neonatal rat primary afferent terminals.

abstract：:1. Although extensively investigated, the extent of differences between receptors mediating negative inotropic and chronotropic responses is still unclear. In the present study atrial and intestinal muscarinic receptors were identified by [3H]-N-methyl-scopolamine ([3H]-NMS) binding and the affinities of some presumab...

journal_title：British journal of pharmacology

authors： Brunner F

更新日期：1989-06-01 00:00:00

abstract：:In recent years there has been a growing recognition of the influence of sex on brain structure and function, and in relation, on the susceptibility, prevalence and response to treatment of psychiatric disorders. Most theories and descriptions of the effects of sex on the brain are dominated by an analogy to the curre...

journal_title：British journal of pharmacology

authors： Joel D,Yankelevitch-Yahav R

更新日期：2014-10-01 00:00:00

abstract：:1. Endothelial cell damage in glomeruli and kidney arterioles appears to play a pivotal role in glomerular inflammatory diseases. Glomerular endothelial cells, a specialized microvascular cell type involved in the regulation of glomerular ultrafiltration, die by apoptosis in response to tumour necrosis factor-alpha (T...

journal_title：British journal of pharmacology

authors： Messmer UK,Winkel G,Briner VA,Pfeilschifter J

更新日期：1999-08-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Hydrogen sulphide (H2 S) is an endogenous gaseous signalling molecule with putative functions in gastrointestinal motility regulation. Characterization of H2 S effects on colonic motility is crucial to establish its potential use as therapeutic agent in the treatment of colonic disorders. EXPERI...

journal_title：British journal of pharmacology

authors： Gil V,Parsons S,Gallego D,Huizinga J,Jimenez M

更新日期：2013-05-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Xaliproden (SR57746A) is a 5-HT(1A) receptor agonist and neurotrophic agent that reduces oxaliplatin-mediated neuropathy in clinical trials. The present study investigated its profile on in vitro transduction, neurochemical responses and acute nociceptive pain tests in rats. EXPERIMENTAL APPROAC...

journal_title：British journal of pharmacology

authors： Martel JC,Assié MB,Bardin L,Depoortère R,Cussac D,Newman-Tancredi A

更新日期：2009-09-01 00:00:00

abstract：:The present study examined the ability of the selective imidazoline I(2)-site ligands 2-(-2-benzofuranyl)-2-imidazoline (2-BFI) and 2-[4,5-dihydroimidaz-2-yl]-quinoline (BU224) and selected monoamine oxidase (MAO) inhibitors to evoke locomotor activity in rats bearing a lesion of the nigrostriatal pathway. Male Spragu...

journal_title：British journal of pharmacology

authors： Macinnes N,Duty S

更新日期：2004-12-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Ajmaline is a widely used antiarrhythmic drug. Its action on voltage-gated ion channels in skeletal muscle is not well documented and we have here elucidated its effects on Na(+) and K(+) channels. EXPERIMENTAL APPROACH:Sodium (I(Na)) and potassium (I(K)) currents in amphibian skeletal muscle fi...

journal_title：British journal of pharmacology

authors： Friedrich O,V Wegner F,Wink M,Fink RH

更新日期：2007-05-01 00:00:00

abstract：:1. The oral sedative potencies of cannabis herb, crude ethanolic and petroleum-ether fractions, were assayed against delta'-trans-tetrahydrocannabinol (THC) administered orally to mice, by measuring spontaneous motor activity over 30 min periods, at selected times, up to 6 h. 2. The THC contents of the extracts were d...

journal_title：British journal of pharmacology

authors： Pickens JT

更新日期：1981-04-01 00:00:00

abstract：BACKGROUND AND PURPOSE:In humans and non-human primates, the 7TM receptor GPR17 exists in two isoforms differing only by the length of the N-terminus. Of these, only the short isoform has previously been characterized. Hence, we investigated gene expression and ligand-binding profiles of both splice variants and furthe...

journal_title：British journal of pharmacology

authors： Benned-Jensen T,Rosenkilde MM

更新日期：2010-03-01 00:00:00

abstract：:Some 865 genes in man encode G-protein-coupled receptors (GPCRs). The heterotrimeric guanine nucleotide-binding proteins (G-proteins) function to transduce signals from this vast panoply of receptors to effector systems including ion channels and enzymes that alter the rate of production, release or degradation of int...

journal_title：British journal of pharmacology

authors： Milligan G,Kostenis E

更新日期：2006-01-01 00:00:00

abstract：:1. Vanadium compounds can mimic actions of insulin through alternative signalling pathways. The effects of three organic vanadium compounds were studied in non-ketotic, streptozotocin-diabetic rats: vanadyl acetylacetonate (VAc), vanadyl 3-ethylacetylacetonate (VEt), and bis(maltolato)oxovanadium (VM). A simple inorga...

journal_title：British journal of pharmacology

authors： Reul BA,Amin SS,Buchet JP,Ongemba LN,Crans DC,Brichard SM

更新日期：1999-01-01 00:00:00

abstract：:1. Action potentials from guinea-pig single ventricular myocytes were interrupted by application of a 300 ms voltage clamp to -40 mV in order to evoke the Ca-activated tail current which is thought to be carried by Na:Ca exchange. Stimulation frequency was 1 Hz and temperature 36 degrees C. 2. The actions of ryanodine...

journal_title：British journal of pharmacology

authors： White E,Terrar DA

更新日期：1990-10-01 00:00:00

abstract：:1. The action of substance P (SP) on the release of gamma-aminobutyric acid (GABA) and acetylcholine (ACh) and on contraction were studied in strips of the guinea-pig urinary bladder. Substance P induced a dose-dependent contraction of strips of guinea-pig urinary bladder (EC50 = 1.2 x 10(-9) M). This contraction was ...

journal_title：British journal of pharmacology

authors： Shirakawa J,Nakanishi T,Taniyama K,Kamidono S,Tanaka C

更新日期：1989-10-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Depolarization-induced suppression of inhibition (DSI) and excitation (DSE) are two forms of cannabinoid CB(1) receptor-mediated inhibition of synaptic transmission, whose durations are regulated by endocannabinoid (eCB) degradation. We have recently shown that in cultured hippocampal neurons mon...

journal_title：British journal of pharmacology

authors： Straiker A,Wager-Miller J,Hu SS,Blankman JL,Cravatt BF,Mackie K

更新日期：2011-11-01 00:00:00

abstract：:1. We examined the gastric mucosal blood flow (GMBF) and ulcerogenic responses following barrier disruption induced by sodium taurocholate (TC) in diabetic rats and investigated the role of capsaicin-sensitive sensory neurons in these responses. 2. Animals were injected streptozotocin (STZ: 70 mg kg(-1), i.p.) and use...

journal_title：British journal of pharmacology

authors： Tashima K,Korolkiewicz R,Kubomi M,Takeuchi K

更新日期：1998-08-01 00:00:00

abstract：:AM-36 is a novel neuroprotective agent incorporating both antioxidant and Na(+) channel blocking actions. In cerebral ischaemia, loss of cellular ion homeostasis due to Na(+) channel activation, together with increased reactive oxygen species (ROS) production, are thought to contribute to neuronal death. Since neurona...

journal_title：British journal of pharmacology

authors： Callaway JK,Beart PM,Jarrott B,Giardina SF

更新日期：2001-04-01 00:00:00

abstract：:1. General anaesthetics disrupt normal cell receptivity and responsiveness while sparing vital respiratory processes. Ultimate elucidation of the molecular basis of general anaesthesia presumes the identification of one or more subcellular components with appropriate sensitivity to the entire array of anaesthetics. 2....

journal_title：British journal of pharmacology

authors： LaBella FS,Chen QM,Stein D,Queen G

更新日期：1997-03-01 00:00:00

abstract：BACKGROUND AND PURPOSE:The sarcoplasmic reticulum Ca²⁺-ATPase (SERCA) plays a role in thermogenesis. The exogenous compound capsaicin increased SERCA-mediated ATP hydrolysis not coupled to Ca²⁺ transport. Here, we have sought to identify endogenous compounds that may function as SERCA uncoupling agents. EXPERIMENTAL A...

journal_title：British journal of pharmacology

authors： Mahmmoud YA,Gaster M

更新日期：2012-08-01 00:00:00

abstract：:1. The effect of in vivo desensitization to leukotriene B4 (LTB4) on eosinophil infiltration in response to recombinant C5a was examined in guinea-pig skin. 2. LTB4 (10-300 ng) and C5a (1-10 micrograms) caused a dose-dependent increase in the levels of eosinophil peroxidase activity (a measure of eosinophil infiltrati...

journal_title：British journal of pharmacology

authors： Pettipher ER,Salter ED,Showell HJ

更新日期：1994-09-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Parabens are commonly added in pharmaceutical, cosmetic and food products because of their wide antibacterial properties, low toxicity, inertness and chemical stability, although the molecular mechanism of their antibacterial effect is not fully understood. Some agonists of the transient receptor...

journal_title：British journal of pharmacology

authors： Fujita F,Moriyama T,Higashi T,Shima A,Tominaga M

更新日期：2007-05-01 00:00:00

abstract：:1. The pharmacokinetics of cyclophosphamide were investigated in cancer patients. The data can be characterized by a two-compartment open model. The half life of the elimination phase of the drug ranged between 3 and 11 hours.2. Extensive tubular reabsorption of the drug resulted in the excretion of only a small perce...

journal_title：British journal of pharmacology

authors： Cohen JL,Jao JY,Jusko WJ

更新日期：1971-11-01 00:00:00

abstract：:1. The alpha 2-adrenoceptor agonists TL99 (2-(N N-dimethyl)amino-6,7-dihydroxy-1,2,3,4-tetrahydronaphthalene) and UK14304 (5-bromo-6-[2-imidazoline-2-yl-aminol]-quinoxaline), in concentrations that are less than 1% of those producing vasoconstriction, enhance vasoconstrictor responses to noradrenaline and phenylephrin...

journal_title：British journal of pharmacology

authors： Xiao XH,Rand MJ

更新日期：1989-11-01 00:00:00

abstract：:1. We measured the effects of agonists and antagonists of metabotropic glutamate (mGlu) receptors (types 1 and 5) on NMDA-induced depolarization of mouse cortical wedges in order to characterize the mGlu receptor type responsible for modulating NMDA responses. We also characterized a number of mGlu receptor agents by ...

journal_title：British journal of pharmacology

authors： Attucci S,Carlà V,Mannaioni G,Moroni F

更新日期：2001-02-01 00:00:00

abstract：:1. We previously demonstrated that cyclopiazonic acid (CPA), an inhibitor of Ca(2+)-ATPase in the sarcoplasmic reticulum, induced rhythmic relaxations of active tension in the endothelium-denuded small arteries of the mesentery and the ear of the rabbit, but that this agent failed to induce rhythmic responses in the e...

journal_title：British journal of pharmacology

authors： Omote M,Mizusawa H

更新日期：1996-05-01 00:00:00

abstract：:Association between staphylococcal infection and pathogenesis of upper airways disease has been reported. This study aimed to investigate the mechanisms underlying the rat pulmonary inflammation induced by airway exposure to staphylococcal enterotoxin A (SEA). SEA (0.3-10 ng trachea(-1)) caused dose-dependent neutroph...

journal_title：British journal of pharmacology

authors： Desouza IA,Franco-Penteado CF,Camargo EA,Lima CS,Teixeira SA,Muscará MN,De Nucci G,Antunes E

更新日期：2005-11-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Inhaled corticosteroids (ICS) are the cornerstone of asthma pharmacotherapy and, acting via the glucocorticoid receptor (GR), reduce inflammatory gene expression. While this is often attributed to a direct inhibitory effect of the GR on inflammatory gene transcription, corticosteroids also induce...

journal_title：British journal of pharmacology

authors： Kelly MM,King EM,Rider CF,Gwozd C,Holden NS,Eddleston J,Zuraw B,Leigh R,O'Byrne PM,Newton R

更新日期：2012-03-01 00:00:00

abstract：:1. The effects of the beta 1- and beta 2-adrenoceptor selective antagonists, CGP 20712A and ICI 118551 respectively, on responses to isoprenaline-induced relaxation of rat distal colon were investigated in order to determine the contributions of these subtypes to relaxation. In addition, the properties of ICI D7114, a...

journal_title：British journal of pharmacology

authors： MacDonald A,Lamont M

更新日期：1993-12-01 00:00:00

abstract：:1. The concentration-response curves for rate of mucus output, labelled-glycoprotein output and smooth muscle contraction in response to methacholine, phenylephrine and salbutamol were determined in the ferret trachea in vitro. 2. The potencies of methacholine and phenylephrine are both in order: smooth muscle contrac...

journal_title：British journal of pharmacology

authors： Kyle H,Widdicombe JG,Wilffert B

更新日期：1988-06-01 00:00:00

abstract：:The role of putative neurotransmitters of the central nervous system in the central gastric antisecretory effect of prostaglandin E2 (PGE2) was investigated in pylorus-ligated rats. Pretreatment of the rats with an intracerebroventricular (i.c.v.) injection of 6-hydroxydopamine (6-OHDA) prevented the antisecretory eff...

journal_title：British journal of pharmacology

authors： Puurunen J

更新日期：1985-05-01 00:00:00

abstract：:The inhibitory effects of three prostanoid analogues, EP 045, EP 092 and pinane thromboxane A2 (PTA2), on the aggregation of human platelets in vitro have been investigated. In diluted platelet-rich plasma (PRP), EP 045 (20 microM) and EP 092 (1 microM) completely inhibited irreversible aggregation responses to thromb...

journal_title：British journal of pharmacology

authors： Armstrong RA,Jones RL,Peesapati V,Will SG,Wilson NH

更新日期：1985-03-01 00:00:00