Mechanistic analysis of the function of agonists and allosteric modulators: reconciling two-state and operational models.

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：:The binding of a series of amide derivatives of methotrexate to Lactobacillus casei dihydrofolate reductase has been studied by inhibition constant measurements and by 1H n.m.r. spectroscopy. Amide modification of the alpha-carboxylate of methotrexate was found to prevent interaction of the gamma-carboxylate with the ...

journal_title：British journal of pharmacology

authors： Antonjuk DJ,Birdsall B,Cheung HT,Clore GM,Feeney J,Gronenborn A,Roberts GC,Tran TQ

更新日期：1984-02-01 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：:1. Peroxisome proliferator-activated receptor alpha (PPARalpha) regulates the expression of the key genes involved in lipid metabolism following activation of this receptor by various ligands. Ginseng, a highly valuable medicine in oriental societies, is also reported to modulate lipid metabolism, although the mechani...

journal_title：British journal of pharmacology

authors： Yoon M,Lee H,Jeong S,Kim JJ,Nicol CJ,Nam KW,Kim M,Cho BG,Oh GT

更新日期：2003-04-01 00:00:00

abstract：:1. Carrier mediated uptake (uptake-1) transport of norepinephrine (NE) plays a key role in the regulation of sympathetic neurotransmission. Recent investigations indicate that nitric oxide (NO) may modulate uptake-1 activity, possibly in a cyclic GMP independent manner. 2. Carrier mediated transport of [(3)H-NE] and [...

journal_title：British journal of pharmacology

authors： Kaye DM,Gruskin S,Smith AI,Esler MD

更新日期：2000-07-01 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:Necroptosis is a form of programmed, caspase-independent, cell death, mediated by receptor-interacting protein kinases, RIPK1 and RIPK3, and the mixed lineage kinase domain-like (MLKL). Necroptosis contributes to the pathophysiology of various inflammatory, infectious, and degenerative diseases. ...

journal_title：British journal of pharmacology

authors： Chen X,Zhuang C,Ren Y,Zhang H,Qin X,Hu L,Fu J,Miao Z,Chai Y,Liu ZG,Zhang H,Cai Z,Wang HY

更新日期：2019-06-01 00:00:00

abstract：:1. U937 cells are a continuous line of human cells of committed monocytic origin which serve as a useful model for studying human monocytic function. The present study investigated the effect of platelet-activating factor (Paf) on intracellular free calcium ion concentration ([Ca2+]i) in U937 cells using the calcium f...

journal_title：British journal of pharmacology

authors： Ward SG,Westwick J

更新日期：1988-04-01 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：:1. The effects of prolonged cold storage on the mechanical and membranal responses to stimulation of alpha- and beta-adrenoceptors by phenylephrine and isoprenaline, respectively, were studied on the guinea-pig taenia caecum.2. Cold storage invariably caused a decrease in the resting membrane potential, and this effec...

journal_title：British journal of pharmacology

authors： Fukuda H,Shibata S

更新日期：1972-11-01 00:00:00

abstract：:1 The beta-adrenoceptor agonist isoprenaline normally causes only a small and inconsistent increase in the membrane potential of cells in guinea-pig liver slices, in contrast to the large hyperpolarizations seen with alpha-agonists. However, after a selective alpha-adrenoceptor agonist has been applied, the response t...

journal_title：British journal of pharmacology

authors： Jenkinson DH,Koller K

更新日期：1977-01-01 00:00:00

abstract：:1. S 16257 is a new bradycardic agent. Its electropharmacological profile has been compared to that of the known bradycardic compound UL-FS 49 (Zatebradine). Intracellular recordings of action potentials (APs) were performed with conventional glass microelectrodes. 2. In the rabbit isolated sino-atrial node (SAN) tiss...

journal_title：British journal of pharmacology

authors： Thollon C,Cambarrat C,Vian J,Prost JF,Peglion JL,Vilaine JP

更新日期：1994-05-01 00:00:00

abstract：:1. Sodium metabisulphite (MBS) can induce bronchoconstriction in patients with asthma. We investigated the effects of MBS aerosol on bronchial blood velocity (Vbr) and pulmonary resistance in intubated conscious sheep. 2. Bronchial blood velocity was measured by implanting a 20 MHz ultrasonic Doppler flow probe on the...

journal_title：British journal of pharmacology

authors： Nichol GM,Parsons GH,Chung KF

更新日期：1994-03-01 00:00:00

abstract：:1. The actions on the taenia of 4-(m-chlorophenylcarbamoyloxy)-2-butynyl-trimethylammonium chloride (McN-A-343), N-benzyl-3-pyrrolidyl acetate methobromide (AHR-602), tetramethylammonium (TMA) and choline phenyl ether have been examined and compared with the actions of acetylcholine, nicotine and 1,1-dimethyl-4-phenyl...

journal_title：British journal of pharmacology

authors： Hobbiger F,Mitchelson F,Rand MJ

更新日期：1969-05-01 00:00:00

abstract：:1 Anthopleurin-B (AP-B, greater than 3 x 10(-9) M), a newly isolated polypeptide from sea anemone (Anthopleura xanthogrammica), caused powerful rhythmic contractions in the guinea-pig isolated vas deferens. The other polypeptides anthopleurin-A from A. xanthogrammica and anthopleurin-C from A. elegantissima, elicited ...

journal_title：British journal of pharmacology

authors： Norton TR,Ohizumi Y,Shibata S

更新日期：1981-09-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Voltage-gated sodium channels (VGSCs) are assembled from two classes of subunits, a pore-bearing α-subunit (NaV 1) and one or two accessory β-subunits (NaV βs). Neurons in mammals can express one or more of seven isoforms of NaV 1 and one or more of four isoforms of NaV β. The peptide μ-conotoxin...

journal_title：British journal of pharmacology

authors： Zhang MM,Wilson MJ,Azam L,Gajewiak J,Rivier JE,Bulaj G,Olivera BM,Yoshikami D

更新日期：2013-04-01 00:00:00

abstract：:1. This study was undertaken to investigate whether, after a brief exposure of guinea-pig isolated ileum and rabbit jejunum to bremazocine, a kappa-opioid agonist also possessing antagonist activity at mu-opioid receptors, the addition of opioid antagonists produced withdrawal contractures. Our aim was to verify in th...

journal_title：British journal of pharmacology

authors： Valeri P,Morrone LA,Romanelli L,Amico MC

更新日期：1995-03-01 00:00:00

abstract：:Burimamide, an H(2)-receptor blocking agent, has been shown capable of blocking the uptake and metabolism of [(14)C]-histamine, both in the guinea-pig isolated atrium and in murine neoplastic mast cells. This occurs even at concentrations far below the dose range capable of blocking the positive chronotropic effect of...

journal_title：British journal of pharmacology

authors： Fantozzi R,Mannaioni PF,Moroni F

更新日期：1973-10-01 00:00:00

abstract：:1 In spontaneously active Purkinje fibres of young cows the dose-response curves of the action of isoprenaline upon different electrophysiological parameters were measured.2 The increase in slope of diastolic depolarization could roughly be described by a one-for-one binding curve with a half maximum effect near 10(-8...

journal_title：British journal of pharmacology

authors： Grabowski W,Lüttgau HC,Schulze JJ

更新日期：1978-07-01 00:00:00

abstract：:1. Sabcomeline (SB-202026, 0.03 mg kg(-1), p.o.), a potent and functionally selective M1 receptor partial agonist, caused a statistically significant improvement in the performance of a visual object discrimination task by marmosets. No such improvement was seen after RS86 (0.1 mg kg(-1), p.o.). 2. Initial learning, w...

journal_title：British journal of pharmacology

authors： Harries MH,Samson NA,Cilia J,Hunter AJ

更新日期：1998-05-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Voltage-operated sodium channels constitute major target sites for local anaesthetic-like action. The clinical use of local anaesthetics is still limited by severe side effects, in particular, arrhythmias and convulsions. These side effects render the search for new local anaesthetics a matter of...

journal_title：British journal of pharmacology

authors： Haeseler G,Karst M,Foadi N,Gudehus S,Roeder A,Hecker H,Dengler R,Leuwer M

更新日期：2008-09-01 00:00:00

abstract：:1. By use of a number of analogues of adenine nucleotides, the structure-activity relationships of the human platelet receptor for adenosine 5'-diphosphate (ADP) mediating increases in intracellular calcium were investigated, and compared with the known structure-activity relationships for induction by ADP of platelet...

journal_title：British journal of pharmacology

authors： Hall DA,Hourani SM

更新日期：1993-03-01 00:00:00

abstract：:1. 5-Hydroxytryptamine (5-HT) transport has been investigated in rat blood platelets poisoned with dinitrophenol-sodium fluoride or ouabain.2. The inhibition of transport produced by different concentrations of the metabolic inhibitors has been correlated with changes in the internal Na(+) and K(+) concentrations of t...

journal_title：British journal of pharmacology

authors： Sneddon JM

更新日期：1971-12-01 00:00:00

abstract：BACKGROUND AND PURPOSE:While the slow delayed rectifier K(+) current (I(Ks)) is known to be enhanced by the stimulation of β-adrenoceptors in several mammalian species, phosphorylation-dependent regulation of the rapid delayed rectifier K(+) current (I(Kr)) is controversial. EXPERIMENTAL APPROACH:In the present study,...

journal_title：British journal of pharmacology

authors： Harmati G,Bányász T,Bárándi L,Szentandrássy N,Horváth B,Szabó G,Szentmiklósi JA,Szénási G,Nánási PP,Magyar J

更新日期：2011-02-01 00:00:00

abstract：:1 alpha-Monofluoromethyldopa (MFMD, RMI 71963), a potent and selective enzyme-activated irreversible inhibitor of aromatic L-amino acid decarboxylase produces a substantial and long-lasting decrease in the catecholamine content of mouse brain, heart and kidney. 2 Single doses of MFMD reduce the 5-hydroxytryptamine con...

journal_title：British journal of pharmacology

authors： Bey P,Jung MJ,Koch-Weser J,Palfreyman MG,Sjoerdsma A,Wagner J,Zraïka M

更新日期：1980-12-01 00:00:00

abstract：:1. An investigation was carried out to determine if the sympathoinhibition caused by urapidil is due to activation of 5-HT1A receptors by investigating whether it could be reversed by the non-selective 5-HT1A receptor antagonist spiperone. To control for the possibility of functional antagonism by spiperone, the abili...

journal_title：British journal of pharmacology

authors： Ramage AG

更新日期：1991-04-01 00:00:00

abstract：:1. Rabbit isolated irides were loaded with [3H]-noradrenaline and superfused with Tyrode solution. The inhibition by the muscarinic agonists (+/-)-methacholine and pilocarpine of the [3H]-noradrenaline overflow into the superfusate evoked by field stimulation (pulses of 1 ms duration, 75 mA) was measured as an index o...

journal_title：British journal of pharmacology

authors： Bognar IT,Pallas S,Fuder H,Muscholl E

更新日期：1988-07-01 00:00:00

abstract：:1 The effect of methylene, thio, and imido substituted analogues of adenosine 5'-triphosphate (ATP) on surfactant phospholipid secretion and calcium mobilization in rat isolated alveolar Type II cells was studied. 2 ATP was the most potent secretagogue of adenine nucleotides studied. The rank order of agonist potency ...

journal_title：British journal of pharmacology

authors： Rice WR,Singleton FM

更新日期：1987-08-01 00:00:00

abstract：:The concentration of intracellular free Ca2+ ( [Ca2+]i) in human blood platelets was measured by use of the fluorescent probe quin-2. 5-Hydroxytryptamine (5-HT) caused a rapid increase of [Ca2+]i in the presence or absence of Ca2+ in the medium. The [Ca2+]i-rise was less marked in the absence of Ca2+ and could be anta...

journal_title：British journal of pharmacology

authors： Erne P,Pletscher A

更新日期：1985-02-01 00:00:00

abstract：:1 A range of opioid receptor agonists were tested for activity in five antinociceptive models: the acetylcholine-induced abdominal constriction, tail-flick and hot plate tests in the mouse and the paw pressure test in the rat and guinea-pig. 2 Agonists acting preferentially at the kappa-opioid receptor were significan...

journal_title：British journal of pharmacology

authors： Hayes AG,Sheehan MJ,Tyers MB

更新日期：1987-08-01 00:00:00