Conversion of sodium channels to a form sensitive to cyclic AMP by component(s) from red cells.

abstract：:1. The binding of 1,3-[3H]-dipropyl-8-cyclopentylxanthine ([3H]-DPCPX), an antagonist radioligand selective for adenosine A1 receptors, was studied in rat duodenum, colon muscularis mucosae and longitudinal muscle, urinary bladder and vasa deferentia. 2. [3H]-DPCPX bound with high affinity to a single site in all memb...

journal_title：British journal of pharmacology

authors： Peachey JA,Hourani SM,Kitchen I

更新日期：1994-12-01 00:00:00

abstract：:The selective monoamine oxidase (MAO) inhibitors clorgyline, selegiline and AGN 1135 did not cause a change in responses of the cat nictitating membrane to preganglionic sympathetic nerve stimulation at 5 Hz. Both selective MAO-A and MAO-B inhibitors markedly potentiated nictitating membrane contractions in response t...

journal_title：British journal of pharmacology

authors： Finberg JP,Youdim MB

更新日期：1985-06-01 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：BACKGROUND AND PURPOSE:While selective, bitter tasting, TAS2R agonists can relax agonist-contracted airway smooth muscle (ASM), their mechanism of action is unclear. However, ASM contraction is regulated by Ca²⁺ signalling and Ca²⁺ sensitivity. We have therefore investigated how the TAS2R10 agonists chloroquine, quinin...

journal_title：British journal of pharmacology

authors： Tan X,Sanderson MJ

更新日期：2014-02-01 00:00:00

abstract：:1 In order to address mechanistic differences between arterial vessel types, we have compared the vasorelaxant actions of anandamide in resistance (G3) and conduit (G0) mesenteric arteries. 2 Anandamide produced concentration-dependent relaxations of pre-constricted G3 arteries with a maximal response that was signifi...

journal_title：British journal of pharmacology

authors： O'Sullivan SE,Kendall DA,Randall MD

更新日期：2004-06-01 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：:1. Pithed rats were respired at a fixed rate of 54 cycles min-1 and with a ventilation volume of either 20 (control) or 10 ml kg-1. In these two preparations, the dose-response relationships for the systemic blood pressure responses to endothelin-1, administered i.v., were examined. Also, cardiac output, its distribut...

journal_title：British journal of pharmacology

authors： MacLean MR,Randall MD,Hiley CR

更新日期：1989-11-01 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：:1. The pharmacological characteristics of cloned mammalian alpha 1A/D-, alpha 1B- and alpha 1C-adrenoceptor subtypes expressed in rat 1 fibroblasts were determined in comparison to the binding and functional properties of these subtypes in rat tissues. 2. Analysis of [3H]-prazosin binding to membrane homogenates from ...

journal_title：British journal of pharmacology

authors： Kenny BA,Naylor AM,Greengrass PM,Russell MJ,Friend SJ,Read AM,Wyllie MG

更新日期：1994-04-01 00:00:00

abstract：BACKGROUND AND PURPOSE:mTOR inhibitors are currently used as immunosuppressants in transplanted patients and as promising anti-cancer agents. However, new-onset diabetes is a frequent complication occurring in patients treated with mTOR inhibitors such as rapamycin (Sirolimus). Here, we investigated the mechanisms asso...

journal_title：British journal of pharmacology

authors： Deblon N,Bourgoin L,Veyrat-Durebex C,Peyrou M,Vinciguerra M,Caillon A,Maeder C,Fournier M,Montet X,Rohner-Jeanrenaud F,Foti M

更新日期：2012-04-01 00:00:00

abstract：:1. Nicotine can activate primary afferent nociceptors, one result of which is to increase neurogenic plasma extravasation. In this study we have demonstrated a novel proinflammatory effect of sub-nanomolar nicotine, mediated by peripheral action at sensory neurons. This action is normally masked by adrenal medulla-der...

journal_title：British journal of pharmacology

authors： Miao FJ,Benowitz NL,Levine JD

更新日期：2001-05-01 00:00:00

abstract：:1. Muscarinic receptors on endothelial cells of bovine thoracic aorta were characterized by binding assays in which (-)-[3H]-N-methyl quinuclidinyl benzilate ([3H]-NMeQNB) was used as radioligand. 2. Binding of [3H]-NMeQNB to crude membranes of freshly isolated endothelial cells was atropine-displaceable and of high a...

journal_title：British journal of pharmacology

authors： Brunner F,Kukovetz WR

更新日期：1991-02-01 00:00:00

abstract：:1. Lowering of the extracellular Mg(2+)-concentration induces various patterns of epileptiform activity in combined rat entorhinal cortex-hippocampal brain slices. After a prolonged period of exposure to Mg(2+)-free medium seizure-like events in the entorhinal cortex change to a state of late recurrent discharges whic...

journal_title：British journal of pharmacology

authors： Pfeiffer M,Draguhn A,Meierkord H,Heinemann U

更新日期：1996-10-01 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：BACKGROUND AND PURPOSE:Emesis is a multi-system reflex, which is usually investigated using in vivo models. The aim of the study is to compare the response induced by emetic compounds across species and investigate whether dogs, ferrets and rats are all similarly predictive of humans. EXPERIMENTAL APPROACH:A systemati...

journal_title：British journal of pharmacology

authors： du Sert NP,Holmes AM,Wallis R,Andrews PL

更新日期：2012-03-01 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：:1. Adenosine 5'-triphosphate (ATP) is known to augment cardiac contractile activity and cause an increase in intracellular Ca(2+) concentration ([Ca(2+)](i)) in isolated cardiomyocytes. However, no information regarding the ATP-mediated signal transduction in the myocardium in congestive heart failure (CHF) is availab...

journal_title：British journal of pharmacology

authors： Saini HK,Shao Q,Musat S,Takeda N,Tappia PS,Dhalla NS

更新日期：2005-01-01 00:00:00

abstract：:1. The effect on membrane currents of infection of mouse neuroblastoma NA cells with rabies virus was studied by using the whole-cell patch clamp technique. 2. Three types of membrane currents, namely voltage-dependent Na+ current (I(Na)), delayed rectifier K+ current (I(K-DR)) and inward rectifier K+ current (I(K-IR)...

journal_title：British journal of pharmacology

authors： Iwata M,Komori S,Unno T,Minamoto N,Ohashi H

更新日期：1999-04-01 00:00:00

abstract：:1. Under normal experimental conditions, the rabbit isolated distal saphenous artery appears to contain a homogeneous population of postjunctional alpha 1-adrenoceptors. Prazosin competitively antagonized responses to noradrenaline (NA) with a pA2 value of 8.6, while a relatively high concentration of rauwolscine (1 m...

journal_title：British journal of pharmacology

authors： Dunn WR,McGrath JC,Wilson VG

更新日期：1991-06-01 00:00:00

abstract：:1. Vascular endothelial and smooth muscle cells generate nitric oxide (NO) via different nitric oxide synthase (NOS) isozymes. Activation of the endothelial constitutive NOS (ecNOS) contributes to the maintenance of cardiovascular homeostasis, whereas expression of the endotoxin- and cytokine-inducible pathway (iNOS) ...

journal_title：British journal of pharmacology

authors： Marczin N,Jilling T,Papapetropoulos A,Go C,Catravas JD

更新日期：1996-07-01 00:00:00

abstract：:1. Studies in rats suggest that PACAP modulates gastric acid secretion through the release of both histamine and somatostatin. 2. We characterized the effects of exogenous PACAP on gastric acid secretion in urethane-anesthetized mice implanted with a gastric cannula and in conscious 2-h pylorus ligated mice, and deter...

journal_title：British journal of pharmacology

authors： Piqueras L,Taché Y,Martínez V

更新日期：2004-05-01 00:00:00

abstract：:Rats were placed on either a low sodium intake (low sodium diet 0.025% dry weight, tap water for drinking) or a high sodium intake (normal sodium diet 0.45% dry weight, 0.9% saline for drinking) for 10 days. The pressor-response curve to angiotensin II in rats previously on a high sodium intake was shifted to the left...

journal_title：British journal of pharmacology

authors： Jones DR,Penner SB,Smyth DD

更新日期：1985-12-01 00:00:00

abstract：:We investigated the rate of penetration into and the intra-relationship between the serum, cerebrospinal fluid (CSF) and regional brain extracellular fluid (bECF) compartments following systemic administration of lamotrigine in rat. The serum pharmacokinetics were biphasic with an initial distribution phase, (half-lif...

journal_title：British journal of pharmacology

authors： Walker MC,Tong X,Perry H,Alavijeh MS,Patsalos PN

更新日期：2000-05-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Inhibition of the T- and B-cell interaction through the CD40/CD40 ligand (L) axis is a favourable approach for inflammatory disease treatment. Clinical studies of anti-CD40L molecules in autoimmune diseases have met challenges because of thromboembolic events and adverse haemostasis. VIB4920 (for...

journal_title：British journal of pharmacology

authors： Nicholson SM,Casey KA,Gunsior M,Drabic S,Iverson W,Cook H,Scott S,O'Day T,Karanth S,Dixit R,Ryan PC

更新日期：2020-03-01 00:00:00

abstract：:The modulatory effects of protein kinase C (PKC) on the activation of cytosolic phospholipase A2 (cPLA2) and adenylyl cyclase (AC) have recently been described. Since the signalling cascades associated with these events play critical roles in various functions of macrophages, we set out to investigate the crosstalk be...

journal_title：British journal of pharmacology

authors： Lin WW,Chen BC

更新日期：1998-12-01 00:00:00

abstract：:1. Angiotensin-converting enzyme (ACE) inhibitors exert their cardiovascular effects not only by preventing the formation of angiotensin II (AII), but also by promoting the accumulation of bradykinin in or at the vessel wall. In addition, certain ACE inhibitors have been shown to augment the vasodilator response to br...

journal_title：British journal of pharmacology

authors： Hecker M,Blaukat A,Bara AT,Müller-Esterl W,Busse R

更新日期：1997-08-01 00:00:00

abstract：:1 To evaluate the role of prostaglandin I(2) (PGI(2)) in allergic inflammation, allergic responses in the airway, skin and T cells were studied in mice lacking the receptor for PGI(2) (the prostanoid IP receptor) through gene disruption. 2 Three inhalations of antigen caused an increase in plasma extravasation, leukoc...

journal_title：British journal of pharmacology

authors： Takahashi Y,Tokuoka S,Masuda T,Hirano Y,Nagao M,Tanaka H,Inagaki N,Narumiya S,Nagai H

更新日期：2002-10-01 00:00:00

abstract：:1. ATP, UTP, ADP and ADP-beta-S elicited Ca2+ -signals in cultured aortic smooth muscle cells although ADP, UDP and ADP-beta-S gave approximately 40% of the maximal response seen with ATP and UTP. Adenosine, AMP or alpha,beta-methylene-ATP had no effect. These responses were attributed to P2Y2/4 and P2Y1 receptors, wh...

journal_title：British journal of pharmacology

authors： Pediani JD,McGrath JC,Wilson SM

更新日期：1999-04-01 00:00:00

abstract：:1. The effects of acetylcholine (ACh) on membrane potential, relaxation and cyclic GMP levels were compared to the NO donor L-nitrosocysteine (Cys-NO) in segments of guinea-pig coronary artery. 2. ACh and Cys-NO produced concentration-dependent relaxations of muscles contracted with the H1 receptor agonist, 2-(2-amino...

journal_title：British journal of pharmacology

authors： Eckman DM,Weinert JS,Buxton IL,Keef KD

更新日期：1994-04-01 00:00:00

abstract：:In this issue MacMillan and McCarron in 2010 demonstrated that the phospholipase C (PLC) inhibitor U-73122 can potently inhibit Ca(2+) release from isolated smooth muscle cells independent of its effect on PLC. Their data suggest that the PLC inhibitor can block the sarcoplasmic/endoplasmic reticulum calcium ATPase pu...

journal_title：British journal of pharmacology

authors： Hollywood MA,Sergeant GP,Thornbury KD,McHale NG

更新日期：2010-07-01 00:00:00