Short-term desensitization of guinea-pig taenia caecum induced by carbachol occurs at intracellular Ca stores and that by histamine at H1-receptors.

abstract：:Opioid drugs such as morphine and meperidine are widely used in clinical pain management, although they can cause some adverse effects. A number of studies indicate that N-methyl-D-aspartate (NMDA) receptors may play a role in the mechanism of morphine analgesia, tolerance and dependence. Being an antitussive with NMD...

journal_title：British journal of pharmacology

authors： Chen SL,Huang EY,Chow LH,Tao PL

更新日期：2005-02-01 00:00:00

abstract：:1 In unanaesthetized cats, the administration of 6-hydroxydopamine (6-OHDA), 750 mug, via the lateral cerebral ventricle produced a pronounced fall in rectal temperature but only a slight fall when repeated 7 days later. At this time hypothalamic noradrenaline concentration had diminished to 4% of control.2 In these a...

journal_title：British journal of pharmacology

authors： Lewis PJ,Rawlins MD,Reid JL

更新日期：1974-06-01 00:00:00

abstract：:Chlorisondamine (CHL) blocks behavioural responses to nicotine for several weeks or months in rats. Persistent blockade has also been demonstrated ex vivo, in assays of nicotine-evoked striatal dopamine release. Central administration of [3H]-CHL leads to long-term retention of radiolabel in nigrostriatal dopaminergic...

journal_title：British journal of pharmacology

authors： Reuben M,Louis M,Clarke PB

更新日期：1998-11-01 00:00:00

abstract：:1. To investigate the underlying mechanism for the angiotensin II-induced desensitization of the contractile response during the prolonged stimulation of the vascular smooth muscle, we determined the effects of angiotensin-II on (1) cytosolic Ca2+ concentration ([Ca2+]i) and tension using fura-2-loaded medial strips o...

journal_title：British journal of pharmacology

authors： Ushio-Fukai M,Yamamoto H,Toyofuku K,Nishimura J,Hirano K,Kanaide H

更新日期：2000-02-01 00:00:00

abstract：:1. The ionic dependence of [(3)H]-metaraminol transport by rabbit ventricular slices was studied.2. Transport was Na(+) dependent. Choline, Li(+), K(+), Rb(+) or Cs(+) could not be substituted for Na(+).3. Transport was K(+) dependent. Rb(+) and Cs(+), but not Li, could be substituted for K(+), their relative potencie...

journal_title：British journal of pharmacology

authors： Paton DM

更新日期：1971-01-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Insulin resistance is often found to be associated with high blood pressure. We propose that in insulin-resistant hypertension, endothelial dysfunction is the consequence of increased activity of vascular MMP-2. As MMP-2 proteolytically cleaves a number of extracellular matrix proteins, we hypoth...

journal_title：British journal of pharmacology

authors： Nagareddy PR,Rajput PS,Vasudevan H,McClure B,Kumar U,Macleod KM,McNeill JH

更新日期：2012-02-01 00:00:00

abstract：:1. We have characterized the human smooth muscle endothelin converting enzyme (ECE) present in the media of the endothelium-denuded human umbilical vein preparation. 2. Endothelin-1 (ET-1) and ET-2 were potent constrictors of umbilical vein with EC50 values of 9.2 nM and 29.6 nM, respectively. ET-1 was at least 30 tim...

journal_title：British journal of pharmacology

authors： Maguire JJ,Johnson CM,Mockridge JW,Davenport AP

更新日期：1997-12-01 00:00:00

abstract：:1. Using gene chip technology, we first identified that PGF(2alpha) (FP agonist) and Butaprost (EP(2) agonist) induced about a five-fold upregulation of Nur77 mRNA expression in hFP-HEK 293/EBNA and hEP(2)-HEK293/EBNA cells. Northern Blot analysis revealed that PGF(2alpha)- and Butaprost-induced upregulation of Nur77 ...

journal_title：British journal of pharmacology

authors： Liang Y,Li C,Guzman VM,Chang WW,Evinger AJ,Pablo JV,Woodward DF

更新日期：2004-06-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Endocannabinoids play an important role in modulating spinal nociceptive signalling, crucial for the development of pain. The cannabinoid CB1 receptor and the TRPV1 cation channel are both activated by the endocannabinoid anandamide, a product of biosynthesis from the endogenous lipid precursor N...

journal_title：British journal of pharmacology

authors： Nerandzic V,Mrozkova P,Adamek P,Spicarova D,Nagy I,Palecek J

更新日期：2018-06-01 00:00:00

abstract：:G protein-coupled receptors are one of the most actively studied families of proteins. However, despite the ubiquity of protein dimerization and oligomerization as a structural and functional motif in biology, until the last decade they were generally considered as monomeric, non-interacting polypeptides. For the meta...

journal_title：British journal of pharmacology

authors： Milligan G

更新日期：2008-03-01 00:00:00

abstract：:Analogues of gamma-aminobutyric acid (GABA) incorporating an isothiouronium salt as a replacement for a protonated amino functional group have been investigated for activity on: GABA receptors in the guinea-pig ileum; [3H]-GABA and [3H]-diazepam binding to rat brain membranes; and GABA uptake and transamination. For t...

journal_title：British journal of pharmacology

authors： Allan RD,Dickenson HW,Hiern BP,Johnston GA,Kazlauskas R

更新日期：1986-06-01 00:00:00

abstract：:Adrenomedullin (AM) has two known receptors formed by the calcitonin receptor-like receptor (CL) and receptor activity-modifying protein (RAMP) 2 or 3: we report the effects of the antagonist fragments of human AM and CGRP (AM22-52 and CGRP8-37) in inhibiting AM at human (h), rat (r) and mixed species CL/RAMP2 and CL/...

journal_title：British journal of pharmacology

authors： Hay DL,Howitt SG,Conner AC,Schindler M,Smith DM,Poyner DR

更新日期：2003-10-01 00:00:00

abstract：:1. Morphine-like analgesic drugs caused depression of twitches of the isolated guinea-pig ileum in response to transmural electrical stimulation. The drugs tested were the narcotic analgesics codeine, diamorphine, fentanyl, morphine, morphine-N-oxide, normorphine, oxymorphone, pethidine, phenazocine and phenoperidine ...

journal_title：British journal of pharmacology

authors： Fennessy MR,Heimans RL,Rand MJ

更新日期：1969-10-01 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. Isolated tissues of the guinea-pig were bathed with Krebs solution at 37 degrees C and subjected to 100 ms pulses of electrical stimulation for 30 min at a frequency of 0.1 or 1.0 Hz. The tissues were then dried, ashed, and the ash analysed for calcium, sodium, potassium and magnesium.2. Gastric smooth muscle, card...

journal_title：British journal of pharmacology

authors： Northover BJ

更新日期：1972-08-01 00:00:00

abstract：:1. Changes in membrane potential (measured with an intracellular microelectrode) and in cyclic nucleotide (adenosine 3':5'-cyclic monophosphate, cyclic AMP and guanosine 3':5'-cyclic monophosphate, cyclic GMP) levels (measured by radioimmunoassay) in response to inhibitory non-adrenergic non-cholinergic (NANC) field s...

journal_title：British journal of pharmacology

authors： Baird AA,Muir TC

更新日期：1990-06-01 00:00:00

abstract：:1. The cardiovascular and behavioural effects elicted by the intracerebroventricular (i.c.v.) injection of substance P (SP), neurokinin A (NKA), [MePhe7]neurokinin B ([MePhe7]NKB) or angiotensin II (AII) in the conscious rat were assessed before and 5 min after i.c.v. pretreatment with antagonists selective for angiot...

journal_title：British journal of pharmacology

authors： Picard P,Chrétien L,Couture R

更新日期：1995-04-01 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 Physiologically, perisinusoidal hepatic stellate cells (HSC) are quiescent and store retinoids. During liver injury and in cell culture, HSC transform into proliferating myofibroblast-like cells that express alpha-smooth muscle actin (alpha-sma) and produce excessive amounts of extracellular matrix. During transform...

journal_title：British journal of pharmacology

authors： Chi X,Anselmi K,Watkins S,Gandhi CR

更新日期：2003-06-01 00:00:00

abstract：BACKGROUND AND PURPOSE:While the 5-HT and Rho-kinase (ROCK) pathways have been implicated in the development of pulmonary arterial hypertension (PAH), the nature of any interactions between them remain unclear. This study investigated a role for ROCK in 5-HT-regulated proliferative responses in lung fibroblasts in vivo...

journal_title：British journal of pharmacology

authors： Mair KM,MacLean MR,Morecroft I,Dempsie Y,Palmer TM

更新日期：2008-10-01 00:00:00

abstract：:1. It has been suggested that the vasoconstrictor response to neuropeptide Y (NPY) is located in the microvessels and that it increases with reduced vessel diameter. The aim of the present study was to analyse quantitatively, on the cat gastrocnemius muscle preparation in vivo, the effects of NPY on total regional vas...

journal_title：British journal of pharmacology

authors： Ekelund U,Erlinge D

更新日期：1997-02-01 00:00:00

abstract：:RSD 921 is a novel, structurally unique, class I Na+ channel blocking drug under development as a local anaesthetic agent and possibly for the treatment of cardiac arrhythmias. The effects of RSD 921 on wild-type heart, skeletal muscle, neuronal and non-inactivating IFMQ3 mutant neuronal Na+ channels expressed in Xeno...

journal_title：British journal of pharmacology

authors： Pugsley MK,Goldin AL

更新日期：1999-05-01 00:00:00

abstract：:1. The effects of long-term treatment with trandolapril, an angiotensin I-converting enzyme inhibitor, on exercise capacity of rats with chronic heart failure (CHF) following coronary artery ligation were examined. CHF was developed by 8 weeks after the coronary artery ligation. 2. The running time of rats with CHF in...

journal_title：British journal of pharmacology

authors： Yamaguchi F,Kawana K,Tanonaka K,Kamano I,Igarashi T,Gen E,Fujimoto Y,Maki T,Sanbe A,Nasa Y,Takeo S

更新日期：1999-04-01 00:00:00

abstract：:Drug induced long QT syndrome (LQTS) can lead to cardiac arrhythmias and sudden death, and has emerged as a worldwide problem. Most drugs that cause this are thought to directly block a specific cardiac ion channel (KCNH2 or hERG) that carries the rapidly activating delayed rectifier potassium current, I(Kr). In this ...

journal_title：British journal of pharmacology

authors： Eckhardt LL,Rajamani S,January CT

更新日期：2005-05-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Adrenoceptors can associate with cardiac caveolae. To investigate the function of vascular caveolae, adrenoceptor-mediated effects were compared in the saphenous artery of caveolin-1 knockout (cav-1KO) and wild-type (WT) mice. EXPERIMENTAL APPROACH:Electronmicroscopy was used to detect caveolae....

journal_title：British journal of pharmacology

authors： Neidhold S,Eichhorn B,Kasper M,Ravens U,Kaumann AJ

更新日期：2007-02-01 00:00:00

abstract：:1 Hypothalamic blood flow (HBF) was measured in conscious rabbits by the 133xenon washout technique. 2 Substance P in a dose of 50 or 500 ng increases HBF while 5 ng is without effect. 3 Cholinoceptor blockade, with either atropine or mecamylamine abolishes the vasodilator effect of substance P. 4 Chemical sympathecto...

journal_title：British journal of pharmacology

authors： Klugman KP,Lembeck F,Markowitz S,Mitchell G,Rosendorff C

更新日期：1980-01-01 00:00:00

abstract：:781094 (2-(2(1, 4-benzodioxanyl))-2-imidazoline hydrochloride) is a potent competitive inhibitor of the aggregatory responses of human platelets induced by adrenaline (pA2 = 7.3) and UK-14304. 781094 is a more potent inhibitor of the pro-aggregatory response to clonidine than of that to methoxamine. The alpha 2/alpha ...

journal_title：British journal of pharmacology

authors： Kerry R,Scrutton MC

更新日期：1983-06-01 00:00:00

abstract：:The phenanthrene-derivative 9-phenanthrol is a recently identified inhibitor of the transient receptor potential melastatin (TRPM) 4 channel, a Ca(2+) -activated non-selective cation channel whose mechanism of action remains to be determined. Subsequent studies performed on other ion channels confirm the specificity o...

journal_title：British journal of pharmacology

authors： Guinamard R,Hof T,Del Negro CA

更新日期：2014-04-01 00:00:00

abstract：:1. Voltage-operated calcium channel (VOCC) antagonists are effective antihypertensive and antianginal agents but they also depress myocardial contractility. 2. We compared four L-type calcium channel antagonists, felodipine, nifedipine, amlodipine and verapamil and a relatively T-type selective calcium channel antagon...

journal_title：British journal of pharmacology

authors： Sarsero D,Fujiwara T,Molenaar P,Angus JA

更新日期：1998-09-01 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