Antagonism by antidepressants of muscarinic acetylcholine receptors of human brain.

abstract：:1 The relationship of agonist efficacy to the rate of G protein-coupled receptor signaling desensitization is controversial. 2 Expressing inwardly rectifying potassium channels (GIRKs) in Xenopus oocytes, we have devised a signaling assay that clearly identifies CB1 cannabinoid receptor agonists with low intrinsic eff...

journal_title：British journal of pharmacology

authors： Luk T,Jin W,Zvonok A,Lu D,Lin XZ,Chavkin C,Makriyannis A,Mackie K

更新日期：2004-06-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Gain of function mutations in TRPC6 channels can cause autosomal dominant forms of focal segmental glomerulosclerosis (FSGS). Validated inhibitors of TRPC6 channels that are biologically active on FSGS-related TRPC6 mutants are eagerly sought. EXPERIMENTAL APPROACH:We synthesized new TRPC6-inhib...

journal_title：British journal of pharmacology

authors： Urban N,Neuser S,Hentschel A,Köhling S,Rademann J,Schaefer M

更新日期：2017-11-01 00:00:00

abstract：:1. A comparative study was carried out to assess the regional haemodynamic effects of intravenous infusion of human alpha- and beta-calcitonin gene-related peptide (CGRP; 0.006, 0.06 and 0.6 nmol h-1) in conscious, unrestrained Wistar rats. 2. With human alpha-CGRP, tachycardia was always accompanied by a fall in mean...

journal_title：British journal of pharmacology

authors： Gardiner SM,Compton AM,Bennett T

更新日期：1989-12-01 00:00:00

abstract：:1. The alpha 2-adrenoceptor binding sites of rabbit spleen and rat kidney, labelled with [3H]-rauwolscine, were characterized using a range of subtype selective ligands. 2. In rabbit spleen, the alpha-2-adrenoceptor binding sites displayed high affinity for oxymetazoline and WB 4101 and low affinity for prazosin and c...

journal_title：British journal of pharmacology

authors： Michel AD,Loury DN,Whiting RL

更新日期：1990-03-01 00:00:00

abstract：:1. The pharmacological characteristics of alpha 1-adrenoceptor binding sites in rat pineal gland membranes, detected by use of a selective alpha 1-adrenoceptor antagonist ([125I]-iodo-2-[beta-(4-hydroxyphenyl) ethylaminomethyl]tetralone, [125I]-HEAT), were investigated with the alkylating agent, chloroethylclonidine (...

journal_title：British journal of pharmacology

authors： Sugden D,Anwar N,Klein DC

更新日期：1996-07-01 00:00:00

abstract：:1. The cyclic analogue of dopamine, 2-amino-6,7-dihydroxy-1,2,3,4-tetrahydronaphthalene (ADTN) was injected into the lateral ventricle or bilaterally into the nucleus accumbens or caudate nucleus of conscious rats and its effect on locomotor activity was investigated. 2. When given intraventricularly, ADTN produced so...

journal_title：British journal of pharmacology

authors： Elkhawad AO,Woodruff GN

更新日期：1975-05-01 00:00:00

abstract：:This work investigates the receptor acted upon by imidazoline compounds in the modulation of morphine analgesia. The effects of highly selective imidazoline ligands on the supraspinal antinociception induced by morphine in mice were determined. 2. Intracerebroventricular (i.c.v.) or subcutaneous (s.c.) administration ...

journal_title：British journal of pharmacology

authors： Sánchez-Blázquez P,Boronat MA,Olmos G,García-Sevilla JA,Garzón J

更新日期：2000-05-01 00:00:00

abstract：:1. The aim of this study was to investigate the cardiovascular effects of a novel, potent and specific phosphodiesterase 5 (PDE 5) inhibitor, 1,3 dimethyl-6-(2-propoxy-5-methane sulphonylamidophenyl)-pyrazolo[3,4-d]pyrimidin-4-(5H)-one (DMPPO) in phenylephrine-precontracted rat aortic rings and different in vivo rat p...

journal_title：British journal of pharmacology

authors： Delpy E,le Monnier de Gouville AC

更新日期：1996-07-01 00:00:00

abstract：:1 We have investigated the effects of loperamide on intracellular Ca(2+) stores and membrane K(+) channels in insulin-secreting hamster insulinoma (HIT-T15) cells. 2 In cell-attached patch-clamp mode, loperamide (3-250 micro M) activated large single-channel currents. The loperamide-activated currents were tentatively...

journal_title：British journal of pharmacology

authors： He LP,Mears D,Atwater I,Rojas E,Cleemann L

更新日期：2003-05-01 00:00:00

abstract：:1. The subtype of alpha1-adrenoceptor mediating contractions to phenylephrine of the rat thoracic aorta, mesenteric artery and pulmonary artery were investigated by use of antagonists which show selectivity between the cloned alpha1-adrenoceptor subtypes in binding studies. 2. Cumulative concentration-contraction curv...

journal_title：British journal of pharmacology

authors： Hussain MB,Marshall I

更新日期：1997-11-01 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

abstract：:1. The role of smooth muscle-derived lipoprotein lipase (LPL) that translocates to the endothelium surface on vascular dysfunction during atherogenesis is unclear. Thus, the role of vascular LPL on blood vessel reactivity was assessed in transgenic mice that specifically express human LPL in the circulatory system. 2....

journal_title：British journal of pharmacology

authors： Esenabhalu VE,Cerimagic M,Malli R,Osibow K,Levak-Frank S,Frieden M,Sattler W,Kostner GM,Zechner R,Graier WF

更新日期：2002-01-01 00:00:00

abstract：BACKGROUND AND PURPOSE:PPAR-γ has been reported to be a protective regulator in ischaemia/reperfusion (I/R) injury. The receptor for advanced glycation end-products (RAGE) plays a major role in the innate immune response, and its expression is associated with PPAR-γ activation. Several angiotensin receptor blockers pos...

journal_title：British journal of pharmacology

authors： Koh EJ,Yoon SJ,Lee SM

更新日期：2013-07-01 00:00:00

abstract：:Multiple sclerosis (MS) is a chronic inflammatory disease of the CNS, and one of the most common causes of disability in young adults. Over the last decade, new disease-modifying therapies have emerged, including monoclonal antibodies (mAbs) that provide highly targeted therapies with greater efficacy than platform th...

journal_title：British journal of pharmacology

authors： Nguyen AL,Gresle M,Marshall T,Butzkueven H,Field J

更新日期：2017-07-01 00:00:00

abstract：:1 Synaptic potentials and the responses of frog spinal cord to various acidic amino acids were examined by means of the sucrose gap recording technique. 2 Divalent cations (50-250 microM) specifically antagonized responses evoked at N-methyl-D-aspartate (NMDA) receptors by N-methyl D,L aspartic acid (NMDLA). The rank ...

journal_title：British journal of pharmacology

authors： Smith PA

更新日期：1982-10-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Metformin, a small molecule, antihyperglycaemic agent, is a well-known activator of AMP-activated protein kinase (AMPK) and protects against cardiac fibrosis. However, the underlying mechanisms remain elusive. TGFβ1 is a key cytokine mediating cardiac fibrosis. Here, we investigated the effects o...

journal_title：British journal of pharmacology

authors： Chen R,Feng Y,Wu J,Song Y,Li H,Shen Q,Li D,Zhang J,Lu Z,Xiao H,Zhang Y

更新日期：2018-04-01 00:00:00

abstract：LINKED ARTICLES:This article is part of a themed section on Nitric Oxide 20 Years from the 1998 Nobel Prize. To view the other articles in this section visit http://onlinelibrary.wiley.com/doi/10.1111/bph.v176.2/issuetoc. ...

journal_title：British journal of pharmacology

authors： Ignarro LJ

更新日期：2019-01-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Substance P (SP) and calcitonin gene-related peptide (CGRP) released from capsaicin-sensitive sensory nerves induce local neurogenic inflammation; somatostatin exerts systemic anti-inflammatory actions presumably via sst4/sst1 receptors. This study investigates the effects of a high affinity, sst...

journal_title：British journal of pharmacology

authors： Helyes Z,Pintér E,Németh J,Sándor K,Elekes K,Szabó A,Pozsgai G,Keszthelyi D,Kereskai L,Engström M,Wurster S,Szolcsányi J

更新日期：2006-10-01 00:00:00

abstract：:1. Arachidonic acid caused larger contractions to indomethacin-tested guinea-pig trachea than in control tracheae. 2. No change in contractions was obtained in tracheae treated with 5,8, 11, 14, eicosatetraynoic acid (ETYA 10 micro M). 3. ETYA (100 micro M) blocked the effect of indomethacin on arachidonic acid-induce...

journal_title：British journal of pharmacology

authors： Mitchell HW

更新日期：1982-08-01 00:00:00

abstract：:Tyrosine sulfation is a post-translational modification of secreted and transmembrane proteins, including many GPCRs such as chemokine receptors. Most chemokine receptors contain several potentially sulfated tyrosine residues in their extracellular N-terminal regions, the initial binding site for chemokine ligands. Su...

journal_title：British journal of pharmacology

authors： Ludeman JP,Stone MJ

更新日期：2014-03-01 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：:1. Ischaemic preconditioning (IP) protects the myocardium against irreversible ischaemic injury by activating protein kinase C (PKC). The mechanism by which PKC protects the myocardium is unknown. We have shown that PKC increases the activity of ecto-5'-nucleotidase (ecto-5'-N) and thereby the production of adenosine ...

journal_title：British journal of pharmacology

authors： Node K,Kitakaze M,Minamino T,Tada M,Inoue M,Hori M,Kamada T

更新日期：1997-01-01 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：BACKGROUND AND PURPOSE:Protease-activated receptor 1 (PAR1) has been demonstrated to be involved in the pathogenesis of viral diseases. However, its role remains controversial. The goal of our study was to investigate the contribution of PAR1 to respiratory syncytial virus (RSV) and human metapneumovirus (hMPV) infecti...

journal_title：British journal of pharmacology

authors： Lê VB,Riteau B,Alessi MC,Couture C,Jandrot-Perrus M,Rhéaume C,Hamelin MÈ,Boivin G

更新日期：2018-01-01 00:00:00

abstract：:1. Plasma exudation and blood flow changes induced by intradermal injection of prostaglandins E2 (PGE2), I2 (PG12), D2 (PGD2) and F2 alpha (PGF2 alpha) were measured in rabbit dorsal skin by the use of [131I]-albumin and 133Xe. 2. Little plasma exudation was produced by any of the prostaglandins when injected alone. 3...

journal_title：British journal of pharmacology

authors： Williams TJ

更新日期：1979-03-01 00:00:00

abstract：BACKGROUND AND PURPOSE:The effects of systemic treatment with indomethacin-loaded nanocapsules (IndOH-NC) were compared with those of free indomethacin (IndOH) in rat models of acute and chronic oedema. EXPERIMENTAL APPROACH:The following models of inflammation were employed: carrageenan-induced acute oedema (measured...

journal_title：British journal of pharmacology

authors： Bernardi A,Zilberstein AC,Jäger E,Campos MM,Morrone FB,Calixto JB,Pohlmann AR,Guterres SS,Battastini AM

更新日期：2009-10-01 00:00:00

abstract：:Since December 2019 SARS-Cov-2 was found responsible for the disease COVID-19, which has spread worldwide. No specific therapies/vaccines are yet available for the treatment of COVID-19. Drug repositioning may offer a strategy and a number of drugs have been repurposed, including lopinavir/ritonavir, remdesivir, favip...

journal_title：British journal of pharmacology

authors： Scavone C,Brusco S,Bertini M,Sportiello L,Rafaniello C,Zoccoli A,Berrino L,Racagni G,Rossi F,Capuano A

更新日期：2020-11-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Hypoxia in tumours is known to cause resistance to conventional chemotherapeutic drugs. In contrast, little is known about the effects of hypoxia on targeted anti-cancer drugs. This study evaluated the effect of hypoxia on a series of clinically approved tyrosine kinase inhibitors (TKIs). EXPERI...

journal_title：British journal of pharmacology

authors： Ahmadi M,Ahmadihosseini Z,Allison SJ,Begum S,Rockley K,Sadiq M,Chintamaneni S,Lokwani R,Hughes N,Phillips RM

更新日期：2014-01-01 00:00:00

abstract：:1. It has recently been shown that both alpha(1)- and alpha(2)-adrenoceptors mediate vasoconstriction in the canine external carotid circulation. The present study set out to identify the specific subtypes (alpha(1A), alpha(1B) and alpha(1D) as well as alpha(2A), alpha(2B) and alpha(2C)) mediating the above response. ...

journal_title：British journal of pharmacology

authors： Willems EW,Valdivia LF,Saxena PR,Villalón CM

更新日期：2001-03-01 00:00:00

abstract：:1. The stimulatory effect of neuropeptide Y (NPY) on food intake is well established but the roles of the receptor subtypes Y(1) and Y(5) have been difficult to define. We have studied the effects of two novel Y(1)-preferring and two Y(5)-preferring agonists on feeding in guinea pigs. 2. The Y(1)-preferring receptor a...

journal_title：British journal of pharmacology

authors： Lecklin A,Lundell I,Salmela S,Männistö PT,Beck-Sickinger AG,Larhammar D

更新日期：2003-08-01 00:00:00