Potent and voltage-dependent block by philanthotoxin-343 of neuronal nicotinic receptor/channels in PC12 cells.

abstract：BACKGROUND AND PURPOSE:Cytochrome P450 (CYP, P450) 3A4 is involved in the metabolism of 50% of drugs and its catalytic activity in vivo is not explained only by hepatic expression levels. We previously demonstrated that UDP-glucuronosyltransferase (UGT) 2B7 suppressed CYP3A4 activity through an interaction. In the pres...

journal_title：British journal of pharmacology

authors： Miyauchi Y,Tanaka Y,Nagata K,Yamazoe Y,Mackenzie PI,Yamada H,Ishii Y

更新日期：2020-03-01 00:00:00

abstract：:Pulmonary hypertension (PH) is defined by elevated mean pulmonary artery pressure following the pathological remodelling of small pulmonary arteries. An increase in right ventricular (RV) afterload results in RV hypertrophy and RV failure. The pathophysiology of PH, and RV remodelling in particular, is not well unders...

journal_title：British journal of pharmacology

authors： Maarman GJ,Schulz R,Sliwa K,Schermuly RT,Lecour S

更新日期：2017-04-01 00:00:00

abstract：:1. The role of sodium-calcium exchanger in acetylcholine (Ach)-induced hyperpolarization of intact endothelial cells was studied in excised rat aorta. The membrane potential was recorded using perforated patch-clamp technique. 2. The mean resting potential of endothelial cells was -44.1+/-1.4 mV. A selective inhibitor...

journal_title：British journal of pharmacology

authors： Bondarenko A

更新日期：2004-09-01 00:00:00

abstract：:1. In vivo microdialysis has been used to investigate the concentration of various amino acids and lactate in the extracellular fluid of the rat cortex following focal ischaemia, the probe being placed in the core of the infarct area. 2. An ischaemic infarct was produced in the cortex by use of a photochemical dye (Ro...

journal_title：British journal of pharmacology

authors： Baldwin HA,Williams JL,Snares M,Ferreira T,Cross AJ,Green AR

更新日期：1994-05-01 00:00:00

abstract：BACKGROUND AND PURPOSE:The passage of drugs across the blood-brain barrier (BBB) limits the efficacy of chemotherapy in brain tumours. For instance, the anticancer drug doxorubicin, which is effective against glioblastoma in vitro, has poor efficacy in vivo, because it is extruded by P-glycoprotein (Pgp/ABCB1), multidr...

journal_title：British journal of pharmacology

authors： Pinzón-Daza M,Garzón R,Couraud P,Romero Ia,Weksler B,Ghigo D,Bosia A,Riganti C

更新日期：2012-12-01 00:00:00

abstract：:1. The ability of PD 128907 to activate dopamine receptors in the ventral tegmental area, substantia nigra pars compacta, and striatum was investigated by use of in vitro electrophysiological recording and fast cyclic voltammetry. The affinity of a novel D2 selective antagonist L-741,626 for receptors activated by thi...

journal_title：British journal of pharmacology

authors： Bowery BJ,Razzaque Z,Emms F,Patel S,Freedman S,Bristow L,Kulagowski J,Seabrook GR

更新日期：1996-12-01 00:00:00

abstract：:1. The vascular actions of the proteinase-activated receptor-2-activating peptides (PAR2APs), SLIGRL-NH2 (SL-NH2) and SLIGKV-NH2 (KV-NH2) as well as the reverse-sequence peptide, LSIGRL-NH2 (LS-NH2) and an N-acylated PAR2AP derivative, trans-cinnamoyl-LIGRLO-NH2 (tcLI-NH2), were studied in rat intact and endothelium-d...

journal_title：British journal of pharmacology

authors： Roy SS,Saifeddine M,Loutzenhiser R,Triggle CR,Hollenberg MD

更新日期：1998-04-01 00:00:00

abstract：:1 The activity and pulmonary metabolism of two peptides, 7-homo Pro-bradykinin and 8-homo Phe-bradykinin were studied in isolated systems. 2 Both analogues were about 50-70 times less active than bradykinin on the guinea-pig ileum and 70-160 times less active on isolated strips of cat terminal ileum. 3 The action of b...

journal_title：British journal of pharmacology

authors： Bakhle YS

更新日期：1977-01-01 00:00:00

abstract：BACKGROUND AND PURPOSE:The aim of the current study was to investigate the role of arachidonic acid (AA) metabolism via cyclooxygenase (COX) in the endothelial dysfunction of penile arteries from pre-diabetic, obese Zucker rats (OZR). EXPERIMENTAL APPROACH:Penile arteries from OZR and from lean Zucker rats (LZR) were ...

journal_title：British journal of pharmacology

authors： Sánchez A,Contreras C,Villalba N,Martínez P,Martínez AC,Bríones A,Salaíces M,García-Sacristán A,Hernández M,Prieto D

更新日期：2010-02-01 00:00:00

abstract：:1. Various neurotransmitters in the brain regulate gastric acid secretion. Previously, we reported that the central injection of kappa-opioid receptor agonists stimulated this secretion in rats. Although the existence of kappa(1)-kappa(3)-opioid receptor subtypes has been proposed, the character is not defined. We inv...

journal_title：British journal of pharmacology

authors： Minowa S,Ishihara S,Tsuchiya S,Horie S,Watanabe K,Murayama T

更新日期：2003-03-01 00:00:00

abstract：:1. Vasorelaxant properties of three nitric oxide (NO) donor drugs (glyceryl trinitrate, sodium nitroprusside and spermine NONOate) in mouse aorta (phenylephrine pre-contracted) were compared with those of endothelium-derived NO (generated with acetylcholine), NO free radical (NO*; NO gas solution) and nitroxyl ion (NO...

journal_title：British journal of pharmacology

authors： Wanstall JC,Jeffery TK,Gambino A,Lovren F,Triggle CR

更新日期：2001-10-01 00:00:00

abstract：:1. We have investigated the role of endogenous nitric oxide on renal vascular reactivity in late pregnancy in in situ blood perfused kidneys of alpha-chloralose anaesthetized Wistar-Kyoto rats. Nitric oxide synthesis inhibition was achieved by intravenous administration of NG-nitro-L-arginine or NG-nitro-L-arginine me...

journal_title：British journal of pharmacology

authors： Chu ZM,Beilin LJ

更新日期：1997-09-01 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：:1 The mechanism underlying the enhancement by superoxide dismutase (SOD) of endothelium-dependent relaxation was investigated in rabbit mesenteric resistance arteries. 2 SOD (200 U ml(-1)) increased the production of H(2)O(2) in smooth muscle cells (as indicated by the use of an H(2)O(2)-sensitive fluorescent dye). 3 ...

journal_title：British journal of pharmacology

authors： Itoh T,Kajikuri J,Hattori T,Kusama N,Yamamoto T

更新日期：2003-05-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Marijuana smoking is widespread in many countries, and the use of smoked synthetic cannabinoids is increasing. Smoking a marijuana joint leads to bronchodilation in both healthy subjects and asthmatics. The effects of Δ(9) -tetrahydrocannabinol and synthetic cannabinoids on human bronchus reactiv...

journal_title：British journal of pharmacology

authors： Grassin-Delyle S,Naline E,Buenestado A,Faisy C,Alvarez JC,Salvator H,Abrial C,Advenier C,Zemoura L,Devillier P

更新日期：2014-06-01 00:00:00

abstract：:The last five years have witnessed a remarkable resurgence of interest in myocardial reperfusion injury. Reperfusion is absolutely essential to salvage ischaemic myocardium but experimental and clinical studies show that reperfusion-associated injury may mask the full benefits of prompt reperfusion in acute myocardial...

journal_title：British journal of pharmacology

authors： Baxter GF,Burley DS

更新日期：2008-01-01 00:00:00

abstract：:1. The 5-hydroxytryptamine (5-HT)1A receptor agonist, 8-hydroxy-2-(di-n-propylamino)tetralin (8-OH-DPAT), has been shown to label 5-HT reuptake sites. 2. To study the functional consequences of this property, the effects of 8-OH-DPAT were compared with those of the 5-HT reuptake inhibitors, paroxetine and clomipramine...

journal_title：British journal of pharmacology

authors： Assié MB,Koek W

更新日期：1996-11-01 00:00:00

abstract：:1. Despite the observation of pharmacological responses to neuropeptide Y (NPY) in mammalian kidneys, there are species differences in the ease with which specific NPY binding sites can be demonstrated; we have investigated whether this can be explained by differential metabolism of NPY by a membrane-bound peptidase. ...

journal_title：British journal of pharmacology

authors： Price JS,Kenny AJ,Huskisson NS,Brown MJ

更新日期：1991-10-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Positive allosteric modulation of α4β2 nicotinic acetylcholine (nACh) receptors could add a new dimension to the pharmacology and therapeutic approach to these receptors. The novel modulator NS9283 was therefore tested extensively. EXPERIMENTAL APPROACH:Effects of NS9283 were evaluated in vitro ...

journal_title：British journal of pharmacology

authors： Timmermann DB,Sandager-Nielsen K,Dyhring T,Smith M,Jacobsen AM,Nielsen EØ,Grunnet M,Christensen JK,Peters D,Kohlhaas K,Olsen GM,Ahring PK

更新日期：2012-09-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Using an innovative chemical approach, peptide welding technology (PWT), a tetrabranched derivative of nociceptin/orphanin FQ (N/OFQ) has been generated and pharmacologically characterized. Both in vitro and in vivo PWT2-N/OFQ displayed the same pharmacological profile to the natural ligand. It w...

journal_title：British journal of pharmacology

authors： Rizzi A,Sukhtankar DD,Ding H,Hayashida K,Ruzza C,Guerrini R,Calò G,Ko MC

更新日期：2015-07-01 00:00:00

abstract：:In the rabbit isolated pulmonary artery, neither the ETA receptor antagonist, BQ-123 (10 microM), nor the ETB receptor antagonist, BQ-788 (10 microM), inhibited the contractions induced by 1 nM endothelin-1 (ET-1). However, the combination of BQ-123 and BQ-788 completely inhibited the ET-1-induced contraction. In cont...

journal_title：British journal of pharmacology

authors： Fukuroda T,Ozaki S,Ihara M,Ishikawa K,Yano M,Nishikibe M

更新日期：1994-10-01 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 U46619, a prostaglandin H2 endoperoxide analogue and thromboxane A2 agonist, dose-dependently inhibited accumulation and metabolism of thromboxane B2 in the isolated perfused lung of the guinea-pig. At similar doses prostaglandins E1, E2, F1 alpha, F2 alpha, I2, 5, 6-trans-PGE2 and 8-iso-PGE1 were ineffective. 2 U46...

journal_title：British journal of pharmacology

authors： Hoult JR,Robinson C

更新日期：1983-01-01 00:00:00

abstract：:The effects of histamine and of H1- and H2-receptor agonists on the response to specific antigen were studied in isolated hearts taken from actively sensitized guinea-pigs. Histamine and H2-receptor agonists (dimaprit, impromidine) dose-dependently decrease the positive chronotropic and inotropic effects, and the seve...

journal_title：British journal of pharmacology

authors： Blandina P,Brunelleschi S,Fantozzi R,Giannella E,Mannaioni PF,Masini E

更新日期：1987-03-01 00:00:00

abstract：BACKGROUND AND PURPOSE:7-Ketocholesterol, an oxysterol present in atherosclerotic lesions, induces smooth muscle cell (SMC) death, thereby destabilizing plaques. Statins protect patients from myocardial infarction, though they induce SMC apoptosis. We investigated whether statins and 7-ketocholesterol exerted additive ...

journal_title：British journal of pharmacology

authors： Martinet W,Schrijvers DM,Timmermans JP,Bult H

更新日期：2008-07-01 00:00:00

abstract：:1. The involvement of peripheral nitric oxide (NO) in febrigenic signaling to the brain has been proposed because peripherally administered NO synthase (NOS) inhibitors attenuate lipopolysaccharide (LPS)-induced fever in rodents. However, how the unstable molecule of NO can reach the brain to trigger fever is unclear....

journal_title：British journal of pharmacology

authors： Steiner AA,Rudaya AY,Ivanov AI,Romanovsky AA

更新日期：2004-04-01 00:00:00

abstract：:Heart disease is a major cause of morbidity and mortality throughout the world. Some cardiovascular conditions can be modulated by lifestyle factors such as increased exercise or a healthier diet, but many require surgical or pharmacological interventions for their management. More targeted and less invasive therapies...

journal_title：British journal of pharmacology

authors： Rietdorf K,MacQueen H

更新日期：2017-10-01 00:00:00

abstract：:1. Effects of KC399, an opener of ATP-sensitive K+ channels were investigated on membrane potential, isometric force and intracellular Ca2+ ([Ca2+]i) mobilization induced by acetylcholine (ACh) in smooth muscle from the rabbit trachea. 2. In these smooth muscle cells, ACh (0.1 and 1 microM) depolarized the membrane in...

journal_title：British journal of pharmacology

authors： Kamei K,Nabata H,Kuriyama H,Watanabe Y,Itoh T

更新日期：1995-08-01 00:00:00

abstract：:1. The responses of bladder strips from control, streptozotocin-diabetic, and sucrose-drinking rats to electrical field stimulation were investigated. Sucrose-drinking rats were included as additional controls because they have enlarged bladders as a result of non-diabetic diuresis. 2. Bladder strips from diabetic rat...

journal_title：British journal of pharmacology

authors： Tammela TL,Briscoe JA,Levin RM,Longhurst PA

更新日期：1994-09-01 00:00:00

abstract：:1 Prolonged exposure (6-12 h) of rat aorta to alpha1-adrenergic receptor (alpha(1)AR) agonist phenylephrine (Phe) leads to a decrease in alpha(1)AR-mediated vasoconstriction. This reduced responsiveness to alpha(1)AR stimulation was strongly dependent on the intactness of the endothelium. 2 We examined the effect of P...

journal_title：British journal of pharmacology

authors： Gürdal H,Can A,Uğur M

更新日期：2005-05-01 00:00:00