Influence of the endothelium on contractile effects of 5-hydroxytryptamine and selective 5-HT agonists in canine basilar artery.

abstract：:Knowledge of the cardiac safety of emerging new drugs is an important aspect of assuring the expeditious advancement of the best candidates targeted at unmet medical needs while also assuring the safety of clinical trial subjects or patients. Present methodologies for assessing drug-induced torsades de pointes (TdP) a...

journal_title：British journal of pharmacology

authors： Bass AS,Darpo B,Breidenbach A,Bruse K,Feldman HS,Garnes D,Hammond T,Haverkamp W,January C,Koerner J,Lawrence C,Leishman D,Roden D,Valentin JP,Vos MA,Zhou YY,Karluss T,Sager P

更新日期：2008-08-01 00:00:00

abstract：:1. Female mice of the Hough/Porton and Tuck/TO strains were found to be more sensitive than male mice to the diuretic effects of oral and intravenous doses of ethacrynic acid. 2. The sensitivity of Hough/Porton male mice to ethacrynic acid was increased after pretreatment with stilboestrol and the sensitivity of femal...

journal_title：British journal of pharmacology

authors： Cooling MJ,Sim MF

更新日期：1977-08-01 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

abstract：BACKGROUND AND PURPOSE:Tooth eruption is a complicated process regulated by the dental follicles (DF). Our recent study discovered that tooth eruption was inhibited upon injection of bleomycin into DF. However, the mechanisms were unknown. EXPERIMENTAL APPROACH:Human dental follicle cells (hDFCs) were treated by bleom...

journal_title：British journal of pharmacology

authors： Li ZZ,Wang HT,Lee GY,Yang Y,Zou YP,Wang B,Gong CJ,Cai Y,Ren JG,Zhao JH

更新日期：2020-10-17 00:00:00

abstract：:Changes in the efficiency of the peristaltic reflex, acetylcholine (ACh) output and motor responses to transmural and periarterial nerve stimulation produced by bicuculline and gamma-aminobutyric acid (GABA) receptor desensitization were investigated in the guinea-pig isolated colon. Bicuculline, at concentrations una...

journal_title：British journal of pharmacology

authors： Frigo GM,Galli A,Lecchini S,Marcoli M

更新日期：1987-01-01 00:00:00

abstract：:Levetiracetam, the alpha-ethyl analogue of the nootropic piracetam, is a widely used antiepileptic drug (AED) that provides protection against partial seizures and is also effective in the treatment of primary generalized seizure syndromes including juvenile myoclonic epilepsy. Levetiracetam was discovered in 1992 thr...

journal_title：British journal of pharmacology

authors： Rogawski MA

更新日期：2008-08-01 00:00:00

abstract：:1. Dopamine efflux following single pulse or train of pulse stimulations was measured in slices of rat caudate putamen, nucleus accumbens and tuberculum olfactorium, using fast cyclic voltammetry at a carbon fibre microelectrode; 1, 5, 10, 20 or 50 pulses were applied at each location at frequencies varying from 10 Hz...

journal_title：British journal of pharmacology

authors： Trout SJ,Kruk ZL

更新日期：1992-06-01 00:00:00

abstract：:The development of myocardial and large vessel stiffness with aging underlies the development of diastolic heart failure and isolated systolic hypertension. Nonenzymatic reaction between glucose and proteins (Maillard reaction) leading to collagen crosslinking in the myocardium and arterial wall has been implicated in...

journal_title：British journal of pharmacology

authors： Aronson D

更新日期：2004-08-01 00:00:00

abstract：:In moderate-to-severe asthma, adding an inhaled long-acting β2 -adenoceptor agonist (LABA) to an inhaled corticosteroid (ICS) provides better disease control than simply increasing the dose of ICS. Acting on the glucocorticoid receptor (GR, gene NR3C1), ICSs promote anti-inflammatory/anti-asthma gene expression. In vi...

journal_title：British journal of pharmacology

authors： Newton R,Giembycz MA

更新日期：2016-12-01 00:00:00

abstract：:We have examined the effects of antagonists on the isometric contraction of the human saphenous vein produced by 5-hydroxytryptamine (5-HT). The 5-HT2-antagonist ketanserin (1 microM) had little effect on the lower part of the concentration-response curve to 5-HT, but markedly shifted the upper part of the curve. Yohi...

journal_title：British journal of pharmacology

authors： Docherty JR,Hyland L

更新日期：1986-09-01 00:00:00

abstract：:The relative potencies of a series of substance P analogues have been determined for spasmogenic activity in the guinea-pig ileum in vitro and for the release of 86Rb and alpha-amylase activity from rat parotid gland slices in vitro. Equipotent molar ratios (EMR), relative to substance P, were determined for all the c...

journal_title：British journal of pharmacology

authors： Gater PR,Jordan CC,Owen DG

更新日期：1982-02-01 00:00:00

abstract：:We investigated the ability of the cannabinoid agonists CP55,940 (CB(1)/CB(2)) and anandamide (endogenous cannabinoid) to modulate electrical field stimulation (EFS)-induced acetylcholine (ACh) release from parasympathetic nerve terminals innervating guinea-pig trachea. We assessed whether modulation of transmitter re...

journal_title：British journal of pharmacology

authors： Spicuzza L,Haddad EB,Birrell M,Ling A,Clarke D,Venkatesan P,Barnes PJ,Belvisi MG

更新日期：2000-08-01 00:00:00

abstract：:1 Noradrenaline and 28 imidazolidine (clonidine-like) and imidazoline (oxymetazoline-like) compounds with various phenyl ring substituents have been examined for their ability to inhibit responses to transmural stimulation and exogenous acetylcholine in ileal preparations from reserpine-treated guinea-pigs.2 The bathi...

journal_title：British journal of pharmacology

authors： Malta E,Raper C,Tawa PE

更新日期：1981-06-01 00:00:00

abstract：:1. The effect of a single injection of the monoamine oxidase inhibitor, tranylcypromine, administered intravenously (20 mg/kg) or into the lateral cerebral ventricle (5-10 mg), on hypothalamic and rectal temperature, has been investigated.2. Intravenous tranylcypromine causes a significant rise in body temperature, wh...

journal_title：British journal of pharmacology

authors： Cranston WI,Rosendorff C

更新日期：1970-05-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Abdominal aortic aneurysm (AAA) is a degenerative disease with irreversible and progressive dilation of the artery. But there are few options for efficacious treatment except for traditional surgery. Probucol has been widely applied to treat hyperlipidaemia and atherosclerosis in clinic, but whet...

journal_title：British journal of pharmacology

authors： Chen C,Wang Y,Cao Y,Wang Q,Anwaier G,Zhang Q,Qi R

更新日期：2020-01-01 00:00:00

abstract：:1. The actions of etorphine, morphine and diprenorphine were investigated on neurones of the cerebral cortex and spinal cord of rats anaesthetized with pentobarbitone.2. In the cerebral cortex, intravenous etorphine increased the latency of the primary evoked response to a peripheral nerve stimulus and suppressed the ...

journal_title：British journal of pharmacology

authors： Biscoe TJ,Duggan AW,Lodge D

更新日期：1972-10-01 00:00:00

abstract：:The ability of chemically detoxified E. coli endotoxins and membrane-active agents to modify the toxicity of native E. coli endotoxin in vivo was examined. The time- and dose-dependent increase in plasma acid phosphatase activity following toxin administration to rats provided a convenient quantitative measure of in v...

journal_title：British journal of pharmacology

authors： Godin DV,Tuchek JM

更新日期：1983-06-01 00:00:00

abstract：BACKGROUND AND PURPOSE:The present study investigated whether the pathophysiological changes induced by burn and smoke inhalation are modulated by parenteral administration of Na(2)S, a H(2)S donor. EXPERIMENTAL APPROACH:The study used a total of 16 chronically instrumented, adult female sheep. Na(2)S was administered...

journal_title：British journal of pharmacology

authors： Esechie A,Enkhbaatar P,Traber DL,Jonkam C,Lange M,Hamahata A,Djukom C,Whorton EB,Hawkins HK,Traber LD,Szabo C

更新日期：2009-11-01 00:00:00

abstract：:1 The butyrophenone tranquilizer, azaperone, was administered intramuscularly, at dose levels of 0.4 and 0.8 mg/kg, to ponies and its effects on cardiovascular and respiratory functions assessed. 2 Arterial blood pH, CO2 tension (PaCO2) and O2 tension (PaO2) remained relatively constant throughout the course of action...

journal_title：British journal of pharmacology

authors： Lees P,Serrano L

更新日期：1976-03-01 00:00:00

abstract：:1. Chronic benzodiazepine administration has been associated with tolerance and with downregulation of gamma-aminobutyric acidA (GABAA)-receptor binding and function. However, effects of individual benzodiazepines on brain regions have varied. 2. To compare the effects of chronic lorazepam and alprazolam, we have admi...

journal_title：British journal of pharmacology

authors： Galpern WR,Miller LG,Greenblatt DJ,Shader RI

更新日期：1990-12-01 00:00:00

abstract：:Histamine has been one of the most studied substances in medicine, playing a major role in diverse (patho)physiological processes. It elicits its multifaceted modulatory functions by activating four types of GPCRs, designated as H1-4 . Despite the heterogeneity and the complexity of histamine receptor pharmacology, ma...

journal_title：British journal of pharmacology

authors： Tiligada E,Ennis M

更新日期：2020-02-01 00:00:00

abstract：BACKGROUND AND PURPOSE:We sought to understand why (-)-cannabidiol (CBD) and (-)-cannabidiol-dimethylheptyl (CBD-DMH) exhibit distinct pharmacology, despite near identical structures. EXPERIMENTAL APPROACH:HEK293A cells expressing either human type 1 cannabinoid (CB1 ) receptors or CB2 receptors were treated with CBD ...

journal_title：British journal of pharmacology

authors： Tham M,Yilmaz O,Alaverdashvili M,Kelly MEM,Denovan-Wright EM,Laprairie RB

更新日期：2019-05-01 00:00:00

abstract：:1. The effect of clofibrate (CFB), bezafibrate (BFB), and gemfibrozil (GFB) on plasma lipoprotein (VLDL and LDL) concentration, composition and resistance to copper-induced oxidation has been studied in male Sprague-Dawley rats after a 15 day treatment. 2. Plasma triglyceride levels were reduced by CFB (41%) and BFB (...

journal_title：British journal of pharmacology

authors： Vázquez M,Merlos M,Adzet T,Laguna JC

更新日期：1996-03-01 00:00:00

abstract：:1. An antisense approach to block nitric oxide (NO) synthesis was developed, complementing the widely used chemical inhibitors and overcoming problems associated with their use in studying the roles of NO. 2. Murine macrophage cell lines (J774.2) were generated expressing a 500 bp sequence from inducible NO synthase (...

journal_title：British journal of pharmacology

authors： Cartwright JE,Johnstone AP,Whitley GS

更新日期：1997-01-01 00:00:00

abstract：:1. We have examined the mechanisms of local oedema formation in the passive cutaneous anaphylactic (PCA) reaction in the rabbit. 2. IgE-containing antiserum was injected i.d. and allowed to sensitize skin sites for periods up to 240 h. Antigen (bovine gamma globulin) was injected i.d. or i.v. and local oedema formatio...

journal_title：British journal of pharmacology

authors： Hellewell PG,Jose PJ,Williams TJ

更新日期：1992-12-01 00:00:00

abstract：:Measurements of affinity and efficacy are fundamental for work on agonists both in drug discovery and in basic studies on receptors. In this review I wish to consider methods for measuring affinity and efficacy at G protein coupled receptors (GPCRs). Agonist affinity may be estimated in terms of the dissociation const...

journal_title：British journal of pharmacology

authors： Strange PG

更新日期：2008-04-01 00:00:00

abstract：:Δ9 -tetrahydrocannabinol, the principal active component in Cannabis sativa extracts such as marijuana, participates in cell signalling by binding to cannabinoid CB1 and CB2 receptors on the cell surface. The CB1 receptors are present in both inhibitory and excitatory presynaptic terminals and the CB2 receptors are fo...

journal_title：British journal of pharmacology

authors： Basavarajappa BS,Joshi V,Shivakumar M,Subbanna S

更新日期：2019-09-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Fatty acid amide hydrolase (FAAH) inhibitors are postulated to possess anti-hypertensive potential, because their acute injection decreases BP in spontaneously hypertensive rats (SHR), partly through normalization of cardiac contractile function. Here, we examined whether the potential hypotensiv...

journal_title：British journal of pharmacology

authors： Pędzińska-Betiuk A,Weresa J,Toczek M,Baranowska-Kuczko M,Kasacka I,Harasim-Symbor E,Malinowska B

更新日期：2017-07-01 00:00:00

abstract：:1. Juvenile male rats treated with parachlorophenylalanine showed hair loss round the head and neck extending down the chest and abdomen.2. Treated isolated rats did not have this loss of hair, while untreated animals living in the same cage as treated rats lost their hair. The loss therefore seems to be caused by inc...

journal_title：British journal of pharmacology

authors： Shillito EE

更新日期：1970-02-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Previous findings suggest that the growth and differentiation factor midkine (Mdk) is a negative regulator of osteoblast activity and bone formation, thereby raising the possibility that a specific Mdk antagonist might improve bone formation during fracture healing. EXPERIMENTAL APPROACH:In the ...

journal_title：British journal of pharmacology

authors： Haffner-Luntzer M,Heilmann A,Rapp AE,Roessler R,Schinke T,Amling M,Ignatius A,Liedert A

更新日期：2016-07-01 00:00:00