Isothiouronium compounds as gamma-aminobutyric acid agonists.

abstract：:1. In isolated Langendorff-perfused, electrically-paced, hearts of guinea-pigs, global low-flow-ischaemia (LFI; at 0.7 ml min-1) resulted in marked increases in the rates of release of lactate, lactate dehydrogenase (LDH) and creatine kinase (CK) over a 30 min period. At the end of the LFI period, tissue ATP content w...

journal_title：British journal of pharmacology

authors： Clarke B,Spedding M,Patmore L,McCormack JG

更新日期：1993-07-01 00:00:00

abstract：:1. Two-electrode voltage clamp was used to study the effects of adenosine 3':5'-cyclic monophosphate (cyclic AMP) and guanosine 3':5'-cyclic monophosphate (cyclic GMP) on voltage-dependent ion channels in salivary gland cells of the leech, Haementeria ghilianii. 2. Intracellular cyclic AMP specifically blocked delayed...

journal_title：British journal of pharmacology

authors： Everill B,Berry MS

更新日期：1995-09-01 00:00:00

abstract：:1 In the isolated basilar artery of the rabbit, gamma-aminobutyrate acid (GABA) (ED50 +/- s.e. mean, 2.4 +/- 1.1 x 10(-5) M) produced a relaxation, if the tone had been increased with 5-hydroxytryptamine (5-HT). 2 3-Aminoproprane sulphonic acid (3-APS) produced a similar, but smaller relaxation, while baclofen had no ...

journal_title：British journal of pharmacology

authors： Anwar N,Mason DF

更新日期：1982-01-01 00:00:00

abstract：:1. Recent studies demonstrated that inhibition or genetic inactivation of the enzyme poly (ADP-ribose) polymerase (PARP) is beneficial in myocardial reperfusion injury. PARP activation in the reperfused myocardium has been assumed, but not directly demonstrated. Furthermore, the issue whether pharmacological PARP inhi...

journal_title：British journal of pharmacology

authors： Liaudet L,Szabó E,Timashpolsky L,Virág L,Cziráki A,Szabó C

更新日期：2001-08-01 00:00:00

abstract：:1. The effects of methylflavonolamine hydrochloride (4'-methyl-7-(2-hydroxy-3-isopropylamino-propoxy)-flavone hydrochloride, MFA) were investigated and compared with verapamil and papaverine on rabbit isolated aortic strips, which were contracted by noradrenaline, calcium and potassium. 2. Pre-incubation for 25 min wi...

journal_title：British journal of pharmacology

authors： Zhang MS,Zhou EF

更新日期：1988-08-01 00:00:00

abstract：:1. Treatment of rat mesangial cells with interleukin 1 beta (IL-1 beta) or tumour necrosis factor alpha (TNF alpha) has been shown to induce a macrophage-type of nitric oxide (NO) synthase. Here we report that adenosine 3':5'-cyclic monophosphate (cyclic AMP) is another mediator that triggers induction of NO synthase ...

journal_title：British journal of pharmacology

authors： Mühl H,Kunz D,Pfeilschifter J

更新日期：1994-05-01 00:00:00

abstract：:The Secretin family of GPCRs are endocrine peptide hormone receptors that share a common genomic organization and are the subject of a wide variety of alternative splicing. All GPCRs contain a central seven transmembrane domain responsible for transducing signals from the outside of the cell as well as extracellular a...

journal_title：British journal of pharmacology

authors： Furness SG,Wootten D,Christopoulos A,Sexton PM

更新日期：2012-05-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Alogliptin, a highly selective dipeptidyl peptidase-4 (DPP-4) inhibitor, enhances incretin action and pioglitazone enhances hepatic and peripheral insulin actions. Here, we have evaluated the effects of combining these agents in diabetic mice. EXPERIMENTAL APPROACH:Effects of short-term treatmen...

journal_title：British journal of pharmacology

authors： Moritoh Y,Takeuchi K,Asakawa T,Kataoka O,Odaka H

更新日期：2009-06-01 00:00:00

abstract：:Muscularis mucosa of the distal oesophagus of the opossum contains nerves which release acetylcholine and substance P(SP)-like material on field stimulation. The release of SP-like material appeared to be inhibited by the presence of exogenous muscarinic agonists and potentiated by muscarinic antagonists. Analysis of ...

journal_title：British journal of pharmacology

authors： Daniel EE,Jury J,Robotham KH

更新日期：1986-07-01 00:00:00

abstract：:1. To characterize the muscarinic receptors on human pulmonary veins associated with the acetylcholine (ACh)-induced relaxation, isolated venous and arterial preparations were pre-contracted with noradrenaline (10 microM) and were subsequently challenged with ACh in the absence or presence of selective muscarinic anta...

journal_title：British journal of pharmacology

authors： Walch L,Gascard JP,Dulmet E,Brink C,Norel X

更新日期：2000-05-01 00:00:00

abstract：:The aim of this study was to evaluate the potency of YM-53601 ((E)-2-[2-fluoro-2-(quinuclidin-3-ylidene) ethoxy]-9H-carbazole monohydrochloride), a new inhibitor of squalene synthase, in reducing both plasma cholesterol and triglyceride levels, compared with 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase in...

journal_title：British journal of pharmacology

authors： Ugawa T,Kakuta H,Moritani H,Matsuda K,Ishihara T,Yamaguchi M,Naganuma S,Iizumi Y,Shikama H

更新日期：2000-09-01 00:00:00

abstract：:In recent years, late-stage clinical drug development that primarily focuses on urogenital targets has centered around four areas of medical need (both unmet need and aiming to improve on existing therapies). These include male sexual dysfunction (MSD), female sexual dysfunction (FSD), prostatic pathology (neoplastic,...

journal_title：British journal of pharmacology

authors： Azam U

更新日期：2006-02-01 00:00:00

abstract：:1.--The small protein Bv8, isolated from the amphibian skin, belongs to a novel family of secreted proteins linked to several biological effects. We describe the expression of Bv8/prokineticins and their receptors in mouse macrophages, and characterize their proinflammatory activities. 2.--The rodent analogue of Bv8, ...

journal_title：British journal of pharmacology

authors： Martucci C,Franchi S,Giannini E,Tian H,Melchiorri P,Negri L,Sacerdote P

更新日期：2006-01-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Strontium ranelate, a drug approved and until recently used for the treatment of osteoporosis, mediates its effects on bone at least in part via the calcium-sensing (CaS) receptor. However, it is not known whether bone-targeted CaS receptor positive allosteric modulators (PAMs; calcimimetics) rep...

journal_title：British journal of pharmacology

authors： Diepenhorst NA,Leach K,Keller AN,Rueda P,Cook AE,Pierce TL,Nowell C,Pastoureau P,Sabatini M,Summers RJ,Charman WN,Sexton PM,Christopoulos A,Langmead CJ

更新日期：2018-11-01 00:00:00

abstract：:The nature of the neurohypophyseal peptide receptor in the anococcygeus muscles from male mice was investigated. The rank order of potency of naturally occurring peptides was oxytocin greater than Arg-vasotocin greater than Arg-vasopressin greater than Lys-vasopressin, which is similar to that found in the uterus and ...

journal_title：British journal of pharmacology

authors： Gibson A

更新日期：1986-05-01 00:00:00

abstract：:1. The ability of the putative, selective post-junctional alpha 2-adrenoceptor antagonist, SK&F 104078 to antagonize the effects of structurally-diverse agonists at pre-junctional alpha 2-adrenoceptors in the guinea-pig ileum and rat vas deferens in vitro and in the rat heart in vivo, and at post-junctional alpha 2-ad...

journal_title：British journal of pharmacology

authors： Akers I,Coates J,Drew GM,Sullivan AT

更新日期：1991-04-01 00:00:00

abstract：:1. Isolated preparations of rat anococcygeus muscle were incubated with [3H]-noradrenaline and the efflux of radioactivity induced by stimulation of intramural sympathetic nerves was used as a measure of release of transmitter noradrenaline. Isometric contractile responses were also measured. 2. Angiotensin I (0.03 mi...

journal_title：British journal of pharmacology

authors： Li CG,Majewski H,Rand MJ

更新日期：1988-10-01 00:00:00

abstract：:1. This study investigated whether (a) cannabinoid CB(1) receptor knockout (CB(1)(-/-)) mice displayed altered gastrointestinal transit and (b) cannabinoid CB(1) and opioid receptors functionally interact in the regulation of gastrointestinal transit. 2. Gastrointestinal transit was assessed by the Whole Gastrointesti...

journal_title：British journal of pharmacology

authors： Carai MA,Colombo G,Gessa GL,Yalamanchili R,Basavarajappa BS,Hungund BL

更新日期：2006-08-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Nociceptin/orphanin FQ (N/OFQ) peptide (NOP) receptor agonists display a promising analgesic profile in preclinical studies. However, supraspinal N/OFQ produced hyperalgesia in rodents and such effects have not been addressed in primates. Thus, the aim of this study was to investigate the effects...

journal_title：British journal of pharmacology

authors： Ding H,Hayashida K,Suto T,Sukhtankar DD,Kimura M,Mendenhall V,Ko MC

更新日期：2015-07-01 00:00:00

abstract：:1. S 16257 is a new bradycardic agent. Its electropharmacological profile has been compared to that of the known bradycardic compound UL-FS 49 (Zatebradine). Intracellular recordings of action potentials (APs) were performed with conventional glass microelectrodes. 2. In the rabbit isolated sino-atrial node (SAN) tiss...

journal_title：British journal of pharmacology

authors： Thollon C,Cambarrat C,Vian J,Prost JF,Peglion JL,Vilaine JP

更新日期：1994-05-01 00:00:00

abstract：:In helical strips cut from the small mesenteric artery of guinea-pig (GPSMA) (0.3-0.6 mm o.d.) relaxations induced by substance P were more susceptible to damage of the endothelium by rubbing than were relaxations evoked by carbachol. Relaxations induced by 2-nicotin-amidoethyl nitrate (SG75) were unaffected by this p...

journal_title：British journal of pharmacology

authors： Bolton TB,Clapp LH

更新日期：1986-04-01 00:00:00

abstract：:The pharmacological properties of endothelin receptors (ETR) were investigated in guinea-pig bronchus by comparing binding and functional results. In binding assays, both the ET(B) agonists, endothelin-3 (ET-3) and N-suc-[Glu9,Ala11,15]ET-1(8-21) (IRL 1620), and the antagonist, N-cis-2,6-dimethylpiperidinocarbonyl-L-g...

journal_title：British journal of pharmacology

authors： Mazzoni MR,Breschi MC,Ceccarelli F,Lazzeri N,Giusti L,Nieri P,Lucacchini A

更新日期：1999-07-01 00:00:00

abstract：:1. Several amino-acid esters and amides have been prepared and their toxicological and pharmacological properties have been investigated. Some of the quaternary esters and amides were lethal to mice at doses below 1 mg/kg; this lethality was usually associated with high nicotinic activity. None of the compounds showed...

journal_title：British journal of pharmacology

authors： Barrass BC,Brimblecombe RW,Parkes DC,Rich P

更新日期：1968-10-01 00:00:00

abstract：:The effects of intravenous doses of Org 6001 and disopyramide (10 mg/kg) known to confer protection against early postligation-induced arrhythmias in the anaesthetized rat when given prophylactically, were assessed following postligation administration. When given 1 min after ligation both drugs greatly reduced the in...

journal_title：British journal of pharmacology

authors： Marshall RJ,Muir AW,Winslow E

更新日期：1982-08-01 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：BACKGROUND AND PURPOSE:4-[3,5-Bis(2-chlorobenzylidene)-4-oxo-piperidine-1-yl]-4-oxo-2-butenoic acid CLEFMA is a new anti-cancer molecule. Here, we investigated changes in apoptosis and inflammatory markers during CLEFMA-induced tumour suppression. EXPERIMENTAL APPROACH:Lung adenocarcinoma H441 and A549, and normal lun...

journal_title：British journal of pharmacology

authors： Yadav VR,Sahoo K,Awasthi V

更新日期：2013-12-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Humanized mice for the nuclear receptor peroxisome proliferator-activated receptor δ (PPARδ), termed PPARδ knock-in (PPARδ KI) mice, were generated for the investigation of functional differences between mouse and human PPARδ and as tools for early drug efficacy assessment. EXPERIMENTAL APPROACH...

journal_title：British journal of pharmacology

authors： Gross B,Hennuyer N,Bouchaert E,Rommens C,Grillot D,Mezdour H,Staels B

更新日期：2011-09-01 00:00:00

abstract：:The endogenous cannabinoid system is involved in numerous physiological and neuropsychological functions. Medications that target this system hold promise for the treatment of a wide variety of disorders. However, as reward is one of the most prominent of these functions, medications that activate this system must be ...

journal_title：British journal of pharmacology

authors： Panlilio LV,Justinova Z,Goldberg SR

更新日期：2010-06-01 00:00:00

abstract：:1. Many apparent actions of adenosine 5'-triphosphate (ATP) are mediated by adenosine produced by enzymatic hydrolysis of the nucleotide. Previously described actions of ATP in the CNS have been partly due to this phenomenon. In the present study analogues of ATP, which are not hydrolysed to adenosine, were used to se...

journal_title：British journal of pharmacology

authors： Stone TW,Cusack NJ

更新日期：1989-06-01 00:00:00

abstract：BACKGROUND AND PURPOSE:An alteration in the communication between the innate and adaptive immune cells is a hallmark of ulcerative colitis (UC). Semaphorin-3E (SEMA3E), a secreted guidance protein, regulates various immune responses. EXPERIMENTAL APPROACH:We investigated the expression of SEMA3E in colonic biopsies of...

journal_title：British journal of pharmacology

authors： Kermarrec L,Eissa N,Wang H,Kapoor K,Diarra A,Gounni AS,Bernstein CN,Ghia JE

更新日期：2019-05-01 00:00:00