Characterization of a novel aquaretic agent, OPC-31260, as an orally effective, nonpeptide vasopressin V2 receptor antagonist.

abstract：BACKGROUND AND PURPOSE:Erectile dysfunction is highly prevalent in diabetic patients and PDE V inhibitors are effective and safe for the treatment of erectile dysfunction in men with diabetes. Therefore, in this study we investigated whether a pharmacokinetic interaction occurs between DA-8159 and metformin, as both dr...

journal_title：British journal of pharmacology

authors： Choi YH,Chung SJ,Lee MG

更新日期：2008-04-01 00:00:00

abstract：:Adenosine 5'-triphosphate (ATP) and adenylyl 5'-(beta, gamma-methylene)-diphosphonate (AMP-PCP) both contracted the guinea-pig urinary bladder, but the response to AMP-PCP was much greater. We synthesized the enantiomer of AMP-PCP, L-adenylyl 5'-(beta, gamma-methylene)-diphosphonate (L-AMP-PCP), and tested it on the g...

journal_title：British journal of pharmacology

authors： Cusack NJ,Hourani SM

更新日期：1984-05-01 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：:The diterpene, forskolin, is shown to produce a concentration-dependent, increase in short circuit current in two epithelial preparations, amphibian skin and rat colon. In the amphibian tissue the increase is sensitive to amiloride and due to an increase in electrogenic transepithelial sodium transport towards the ser...

journal_title：British journal of pharmacology

authors： Cuthbert AW,Spayne JA

更新日期：1982-05-01 00:00:00

abstract：:1. The aim of this study was to characterize the tachykinin NK2 receptor subtype mediating the spasmogenic response in the human isolated bronchus. The motor response to neurokinin A (NKA) and the selective NK2 agonist [beta Ala8]NKA(4-10), as well as the antagonistic effects of cyclic (L659,877) and linear (MEN 10376...

journal_title：British journal of pharmacology

authors： Astolfi M,Treggiari S,Giachetti A,Meini S,Maggi CA,Manzini S

更新日期：1994-02-01 00:00:00

abstract：:1. Short-circuit current (SCC) technique was used to study the adrenoceptors involved in the electrogenic chloride secretion by cultured cauda epididymal epithelium of rats. Stimulation of the epithelium with noradrenaline (primarily beta 1-adrenoceptor selective agonist), salbutamol (beta 2-adrenoceptor selective ago...

journal_title：British journal of pharmacology

authors： Leung AY,Yip WK,Wong PY

更新日期：1992-09-01 00:00:00

abstract：:Free radicals as well as the AT1 receptor are involved in the pathogenesis of cardiovascular disease. Both the intracellular mechanisms of AT1 receptor regulation and the effect of free radicals on AT1 receptor expression are currently unknown. This study investigates the role of free radicals in the modulation of AT1...

journal_title：British journal of pharmacology

authors： Nickenig G,Strehlow K,Bäumer AT,Baudler S,Wassmann S,Sauer H,Böhm M

更新日期：2000-10-01 00:00:00

abstract：:1. The irritant fungal terpenoid isovelleral caused protective eye-wiping movements in the rat upon intraocular instillation and showed cross-tachyphylaxis with capsaicin, the pungent principle in hot pepper. 2. Isovelleral induced a dose-dependent calcium uptake by rat dorsal root ganglion neurones cultured in vitro ...

journal_title：British journal of pharmacology

authors： Szallasi A,Jonassohn M,Acs G,Bíró T,Acs P,Blumberg PM,Sterner O

更新日期：1996-09-01 00:00:00

abstract：BACKGROUND AND PURPOSE:We have previously shown that lipid mediators, produced by phospholipase D and C, are generated in OX(1) orexin receptor signalling with high potency, and presumably mediate some of the physiological responses to orexin. In this study, we investigated whether the ubiquitous phospholipase A(2) (PL...

journal_title：British journal of pharmacology

authors： Turunen PM,Ekholm ME,Somerharju P,Kukkonen JP

更新日期：2010-01-01 00:00:00

abstract：:1. The effects of the nitrosothiol, S-nitroso N-acetylpenicillamine (SNAP) which liberates nitric oxide (NO), on ethanol-mediated gastric damage, blood flow and cyclic GMP levels in siaoloadenectomized (SALX) rats have been investigated. 2. Intraluminal instillation of ethanol (5-50% w/v) dose-dependently induced haem...

journal_title：British journal of pharmacology

authors： Tripp MA,Tepperman BL

更新日期：1995-05-01 00:00:00

abstract：:1. We studied the biochemical and contractile responses of isolated human myocardial tissue expressing native receptor variants of the 389G>R beta(1)-adrenoceptor polymorphism. 2. Right atrial appendage was obtained from homozygous RR patients (n=37) and homozygous GG patients (n=17) undergoing elective cardiac surger...

journal_title：British journal of pharmacology

authors： Sandilands AJ,O'Shaughnessy KM,Brown MJ

更新日期：2003-01-01 00:00:00

abstract：:1. Aggressive behaviour was elicited in rats that had been deprived of food for 20 h daily (starved), by chronic administration of Cannabis sativa extract or (-)-Delta(9)-trans-tetrahydrocannabinol.2. The influence of intraperitoneal (i.p.) or oral glucose administration, cold environment, acidosis, and corn, and prot...

journal_title：British journal of pharmacology

authors： Carlini EA,Hamaoui A,Märtz RM

更新日期：1972-04-01 00:00:00

abstract：:1 The effects of a subconstrictor dose of histamine (9 x 10(-7) mol/l) on the responses of the isolated perfused ear artery of the rabbit to electrical stimulation (E.S.) and to exogenous noradrenaline (NA) were investigated.2 Both intraluminal (I/L) and extraluminal (E/L) histamine potentiated responses to E.S. and t...

journal_title：British journal of pharmacology

authors： Foldes A,Hall RC

更新日期：1979-11-01 00:00:00

abstract：:The oestrogenic and antioestrogenic activities of a series of substituted derivatives of 1,1,2 triphenylbut-1-ene have been determined using primary cultures of rat pituitary gland cells to monitor prolactin synthesis in vitro. The relative binding affinity of the agonists for the oestrogen receptor was consistent wit...

journal_title：British journal of pharmacology

authors： Jordan VC,Koch R,Mittal S,Schneider MR

更新日期：1986-01-01 00:00:00

abstract：:1. The similarity in molecular structure between the histamine H2-agonist dimaprit (3-dimethylamino-propyl-isothiourea) and the endogenous nitric oxide synthase (NOS) substrate L-arginine prompted us to study the effect of dimaprit and some dimaprit analogues on NOS activity. Dimaprit and some of its analogues were te...

journal_title：British journal of pharmacology

authors： Paquay JB,Hoen PA,Voss HP,Bast A,Timmerman H,Haenen GR

更新日期：1999-05-01 00:00:00

abstract：:1. The noradrenaline concentration in the lung was less than 0.5 mug/g in eight animal species.2. In the cat, dog, rabbit and goat, tyramine produced a fall in pulmonary resistance, which was reduced by the administration of either reserpine or cocaine. Although an infusion of noradrenaline increased the content of th...

journal_title：British journal of pharmacology

authors： Aviado DM,Sadavongvivad C

更新日期：1970-02-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Tobacco smoke represents a relevant risk factor for coronary heart disease (CHD). Although peroxisome proliferator-activated receptor (PPAR)gamma activation reduces inflammation and atherosclerosis, expression of PPARgamma in cells and its modulation by smoking are poorly investigated. We previou...

journal_title：British journal of pharmacology

authors： Amoruso A,Gunella G,Rondano E,Bardelli C,Fresu LG,Ferrero V,Ribichini F,Vassanelli C,Brunelleschi S

更新日期：2009-11-01 00:00:00

abstract：:Ginsenoside Rg1, an active ingredient in ginseng, was previously shown to be a novel class of potent phytoestrogen. The present study aims at investigating the molecular mechanisms involved in mediating its actions in human breast cancer (MCF-7) cells. Rg1 (1 pM) stimulates cell proliferation (P<0.01) and estrogen-res...

journal_title：British journal of pharmacology

authors： Chen WF,Lau WS,Cheung PY,Guo DA,Wong MS

更新日期：2006-03-01 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：:1. The present study was undertaken to determine the mechanism of action of endothelin-1 (ET-1)-induced contraction of the guinea-pig isolated trachea. 2. ET-1 (1 nM-0.3 microM) produces a concentration-dependent contraction of guinea-pig trachea with an EC50 of approximately 25 nM. The combination of the peptidoleuko...

journal_title：British journal of pharmacology

authors： Hay DW,Hubbard WC,Undem BJ

更新日期：1993-11-01 00:00:00

abstract：:The opioid receptors are key targets in the treatment of acute and chronic pain, and the development of novel analgesics with reduced side effects is crucial in the search for more effective medications. The crystal structures of opioid receptors have provided a wealth of knowledge on many aspects of opioid receptor p...

journal_title：British journal of pharmacology

authors： Marino KA,Shang Y,Filizola M

更新日期：2018-07-01 00:00:00

abstract：:1. In the neuronally isolated cortex of the cat, local application of bemegride, picrotoxin, nikethamide, caffeine and strychnine facilitated the surface positive response of the isolated cortex and lowered the stimulus threshold for this response. Excepting nikethamide, they all produced convulsive discharge in the i...

journal_title：British journal of pharmacology

authors： Frank GB,Jhamandas K

更新日期：1970-08-01 00:00:00

abstract：:1. TRPM2 is a Ca2+ -permeable nonselective cation channel activated by intracellular ADP-ribose (ADPR) and by hydrogen peroxide (H2O2). We investigated the modulation of TRPM2 activity by N-(p-amylcinnamoyl)anthranilic acid (ACA). ACA has previously been reported to inhibit phospholipase A2 (PLA2). 2. Using patch-clam...

journal_title：British journal of pharmacology

authors： Kraft R,Grimm C,Frenzel H,Harteneck C

更新日期：2006-06-01 00:00:00

abstract：:1. Acute SR 58611A (0.25 mg kg-1), was effective in reducing the blood glucose response to a glucose tolerance test (GTT) in normal lean (control) and spontaneously obese/diabetic CBA/Ca mice and to be equipotent to 1.25 mg kg-1 glibenclamide in lean mice. 2. Neither brown (BAT) nor white (WAT) adipose tissue lipogene...

journal_title：British journal of pharmacology

authors： Williams CA,Shih MF,Taberner PV

更新日期：1999-12-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Endothelin-1 (ET-1) is increased in patients with sickle cell disease and may contribute to the development of sickle cell nephropathy. The current study was designed to determine whether ET-1 acting via the ETA receptor contributes to renal injury in a mouse model of sickle cell disease. EXPERI...

journal_title：British journal of pharmacology

authors： Heimlich JB,Speed JS,O'Connor PM,Pollock JS,Townes TM,Meiler SE,Kutlar A,Pollock DM

更新日期：2016-01-01 00:00:00

abstract：:We have examined whether modulation of the polyamine biosynthetic pathway, through inhibition by alpha-difluoromethylornithine (DFMO) of the rate limiting enzyme, ornithine decarboxylase (ODC), modulates NO synthesis in J774 macrophages. DFMO potentiated LPS-stimulated nitrite production in both a concentration- and t...

journal_title：British journal of pharmacology

authors： Baydoun AR,Morgan DM

更新日期：1998-12-01 00:00:00

abstract：:1. Orexin-containing neurons have been implicated in feeding, sleep-wake cycles and more recently in drug-seeking behaviour. 2. Pretreatment of alcohol-preferring (iP) rats with an orexin1 receptor antagonist (SB-334867, 20 mg kg(-1), intraperitoneally) completely abolished an olfactory cue-induced reinstatement of al...

journal_title：British journal of pharmacology

authors： Lawrence AJ,Cowen MS,Yang HJ,Chen F,Oldfield B

更新日期：2006-07-01 00:00:00

abstract：:1 A study was made of desensitization in chronically denervated and in normally innervated mouse soleus muscles. 2 Very high concentrations of acetylcholine produced small contractions of the innervated muscles; these were reduced in size when the addition was repeated 1 min after wash-out. 3 Desensitization in innerv...

journal_title：British journal of pharmacology

authors： Hall MT,Maleque MA,Wadsworth RM

更新日期：1975-09-01 00:00:00

abstract：:1. The effects of a series of nine GABAB receptor antagonists of widely varying potencies on electrically stimulated release from cortical slices of [3H]-GABA in the absence or presence of 10 microM of the GABAB agonist, (-)-baclofen and of endogenous glutamate in the presence of (-)-baclofen were compared. 2. The con...

journal_title：British journal of pharmacology

authors： Waldmeier PC,Wicki P,Feldtrauer JJ,Mickel SJ,Bittiger H,Baumann PA

更新日期：1994-12-01 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