Inverse agonist and neutral antagonist actions of synthetic compounds at an insect 5-HT1 receptor.

abstract：BACKGROUND AND PURPOSE:N-docosahexaenoylethanolamine (DHEA) is the ethanolamine conjugate of the long-chain polyunsaturated n-3 fatty acid docosahexaenoic (DHA; 22: 6n-3). Its concentration in animal tissues and human plasma increases when diets rich in fish or krill oil are consumed. DHEA displays anti-inflammatory pr...

journal_title：British journal of pharmacology

authors： Meijerink J,Poland M,Balvers MG,Plastina P,Lute C,Dwarkasing J,van Norren K,Witkamp RF

更新日期：2015-01-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Protocatechuic acid (PCA) is plentiful in edible fruits and vegetables and is thus one anti-oxidative component of normal human diets. However, the molecular mechanisms involved in the chemopreventive activity of PCA are poorly understood. Here, we investigated the mechanism(s) underlying the ant...

journal_title：British journal of pharmacology

authors： Lin HH,Chen JH,Chou FP,Wang CJ

更新日期：2011-01-01 00:00:00

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：:1. We investigated the nitric oxide (NO) dependence of vasorelaxation in response to different calcium channel blockers (CCB), in rabbit femoral artery in vivo. 2. Anaesthetized rabbits underwent femoral artery ligation, and blood from the proximal artery was returned distal to the ligature through a constant infusion...

journal_title：British journal of pharmacology

authors： Xu B,Xiao-hong L,Lin G,Queen L,Ferro A

更新日期：2002-06-01 00:00:00

abstract：:5-Hydroxytryptamine (5-HT) evoked potent contractile responses in phenoxybenzamine-treated ring segments of rat caudal artery, partially contracted with U46619. Responses were mimicked by 5-HT1-selective agonists with the potency order: RU24969 > 5-carboxamidotryptamine > 5-HT = CP-93,129 > sumatriptan. 8-Hydroxy-N,N-...

journal_title：British journal of pharmacology

authors： Craig DA,Martin GR

更新日期：1993-07-01 00:00:00

abstract：:1 This study investigated the effects of soluble complement receptor type 1 (sCR1) or sCR1sLex, agents which function as a complement inhibitor or as a combined complement inhibitor and selectin adhesion molecule antagonist, respectively, on the infarct size and cardiac troponin T (cTnT) release caused by regional myo...

journal_title：British journal of pharmacology

authors： Zacharowski K,Otto M,Hafner G,Marsh HC Jr,Thiemermann C

更新日期：1999-11-01 00:00:00

abstract：:In non-allergic subjects, histamine induced a reduction of minimal nasal cross-sectional area (Amin) and an increase in albumin release into nasal lavage. The effect of histamine on albumin release was inhibited by pretreatment with NG-nitro-L-arginine methyl ester (L-NAME), 1 mumol but not by D-NAME, 1 mumol. L-NAME,...

journal_title：British journal of pharmacology

authors： Dear JW,Scadding GK,Foreman JC

更新日期：1995-09-01 00:00:00

abstract：:1. Increased calcium (Ca2+) influx has been incriminated as a potential pathological mechanism in the chronic skeletal muscle degeneration exhibited by Duchenne muscular dystrophy (DMD) patients. We have studied the influence of the glucocorticoid alpha-methylprednisolone (PDN), the only drug known to have a beneficia...

journal_title：British journal of pharmacology

authors： Metzinger L,Passaquin AC,Leijendekker WJ,Poindron P,Rüegg UT

更新日期：1995-12-01 00:00:00

abstract：BACKGROUND AND PURPOSE:The dietary trace amines tyramine and beta-phenylethylamine (beta-PEA) can increase blood pressure. However, the mechanisms involved in the vascular effect of trace amines have not been fully established. The purpose of this study was to evaluate whether trace amine-dependent vasoconstriction was...

journal_title：British journal of pharmacology

authors： Herbert AA,Kidd EJ,Broadley KJ

更新日期：2008-10-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Certain 5-lipoxygenase (5-LO) inhibitors exhibit anti-carcinogenic activities against 5-LO overexpressing tumour types and cultured tumour cells. It has been proposed therefore that 5-LO products significantly contribute to tumour cell proliferation. To date, the relationship between the inhibito...

journal_title：British journal of pharmacology

authors： Fischer AS,Metzner J,Steinbrink SD,Ulrich S,Angioni C,Geisslinger G,Steinhilber D,Maier TJ

更新日期：2010-10-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Immunomodulatory tetracyclines are well-characterized drugs with a pharmacological potential beyond their antibiotic properties. Specifically, minocycline and doxycycline have shown beneficial effects in experimental colitis, although pro-inflammatory actions have also been described in macrophag...

journal_title：British journal of pharmacology

authors： Garrido-Mesa J,Rodríguez-Nogales A,Algieri F,Vezza T,Hidalgo-Garcia L,Garrido-Barros M,Utrilla MP,Garcia F,Chueca N,Rodriguez-Cabezas ME,Garrido-Mesa N,Gálvez J

更新日期：2018-12-01 00:00:00

abstract：:N-methyl-d-aspartate (NMDA) receptors have been demonstrated to be a pivotal target for ethanol action. The present study examined the actions of acute ethanol exposure on NMDA-induced responses and the acute tolerance to ethanol actions in rat sympathetic preganglionic neurons (SPNs) in vitro and in vivo. NMDA (50 mi...

journal_title：British journal of pharmacology

authors： Lin HH,Hsieh WK,Shiu JY,Chiu TH,Lai CC

更新日期：2003-11-01 00:00:00

abstract：:1. In this study we examined the effects of cortistatin, a putative endogenous ligand for somatostatin (SRIF) receptors, on the membrane properties of rat locus coeruleus (LC) neurones in vitro, by use of intracellular and whole cell patch clamp recording. We have compared the actions of cortistatin with those of SRIF...

journal_title：British journal of pharmacology

authors： Connor M,Ingram SL,Christie MJ

更新日期：1997-12-01 00:00:00

abstract：:1 In cats anaesthetized with pentobarbitone, saxitoxin and, on a few occasions, tetrodotoxin were injected into a lateral cerebral ventricle or into the subarachnoid space of the lower brain stem. Observations were made on frequency and tidal volume of breathing, on CO(2) responsiveness and on electrical responsivenes...

journal_title：British journal of pharmacology

authors： Borison HL,McCarthy LE

更新日期：1977-12-01 00:00:00

abstract：:1. The effect of the myorelaxant drugs baclofen, diazepam and tizanidine have been compared on in vitro preparations of baby rat spinal cord and adult rat superior cervical ganglion. 2. Dorsal root-elicited long duration (time to half decay 9.71 +/- 0.29 s.e. mean, n = 31) ipsilateral ventral root reflexes (DR-VRP), m...

journal_title：British journal of pharmacology

authors： Siarey RJ,Long SK,Evans RH

更新日期：1992-10-01 00:00:00

abstract：:1. The present study shows the effects of imipramine in a single dose (10 mg kg(-1), p.o.) or following repeated (14 days, twice a day) treatment on the level of mRNA coding for D2 dopamine receptors in the rat caudate putamen (CP). Repeated administration of imipramine resulted in the increase of the level of mRNA co...

journal_title：British journal of pharmacology

authors： Dziedzicka-Wasylewska M,Rogoz R

更新日期：1998-03-01 00:00:00

abstract：:The pharmacological properties of fatty acid amidohydrolase (FAAH) were investigated in brains of 35-day-old chickens, since nothing is known about the enzyme in avian species. FAAH activity towards both [(3)H]-palmitoylethanolamide (PEA) [K(M)=1.5 microM] and [(3)H]-anandamide (AEA) [K(M)=5.4 microM] was demonstrated...

journal_title：British journal of pharmacology

authors： Fowler CJ,Börjesson M,Tiger G

更新日期：2000-10-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Saponins isolated from Panax notoginseng (Burk.) F.H. Chen have been shown to relieve thrombogenesis and facilitate haemostasis. However, it is not known which saponin accounts for this haemostatic effect. Hence, in the present study we aimed to identify which saponins contribute to its haemostat...

journal_title：British journal of pharmacology

authors： Gao B,Huang L,Liu H,Wu H,Zhang E,Yang L,Wu X,Wang Z

更新日期：2014-01-01 00:00:00

abstract：:1 The recently discovered benzodiazepine receptor exists in high concentration in the cerebral cortex. We have, therefore, examined the effects of diazepam and chlordiazepoxide on cortical neurone responses to excitatory and inhibitory amino acids and acetylcholine, in the cortex of rats anaesthetized with urethane.2 ...

journal_title：British journal of pharmacology

authors： Assumpção JA,Bernardi N,Brown J,Stone TW

更新日期：1979-12-01 00:00:00

abstract：:1. The effect of in vivo desensitization to leukotriene B4 (LTB4) on eosinophil infiltration in response to recombinant C5a was examined in guinea-pig skin. 2. LTB4 (10-300 ng) and C5a (1-10 micrograms) caused a dose-dependent increase in the levels of eosinophil peroxidase activity (a measure of eosinophil infiltrati...

journal_title：British journal of pharmacology

authors： Pettipher ER,Salter ED,Showell HJ

更新日期：1994-09-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Fibroblast-to-myofibroblast differentiation is associated with scarring, an important issue in corneal surgery. Moxifloxacin (MOX), commonly applied to prevent post-operative infection, would benefit more if it modifies fibroblast-to-myofibroblast differentiation other than antimicrobial activity...

journal_title：British journal of pharmacology

authors： Chen TC,Chang SW,Wang TY

更新日期：2013-03-01 00:00:00

abstract：:Melatonin receptors are seven transmembrane-spanning proteins belonging to the GPCR superfamily. In mammals, two melatonin receptor subtypes exist - MT1 and MT2 - encoded by the MTNR1A and MTNR1B genes respectively. The current review provides an update on melatonin receptors by the corresponding subcommittee of the I...

journal_title：British journal of pharmacology

authors： Jockers R,Delagrange P,Dubocovich ML,Markus RP,Renault N,Tosini G,Cecon E,Zlotos DP

更新日期：2016-09-01 00:00:00

abstract：:1 The responses of the smooth muscle of the capsule and blood vessels of the isolated, blood-perfused spleen of the dog to angiotensin, oxytocin and vasopressin have been investigated and compared to the actions of the catecholamines, adrenaline and noradrenaline.2 Increasing doses of each of the three polypeptides ca...

journal_title：British journal of pharmacology

authors： Davies BN,Withrington PG

更新日期：1975-06-01 00:00:00

abstract：:1. Experiments were designed to determine whether endothelium-dependent relaxing factor(s) released by acetylcholine from the canine femoral artery influences the membrane potential of coronary arterial smooth muscle. 2. The membrane potential was recorded in small canine coronary arteries (internal diameter less than...

journal_title：British journal of pharmacology

authors： Feletou M,Vanhoutte PM

更新日期：1988-03-01 00:00:00

abstract：BACKGROUND AND PURPOSE:To determine whether there is an association between vascular NADPH oxidase (NOX), superoxide, the small GTPase Rac(1) and PDE type 5 (PDE5) in human vascular smooth muscle cell (hVSMCs). EXPERIMENTAL APPROACH:hVSMCs were incubated with xanthine-xanthine oxidase (X-XO; a superoxide generating sy...

journal_title：British journal of pharmacology

authors： Muzaffar S,Shukla N,Bond M,Sala-Newby GB,Newby AC,Angelini GD,Jeremy JY

更新日期：2008-11-01 00:00:00

abstract：:1. The effect on systemic haemodynamics of BQ-123, a selective endothelin A (ETA) receptor antagonist, was investigated in healthy men by giving, on separate occasions, ascending intravenous doses of 100, 300, 1000 and 3000 nmol min(-1) BQ-123, each for 15 min, in a randomized, placebo-controlled, double-blind study. ...

journal_title：British journal of pharmacology

authors： Spratt JC,Goddard J,Patel N,Strachan FE,Rankin AJ,Webb DJ

更新日期：2001-10-01 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：:1 The relative potencies of methotrimeprazine, (+)-methotrimeprazine, (+/-)-10-(3-dimethylamino-2-methylpropyl)-2-valeroyl phenothiazine hydrochloride (M & B 18,706) and (+)-M & B 18,706 in reducing the pressor action of noradrenaline in the spinal cat, reducing intercollicular decerebrate rigidity, and muscle spindle...

journal_title：British journal of pharmacology

authors： Maxwell DR,Sumpter EA

更新日期：1974-03-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Parabens are commonly added in pharmaceutical, cosmetic and food products because of their wide antibacterial properties, low toxicity, inertness and chemical stability, although the molecular mechanism of their antibacterial effect is not fully understood. Some agonists of the transient receptor...

journal_title：British journal of pharmacology

authors： Fujita F,Moriyama T,Higashi T,Shima A,Tominaga M

更新日期：2007-05-01 00:00:00

abstract：:The uncoupling activity of oxyclozanide in warm blooded animals has been studied in whole animals, isolated tissue in vitro and on mitochondrial preparations. The onset of post mortem rigidity in mice and rats is accelerated and a contracture of striated muscle is produced. Oxyclozanide (1 muM) stimulated rat liver mi...

journal_title：British journal of pharmacology

authors： Veenendaal GH,de Waal MJ

更新日期：1974-03-01 00:00:00