ICI D7114 a novel selective beta-adrenoceptor agonist selectively stimulates brown fat and increases whole-body oxygen consumption.

abstract：BACKGROUND AND PURPOSE:Transient receptor potential melastatin 3 (TRPM3) proteins form non-selective but calcium-permeable membrane channels, rapidly activated by extracellular application of the steroid pregnenolone sulphate and the dihydropyridine nifedipine. Our aim was to characterize the steroid binding site by an...

journal_title：British journal of pharmacology

authors： Drews A,Mohr F,Rizun O,Wagner TF,Dembla S,Rudolph S,Lambert S,Konrad M,Philipp SE,Behrendt M,Marchais-Oberwinkler S,Covey DF,Oberwinkler J

更新日期：2014-02-01 00:00:00

abstract：:Stimulation of acid secretion by muscarinic cholinomimetic agents depended on the periodic interdigestive activity of the stomach. This explains the peak and following fade. Pentagastrin stimulated gastric secretion after a fixed interval and did not depend on the interdigestive activity. Neither gastrin nor methachol...

journal_title：British journal of pharmacology

authors： Magee DF,Naruse S,Pap A

更新日期：1985-02-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Gallium (Ga) has been shown to be effective in the treatment of disorders associated with accelerated bone loss, including cancer-related hypercalcemia and Paget's disease. These clinical applications suggest that Ga could reduce bone resorption. However, few studies have studied the effects of G...

journal_title：British journal of pharmacology

authors： Verron E,Masson M,Khoshniat S,Duplomb L,Wittrant Y,Baud'huin M,Badran Z,Bujoli B,Janvier P,Scimeca JC,Bouler JM,Guicheux J

更新日期：2010-04-01 00:00:00

abstract：:1. We have taken advantage of our recent development of highly potent and specific phosphinic inhibitors of endopeptidase 3.4.24.15 to examine the putative contribution of the enzyme in the secretion of A beta by HK293 transfected cells overexpressing the wild type and the Swedish (Sw) double mutated form of beta APP7...

journal_title：British journal of pharmacology

authors： Chevallier N,Jiracek J,Vincent B,Baur CP,Spillantini MG,Goedert M,Dive V,Checler F

更新日期：1997-06-01 00:00:00

abstract：:1 In order to address mechanistic differences between arterial vessel types, we have compared the vasorelaxant actions of anandamide in resistance (G3) and conduit (G0) mesenteric arteries. 2 Anandamide produced concentration-dependent relaxations of pre-constricted G3 arteries with a maximal response that was signifi...

journal_title：British journal of pharmacology

authors： O'Sullivan SE,Kendall DA,Randall MD

更新日期：2004-06-01 00:00:00

abstract：:1. The effects of paracetamol and lysine acetylsalicylate (L-AS) on high-threshold mechanonociceptors have been investigated by recording neural activity from the inflamed ankle joint in anaesthetized rats with mild adjuvant-induced monoarthritis. 2. Paracetamol (50 mg kg-1, i.v.) and L-AS (100 mg kg-1, i.v., equivale...

journal_title：British journal of pharmacology

authors： McQueen DS,Iggo A,Birrell GJ,Grubb BD

更新日期：1991-09-01 00:00:00

abstract：:1. Experiments were carried out to characterize the receptors mediating the indirect excitatory response to 5-hydroxytryptamine (5-HT) in the guinea-pig isolated trachea. 2. 5-HT caused concentration-dependent contractions of tracheal strips, and the resulting concentration-response curve was biphasic in nature. The f...

journal_title：British journal of pharmacology

authors： Lucchelli A,Santagostino-Barbone MG,Barbieri A,Tonini M

更新日期：1994-07-01 00:00:00

abstract：:1. Voltage-operated calcium channel (VOCC) antagonists are effective antihypertensive and antianginal agents but they also depress myocardial contractility. 2. We compared four L-type calcium channel antagonists, felodipine, nifedipine, amlodipine and verapamil and a relatively T-type selective calcium channel antagon...

journal_title：British journal of pharmacology

authors： Sarsero D,Fujiwara T,Molenaar P,Angus JA

更新日期：1998-09-01 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:Rhythmical transient constrictions of the lymphatic vessels provide the means for efficient lymph drainage and interstitial tissue fluid balance. This activity is critical during inflammation, to avoid or limit oedema resulting from increased vascular permeability, mediated by the release of vari...

journal_title：British journal of pharmacology

authors： Rehal S,Blanckaert P,Roizes S,von der Weid PY

更新日期：2009-12-01 00:00:00

abstract：:1. To elucidate the role of thapsigargin-induced Ca2+ entry in endothelial cells in the regulation of vascular tone, changes in Ca2+ and force of smooth muscle were simultaneously monitored in fura-2-loaded strips of porcine renal artery. 2. During phenylephrine-induced sustained contraction, thapsigargin caused an en...

journal_title：British journal of pharmacology

authors： Ihara E,Hirano K,Nishimura J,Nawata H,Kanaide H

更新日期：1999-10-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Inhibitory neurotransmission plays an important role in controlling excitability within nociceptive circuits of the spinal cord dorsal horn. Loss of inhibitory signalling is thought to contribute to the development of pathological pain. Preclinical studies suggest that increasing inhibitory glyci...

journal_title：British journal of pharmacology

authors： Winters BL,Rawling T,Vandenberg RJ,Christie MJ,Bhola RF,Imlach WL

更新日期：2018-06-01 00:00:00

abstract：:1. The cardiovascular and behavioural effects elicted by the intracerebroventricular (i.c.v.) injection of substance P (SP), neurokinin A (NKA), [MePhe7]neurokinin B ([MePhe7]NKB) or angiotensin II (AII) in the conscious rat were assessed before and 5 min after i.c.v. pretreatment with antagonists selective for angiot...

journal_title：British journal of pharmacology

authors： Picard P,Chrétien L,Couture R

更新日期：1995-04-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Calu-3 cells are derived from serous cells of human lung submucosal glands, a prime target for therapy in cystic fibrosis (CF). Calu-3 cells can be cultured to form epithelia capable of transepithelial transport of chloride. A CF Calu-3 cell is not available. EXPERIMENTAL APPROACH:A retroviral v...

journal_title：British journal of pharmacology

authors： MacVinish LJ,Cope G,Ropenga A,Cuthbert AW

更新日期：2007-04-01 00:00:00

abstract：:1. We have shown earlier that pilocarpine strongly inhibits mouse and human liver coumarin 7-hydroxylase activity of CYP 2A and pentoxyresorufin O-deethylase activity of CYP 2B in vitro. Since pilocarpine, like coumarin, contains a lactone structure we have studied in more detail its inhibitory potency on mouse and hu...

journal_title：British journal of pharmacology

authors： Kinonen T,Pasanen M,Gynther J,Poso A,Järvinen T,Alhava E,Juvonen RO

更新日期：1995-11-01 00:00:00

abstract：BACKGROUND AND PURPOSE:The increased proliferation and migration of vascular smooth muscle cells (VSMCs) after arterial injury contributes greatly to the pathogenesis of neointimal hyperplasia. As a major component of epigenetics, histone methylation plays an important role in several cardiovascular diseases. However, ...

journal_title：British journal of pharmacology

authors： Liang J,Li Q,Cai W,Zhang X,Yang B,Li X,Jiang S,Tian S,Zhang K,Song H,Ai D,Zhang X,Wang C,Zhu Y

更新日期：2019-09-01 00:00:00

abstract：:1. By use of the whole-cell configuration of the patch-clamp technique, membrane currents induced by cyclopiazonic acid (CPA; an inhibitor of the sarcoplasmic reticulum (SR) calcium-ATPase) were investigated in single smooth muscle cells freshly dispersed from the mouse anococcygeus. Voltage-dependent calcium currents...

journal_title：British journal of pharmacology

authors： Wayman CP,McFadzean I,Gibson A,Tucker JF

更新日期：1996-02-01 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. The effect of prolonged anti-hypertensive drug treatment on the blood pressure of conscious spontaneously hypertensive rats (SH-rats), and of age-matched normotensive Sprague-Dawley rats was determined during the development of hypertension in SH-rats and in the early stages of established hypertension. A compariso...

journal_title：British journal of pharmacology

authors： Hamilton TC

更新日期：1975-08-01 00:00:00

abstract：:1. The influence of sodium and potassium on the accumulation of 5-hydroxytryptamine (5-HT) by rat blood platelets was investigated.2. An absolute dependence of 5-HT uptake on the sodium concentration in the medium was found.3. Removal of potassium reduced the uptake by about 60%. High concentrations of potassium inhib...

journal_title：British journal of pharmacology

authors： Sneddon JM

更新日期：1969-11-01 00:00:00

abstract：:1. Yawning was induced by subcutaneous (s.c.) injection of low doses of apomorphine to rats. This effect decreased with increasing doses of the drug. 2. Intraperitoneal (i.p.) pretreatment of animals with sulpiride (D2-receptor blocker) reduced the frequency of the yawns induced by apomorphine, while SCH 23390 (D1-rec...

journal_title：British journal of pharmacology

authors： Zarrindast MR,Poursoltan M

更新日期：1989-04-01 00:00:00

abstract：:1. The effects of intracameral injections of prostaglandins E(1), E(2), F(1a), F(2a), and A(1) were studied on the intraocular pressure (IOP) of rabbits anaesthetized with urethane.2. With the exception of prostaglandin F(1a), all the prostaglandins studied were found to be capable of producing a large, sustained rise...

journal_title：British journal of pharmacology

authors： Beitch BR,Eakins KE

更新日期：1969-09-01 00:00:00

abstract：BACKGROUND AND PURPOSE:In mammalian cells, the anti-parasitic drug ivermectin is known as a positive allosteric modulator of the ATP-activated ion channel P2X4 and is used to discriminate between P2X4- and P2X7-mediated cellular responses. In this paper we provide evidence that the reported isoform selectivity of iverm...

journal_title：British journal of pharmacology

authors： Nörenberg W,Sobottka H,Hempel C,Plötz T,Fischer W,Schmalzing G,Schaefer M

更新日期：2012-09-01 00:00:00

abstract：:1. Phenylarsine oxide (PAO) is commonly used to inhibit tyrosine phosphatase activity. However, PAO can affect a variety of different processes because of its ability to promote sulfhydryl oxidation. In the present study, we investigated the effects that PAO has on basal and beta-adrenergically stimulated L-type Ca(2+...

journal_title：British journal of pharmacology

authors： Sims C,Harvey RD

更新日期：2004-06-01 00:00:00

abstract：:1. Microinjection of peptide YY (PYY, 7-46 pmol) into the dorsal vagal complex (DVC) stimulated gastric acid secretion in urethane-anaesthetized rats. Using a variety of neuropeptide Y (NPY) and PYY derivatives, we characterized the pharmacological profile of the receptor mediating the acid secretory response to PYY. ...

journal_title：British journal of pharmacology

authors： Yang H,Li WP,Reeve JR Jr,Rivier J,Taché Y

更新日期：1998-04-01 00:00:00

abstract：:The concentration in rat striatum of the meta and para isomers of tyramine and alpha-methyltyramine, after the administration of (+)-amphetamine, alpha-methyl-p-tyrosine (AMPT) and alpha-methylphenylalanine (AMPA) has been determined using chemical ionization gas chromatography mass spectrometry (c.i.g.c.m.s.). Twenty...

journal_title：British journal of pharmacology

authors： Dougan DF,Duffield AM,Duffield PH,Wade DN

更新日期：1983-10-01 00:00:00

abstract：:1 The effects of the prostaglandin synthetase inhibitor, indomethacin and the prostaglandin antagonist SC-19220 (1-acetyl-2-[8-chloro-10,11-dihydrodibenz (b,f) (1,4)oxazepine-10-carbonyl] hydrazine), were examined on the tone of the guinea-pig isolated tracheal preparation and on the responses of the preparation to pr...

journal_title：British journal of pharmacology

authors： Farmer JB,Farrar DG,Wilson J

更新日期：1974-12-01 00:00:00

abstract：:Prostanoids, generated from cyclooxygenase (COX) isoenzymes, play a role in the physiological function of the lower urinary tract and are important mediators of inflammatory hyperalgesia. The present work evaluates the effects of the COX-1/COX-2 inhibitor dexketoprofen as well as of a selective COX-2 inhibitor, NS-398...

journal_title：British journal of pharmacology

authors： Lecci A,Birder LA,Meini S,Catalioto RM,Tramontana M,Giuliani S,Criscuoli M,Maggi CA

更新日期：2000-05-01 00:00:00

abstract：:1 Vasoactive intestinal polypeptide (VIP, 0.01- MicroM) produced dose-related relaxations of the mouse anococcygeus muscle. 2 Following incubation with indomethacin (2.8 microM 1 h) adenosine 5'-triphosphate (ATP, 0.5-10 mM) produced dose-related relaxations of the mouse anococcygeus. 3 Haemolysed blood reduced inhibi...

journal_title：British journal of pharmacology

authors： Gibson A,Tucker JF

更新日期：1982-09-01 00:00:00

abstract：:1. (+)-Tubocurarine, hexamethonium, atropine, ouabain, and removal of potassium from the bathing medium were examined for their effects on indirectly evoked twitches (IT) of mouse phrenic nerve-diaphragm muscles in the presence or absence of neostigmine. 2. Neostigmine increased the amplitude of IT. The twitch potenti...

journal_title：British journal of pharmacology

authors： Nishimura M,Ohtani H,Yagasaki O

更新日期：1989-01-01 00:00:00