Identification of a potent and highly efficacious, yet slowly desensitizing CB1 cannabinoid receptor agonist.

abstract：:1. We have investigated pre- and post-junctional responsiveness in vas deferens from wild-type and alpha(2A/D)-adrenoceptor knockout mice. The response to a single stimulus was not significantly different between wild-type and knock-out mice. The isometric contraction to 10 Hz stimulation for 4 s was significantly lar...

journal_title：British journal of pharmacology

authors： Cleary L,Vandeputte C,Docherty JR

更新日期：2002-07-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Resurgence in the use of chloroquine as a potential treatment for COVID-19 has seen recent cases of fatal toxicity due to unintentional overdoses. Protocols for the management of poisoning recommend diazepam, although there are uncertainties in its pharmacology and efficacy in this context. The a...

journal_title：British journal of pharmacology

authors： Hughes DA

更新日期：2020-11-01 00:00:00

abstract：:1. The natriuretic and diuretic effects of atriopeptin III (125, 250 and 500 ng kg-1, i.v.) were studied in groups of rats anaesthetized with pentobarbitone which were either sham controls, unilaterally nephrectomized controls, adenine-fed or subtotal nephrectomy chronic renal failure models. 2. Atriopeptin III given ...

journal_title：British journal of pharmacology

authors： Johns EJ,Rutkowski B

更新日期：1990-02-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Increases in intracellular cyclic AMP (cAMP) augment the release/secretion of glucagon-like peptide-1 (GLP-1). As cAMP is hydrolysed by cAMP phosphodiesterases (PDEs), we determined the role of PDEs and particularly PDE4 in regulating GLP-1 release. EXPERIMENTAL APPROACH:GLP-1 release, PDE expre...

journal_title：British journal of pharmacology

authors： Ong WK,Gribble FM,Reimann F,Lynch MJ,Houslay MD,Baillie GS,Furman BL,Pyne NJ

更新日期：2009-06-01 00:00:00

abstract：:Lignocaine suppresses insulin-stimulated glucose transport into the cells and insulin-stimulated glycogenesis at doses equivalent to that used in the treatment of muscle pain disorder. We evaluated the direct effect of lignocaine on insulin receptor (IR) kinase activity. After lignocaine (40 mM, approximately equivale...

journal_title：British journal of pharmacology

authors： Hirose M,Martyn JA,Kuroda Y,Marunaka Y,Tanaka Y

更新日期：2002-05-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Nitric oxide (NO) is known to activate NO-sensitive guanylyl cyclase (NO-GC) and to elicit cGMP production. However, NO has also been proposed to induce cGMP-independent effects. It is accepted practice to use specific NO-GC inhibitors, such as ODQ or NS2028, to assess cGMP-dependent NO effects. ...

journal_title：British journal of pharmacology

authors： Lies B,Groneberg D,Gambaryan S,Friebe A

更新日期：2013-09-01 00:00:00

abstract：:1. The responses of bladder strips from control, streptozotocin-diabetic, and sucrose-drinking rats to electrical field stimulation were investigated. Sucrose-drinking rats were included as additional controls because they have enlarged bladders as a result of non-diabetic diuresis. 2. Bladder strips from diabetic rat...

journal_title：British journal of pharmacology

authors： Tammela TL,Briscoe JA,Levin RM,Longhurst PA

更新日期：1994-09-01 00:00:00

abstract：:1. The effect of several clinically used dyes on prostaglandin E2 (PGE2) inactivation was studied in rat and human isolated lung. 2. All the dyes, given as infusions through the pulmonary circulation, inhibited the inactivation of PGE2 as measured by bioassay. The action of the dyes was readily reversible on stopping ...

journal_title：British journal of pharmacology

authors： Bakhle YS

更新日期：1981-04-01 00:00:00

abstract：BACKGROUND AND PURPOSE:The effect of age on the distribution of morphine and morphine-3-glucuronide (M3G) across the blood-brain barrier (BBB) was studied in a sheep model utilizing intracerebral microdialysis. The effect of neonatal asphyxia on brain drug distribution was also studied. EXPERIMENTAL APPROACH:Microdial...

journal_title：British journal of pharmacology

authors： Bengtsson J,Ederoth P,Ley D,Hansson S,Amer-Wåhlin I,Hellström-Westas L,Marsál K,Nordström CH,Hammarlund-Udenaes M

更新日期：2009-07-01 00:00:00

abstract：:1. The class III antiarrhythmic azimilide has previously been shown to inhibit I(Ks) and I(Kr) in guinea-pig cardiac myocytes and I(Ks) (minK) channels expressed in Xenopus oocytes. Because HERG channels underly the conductance I(Kr), in human heart, the effects of azimilide on HERG channels expressed in Xenopus oocyt...

journal_title：British journal of pharmacology

authors： Busch AE,Eigenberger B,Jurkiewicz NK,Salata JJ,Pica A,Suessbrich H,Lang F

更新日期：1998-01-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Haem oxygenase-1 (HO-1) is induced by thiazolidinediones including rosiglitazone and exerts anti-inflammatory effects in various models. However, the molecular mechanisms underlying rosiglitazone-induced HO-1 expression remain largely unknown in human pulmonary alveolar epithelial cells (HPAEpiCs...

journal_title：British journal of pharmacology

authors： Cho RL,Yang CC,Tseng HC,Hsiao LD,Lin CC,Yang CM

更新日期：2018-10-01 00:00:00

abstract：:1. Heterologous desensitization or intermolecular cross-talk plays a critical role in regulating intracellular signalling by diverse members of the G-protein-coupled receptor superfamily. We have previously established that the alpha and beta isoforms of the human thromboxane A(2) receptor (TP) undergo differential de...

journal_title：British journal of pharmacology

authors： Kelley-Hickie LP,Kinsella BT

更新日期：2004-05-01 00:00:00

abstract：BACKGROUND AND PURPOSE:PPAR-γ has been reported to be a protective regulator in ischaemia/reperfusion (I/R) injury. The receptor for advanced glycation end-products (RAGE) plays a major role in the innate immune response, and its expression is associated with PPAR-γ activation. Several angiotensin receptor blockers pos...

journal_title：British journal of pharmacology

authors： Koh EJ,Yoon SJ,Lee SM

更新日期：2013-07-01 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：:The physiological regulation of the immune system encompasses comprehensive anti-inflammatory mechanisms that can be harnessed for the treatment of infectious and inflammatory disorders. Recent studies indicate that the vagal nerve, involved in control of heart rate, hormone secretion and gastrointestinal motility, is...

journal_title：British journal of pharmacology

authors： de Jonge WJ,Ulloa L

更新日期：2007-08-01 00:00:00

abstract：:1 We have examined the effect of the histone deacetylase inhibitors apicidin, trichostatin A (TSA) and n-butyrate on the histone acetylation and the differentiation of human eosinophilic leukemia HL-60 clone 15 cells into eosinophils. 2 Viability of the cells incubated with apicidin (100 nm), TSA (30 nm) or n-butyrate...

journal_title：British journal of pharmacology

authors： Ishihara K,Hong J,Zee O,Ohuchi K

更新日期：2004-07-01 00:00:00

abstract：:1. We examined the effects of eprosartan, an AT(1) receptor antagonist, on the progression of left ventricular (LV) dysfunction and remodelling in dogs with heart failure (HF) produced by intracoronary microembolizations (LV ejection fraction, EF 30 to 40%). 2. Dogs were randomized to 3 months of oral therapy with low...

journal_title：British journal of pharmacology

authors： Suzuki G,Mishima T,Tanhehco EJ,Sharov VG,Todor A,Rostogi S,Gupta RC,Chaudhry PA,Anagnostopoulos PV,Nass O,Goldstein S,Sabbah HN

更新日期：2003-01-01 00:00:00

abstract：:1. Incubation of bovine adrenal chromaffin cells with veratridine (10-100 microM) during 24 h, caused a concentration-dependent release of the cytosolic lactate dehydrogenase (LDH) into the bathing medium, an indicator of cell death. Lubeluzole or its R(-) enantiomer, R91154, did not enhance LDH release. Both lubeluzo...

journal_title：British journal of pharmacology

authors： Cano-Abad MF,López MG,Hernández-Guijo JM,Zapater P,Gandía L,Sánchez-García P,García AG

更新日期：1998-07-01 00:00:00

abstract：:Dopamine, noradrenaline (NA) and adrenaline (Ad) depletion by 6-hydroxydopamine (6-OHDA) and pargyline plus 6-OHDA was investigated in the cat left ventricle, mesenteric and renal arteries, renal cortex, renal medulla and adrenal medulla. Catecholamine concentrations in plasma were also analyzed in these two experimen...

journal_title：British journal of pharmacology

authors： Caramona MM,Soares-da-Silva P

更新日期：1985-10-01 00:00:00

abstract：:1 We have investigated the effects of loperamide on intracellular Ca(2+) stores and membrane K(+) channels in insulin-secreting hamster insulinoma (HIT-T15) cells. 2 In cell-attached patch-clamp mode, loperamide (3-250 micro M) activated large single-channel currents. The loperamide-activated currents were tentatively...

journal_title：British journal of pharmacology

authors： He LP,Mears D,Atwater I,Rojas E,Cleemann L

更新日期：2003-05-01 00:00:00

abstract：:1 Tissue was taken from guinea-pigs that had been injected with guanethidine (100 mg/kg, i.p.) 24 h before they were killed, and from paired control animals.2 Pretreatment with guanethidine caused a significant, substantial, and sometimes complete reduction of the nerve-mediated contractions of the vas deferens. There...

journal_title：British journal of pharmacology

authors： Furness JB

更新日期：1974-01-01 00:00:00

abstract：:1 Cumulative concentration-response relationships for the chronotropic effects of histamine, oxymetazoline, clonidine and thirteen clonidine-like imidazolidine derivatives were examined in isolated spontaneously beating guinea-pig atria.2 The following compounds induced positive chronotropic effects: histamine, clonid...

journal_title：British journal of pharmacology

authors： McCulloch MW,Medgett IC,Rand MJ,Story DF

更新日期：1980-07-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Cigarette smoke is a major cause for chronic obstructive pulmonary disease (COPD). Andrographolide is an active biomolecule isolated from the plant Andrographis paniculata. Andrographolide has been shown to activate nuclear factor erythroid-2-related factor 2 (Nrf2), a redox-sensitive antioxidant...

journal_title：British journal of pharmacology

authors： Guan SP,Tee W,Ng DS,Chan TK,Peh HY,Ho WE,Cheng C,Mak JC,Wong WS

更新日期：2013-04-01 00:00:00

abstract：:1. Optimal dipeptide and peptidomimetic drug transport across the intestinal mucosal surface is dependent upon the co-operative functional activity of the di/tripeptide transporter hPepT1 and the Na(+)/H(+) exchanger NHE3. The ability of the anti-absorptive enteric neuropeptide VIP (vasoactive intestinal peptide) to m...

journal_title：British journal of pharmacology

authors： Anderson CM,Mendoza ME,Kennedy DJ,Raldua D,Thwaites DT

更新日期：2003-02-01 00:00:00

abstract：:1. We have previously found that human chymase cleaves big endothelins (ETs) at the Tyr31-Gly32 bond and produces 31-amino acid ETs (1-31), without any further degradation products. In this study, we investigated the effect of synthetic ET-1 (1-31) on the proliferation of cultured human coronary artery smooth muscle c...

journal_title：British journal of pharmacology

authors： Yoshizumi M,Kim S,Kagami S,Hamaguchi A,Tsuchiya K,Houchi H,Iwao H,Kido H,Tamaki T

更新日期：1998-11-01 00:00:00

abstract：:1. The effects of intrathecally (i.t.) injected substance P (SP), neurokinin A (NKA), [beta-Ala8]NKA (4-10) and [MePhe7]neurokinin B (NKB) at T13 thoracic spinal cord level were investigated on renal excretion of water, sodium and potassium in the conscious saline-loaded rat. Antagonists selective for NK1 (RP 67580), ...

journal_title：British journal of pharmacology

authors： Yuan YD,Couture R

更新日期：1997-07-01 00:00:00

abstract：:1. The effect of the A2A adenosine receptor agonist, 2-p-(2-carboxyethyl)phenethyl-amino-5'-N-ethylcarboxamidoadenosine (CGS 21680) on the potassium evoked release of [3H]-gamma-aminobutyric acid ([3H]-GABA) from nerve terminals derived from the caudate-putamen and the globus pallidus of the rat was compared. In both ...

journal_title：British journal of pharmacology

authors： Kurokawa M,Kirk IP,Kirkpatrick KA,Kase H,Richardson PJ

更新日期：1994-09-01 00:00:00

abstract：:1. Effects of indomethacin, the selective cyclo-oxygenase (COX)-2 inhibitors NS-398 and DFU, and dexamethasone on gastric damage induced by 30 min ischaemia followed by 60 min reperfusion (I-R) were investigated in rats. Modulation of gastric levels of COX-1 and COX-2 mRNA by I-R was evaluated using Northern blot and ...

journal_title：British journal of pharmacology

authors： Maricic N,Ehrlich K,Gretzer B,Schuligoi R,Respondek M,Peskar BM

更新日期：1999-12-01 00:00:00

abstract：:1. In rats, recovery of sensory-motor function following a crush lesion of the sciatic or tibial nerve was monitored by measuring foot reflex withdrawal from a local noxious stimulation of the foot sole. 2. Putative neurotrophic compounds were tested on this functional recovery model: melanocortins (peptides derived f...

journal_title：British journal of pharmacology

authors： Van der Zee CE,Brakkee JH,Gispen WH

更新日期：1991-05-01 00:00:00

abstract：:Aspirin at therapeutic concentrations does not inhibit the uptake of 5-hydroxytryptamine (5-HT) by blood platelets nor induce release of 5-HT from platelets, although platelet aggregation responses to collagen and arachidonic acid (which are dependent on platelet prostaglandin synthesis) are abolished. This does not s...

journal_title：British journal of pharmacology

authors： Drummond AH,MacIntyre DE,Olverman HJ

更新日期：1977-04-01 00:00:00