Overexpression of Orphan Receptor GPR61 Increases cAMP Levels upon Forskolin Stimulation in HEK293 Cells: in vitro and in silico Validation of 5-(Nonyloxy)Tryptamine as a Low-Affinity Inverse Agonist.

abstract：:To determine the existence of beta 3-adrenoceptors in functional assays in isolated preparations for which data are lacking, we compared the effects of SR 58611A, a selective beta 3-adrenoceptor agonist, and isoprenaline in the guinea pig common bile duct, distal colon and urinary bladder. SR 58611A and isoprenaline r...

journal_title：Pharmacology

authors： De Ponti F,Gibelli G,Crema F,Lecchini S

更新日期：1995-11-01 00:00:00

abstract：:We compared detailed efficacy of efonidipine and nifedipine, dihydropyridine analogues, and mibefradil using recombinant T- and L-type Ca2+ channels expressed separately in mammalian cells. All these Ca2+ channel antagonists blocked T-type Ca2+ channel currents (I(Ca(T))) with distinct blocking manners: I(Ca(T)) was b...

journal_title：Pharmacology

authors： Lee TS,Kaku T,Takebayashi S,Uchino T,Miyamoto S,Hadama T,Perez-Reyes E,Ono K

更新日期：2006-01-01 00:00:00

abstract：BACKGROUND/AIMS:Stent thrombosis is a serious complication after percutaneous coronary intervention and femoropopliteal endovascular intervention. The aim of this study was to determine the antithrombotic effects of a direct factor Xa inhibitor edoxaban alone or in combination with antiplatelet agents in a rat model of...

journal_title：Pharmacology

authors： Morishima Y,Honda Y,Kamisato C

更新日期：2019-01-01 00:00:00

abstract：:The present study was designed to examine the reaction pathway of colloidal bismuth subcitrate (CBS) with thiols. Studies were performed using the monothiol glutathione (GSH), the dithiol dithiothreitol (DTT) and the thiol enzymes papain and H+/K(+)-ATPase. UV-vis spectra showed that CBS forms complexes with GSH and D...

journal_title：Pharmacology

authors： Beil W,Bierbaum S,Sewing KF

更新日期：1993-08-01 00:00:00

abstract：:The influence of hyperthyroidism on the functional vascular responsiveness of isolated coronary and renal resistance vessels was investigated. Hyperthyroidism was established by feeding rats for 1 and 4 weeks with 5 mg/kg L-thyroxine (T4)-containing rat chow. Preparations of either coronary or renal resistance vessels...

journal_title：Pharmacology

authors： Zwaveling J,Pfaffendorf M,van Zwieten PA

更新日期：1997-09-01 00:00:00

abstract：:Increased concentrations of immunoreactive methionine-enkephalin but not leucine-enkephalin were measured in fractions of cerebrospinal fluid perfusate collected from ventricular-cisternally perfused, urethane-anesthetized rats exposed to a mixture of 75% nitrous oxide/25% oxygen for 60 min. These findings suggest tha...

journal_title：Pharmacology

authors： Quock RM,Kouchich FJ,Tseng LF

更新日期：1985-01-01 00:00:00

abstract：:The effect of fenfluramine, administered orally in a daily dose of 1 mg/kg for 40 days, on the disposition and rate of elimination of antipyrine was studied in 15 obese patients. Although the plasma half-life of antipyrine was unchanged, the apparent volume of distribution (1/kg) fell by 11.6% (p less than 0.001) and ...

journal_title：Pharmacology

authors： O'Malley K,Stevenson IH,West M

更新日期：1975-01-01 00:00:00

abstract：:It has previously been demonstrated in several species that the secretory granules of pancreatic beta-cells have the ability to store substantial amounts of calcium and bioactive amines, such as dopamine and serotonin. Furthermore, evidence for a similar topographical localization for amine and calcium within the peri...

journal_title：Pharmacology

authors： Ahrén B,Lundquist I

更新日期：1985-01-01 00:00:00

abstract：:An increase in pulmonary vascular resistance (PVR) after cyclooxygenase inhibition (COI) is well documented in the dog, but the site of vasoconstriction to chemically distinct cyclooxygenase inhibitors is largely unknown. The purpose of the present study was to examine and compare equimolar concentrations of three che...

journal_title：Pharmacology

authors： Endrédi J,el-Kashef HA,Hofman WF,Ehrhart IC

更新日期：1992-01-01 00:00:00

abstract：:The isolated whole stomach of the mouse has been used to study the effect of atropine on gastic acid secretion stimulated by acetylcholine, bethanechol and histamine. Atropine inhibited acid secretory response to acetylcholine and bethanechol in a competitive manner. The following pA2 values for atropine were calculat...

journal_title：Pharmacology

authors： Szelenyi I,Vergin H

更新日期：1980-01-01 00:00:00

abstract：:Hamster renal cytosol binds [3H]-2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD) with high specificity. Sucrose density gradient centrifugation revealed two binding entities- one with a low sedimentation coefficient of 4-5 S which was displaced by neither TCDD nor other polycyclic aromatic hydrocarbons (PAHs) and another w...

journal_title：Pharmacology

authors： Kurl RN,Loring JM,Villee CA

更新日期：1985-01-01 00:00:00

abstract：:Zinc acexamate (NAS-501), an anti-ulcer agent, has been reported to prevent various acute experimental gastric mucosal lesions and duodenal ulcers in rats. In order to clarify the mechanisms by which NAS-501 exhibits the anti-ulcer effects, we investigated the anti-oxidative effects of NAS-501 in vitro and in vivo. NA...

journal_title：Pharmacology

authors： Tsutsui Y,Nakamura Y,Yamaguchi S,Kawanaka N,Sato M

更新日期：1999-04-01 00:00:00

abstract：:A potential cytokine-drug interaction between interleukin 6 (IL-6) and itraconazole (ITZ) was studied using human hepatocytes in primary culture. Cultures from 5 adult males (mean age 42 +/- 15 years) who had not received any medicines known to interact with CYP3A4 were studied. Cultures were exposed to ITZ 500 ng/ml,...

journal_title：Pharmacology

authors： Gubbins PO,Melchert RB,McConnell SA,Franks AM,Penzak SR,Gurley BJ

更新日期：2003-04-01 00:00:00

abstract：:The purpose of this investigation on human umbilical arteries was: (1) to analyze the effects of magnesium (Mg2+) in the prevention of contractions induced by 5-hydroxytryptamine (5-HT), KCl, Bay K 8644 and BaCl2; (2) to determine whether the presence of Mg2+ could modulate the response to caffeine in Ca2+-free medium...

journal_title：Pharmacology

authors： Tiritilli A

更新日期：1998-12-01 00:00:00

abstract：:The influence of changes in the sodium balance on angiotensin II-induced pressor responses were studied in the pithed rat preparation, which is characterized by a highly activated renin-angiotensin-aldosterone system (RAAS) with high plasma renin and angiotensin II concentrations. The pressor response to angiotensin I...

journal_title：Pharmacology

authors： Knape JT,van Zwieten PA

更新日期：1988-01-01 00:00:00

abstract：:A comparison was made of the anti-ischemic effects of dihydropyridine calcium antagonists in isolated globally ischemic rat hearts. Pretreatment with amlodipine, nifedipine, nitredipine, or nisoldipine reduced reperfusion enzyme (lactate dehydrogenase) release and contracture after 25 min of global ischemia and 30 min...

journal_title：Pharmacology

authors： Grover GJ,Dzwonczyk S,Sleph PG

更新日期：1990-01-01 00:00:00

abstract：:Cimetidine infused intravenously into 6 healthy volunteers did not induce significant changes in plasma levels of prolactin (hPRL), thyreotropin (hTSH), gonadotropin (hLH and hFSH) and growth hormone (hGH). Conversely it caused a significant increase in prolactin response to TRH without modifying the hTSH response to ...

journal_title：Pharmacology

authors： Scarpignato C,Valenti G,Ceda GP,Bertaccini G

更新日期：1979-01-01 00:00:00

abstract：:Although proton pump inhibitors (PPI) are generally well tolerated, with most adverse effects being minor and self-limiting, there are singular reports on hypersensitivity immune reactions triggered by a PPI or its metabolites. Here we report a case of acute drug-induced fever with leukocytosis and a transient increas...

journal_title：Pharmacology

authors： Schiller D,Maieron A,Schöfl R,Donnerer J

更新日期：2014-01-01 00:00:00

abstract：:Five healthy subjects performed submaximal physical exercise approximately 20 h after a single oral dose of phenytoin (5 mg/kg of the sodium salt). The plasma levels of free fatty acids (FFA) increased 2- to 3-fold in the post-exercise period. In spite of this, the degree of plasma binding of phenytoin and its total c...

journal_title：Pharmacology

authors： Borgå O,Juhlin-Dannfeldt A,Dahlqvist R

更新日期：1978-01-01 00:00:00

abstract：:The mechanisms underlying the fade of the tetanic contraction induced by pancuronium were studied in vitro by means of myographical and electrophysiological techniques in the extensor digitorum longus muscle of the rat. Pancuronium (0.5 mumol/l) induced a complete fade of the tetanic contraction while leaving the twit...

journal_title：Pharmacology

authors： Gallacci M,Oliveira AC

更新日期：1994-10-01 00:00:00

abstract：:The activity of myocardial adenylate cyclase from two age groups (10-11 and 18-19 weeks old, respectively) of male spontaneously hypertensive rats (SHR) and their age-matched normotensive Wistar-Kyoto rats (WKY) was examined. Stimulation of the enzyme by isoproterenol and 5'-guanylyl-imidodiphosphate (GMP-PNP) was dec...

journal_title：Pharmacology

authors： Chiu TH

更新日期：1981-01-01 00:00:00

abstract：:Altered vascular reactivity due to endothelial dysfunction, consequent to vascular damage, is observed in rheumatoid arthritis. We investigated the effect of angiotensin (Ang)-(1-7) on vasculature changes in arthritis induced by complete Freund's adjuvant in male Wistar rats. Arthritis decreased soluble receptor for a...

journal_title：Pharmacology

authors： Açikalin Ö,Bölükbaşi Hatip FF,Tan RF,Hatip-Al-Khatib I

更新日期：2016-01-01 00:00:00

abstract：:In isolated perfused rat hearts with coronary occlusion and reperfusion, the effect of adenosine antagonists on the release of adenosine and its degradation products inosine, hypoxanthine, xanthine and uric acid was investigated. An antagonist with high selectivity for the A1 receptor, 8-phenyltheophylline, was applie...

journal_title：Pharmacology

authors： Bernauer W

更新日期：1996-11-01 00:00:00

abstract：AIM:This study investigates factors influencing the severity of opiate withdrawal symptoms, focusing on the relationship between methadone dose and withdrawal severity among opiate-dependent in-patients receiving methadone detoxification. METHODS:The sample comprised 48 opiate-dependent patients admitted to a speciali...

journal_title：Pharmacology

authors： Glasper A,Gossop M,de Wet C,Reed L,Bearn J

更新日期：2008-01-01 00:00:00

abstract：:The haemodynamic changes during epidural anaesthesia and following the administration of dihydroergotamine (DHE; 10 micrograms/kg i.v.) were studied in 7 dogs (epidural group). Epidural anaesthesia was associated with reductions in mean arterial, mean pulmonary arterial and mean right atrial pressures. Femoral flow wa...

journal_title：Pharmacology

authors： Zimpfer M,Schwarz M,Stanek B,Raberger G

更新日期：1981-01-01 00:00:00

abstract：AIM:To evaluate the efficacy and safety of 2 analogs of L-carnitine on rats made insulin resistant by a high-fructose diet. METHODS:Using rats made insulin resistant by a high-fructose diet, we investigated the impact of 2 analogs of L-carnitine (25 mg/kg) and L-carnitine (250 mg/kg) on glucose, triglycerides and chol...

journal_title：Pharmacology

authors： Gómez-Solís A,De la Cruz-Cordero R,Avalos-Soriano A,Duarte-Vázquez MA,Reyes-Esparza J,Rodríguez-Fragoso L

更新日期：2011-01-01 00:00:00

abstract：:We established an Ascaris-induced biphasic skin allergic reaction in mice. In the early-phase reaction (EPR), mast cell degranulation was observed, and tranilast inhibited ear edema. In mast-cell-deficient mice (WBB6F(1)-W/W(V) mice), ear edema in the EPR disappeared, whereas that in the late-phase reaction (LPR) rema...

journal_title：Pharmacology

authors： Sengoku T,Sato S,Sakuma S,Ogawa T,Ohkubo Y,Goto T

更新日期：2001-01-01 00:00:00

abstract：:Metabotropic G protein-coupled receptors have recently been recognized as targets for anesthetics and analgesics. In particular, G(q)-coupled receptors such as muscarinic M(1) receptors (M(1)R) and 5-hydroxytryptamine (5-HT) type 2A receptors have been reported to be targets for anesthetics. Much less is known, howeve...

journal_title：Pharmacology

authors： Minami K,Uezono Y,Shiraishi M,Okamoto T,Ogata J,Horishita T,Taniyama K,Shigematsu A

更新日期：2004-11-01 00:00:00

abstract：:We investigated the total urinary kallikrein levels, left-ventricular wall thickness and mean arterial blood pressure of nontreated and captopril-treated diabetic and nondiabetic spontaneously hypertensive rats. The mean arterial blood pressure was significantly elevated in diabetic spontaneously hypertensive rats as ...

journal_title：Pharmacology

authors： Sharma JN,Kesavarao U

更新日期：2002-04-01 00:00:00

abstract：:Mast cells from different locations are shown to vary in their histochemical, ultrastructural, cytochemical and functional properties. The clinical consequences of this heterogeneity and possible reasons for its origin are discussed. ...

journal_title：Pharmacology

authors： Pearce FL

更新日期：1986-01-01 00:00:00