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#1Sho-Ya Wang (University at Albany, SUNY)H-Index: 36
#2Edward Moczydlowski (Clarkson University)H-Index: 32
Last. Ging Kuo Wang (Brigham and Women's Hospital)H-Index: 6
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After transient transfection of an hNav1.4-L443C/A444W mutant clone, HEK-293 cells exhibited large inactivation-deficient Na+ currents. We subsequently established a stable cell line expressing robust inactivation-deficient Na+ currents. Persistent late Na+ currents were far more sensitive to block by class 1 anti-arrhythmic flecainide, mexiletine, propafenone, and amiodarone at 10 μ M than peak Na+ currents. Such results support a hypothesis that persistent late Na+ currents are in vivo targets...
3 CitationsSource
#1Robert S. Ames (GSK: GlaxoSmithKline)H-Index: 28
#2Parvathi Nuthulaganti (GSK: GlaxoSmithKline)H-Index: 12
Last. Nabil Elshourbagy (GSK: GlaxoSmithKline)H-Index: 27
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Recombinant baculoviruses, in which the insect cell–specific polyhedrin promoter has been replaced with a mammalian cell–active expression cassette (BacMam viruses), are efficient gene delivery vehicles for many mammalian cell types. BacMam viruses have been generated for expression of G protein–coupled receptors (GPCRs) and used to establish Ca2+mobilization assays in HEK-293 human embryonic kidney cells and U-2 OS human osteosarcoma cells. U-2 OS cells are highly susceptible to BacMam-based ge...
27 CitationsSource
#1Robert S. Ames (GSK: GlaxoSmithKline)H-Index: 28
#2James A. Fornwald (GSK: GlaxoSmithKline)H-Index: 10
Last. Michael A. Romanos (GSK: GlaxoSmithKline)H-Index: 15
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With completion of the sequencing of the human and mouse genomes, the primary sequences of close to 400 non-olfactory G protein–coupled receptors (GPCRs) have been determined. There are intensive efforts within the pharmaceutical industry to discover and develop new therapeutic agents acting via GPCRs. In addition, there is a concerted effort to identify potential new drug targets from the remaining 150+ orphan GPCRs through the identification of their ligands. Access to functionally expressed r...
56 CitationsSource
#1Scott R. HamannH-Index: 12
#2Hammad MalikH-Index: 1
Last. Elzbieta P. WalaH-Index: 14
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Sex and age influence morphine analgesia in humans and animals. Mature rats show greater morphine analgesia in males than in females. Ultra-low doses of naltrexone enhance morphine analgesia. In mature rats (18–22 weeks), naltrexone (0.002–2.0 mg/kg)-morphine (2 mg/kg) cotreatment enhanced morphine analgesia in females, an effect inversely related to naltrexone dose. Conversely, in mature male rats, naltrexone tended to decrease morphine analgesia with increasing dose. In young rats (8–10 weeks)...
13 CitationsSource
#2S RoseH-Index: 2
Last. V BozonH-Index: 3
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The initial objective of this work was to examine the effects of an antibody (Anti-G21V) directed against the second extracellular loop of human heart 5-HT4 receptors expressed in Chinese hamster ovary (CHO) cells. The antibody anti-G21V had no effect upon either basal cAMP– or 5-HT–evoked increases in cAMP in CHO cells, whereas it had shown an agonist-like effect in COS-7 cells. Analysis of agonist fractions of h5-HT4(e) receptors in CHO and COS-7 cells revealed that equilibrium constant could ...
2 CitationsSource
#1Janusz Gabrys (Medical University of Silesia)H-Index: 6
#2Janusz Konecki (Medical University of Silesia)H-Index: 5
Last. Jashovam Shani (HUJI: Hebrew University of Jerusalem)H-Index: 28
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Tissue levels of nineteen amino acids and total free amino acids, were assayed by gas-liquid chromatography in cytosols of rat atrial and ventricular muscle cardiomiocytes. The tissues were assayed after the rats had been administered IP with the three cardioactive drugs, exerting a significant effect on their heart action: propranolol, pentylenetetrazol and reserpine. It was demonstrated that while in the atrial and ventricular cardiac muscle cytosols of control rats, arginine, glutamine and cy...
2 CitationsSource
#2Ian FindlayH-Index: 15
Last. V BozonH-Index: 3
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In human atrial myocytes, serotonin rather than sympathetic, stimulation is more frequently associated with atrial fibrillation. So does the arrhythmogenic effect of serotonin result from the mechanism of action of the receptor or the context of its action upon cardiac myocytes? The capacity of agonists to produce cAMP followed the sequence 5-HT < Iso < Forskolin to increase ICaL with 5-HT = Iso = Forskolin. The simultaneous application of threshold concentrations of 5-HT and Iso maximally incre...
3 CitationsSource
#1Mahmoud M. KhattabH-Index: 16
Last. M. RazaH-Index: 14
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Objectives were to investigate the effect of nonselective nitric oxide synthase (NOS) inhibitor, L-NAME on codeine-induced analgesia and to see the role of NO in its antinociceptive effect. Also, to see if L-NAME can potentiate the antinociceptive response of sub-effective dose of codeine and to explore if opioid receptors have some role to play in L-NAME effects. Mice were injected with selected doses of codeine or other selected agents intraperitoneally and the latency to hot plate was recorde...
3 CitationsSource
#1Janusz Gabrys (Medical University of Silesia)H-Index: 6
#2Janusz Konecki (Medical University of Silesia)H-Index: 5
Last. Jashovam Shani (HUJI: Hebrew University of Jerusalem)H-Index: 28
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Levels of the 19 proteinous amino acids and total free amino acids were assayed by gas-liquid chromatography in cytosols of rat atrial and ventricular muscle cardiomiocytes. The tissues were assayed after the rats had been exposed to the cardioactive drugs digoxin, caffeine, and isoproterenol, each having different mechanisms of action. We demonstrated that, in the atrial and ventricular cardiac muscle cytosol of control (untreated) rats, arginine, glutamine, and cysteine existed in their highes...
1 CitationsSource
#1Mahmoud M. Khattab (KSU: King Saud University)H-Index: 16
#2Mobasher Ahmad (KSU: King Saud University)H-Index: 3
Last. M. Raza (KSU: King Saud University)H-Index: 14
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Losartan, an angiotensin II type-1 receptor (AT1) antagonist, was used to investigate whether it can offer protection against the sustained hypertension, cardiac hypertrophy, and renal damage induced by chronic inhibition of nitric oxide (NO) by Nω-nitro-L-arginine methyl ester (L-NAME). We studied the involvement of both NO metabolism and oxidative stress in L-NAME-induced hypertension, and how AT1 receptor antagonism may interact. Male Wistar albino rats were subjected to NO synthesis inhibiti...
13 CitationsSource
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