Search Results - "Beleta, J."

The human area postrema and other nuclei related to the emetic reflex express cAMP phosphodiesterases 4B and 4D by Mori, F., Pérez-Torres, S., De Caro, R., Porzionato, A., Macchi, V., Beleta, J., Gavaldà, A., Palacios, J.M., Mengod, G.

“…Phosphodiesterase 4 (PDE4) inhibitors, i.e. rolipram, are being extensively investigated as therapeutic agents in several diseases. Emesis is one of the most…”
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Pharmacological blockade of CCR1 ameliorates murine arthritis and alters cytokine networks in vivo by Amat, M, Benjamim, C F, Williams, L M, Prats, N, Terricabras, E, Beleta, J, Kunkel, S L, Godessart, N

“…Background and purpose: The chemokine receptor CCR1 is a potential target for the treatment of rheumatoid arthritis. To explore the impact of CCR1 blockade in…”
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Bronchodilator and anti‐inflammatory activities of glaucine: In vitro studies in human airway smooth muscle and polymorphonuclear leukocytes by Cortijo, J, Villagrasa, V, Pons, R, Berto, L, Martí‐Cabrera, M, Martinez‐Losa, M, Domenech, T, Beleta, J, Morcillo, E J

“…Selective phosphodiesterase 4 (PDE4) inhibitors are of potential interest in the treatment of asthma. We examined the effects of the alkaloid S‐(+)‐glaucine, a…”
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Characterization of human serotonin 1D and 1B receptors using [3H]-GR-125743, a novel radiolabelled serotonin 5HT1D/1B receptor antagonist by Doménech, T, Beleta, J, Palacios, J M

“…The study of serotonin (5-HT) receptors from the points of view of their anatomical localization and pharmacological characterization has been linked to the…”
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Investigation into the role of phosphodiesterase IV in bronchorelaxation, including studies with human bronchus by Cortijo, J., Bou, J., Beleta, J., Cardelús, I., Llenas, J., Morcillo, E., Gristwood, R.W.

“…1 We have investigated the role of cyclic nucleotide phosphodiesterase IV (PDEIV) in the relaxation of human bronchus and guinea‐pig trachea in vitro and in…”
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Selective induction of cyclo‐oxygenase‐2 activity in the permanent human endothelial cell line HUV‐EC‐C: biochemical and pharmacological characterization by Miralpeix, Montserrat, Camacho, Mercedes, López‐Belmonte, Jesús, Canalías, Francesca, Beleta, Jordi, Ma Palacios, José, Vila, Luis

“…Cyclo‐oxygenase (COX), the enzyme responsible for the conversion of arachidonic acid (AA) to prostaglandin H2 (PGH2), exists in two forms, termed COX‐1 and…”
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Synthesis and biological evaluation of a conformationally free seco-analogue of the immunosuppressant FR901483 by BONJOCH, J, DIABA, F, PUIGBO, G, SOLE, D, SEGARRA, V, SANTAMARIA, L, BELETA, J, RYDER, H, PALACIOS, J.-M

“…The synthesis of an azaspirocyclic analogue of FR901483, phosphate 2, is described based on the implementation of a key 5-endo aminocyclization promoted by…”
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Second messenger systems as targets for new therapeutic agents: focus on selective phosphodiesterase inhibitors by Palacios, J M, Beleta, J, Segarra, V

“…Second messengers are intracellular substances whose concentration is regulated by the action on their specific receptors of extracellular regulatory molecules…”
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Resident Cell Chemokine Expression Serves as the Major Mechanism for Leukocyte Recruitment During Local Inflammation by Garcia-Ramallo, Eva, Marques, Teresa, Prats, Neus, Beleta, Jordi, Kunkel, Steven L, Godessart, Nuria

“…The mechanistic relationships between initiating stimulus, cellular source and sequence of chemokine expression, and leukocyte recruitment during inflammation…”
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Studies on the cardiac actions of flosequinan in vitro by Gristwood, R.W., Beleta, J., Bou, J., Cardelús, I., Fernández, A.G., Llenas, J., Berga, P.

“…1 We have investigated the in vitro cardiac actions of flosequinan and of its major metabolite in man, BTS 53554. 2 Positive inotropic activity was seen with…”
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Identification and characterization of serotonin 5-HT4 receptor binding sites in human brain: comparison with other mammalian species by Doménech, T, Beleta, J, Fernández, A G, Gristwood, R W, Cruz Sánchez, F, Tolosa, E, Palacios, J M

“…Specific binding for the 5-HT4-selective radioligand [3H]GR 113808 has been identified in human and calf brain membranes. Using human tissue the distribution…”
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Synthesis and Biological Evaluation of 3,4-Diaryloxazolones:  A New Class of Orally Active Cyclooxygenase-2 Inhibitors by Puig, Carles, Crespo, María I, Godessart, Núria, Feixas, Joan, Ibarzo, Javier, Jiménez, Juan-Miguel, Soca, Lídia, Cardelús, Ignasi, Heredia, Ascensión, Miralpeix, Montserrat, Puig, Jaume, Beleta, Jordi, Huerta, Josep M, López, Manel, Segarra, Victor, Ryder, Hamish, Palacios, José M

“…A series of 3,4-diaryloxazolones were prepared and evaluated for their ability to inhibit cyclooxygenase-2 (COX-2). Extensive structure−activity relationship…”
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Synthesis and Biological Evaluation of 2-Phenylpyran-4-ones:  A New Class of Orally Active Cyclooxygenase-2 Inhibitors by Caturla, Francisco, Jiménez, Juan-Miguel, Godessart, Núria, Amat, Mercè, Cárdenas, Alvaro, Soca, Lídia, Beleta, Jordi, Ryder, Hamish, Crespo, María I

“…A series of 2-phenylpyran-4-ones were prepared and evaluated for their ability to inhibit cyclooxygenase-2 (COX-2). Extensive structure−activity relationship…”
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Synthesis and Structure−Activity Relationships of Novel Histamine H 1 Antagonists:  Indolylpiperidinyl Benzoic Acid Derivatives by Fonquerna, Silvia, Miralpeix, Montse, Pagès, Lluís, Puig, Carles, Cardús, Arantxa, Antón, Francisca, Cárdenas, Álvaro, Vilella, Dolors, Aparici, Mónica, Calaf, Elena, Prieto, José, Gras, Jordi, Huerta, Josep M., Warrellow, Graham, Beleta, Jorge, Ryder, Hamish

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Discovery and Characterization of 4'-(2-Furyl)-N-pyridin-3-yl-4,5'-bipyrimidin-2'-amine (LAS38096), a Potent, Selective, and Efficacious A sub(2B) Adenosine Receptor Antagonist by Vidal, B, Nueda, A, Esteve, C, Domenech, T, Benito, S, Reinoso, R F, Pont, M, Calbet, M, Lopez, R, Cadavid, MI, Loza, MI, Cirdenas, A, Godessart, N, Beleta, J

“…A novel series of N-heteroaryl 4'-(2-furyl)-4,5'-bipyrimidin-2'-aniines has been identified as potent and selective A sub(2B) adenosine receptor antagonists…”
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Benzyl Derivatives of 2,1,3-Benzo- and Benzothieno[3,2-a]thiadiazine 2,2-Dioxides:  First Phosphodiesterase 7 Inhibitors by Martínez, Ana, Castro, Ana, Gil, Carmen, Miralpeix, Montserrat, Segarra, Victor, Doménech, Teresa, Beleta, Jorge, Palacios, Jose M, Ryder, Hamish, Miró, Xavier, Bonet, Carles, Casacuberta, Josep M, Azorín, Ferran, Piña, Benjamí, Puigdoménech, Pere

“…The synthesis of a new family of benzyl derivatives of 2,1,3-benzo- and benzothieno[3,2-a]thiadiazine 2,2-dioxides was achieved. The biological data revealed…”
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Pharmacological characterization of almotriptan: an indolic 5-HT receptor agonist for the treatment of migraine by Bou, Josep, Domènech, Teresa, Puig, Jaume, Heredia, Ascensión, Gras, Jordi, Fernández-Forner, Dolors, Beleta, Jorge, Palacios, José M.

“…Almotriptan (3-[2-(dimethylamino)ethyl]-5-(pyrrolidin-1-ylsulfonylmethyl)-1 H-indole) has been studied in several models predictive of activity and selectivity…”
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Synthesis and structure–activity relationships of piperidinylpyrrolopyridine derivatives as potent and selective H 1 antagonists by Fonquerna, Silvia, Miralpeix, Montse, Pagès, Lluís, Puig, Carles, Cardús, Arantxa, Antón, Francisca, Vilella, Dolors, Aparici, Mónica, Prieto, José, Warrellow, Graham, Beleta, Jorge, Ryder, Hamish

“…[Display omitted] The synthesis and structure–activity relationships of piperidinylpyrrolopyridines as potent and selective H 1 antagonists are discussed. It…”
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Synthesis and biological evaluation of 2,5-dihydropyrazolo[4,3- c]quinolin-3-ones, a novel series of PDE 4 inhibitors with low emetic potential and antiasthmatic properties by Crespo, Marı́a I, Gràcia, Jordi, Puig, Carles, Vega, Armando, Bou, Josep, Beleta, Jordi, Doménech, Teresa, Ryder, Hamish, Segarra, Vı́ctor, Palacios, José M

“…A novel series of 2,5-dihydropyrazolo[4,3- c]quinolin-3-ones has been prepared. These compounds showed good PDE 4 inhibitory activity and weak affinity for…”
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Pharmacological Profile of LAS 31180, a New Inotropic/Vasodilator Quinolone Derivative by Gras, Jordi, Cardelûs, Ignasi, Beleta, Jorge, Gristwood, Robert W, Maria Palacios, José, Llenas, Jesús

“…Summary LAS 31180 (3-methylsulphonylamino-l-methyl-4(1H)-quinolone, CAS 137338-43-3) was found to have positive inotropic and vasodilator properties through…”
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