Jesús Llenas

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Aclidinium bromide is a novel potent, long-acting inhaled muscarinic antagonist in development for the treatment of chronic obstructive pulmonary disease. Aclidinium showed subnanomolar affinity for the five human muscarinic receptors (M(1)-M(5)). [(3)H]Aclidinium dissociated slightly faster from M(2) and M(3) receptors than [(3)H]tiotropium but much more(More)
1. We have investigated the role of cyclic nucleotide phosphodiesterase IV (PDE IV) in the relaxation of human bronchus and guinea-pig trachea in vitro and in guinea-pigs in vivo. 2. Functional studies showed that the selective PDE IV inhibitors, rolipram and denbufylline, relaxed human and guinea-pig preparations in vitro. 3. Two clinically used xanthine(More)
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 flosequinan in guinea-pig isolated ventricles, the threshold concentration for effect being less than 1 x 10(-5) M. BTS 53554 was approximately half as potent as the parent compound. 3. In guinea-pig(More)
In an attempt to extend the hypothesis that activation of vascular postsynaptic alpha 2-adrenoceptors requires an influx of Ca2+ ions, the effects of 2 calcium entry blocking drugs verapamil and cinnarizine have been examined as inhibitors of the pressor responses to methoxamine and B-HT 920 in autoperfused dog hindlimb preparations. Verapamil (0.1-1 mg(More)
The group of drugs known as "calcium antagonists' is under extensive investigation in experimental animals and man and a re-evaluation of their pharmacological properties is overdue. Recent proposals to adopt the more specific nomenclature of calcium entry blockers for some of these compounds (Vanhoutte & Bohr, 1981) should be supported since there is much(More)
We have carried out experiments to re-evaluate the influence of ketoconazole (400 mg kg-1,p.o.) on the effects of ebastine, terfenadine and loratadine on the QTc interval in conscious guinea-pigs. Following a previously described protocol of oral drug administration, but using telemetric recording of the ECG, we have found that the prolongation of the QTc(More)
Sepsis is intricately associated with mesenteric ischemia. The remote complications of mesenteric ischemia are essentially those of sepsis, whether as a cause or as a consequence. Experimental endotoxic shock induces bowel hypoperfusion, erythrocyte extravasation and intestinal necrosis. The effects of pentoxifylline, rolipram and denbufylline, three(More)
OBJECTIVE The clinical use of some nonsedating H1 antihistamines (histamine H1 receptor antagonists) has been associated with a rare but life-threatening type of arrhythmia, torsade de pointes, especially when these drugs are coadministered with cytochrome P450 (CYP) 3A4 enzyme inhibitors. On the basis of the latter observation and the fact that most of(More)
This paper describes the vascular effects of almotriptan in comparison with sumatriptan in human vessels and tissues in vitro. The contractile properties of almotriptan and sumatriptan were evaluated in vitro in the following arteries: meningeal, temporal, basilar, internal carotid, ophthalmic, pulmonary and coronary. In addition, the effects of almotriptan(More)
A series of arylimino-1,2,4-thiadiazolidines were prepared using an efficient synthesis starting from thiadiazolopyridinium chlorides. All the compounds showed smooth muscular relaxant properties in rat portal veins. The different behaviour under highly depolarized conditions and the reduction of the biological effect by glyburide suggests that the(More)