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The sphingosine-1-phosphate receptor-1 antagonist, W146, causes early and short-lasting peripheral blood lymphopenia in mice.

The results support the hypothesis that lymphopenia evoked by S1P1 agonists is due to functional antagonism of S 1P1 in lymphocytes, and it is shown that both the S1p1 antagonist and a S1 P1 agonist cause lymph Openia in vivo in spite of their different effects on receptor expression in vitro.
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Prediction of the skin permeability of topical drugs using in silico and in vitro models.

Overall, the studied in silico and the in vitro models are useful tools to support selection and characterization of research compounds in terms of skin permeability.
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Discovery of imidazo[1,2-b][1,2,4]triazines as GABA(A) alpha2/3 subtype selective agonists for the treatment of anxiety.

Compound 11 shows good bioavailability and half-life in preclinical species, and it is a nonsedating anxiolytic in both rat and squirrel monkey behavioral models, leading to the identification of a clinical candidate.
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Ultra-performance liquid chromatography coupled to time-of-flight mass spectrometry for robust, high-throughput quantitative analysis of an automated metabolic stability assay, with simultaneous…

The application of ultra-performance liquid chromatography coupled to time-of-flight mass spectrometry (UPLC/TOFMS) for high-throughput analysis of a 96-well plate based metabolic stability assay has been investigated, producing quantitative data for the test compound equivalent to that obtained by high-performanceliquid chromatography with tandem mass Spectrometric detection on a triple quadrupole instrument.
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Discovery of a Potent, Selective, and Orally Available PI3Kδ Inhibitor for the Treatment of Inflammatory Diseases.

The optimization of a series of pyrrolotriazinones as potent and selective PI3Kδ inhibitors is described, leading to the identification of LAS191954 as a candidate for clinical development.
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Novel triazolopyridylbenzamides as potent and selective p38α inhibitors.

Synthesis and SAR was directed towards the improvement of binding affinity, as well as ADME properties for this new class of p38α inhibitors and ultimately afforded compounds showing good in vivo efficacy.
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Non-basic ligands for aminergic GPCRs: the discovery and development diaryl sulfones as selective, orally bioavailable 5-HT2A receptor antagonists for the treatment of sleep disorders.

This work further demonstrate that oral bioavailability of a given series can be enhanced by improving physicochemical parameters such as log P, and corroborates the growing evidence that a protonated amine is not essential for affinity at aminergic GPCRs.
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A novel inhaled PI3Kδ inhibitor, LAS194223 reduces allergen-induced airway inflammation in rat

The inhaled administration of the LAS194223 inhibits OVA induced changes in lung function and inflammation and suggests that PI3Kd inhibition, by inhaled route could be a potential treatment for asthma and COPD.

Discovery of a novel class of zwitterionic, potent, selective and orally active S1P₁ direct agonists.

Amido-1,3,4-thiadiazoles have been identified as a novel structural class of potent and selective sphingosine-1-phosphate receptor subtype 1 agonists with good selectivity and excellent in vivo efficacy in rat models.
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NK1 antagonists based on seven membered lactam scaffolds.

A new class of high affinity hNK1R antagonists based on seven-membered ring cores has been identified, which includes compounds with high affinity, good selectivity, and promising in vivo properties.
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