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5-HT2C receptor agonists: pharmacological characteristics and therapeutic potential.
TLDR
The results suggest that 5-HT2C receptor agonism is associated with therapeutic potential in obsessive compulsive disorder and depression. Expand
An NS3 protease inhibitor with antiviral effects in humans infected with hepatitis C virus
TLDR
Administration of BILN 2061 to patients infected with HCV genotype 1 for 2 days resulted in an impressive reduction of HCV RNA plasma levels, and established proof-of-concept in humans for an HCV NS3 protease inhibitor, illustrating the potential of the viral-enzyme-targeted drug discovery approach for the development of new HCV therapeutics. Expand
Characterization of Ro 04‐6790 and Ro 63‐0563: potent and selective antagonists at human and rat 5‐HT6 receptors
TLDR
In rats habituated to observation cages, Ro 04‐6790 produced a behavioural syndrome similar to that seen following treatment with antisense oligonucleotides designed to reduce the expression of 5‐HT6 receptors, suggesting that the compounds are neither agonists nor inverse agonists at the 5‐ HT6 receptor. Expand
Influence of the 5-HT6 receptor on acetylcholine release in the cortex: pharmacological characterization of 4-(2-bromo-6-pyrrolidin-1-ylpyridine-4-sulfonyl)phenylamine, a potent and selective 5-HT6
TLDR
A functional correlation between 5-HT(6) receptors and cholinergic neurotransmission could be shown, supporting the therapeutic potential of 5- HT( 6) receptors in the treatment of cognitive deficits. Expand
The 5-hydroxytryptamine6 receptor-selective radioligand [3H]Ro 63-0563 labels 5-hydroxytryptamine receptor binding sites in rat and porcine striatum.
TLDR
The affinities of 14 5-HT6 receptor ligands at this binding site were similar to those found for the recombinant rat and human 5- HT6 receptor, which suggested the presence of 5-hydroxytryptamine6 receptors in porcine striatum. Expand
Involvement of 5‐HT6 receptors in nigro‐striatal function in rodents
TLDR
The data support earlier conclusions from experiments with antisense oligonucleotides that the 5‐HT6 receptor is involved in the control of acetylcholine neurotransmission in the rat brain. Expand
Discovery of BI 224436, a Noncatalytic Site Integrase Inhibitor (NCINI) of HIV-1.
TLDR
An assay recapitulating the 3' processing activity of HIV-1 integrase (IN) was used to screen the Boehringer Ingelheim compound collection, leading to the discovery of compound 26 (BI 224436), the first NCINI to advance into a phase Ia clinical trial. Expand
5-HT(6) receptor antagonists: lead optimisation and biological evaluation of N-aryl and N-heteroaryl 4-amino-benzene sulfonamides.
TLDR
Compounds with a logD profile indicative of brain penetration have been subjected to in vivo testing for reversal of a scopolamine-induced retention deficit in a passive avoidance paradigm and RO-04-6790 (6a) has been identified. Expand
Preclinical Profile of BI 224436, a Novel HIV-1 Non-Catalytic-Site Integrase Inhibitor
TLDR
BI 224436 has drug-like in vitro absorption, distribution, metabolism, and excretion properties, including Caco-2 cell permeability, solubility, and low cytochrome P450 inhibition, and has an additive effect in combination with most approved antiretrovirals, including INSTIs. Expand
5HT2C receptor agonists exhibit antidepressant-like properties in the anhedonia model of depression in rats
TLDR
A role for 5HT2C receptors in some aspects of depression, and potential antidepressant properties for selective 5 HT2C receptor agonists were investigated in stress-induced anhedonia, a validated simulation of depression are suggested. Expand
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