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Structure-based discovery of opioid analgesics with reduced side effects
TLDR
PZM21 is a potent Gi activator with exceptional selectivity for μOR and minimal β-arrestin-2 recruitment and is devoid of both respiratory depression and morphine-like reinforcing activity in mice at equi-analgesic doses. Expand
Regulation of Salmonella pathogenicity island 2 genes by independent environmental signals.
TLDR
It is reported that expression of SPI2 genes can be induced independently by two different environmental stimuli and limitation of inorganic phosphate in the growth media led to activation of SPI1 genes in the late exponential growth phase and was independent of the media pH. Expand
Tricyclic antidepressants, quinacrine and a novel, synthetic chimera thereof clear prions by destabilizing detergent‐resistant membrane compartments
TLDR
The data suggest that a cocktail of drugs targeting the lipid metabolism that controls PrP conversion may be the most efficient in treating Creutzfeldt‐Jakob disease. Expand
Recent advances in the search for D3- and D4-selective drugs: probes, models and candidates.
TLDR
The very recent publication of the X-ray crystal structure of D(3) should facilitate efficient discovery of unprecedented chemotypes and the development of D (3)-selective agonists, functionally selective ligands and the exploitation of homo- and heteromers remain challenging. Expand
GPCR crystal structures: Medicinal chemistry in the pocket.
TLDR
The current state of solved GPCR structures are summarized, with a particular focus on ligand-receptor interactions in the binding pocket, and how this can contribute to the design of G PCR ligands with better affinity, subtype selectivity or efficacy. Expand
Azaindole derivatives with high affinity for the dopamine D4 receptor: synthesis, ligand binding studies and comparison of molecular electrostatic potential maps.
TLDR
Piperazinylmethyl substituted pyrazolo[1,5-a]pyridines and related heterocycles were synthesized and found to recognize selectively the dopamine D4 receptor and a Ki value of 2.0 nM was observed. Expand
FAUC 213, a highly selective dopamine D4 receptor full antagonist, exhibits atypical antipsychotic properties in behavioural and neurochemical models of schizophrenia
TLDR
Evidence is gathered that FAUC 213 exhibits atypical antipsychotic characteristics and is not believed to mediate the above-mentioned effects via D2 receptor antagonism, but a partial involvement of 5-HT2- and α1-receptors cannot be ruled out at present. Expand
Epidermal growth factor and prostaglandin E2 accelerate mucosal recovery from stress-induced gastric lesions via inhibition of apoptosis
TLDR
EGF and PGE accelerate healing of stress-induced lesions due to the attenuation of apoptosis via upregulation of bcl-2 in gastric mucosa in rats pretreated with EGF or 16,16 dm-PGE(2). Expand
Tissue distribution of radioiodinated FAUC113: assessment of a pyrazolo(1,5-a) pyridine based dopamine D4 receptor radioligand candidate.
TLDR
Radioiodinated FAUC 113 does not allow imaging of D4 receptors in the rat brain in vivo nor in vitro, and further work should aim at the development of selective dopamine D4 radioligands with improved tracer characteristics, such as receptor affinity and subtype selectivity, specific activity or blood-brain barrier permeability. Expand
Synthesis and binding profile of haloperidol-based bivalent ligands targeting dopamine D(2)-like receptors.
TLDR
The development of a series of novel bivalent molecules with a pharmacophore derived from the dopamine receptor antagonist haloperidol is described, which indicated a bivalent binding mode with a simultaneous occupancy of two neighboring binding sites. Expand
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