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The novel antiepileptic drug levetiracetam (ucb L059) appears to act via a specific binding site in CNS membranes.
TLDR
The presence of specific binding sites for [3H]levetiracetam in rat central nervous system (CNS) and a possible role of this binding site in the anticonvulsant activity of levetir acetam support the singular pharmacological profile of this compound.
Anti‐proliferative and apoptotic effects of anandamide in human prostatic cancer cell lines: Implication of epidermal growth factor receptor down‐regulation and ceramide production
Anandamide (ANA) is an endogenous lipid which acts as a cannabinoid receptor ligand and with potent anticarcinogenic activity in several cancer cell types.
Pharmacological and functional characterisation of the wild-type and site-directed mutants of the human H1 histamine receptor stably expressed in CHO cells.
TLDR
A cDNA clone for the human histamine H1 receptor was isolated from a lung cDNA library and stably expressed in CHO cells, resulting in a dramatic decrease of the affinity for histamine binding, and for the histamine-induced polyphosphoinositides breakdown, whereas the affinity towards antagonists was not significantly modified.
Scavenger and antioxidant properties of ten synthetic flavones.
TLDR
It is found that the presence of the pyrogallol moiety in the B component of flavones gave rise to radical scavenger activity and that C-6 substituted hydroxyl group may also provide the basis for biological activity.
Novel 4-oxo-1,4-dihydroquinoline-3-carboxamide derivatives as new CB2 cannabinoid receptors agonists: synthesis, pharmacological properties and molecular modeling.
TLDR
4-oxo-1,4-dihydroquinoline-3-carboxamide derivatives constitute a new class of potent and selective CB(2) cannabinoid receptors agonists.
Benzoselenazolinone derivatives designed to be glutathione peroxidase mimetics feature inhibition of cyclooxygenase/5-lipoxygenase pathways and anti-inflammatory activity.
TLDR
The diselenides were shown to be very potent (up to 3 times the activity of ebselen), whereas the benzoselenazolinones were inactive, thus confirming the hypothesis that glutathione peroxidase mimics have anti-inflammatory properties.
Structural insights into human 5-lipoxygenase inhibition: combined ligand-based and target-based approach.
TLDR
The human 5-LOX enzyme and its interaction with competitive inhibitors were investigated by means of a combined ligand-based and target-based approach and the proposal of an interaction model inside the 5- LOX active site.
Antiproliferative effects of isopentenylated coumarins isolated from Phellolophium madagascariense Baker
TLDR
The anticancer activity of the three isolated compounds and of a synthetic sample of osthol was evaluated on L1210 mouse leukemia and on human prostatic cancer hormonosensitive LNCaP and hormonoindependent PC3 and DU145 cell lines.
New Advances on Prostate Carcinogenesis and Therapies: Involvement of EGF-EGFR Transduction System
TLDR
Last advances on molecular mechanisms that might be responsible for sustained growth and survival of PC cells are described and emphasis is on intracellular signaling cascades which are involved in the mitogenic and antiapoptotic effects of epidermal growth factor EGF-EGFR system.
Synthesis and biological evaluation of phenstatin metabolites.
TLDR
Eight main metabolites of phenstatin have been confirmed by synthesis and their biological properties have been reported, and the identification of this active metabolite led to the design and synthesis of analogs with potent in vitro cytotoxicity and inhibition of microtubule assembly.
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