Prevention of Colorectal Carcinogenesis by DNA-Binding Small-Molecule Curaxin CBL0137 Involves Suppression of Wnt Signaling.

Chemoprevention is considered a valid approach to reduce the incidence of colorectal cancer, one of the most common malignancies worldwide. Here, we investigated the tumor-preventive activity of curaxin CBL0137. This compound represents a new class of nonmutagenic DNA-binding small molecules that alter chromatin stability and inhibit the function of the histone chaperone FACT.

AVN-492, A Novel Highly Selective 5-HT6R Antagonist: Preclinical Evaluation.

Discovery of 5-HT6 receptor subtype and its exclusive localization within the central nervous system led to extensive investigations of its role in Alzheimer's disease, schizophrenia, and obesity. In the present study, we present preclinical evaluation of a novel highly-potent and highly-selective 5-HT6R antagonist, AVN-492. The affinity of AVN-492 to bind to 5-HT6R (Ki = 91 pM) was more than three orders of magnitude higher than that to bind to the only other target, 5-HT2BR, (Ki = 170 nM).

BP101 Peptide Promotes Female Sexual Receptivity in the Rat.

Introduction: Low sexual desire is a frequent sexual problem in women, with only one drug for the condition approved by the Food and Drug Administration.

Aim: To evaluate the ability of a novel synthetic peptide, BP101, to facilitate sexual behavior after intranasal administration or infusion into certain brain areas in female rats.

Methods: Bilaterally ovariectomized female rats, primed with a suboptimal combination of estradiol benzoate (EB) and progesterone, were used as a model of low sexual motivation.

Rapatar, a nanoformulation of rapamycin, decreases chemically-induced benign prostate hyperplasia in rats.

Benign prostatic hyperplasia (BPH) is the most common age-related disease in men. Here we tested the efficacy of Rapatar, a micellar nanoformulation of rapamycin, in two rat models of BPH: testosterone-induced and sulpiride-induced hyperplasia in ventral lobes and lateral/dorsal lobes, respectively. We found that Rapatar prevented hypertrophic and hyperplastic abnormalities and degenerative alterations in both BPH models.

Exploratory behavior of F2 crosses of mouse lines selected for different brain weight: a multivariate analysis.

Principal component analysis of behavioural measures together with body and brain weight of hybrid F2 mice crosses between two lines selected for large (LB) and small (SB) brain weight yielded eight-factor solution explaining 75.1% of total variance. Two of eight factors had sufficient loading on brain weight and several behavioural measures.

Differential effects of saccharin supplementation on alcohol and water consumption by Wistar rats from different sources.

The study was aimed to elucidate whether the dissimilar effects of concurrent presentation of sweet water on alcohol consumption previously reported for Wistar rats from different sources remain unchanged when alcohol is also flavored with 0.1% saccharin. Male Wistar rats from Laboratory of Experimental Biological Models (LEBM) and Krukovo animal farm (K) stocks having had 2 months free access to food, tap water, and 10% alcohol were given four consecutive two-bottle drinking tests: alcohol versus water, alcohol versus sweet water, sweet alcohol versus water, or sweet alcohol versus sweet water.