Radiotracers suitable for positron emission tomography studies often serve as preclinical tools for in vivo receptor occupancy. The serotonin 1B receptor (5-HT(1B)) subtype is a pharmacological target used to discover treatments for various psychiatric and neurological disorders. In psychiatry, 5-HT(1B) antagonists may provide novel therapeutics for depression and anxiety. We report on the in v...

Three novel new compounds derived from antiparasitic precursors have been synthesized and tested for their antiamoebic and antigiardial activities. The condensation of 2-(2-methyl-5-1H-nitroimidazolyl)ethylamine (6) with 5-nitro-2-furylacrylic acid (7) gave 3-(5-nitrofuran-2-yl)-N-[2-(5-nitroimidazol-1-yl)ethyl]acrylamide (8). Condensation of 7 with 7-chloro-4-(piperazin-1-yl)quinoline (9) affo...

This article describes the biosynthesis and identification of a new class of metabolites, a piperazine N-oxide/N-glucuronide metabolite 4-[2-(2,4-dimethyl-phenylsulfanyl)-phenyl]-1-β-D-glucuronic acid-piperazine 1-oxide (4). The metabolite was found in urine and plasma from humans and animals dosed with 1-[2-(2,4-dimethyl-phenylsulfanyl)-phenyl]-piperazine hydrobromide (Lu AA21004, 1), as a nov...

The cyclin-dependent kinase (Cdk)-cyclin D/retinoblastoma (pRb)/E2F cascade, which controls the G1/S transition of cell cycle, has been found to be altered in many neoplasias. Inhibition of this pathway by using, for example, selective Cdk4 inhibitors has been suggested to be a promising approach for cancer therapy. We hypothesized that appropriately radiolabeled Cdk4 inhibitors are suitable pr...

We describe a novel class of designed multiple ligands (DMLs) combining serotonin 5-HT6 receptor (5-HT6R) antagonism with dopamine D2 receptor (D2R) partial agonism. Prototype hybrid molecules were designed using docking to receptor homology models. Diverse pharmacophore moieties yielded 3 series of hybrids with varying in vitro properties at 5-HT6R and D2R, and at M1 receptor and hERG channel ...

in this paper, a novel patch geodesic derivative pattern (pgdp) describing the texture map of a face through its shape data is proposed. geodesic adjusted textures are encoded into derivative patterns for similarity measurement between two 3d images with different pose and expression variations. an extensive experimental investigation is conducted using the publicly available bosphorus and bu-3...

in this paper a new method is proposed for interpretation of 2d magnetic data, using multiples of the analytic signal method, in which the analytic signal of magnetic anomaly is used directly to compute the depth and the structural index of the source instead of using its higher order derivatives. this method only needs the computation of the first order derivatives of the magnetic anomaly, so ...

for every $1leq s< n$, the $s^{th}$ derivative of a polynomial $p(z)$ of degree $n$ is a polynomial $p^{(s)}(z)$ whose degree is $(n-s)$. this paper presents a result which gives generalizations of some inequalities regarding the $s^{th}$ derivative of a polynomial having zeros outside a circle. besides, our result gives interesting refinements of some well-known results.