HgSO4 catalyzed hydrative cyclization of 1,6-heptadiynes is present. This reaction proceeded smoothly under the mild condition for differently 4-sustituted 1,6-diynic substrates giving corresponding 3-methyl-2-cyclohexenones with high to excellent yield. The microwave assisted aldol condensation...

Hindered rotation analogs of the antipsychotic mazapertine (1) were prepared. These compounds exhibited high affinity for the HT-1A receptor, but not for other serotonin or dopamine receptors. The related β-carboline structures were also sybthetized and were found to be potent 5-HT1A ligands.

Several of the key metabolites of mazapertine, a novel antipyschotic agent, were prepared in order to firmly establish their chemical structure and to obtain samples for biological testing. Hydroxymazapertine 3 was synthesized via a multi-step procedure starting from 5-fluoro-2-nitrophenol (8). ...

The pharmacokinetics and drug disposition of 14C 1-[3-[[4-[2-(1-methylethoxy)phenyl]-1-piperazinyl]methyl]benzoy]piperidine succinate (RWJ-37796, mazapertine, Mz) have been investigated in male and female Sprague–Dawley rats. Approximately 93% of the orally administered radioactive dose (30 mg/...

Hemolin is a specific immune protein belonging to immunoglobulin superfamily and firstly identified in insects. Growing evidences suggest that Hemolin can be activated by bacterial and viral infections and may play an important role in antimicrobial immunity. In this paper, we firstly identified...

Fibroblasts are the main cellular component of connective tissues and play important roles in health and disease through the production of collagen, fibronectin and growth factors. Under certain conditions, such as wound healing, fibroblasts intensify their metabolic demand, while the restrictio...

Hemolin belongs to the immunoglobulin superfamily and plays an important role in innate immune response of insects. In this study, a hemolin-like cDNA of 1418 bp was obtained from Antheraea pernyi (Ap-hemolin-like). Sequence analysis revealed Ap-hemolin-like was homologous to those hemolins from...

Hemolins play an important role in development and innate immunity in insects. In this study, a hemolin cDNA of 1412 bp in Actias selene (As-HEM) was isolated and its open reading frames (ORFs) were 420 amino acid residues. Sequence analysis indicated As-HEM was homologous to those hemolins from...

ABSTRACTSecretory expression is most often desired but usually hampered by limitations of signal peptide processing and protein folding in the methylotrophic yeast Pichia pastoris. To alleviate such limitations, novel endogenous signal peptides (Dan4, Gas1, Msb2, and Fre2) and folding factors (M...

We previously showed that overexpression of IoGAS1, which was isolated from the multiple stress-tolerant yeast Issatchenkia orientalis, endows Saccharomyces cerevisiae cells with the ability to grow and ferment under acidic and high-salt conditions. The deduced amino acid sequence of the IoGAS1 ...

Environmental and medical examinations in workers exposed to the isopropylbiphenyl (IPBs) mixture, Sure Sol-250, in a capacitor-manufacturing plant were carried out once a year for three years. Levels of the total IPBs ranged from 0.03 to 36.6 mg/m3 with a mean of 5.6 mg/m3. The time-weighted av...

The liquid-phase fluorination of pentachlorotrifluoro-propane (1) and tetrachlorotetrafluoropropane (2) of defined isomer composition at atmospheric or autogenous pressure by means of the Henne-Swarts reagent yielded from 60% to 70% of tetrachlorotetrafluoropropane (2) and trichloropentafluoropr...

13C NMR chemical shifts of 3,3-dichloro-1,1,1-trifluoropropanes (CF3-CXY-CHCl2), 3-chloro-2,2,3,3-tetrafluoropropanes (CClF2-CF2-R), and diastereomers of 1,3-dichloro-1,1,2,3-tetrafluoropropane were studied by analysis using MNDO calculations. In CF3-CXY-CHCl2, 13C NMR chemical shifts of the met...

Conformational energies and compositions at 300 K have been estimated for mixed chlorofluoropropanes having conformational equilibria in the gas phase.

A series of high-temperature vulcanization (HTV) silicone rubber was prepared with polyamidoamine (PAMAM) dendrimers as concentrative cross-linkers and polysiloxane containing 3-chloropropyl groups (CPPS) as gums in a novel curing system. The curing, mechanical, and thermal properties of this no...

(+)-2-Aminobicyclo[3.1.0]hexane-2,6-dicarboxylic acid (LY354740) is a conformationally restricted glutamate analogue that is a potent, selective and orally active group 2 metabotropic glutamate receptor agonist possessing anticonvulsant and anxiolytic properties. Herein, we describe a stereosele...

The CuI and Rh2(OAc)4 catalyzed decomposition of ethyl 2-diazo-4,5-isopropylidenedioxy-3-oxo-6-heptenoate results in intramolecular cyclopropanation products with opposite diastereoselectivity. In contrast, decomposition of the respective iodonium ylide can proceed without catalysts to give the ...

A new stereocontrolled synthesis of (+)-2-aminobicyclo[3.1.0]hexane-2.6-dicarboxylic acid (LY354740) 1, a potent and selective 2mGluR agonist, has been accomplished in four steps with an overall yield of 27% starting from the enantiopure (+)-(R)-2-(p-tolylsulfinyl)cyclopent-2-enone 3. The key st...

BackgroundHaemoglobin Roma [β115(G17)Ala → Val] is a new adult haemoglobin variant found in a patient presenting a mild hypochromia and microcytosis. We studied this previously uncharacterised variant in order to evaluate the effect on the structural and funcional properties of the Ala → Val ...

A 23-year-old man with an elevated blood hemoglobin was found to have hemoglobin (Hb) Johnstown, a high oxygen-affinity hemoglobin and an elevated red cell hemoglobin content. The hemoglobin mutation was present in all family members who consented to molecular investigation. No elevation of the ...