1-Benzyl-1,2,3,4-tetrahydroisoquinoline hydrochloride (1BnTIQ·HCl) (22 mg/kg per day) was subcutaneously injected into a monkey, Macaca fascicularis for 66 days to investigate its acute and chronic effects. Parkinsonism-like motor symptoms appeared, and the acute toxicity was stronger than the ...

We administered 1-benzyl-1,2,3,4-tetrahydroisoquinoline (1-BnTIQ; 80 mg/kg, i.p.), an endogenous neurotoxin known to cause bradykinesia, the Parkinson’s disease-like symptom, in order to obtain biochemical and pathological evidence of behavioral abnormalities. Immunohistochemical analysis demon...

We performed a combined neurochemical and behavioral study to determine the effects of 1-benzyl-1,2,3,4-tetrahydroisoquinoline (1-BnTIQ) on the extracellular dopamine concentrations in the striatum. Single dose administration of 1-BnTIQ (20, 40, and 80 mg/kg i.p.) increased striatal dopamine ext...

Endogenous MPTP-like neurotoxins such as 1-benzyl-1,2,3,4-tetrahydroisoquinoline (1BnTIQ) have been suspected in the etiology of Parkinson’s disease (PD). 1BnTIQ was found in a concentration three times higher in cerebrospinal fluid of PD brains than control subjects [J. Neurochem. 65 (6) (1995...

Organotypic slice co-culture of the ventromedial portion of the mesencephalon and striatum was used to evaluate the neurotoxicity of 1-benzyl-1,2,3,4-tetrahydroisoquinoline, an endogenous brain amine related to Parkinson’s disease. 1-Benzyl-1,2,3,4-tetrahydroisoquinoline is specifically increas...

1-Benzyl-1,2,3,4-tetrahydroisoquinoline (1-BnTIQ) and TIQ are endogenous substances inducing bradykinesia, one of the symptoms of parkinsonism, in rodents and primates, and 2-methyl-TIQ is postulated to be an active form of TIQ. We investigated the effect of 1-BnTIQ-, TIQ- or 2-methyl-TIQ-treatm...

A chemoenzymatic strategy for the synthesis of enantiomerically pure novel alkaloids (1S,3R)-1-benzyl-2,3-dimethyl-1,2,3,4-tetrahydroisoquinolines is presented. The key steps are the biocatalytic stereoselective reductive amination of substituted 1-phenylpropan-2-one derivatives to yield chiral ...

Previous work has established that 1-benzyl-1,2,3,4-tetrahydroisoquinoline (1-BnTIQ) causes a parkinsonian syndrome in rats. The present study reports the blood–brain barrier (BBB) permeability of 1-BnTIQ in freely moving rats with the aid of in vivo microdialysis-based measurements. The microd...

An expression of UDP-glucose: poriferasterol glucosyltransferase activity associated with differentiation of a true slime mold, Physarum polycephalum, from haploid myxoamoebae to diploid plasmodia was demonstrated. In the haploid cells, this enzyme activity was not detected, but after conjugatio...

A one-pot synthetic route for preparing functionalized p-terphenyl derivatives 1 and 4 is developed. The route is easily carried from the treatment of cinnamyl aldehydes 2 with substituted allylsulfones 3 in good yields via the tandem intermolecular aldol condensation/intramolecular electrocycli...

Mild dehydration of 2-benzenesulfonyl allylic alcohols 8 afforded a series of (E)-2-benzenesulfonyl-1,3-alkadienes 1 which dimerized to functionalized vinylcyclohexenes 3 in regio- and stereodefined manner. The configuration at C-3 in 3e was determined by X-ray crystallography.

A novel series of N-benzenesulfonyl matrinic amine/amide and matrinic methyl ether analogues were designed, synthesized and evaluated for their in vitro anti-coxsackievirus B3 (CVB3) activities. The structure–activity relationship (SAR) studies revealed that introduction of a suitable amide sub...

Two lead compounds with benzenesulfonamide were found through virtual screening based on the 3D structure of the subunit H of V-ATPase in previous study. 74 benzenesulfonyl derivatives were synthesized and their insecticidal activities were evaluated. The derivatives with propargyl substituents ...

The synthesis of aromatic fluoromonomer compounds functionalized by halogen atoms, organic functions or acid groups prepared and characterized by different methods, are described in this review. This review deals with the synthesis and the polymerization of fluorostyrene bearing the fluorine ato...

The H-assisted isomerization of fulvene to benzene is characterized in detail using quantum chemistry, transition state theory, classical trajectory, and master equation calculations. This multistep isomerization involves 10 transition states, nine of which are found to contribute non-negligibly...

The molecular-programmed approach based on the use as ligands of tailor-made metalloligands containing stable six-coordinate rhenium(IV) as paramagnetic centres is presented in this review article. A relatively large amount of spin density is covalent-delocalized away from the rhenium to the per...

This study presents a facile synthesis of biomimetic hydroxyapatite nanorod/poly(d,l) lactic acid (HAp/PDLLA) scaffolds with the use of solvent casting combined with a salt-leaching technique for bone-tissue engineering. Field emission scanning electron microscopy, Fourier transform infrared spe...

Bile acids (BAs) influence the metabolism of glucose, lipids, and energy expenditure. We hypothesized that BA concentrations and related gene expression would be altered in lean (low-fat diet fed; LFD) vs diet-induced obese (high-fat diet fed; HFD) groups of mice and that some detected changes w...

Over half of the active pharmaceutical ingredients currently approved within the US are pharmaceutical salts. Selection of suitable pharmaceutical salts is carried out during late research or early development phase. Therefore several properties of different pharmaceutical salts of a new chemica...

The medium containing ionic products of dicalcium silicate (Ca2SiO4) for culturing the osteoblast-like cells (MG63) were prepared by immersing the plasma sprayed Ca2SiO4 coatings in DMEM solution for 24 h. The normal DMEM was also used to culture the MG63 cells as the control group. The results ...