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Haijun Qu,Xiaoxiao Hu,Xiaoli Shi,Chuan Wang,Longyuan Wang,Guoping Wang 한국통합생물학회 2019 Animal cells and systems Vol.23 No.3
N-(2-pyridylmethyl)-2-hydroxiymethyl-1-pyrrolidinyl-4-(3-chloro-4-methoxy-benzylamino)-5- pyrimidine-carboxamide (NHPPC) is a new potential of type 5 phosphodiesterase (PDE5) inhibitors, synthesized from the avanafil analogue for the treatment of erectile dysfunction. The targets of this article were to assess plasma protein binding, liver microsomal metabolic stability, inhibition and induction on cytochrome P450 isozymes and the pharmacokinetics of NHPPC. Equilibrium dialysis technique was applied to determine Plasma protein binding (PPB) and NHPPC was evaluated in male Sprague–Dawley rats and Beagle dogs in vivo pharmacokinetic. The NHPPC was highly bound to plasma proteins in rats, dogs and human tested and the mean values for PPB rate were 96.2%, 99.6% and 99.4%, respectively. After in vitro liver microsomes incubated for 60 min, the percent remaining of NHPPC was 42.8%, 0.8% and 42.0% in rats, dogs and human, respectively. In vitro intrinsic clearance was found to be 0.0233, 0.1204 and 0.0214 mL/min/mg protein in rat, dog and human liver microsomes of NHPPC, respectively. NHPPC showed no significant inhibitory effects on major CYP450 enzymes, and had no significant induction potential on CYP1A2 and CYP3A4. Following oral administration in rats and dogs, tmax was 6 and 0.5 h, respectively. The clearance for NHPPC was 1.19 and 1.46 L/h/kg in rats and dogs, respectively. And absolute bioavailability in rat and dog were approximately 34.5% and 53.1%, respectively. These results showed that NHPPC has a good development prospect.
Benzothiazole-based fluorescent probe for N2H4
Hanlin Wang,Jiexun Huang,Weidong Huang,Longyuan Yang 대한화학회 2023 Bulletin of the Korean Chemical Society Vol.44 No.1
A fluorescence enhancement probe 2-[2-(1,3-benzothiazol-2-yl)phenyl]-1H- isoin-dole-1,3(2H)-dione (HL1) for N2H4 was synthesized and characterized by using 2-(2-aminophenyl)benzothiazole as a fluorophore, and its spectroscopic properties had been researched. The results exhibited that HL1 was highly selective and sensitive to N2H4, and it had the excellent anti-interference ability and displayed a fast response. The fluorescent intensity of HL1 showed a good linear relationship with the concentration of N2H4 (1.5–12.5 μmolL1), and its detection limit was 0.12 μmol/L. In addition, HL1 was also applied for determin- ing N2H4 levels in real water samples and imaging N2H4 in living HeLa cells.