The novel series of substituted-N-(5,6-diphenyl-1,2,4-triazin-3-yl) benzamides (R: 1-12) were designed, synthesized and evaluated for in-vitro and in-vivo antidepressant-like activity. In MAO-A inhibition assay, compound R: 5 and R: 9 displayed most potent activity with IC₅₀ = 0.12 and 0.30 µM. R: 5 and R: 9 were also evaluated for in-vivo antidepressant using FST and TST. In both models, the test samples R: 5 and R: 9 showed noteworthy antidepressant effect. R: 5 showed 46.48 % and 45.96 % reduction in immobility in FST and TST respectively at dosage of 30 mg/kg (p.o). Whereas compound R: 9 reduced the immobility time by 52.76 % and 47.14 % as compared to control in FST and TST, respectively at same dosage. Both the compounds were also tested for behavioural study using actophotometer and grip tests. None of compounds exhibited decrease in locomotor activity. Further, these compounds were subjected to in silico studies to determine their ADME properties along with binding energies and binding orientions. In ADME studies none of the compounds violated the Lipinski rule and all other parameters were also within the acceptable ranges. In docking study R: 5 (-10.7) and R: 9 (-10.4) were also displayed highest docking score. These encouraging results present the pharmacophoric features of substituted-N-(5,6-diphenyl-1,2,4-triazin-3-yl) benzamides as interesting lead for further development of new antidepressant drug molecules.

2008-04-01·Zhong yao cai = Zhongyaocai = Journal of Chinese medicinal materials

[The breeding of Phellinus baumii by protoplast fusion].

Article

作者: Wang, Qiu-Ying ; Su, Ming-Sheng ; Zeng, Nian-Kai

OBJECTIVETo breed good strains by protoplast fusion in Phellinus baumii.METHODS5.8S rDNA-ITS sequences, mycelial growth rate, mycelial biomass and exopolysaccharides (EPS) production of 7 strains in different origins were analyzed, respectively. Then the inactivated parent protoplast and the PEG induction were used in the process of protoplast fusion.RESULTSThe strain P. baumii SA02 and P. baumii SA04 were selected as the parent strains. R002, R003 and R005 had antagonistic effects with parent strains.CONCLUSIONR002, R003 and R005 are fusants of the parent strains.

2000-12-05·Journal of Biomedical Materials Research

Evaluation of calcium phosphates and experimental calcium phosphate bone cements using osteogenic cultures

Article

作者: D. Reif ; F. C. M. Driessens ; R. Fitzner ; C. Knabe ; G. Berger ; R. Gildenhaar ; U. Gross ; R. J. Radlanski ; J. A. Planell

In this study, rat bone marrow cells (RBM) were used to evaluate two biodegradable calcium phosphate bone cements and bioactive calcium phosphate ceramics. The substances investigated were: two novel calcium phosphate cements, Biocement F and Biocement H, tricalcium phosphate (TCP), surface-modified alpha-tricalcium phosphate [TCP (s)] and a rapid resorbable calcium phosphate ceramic consisting of CaKPO(4) (sample code R5). RBM cells were cultured on disc-shaped test substrates for 14 days. The culture medium was changed daily and also examined for calcium, phosphate, and potassium concentrations. Specimens were evaluated using light microscopy, and morphometry of the cell-covered substrate surface, scanning electron microscopy, and energy dispersive X-ray analysis and morphometry of the cell-covered substrate surface. Areas of mineralization were identified by tetracyline labeling. Except for R 5, rat bone-marrow cells attached and grew on all substrate surfaces. Of the different calcium phosphate materials tested, TCP and TCP (s) facilitated osteoblast growth and extracellular matrix elaboration to the highest degree, followed by Biocements H and F. The inhibition of cell growth encountered with R 5 seems to be related to its high phosphate and potassium ion release.

100 项与 R-005 相关的药物交易

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