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排名前五的药物类型	数量

小分子化药	1

排名前五的靶点	数量

chymase(糜蛋白酶)	1

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1

项与 Welfide Corp. 相关的药物

Y-40018

靶点

chymase

作用机制

chymase抑制剂

在研机构

Welfide Corp.

原研机构

Welfide Corp.

在研适应症-

非在研适应症-

最高研发阶段临床前

首次获批国家/地区-

首次获批日期-

100 项与 Welfide Corp. 相关的临床结果

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0 项与 Welfide Corp. 相关的专利（医药）

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205

项与 Welfide Corp. 相关的文献（医药）

2011-04-12·Journal of Pharmacy and Pharmacology3区 · 医学

Pharmacokinetic behaviour in polymorphonuclear leucocytes of N,N-dimethylcarbamoylmethyl α,2-dimethyl-5H-[1]benzopyrano[2,3-b]-pyridine-7-acetate (Y-23023), a new prodrug type of antiinflammatory agent, and indomethacin after oral administrations in rats

3区 · 医学

Article

作者: Yamada, Ichimaro ; Nagamatsu, Yuko ; Tsuji, Akira ; Shibata, Masahiro ; Imayoshi, Tomonori

AbstractN,N-Dimethylcarbamoylmethyl α,2-dimethyl-5H-[1]-benzopyrano[2,3-b]pyridine-7-acetate (Y-23023) is a prodrug developed as a new non-steroidal anti-inflammatory drug (NSAID). Y-23023 is rapidly hydrolysed to an active metabolite, α,2-dimethyl-5H-[1]benzopyrano[2,3-b]pyridine-7-acetic acid (M1) following its absorption and then exhibits a strong anti-inflammatory activity. We have examined the pharmacokinetic behaviour in polymorphonuclear leucocytes (PMNs) of M1 and of indomethacin after oral administration to rats of Y-23023 and indomethacin, respectively. Y-23023 was rapidly absorbed, producing a mean Cmax (1·13 μg mL−1) of M1 after 1 h in plasma. Indomethacin was less rapidly absorbed, producing a mean Cmax (3·38 μg mL−1) after 3 h in plasma. The mean AUC of M1 and indomethacin in plasma were 5·45 μg h mL−1 and 22·49 μg h mL−1, respectively. The mean tmax, Cmax and AUC of M1 in PMNs were 1 h, 11·1 ng (41 pmol)/108 cells and 58·6 ng (164 pmol) h/108 cells, respectively. The same parameters for indomethacin in the PMNs were 3 h, 15·4 ng (57 pmol)/108 cells and 95·2 ng (266 pmol) h/108 cells, respectively. The PMNs/plasma ratio of M1 was about 2·8 times that of indomethacin. These results indicate that the association of M1, an active metabolite of Y-23023, from blood to the PMNs is greater than that of indomethacin.

2002-04-01·Journal of Endotoxin Research

Investigation into the interaction of recombinant human serum albumin with Re-lipopolysaccharide and lipid A

作者: Koch, Michel H.J. ; Brandenburg, Klaus ; Garidel, Patrick ; Müller, Mareike ; Blume, Alfred ; Jürgens, Gudrun ; Nakakubo, Hiroshi

The interaction of bacterial endotoxins, deep rough mutant lipopolysaccharide LPS Re and the `endotoxic principle' lipid A, with recombinant human serum albumin (rHSA) was investigated with a variety of physical techniques and biological assays. With Fourier-transform infrared spectroscopy and differential scanning calorimetry, the influence of albumin on the acyl chain melting behavior of the endotoxins was measured. Also, the effect on the functional groups of the endotoxins, in particular with respect to their orientation, was studied, including competition experiments with polymyxin B. Furthermore, the influence of endotoxin binding to rHSA on the protein's secondary structure was investigated. The results indicate a non-electrostatic binding with no change of the backbone orientation of LPS and only a slight change of the secondary structure of rHSA. Correspondingly, the amount of charge neutralization of the endotoxins due to rHSA measured by the electrophoretic mobility exhibited only a slight reduction of the surface potential. From these measurements and isothermal titration calorimetry, the lipid:protein binding stoichiometry was estimated to [LPS]:[rHSA], 10:1 molar. The determination of the aggregate structure of the endotoxins by X-ray small-angle scattering exhibited a complex change of a cubic into a non-lamellar structure. No influence of rHSA on endotoxin intercalation into phospholipid liposomes induced by lipopolysaccharide-binding protein could be detected by fluorescence resonance energy transfer. Finally, the LPS-induced cytokine production of human mononuclear cells was only slightly increased at high molar rHSA excess, while the coagulation of amebocyte lysate in the Limulus test yielded a complex change due to rHSA binding of LPS.

2002-02-01·Pediatrics International4区 · 医学

Increased production of serum IgA‐class antibody to lipid A in Kawasaki disease

4区 · 医学

Article

作者: Seiichiro Takeshita ; Maki Yoshida ; Isao Sekine ; Tooru Shimizu ; Hiroko Kawase

AbstractBackground: The etiology of Kawasaki disease (KD) remains unknown. To investigate whether a conventional bacterial antigen is involved in the pathogenesis of KD, we studied the serum response to lipopolysaccharide (LPS).Methods: We measured the serum levels of IgG‐, IgM‐ and IgA‐class antibodies (Ab) to lipid A, a toxic site of LPS, using enzyme‐linked immunosorbent assay in 20 patients with KD, 11 patients with Gram‐negative bacterial infection (GNBI), 27 healthy children and 12 healthy adults.Results: The serum levels of anti‐lipid A IgG, IgM and IgA tended to increase with advancing age in healthy children older than 6 months of age. The mean level of anti‐lipid A IgM in the acute phase of GNBI and the mean levels of anti‐lipid A IgM and IgA in the acute phase of KD were found to increase significantly, in comparison to the age‐matched controls. Furthermore, the mean level of anti‐lipid A IgA also showed a significant increase from the acute to the subacute phases of KD. Regarding the IgA‐subclass response, higher titers of anti‐lipid A specific Ab were seen in the IgA2 subclass than in the IgA1 subclass.Conclusion: These findings indicate that KD patients demonstrate an intense response to lipid A in the IgA, especially IgA2‐subclass, thus suggesting that an unusual activation of the mucosal immune response to a ubiquitous antigen derived from Gram‐negative bacteria may be involved in the pathogenesis of KD.

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100 项与 Welfide Corp. 相关的转化医学

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