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K Tamazawa H Arima T Kojima Y Isomura M Okada S Fujita T Furuya T Takenaka O Inagaki M Terai 《Journal of medicinal chemistry》1986,29(12):2504-2511
Four enantiomers (3a-d) of the title compound, YM-09730 (3), were synthesized by the reaction of (-)- or (+)-5-(methoxycarbonyl)-2, 6-dimethyl-4-(m-nitrophenyl)-1,4-dihydropyridine-3-carboxylic acid (1a or 1b) with (S)- or (R)-1-benzyl-3-pyrrolidinol (2a or 2b). [3H]Nitrendipine binding affinity and coronary vasodilating activity of these compounds were evaluated. The absolute configuration of the most potent enantiomer (3a) with the longest duration was unequivocally determined to be (S)-1,4-dihydropyridine-C4 and (S)-pyrrolidine-C3 (S,S) by X-ray crystallographic study on 3a X HBr as well as 3a X HCl. The configuration of 1a corresponds to R, and the other enantiomers of 3 were respectively determined by chemical correlation. The potency order of the four enantiomers was (S,S)-3a greater than (S,R)-3b greater than (R,R)-3d greater than (R,S)-3c. Latent chiral characters of nifedipine derivatives with the identical ester groups were assigned by comparison of their puckering modes of 1,4-dihydropyridine (DHP) rings with those found in 3a X HCl or 3a X HBr. On the basis of the assignment, it has been revealed that the (S)-DHP nifedipine derivatives possess the synperiplanar carbonyl group at C5. The conformational restriction may be a factor causing stereoselectivity of antagonism. 相似文献
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K. Arima Minako Nakamura Nobuhiko Sunohara Masafumi Ogawa Midori Anno Yoko Izumiyama Shigeo Hirai Kazuhiko Ikeda 《Acta neuropathologica》1997,93(6):558-566
Coiled bodies and interfascicular threads are conspicuous white matter abnormalities of brains of patients with progressive
supranuclear palsy (PSP). Both structures are argyrophilic and immunoreactive for the microtubule-binding protein tau. This
report concerns the ultrastructural localization of interfascicular threads and their relationship to coiled bodies in five
PSP patients. We showed for the first time that abnormal tubules with a 13- to 15-nm diameter and fuzzy outer contours were
the common structures of coiled bodies in the oligodendroglial perikarya and of interfascicular threads. Moreover, the tubules
were immunolabeled by anti-tau antibodies. The abnormal tau-positive tubules of interfascicular threads were located in the
inner loop of the myelin sheath. Our study further indicated that the thread-like structures in the white matter comprised,
at least in part, oligodendroglial processes, and that they were also present in gray matter. We consider that the formation
of coiled bodies in the perikarya and of interfascicular threads represents a common cytoskeletal abnormality of the oligodendroglia
of PSP patients. Moreover, even though the white matter alterations of PSP resemble those of corticobasal degeneration, there
are certain ultrastructural differences in the abnormal oligodendroglial tubules of the two diseases.
Received: 4 October 1996 / Accepted: 6 December 1996 相似文献
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Jose S. Pulido Ikuko Sugaya Jordan Comstock Kiminobu Sugaya 《Albrecht von Graefes Archiv fur klinische und experimentelle Ophthalmologie》2007,245(6):889-893
Purpose Reelin is important in the guidance of neuronal stem cells in the central nervous system during normal development. We wished
to determine whether reelin is expressed in the retina and cornea after injury.
Methods Mice underwent laceration of their retina as well as corneal epithelial debridement. The mice were sacrificed at 3 days, and
eyes were fixed and stained for reelin expression and reelin messenger ribonucleic acid (mRNA).
Results In normal eyes, reelin was expressed only at very low levels in the ganglion cell layer of the retina and the endothelial
cell layer of the cornea. In injured eyes, there was marked expression in reelin immunoreactivity in the retina and cornea.
Reelin gene expression was seen in the retina and cornea.
Conclusions Reelin is expressed during normal retinogenesis. This study shows that reelin is also upregulated following injury to the
retina and cornea. The expression of reelin following injury suggests that reelin may play an important role in regulating
stem cell trafficking in neuronal and nonneuronal tissues following injury similar to its role in normal organogenesis.
For consideration of publication in Graefe’s Archive for Clinical and Experimental Ophthalmology. 相似文献
8.
Photoaging and oxidative stress 总被引:5,自引:0,他引:5
Chikako Nishigori† Yukari Hattori Yaeno Arima Yoshiki Miyachi 《Experimental dermatology》2003,12(S2):18-21
9.
A total 37 patients with Crohn's disease who underwent intraoperative endoscopy during resection of the affected intestine were evaluated in this study. The average age of the patients at surgery was 23.2 years. The residual lesions in the remaining intestine identified by intraoperative endoscopy were classified according to their pathologic profiles into three groups: A, B and C. In group A, comprising patients with longitudinal ulcers and/or a cobblestone appearance, 10 of 12 patients had recurrence. In 5 of these 10, the residual lesions were exacerbated and 2 required a further operation. The remaining 5 patients showed recurrence at the site of previous anastomosis and 2 of these 5 required additional surgery.In group B, comprising patients with small ulcers, aphthoid ulcers, or scars, and group C, comprising patients with no residual lesions, recurrence was observed in 13 of 16, and 3 of 9 patients, respectively. The recurrent lesions were all found proximal to, or at the site of previous anastomosis. Additional operations were performed on 3 of the group B patients. The findings of this study revealed that recurrence requiring additional surgery is more frequent at the site of anastomosis, regardless of the endoscopic appearance of the residual lesions. 相似文献
10.