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  • 1
    Electronic Resource
    Electronic Resource
    Sulfation of Minoxidil in Keratinocytes and Hair Follicles and the Stimulatory Effect of Minoxidil on the Biosynthesis of Glycosaminoglycans (1991)
    Oxford, UK : Blackwell Publishing Ltd
    Annals of the New York Academy of Sciences 642 (1991), S. 0 
    Details
    ISSN: 1749-6632
    Source: Blackwell Publishing Journal Backfiles 1879-2005
    Topics: Natural Sciences in General
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1111/j.1749-6632.1991.tb24422.x
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  • 2
    Electronic Resource
    Electronic Resource
    Spermine-like functions of N^1, N^1^2-bis(ethyl)spermine: Stimulation of protein synthesis and cell growth and inhibition of gastric ulceration
    Amsterdam : Elsevier
    Biochemical and Biophysical Research Communications 172 (1990), S. 715-720 
    Details
    ISSN: 0006-291X
    Source: Elsevier Journal Backfiles on ScienceDirect 1907 - 2002
    Topics: Biology , Chemistry and Pharmacology , Physics
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1016/0006-291X(90)90733-4
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  • 3
    Electronic Resource
    Electronic Resource
    Enhanced contractile effect of phorbol dibutyrate in portal veins from hypertensive rats
    Amsterdam : Elsevier
    Biochemical and Biophysical Research Communications 176 (1991), S. 1552-1556 
    Details
    ISSN: 0006-291X
    Source: Elsevier Journal Backfiles on ScienceDirect 1907 - 2002
    Topics: Biology , Chemistry and Pharmacology , Physics
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1016/0006-291X(91)90464-I
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  • 4
    Electronic Resource
    Electronic Resource
    NS-398, a new anti-inflammatory agent, selectively inhibits prostaglandin G/H synthase/cyclooxygenase (COX-2) activity in vitro
    Amsterdam : Elsevier
    Prostaglandins 47 (1994), S. 55-59 
    Details
    ISSN: 0090-6980
    Source: Elsevier Journal Backfiles on ScienceDirect 1907 - 2002
    Topics: Medicine
    Type of Medium: Electronic Resource
    URL: http://linkinghub.elsevier.com/retrieve/pii/0090-6980(94)90074-4
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  • 5
    Electronic Resource
    Electronic Resource
    Calcium regulating activity of 26,27-dimethyl analog of 24R,25-dihydroxyvitamin D3 (1994)
    Springer
    Calcified tissue international 55 (1994), S. 190-197 
    Details
    ISSN: 1432-0827
    Keywords: Bone resorption ; Osteoclast-like cell formation ; Bone Ca mobilization ; Intestinal Ca transport ; 24R,25-dihydroxy-26,27-dimethylvitamin D3
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Medicine , Physics
    Notes: Abstract To determine the possibility that methyl substitution in 26- and 27-positions of 24R,25-dihydroxyvitamin D3 [24,25(OH)2D3] alters activities of the original compound, the effects of 24,25(OH)2D3 on calcium (Ca) regulating activity were compared with those of its methyl analog [24,25(OH)2(CH3)2D3] in addition to 1α,25-dihydroxyvitamin D3 [1,25(OH)2D3]. 24,25(OH)2D3 at 10-6 M and 24,25(OH)2(CH3)2D3 at 10-7 M and above significantly stimulated both bone resorption in neonatal mouse calvaria cultures and formation of osteoclast-like multinucleated cells (MNC) in mouse bone marrow cultures. A stimulative effect of 1,25(OH)2D3 on bone resorption and MNC formation was recognized in very low concentrations (10-11 M and above). Although a potency of 24,25(OH)2(CH3)2D3 in stimulating bone calcium (Ca) mobilization and intestinal Ca transport was higher than that of 24,25(OH)2D3, the potencies of both compounds were similar to that of 1,25(OH)2D3 unlike in vitro experiments. As 1,24R,25-trihydroxy-26,27-dimethylvitamin D3 showed almost the same effect as 24,25(OH)2(CH3)2D3, the dihydroxy form is suggested to be hydroxylated at 1α position and converted to trihydroxy form in vitamin D-deficient rats. From these results, methyl substitution in 26- and 27-position of 24,25(OH)2D3 was found to elevate Ca regulating activity of the original compound. In addition, it is suggested that the basis for a similarity in potency between 1,25(OH)2D3 and 24,25(OH)2D3 or its dimethyl analog in vitamin D-deficient rats is likely the result of 1 α-hydroxylation.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00425874
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  • 6
    Electronic Resource
    Electronic Resource
    Elongation of the side chain of analogs of 1α,25-dihydroxyvitamin D3 prevents osteopenia in a rat model (1995)
    Springer
    Calcified tissue international 56 (1995), S. 220-226 
    Details
    ISSN: 1432-0827
    Keywords: Bone density ; Dual energy X-ray absorptiometry ; Elongating side chain of analogs of 1α,25-dihydroxyvitanin D3 ; Prevention of osteopenia
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Medicine , Physics
    Notes: Abstract Five analogs of 1α,25-dihydroxyvitamin D3 [1,25(OH)2D3] [1], 26,27-dimethyl-1α,25-dihydroxyvitamin D3 [1,25(OH)2(Me)2D3] [2], 26,27-dimethyl-1α,25-dihydroxyvitamin D3 [1,25(OH)2(Et)2D3] [3], 26,27-dipropyl-1α, 25-dihydroxyvitamin D3 [1,25(OH)2(Pr)2D3] [4], 26,27-dimethyl-24, 24-difluoro-1α,25-dihydroxyvitamin D3 [24F2-1,25(OH)2(Me)2D3, and [5] 24a-homo-24,24-difluoro-1α,25-dihydroxyvitamin D3 [24aF2-homo-1,25(OH)2D3] were investigated to clarify the possibility that prevents osteopenia induced in rats by ovariectomy and sciatic neurotomy. The objective of our studies was to determine whether these analogs may be effective for treatment of subjects with osteoporosis. 1,25(OH)2(Me)2D3, 24F2-1,25(OH)2(Me)2D3, and 24aF2-homo-1,25(OH)2D3 prevented decreases in bone mineral density (BMD) of the femur, as measured by dual energy X-ray absorptiometry (DXA). The potency of 1,25(OH)2(Me)2D3 in this test was higher than that of 1,25(OH)2D3. The potencies of 24F2-1,25(OH)2(Me)2D3 and 24aF2-homo-1,25(OH)2D3 were similar to that of 1,25(OH)2D3. On the other hand, though 1,25(OH)2(Et)2D3 and 1,25(OH)2(Pr)2D3 had a preventive effect on the decease in BMD, the potency of two analogs was lower than that of 1,25(OH)2D3. Decreases in cortical and trabecular bone areas of the femur were prevented by three analogs of 1,25(OH)2D3, 1,25(OH)2(Me)2D3, 24F2-1,25(OH)2(Me)2D3, and 24aF2-homo-1,25(OH)2D3. Serum calcium (Ca) concentration was elevated at the last administration of three analogs of 1,25(OH)2D3, 1,25(OH)2(Me)2D3, 24F2-1,25(OH)2(Me)2D3 and 24aF2-homo-1,25(OH)2D3. Decreases in the Ca concentration in untreated rats were noted a few days after the last administration. In light of these positive effects, we are continuing research on 1,25(OH)2(Me)2D3, 24F2-1,25(OH)2(Me)2D3, and 24aF2-homo-1,25(OH)2D3 as putative treatment for osteoporosis.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00298614
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  • 7
    Electronic Resource
    Electronic Resource
    Suppression of pulmonary granulomatous inflammation by immunomodulating agents (1992)
    Springer
    Inflammation research 37 (1992), S. 99-106 
    Details
    ISSN: 1420-908X
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract We demonstrated previously that macrophages and macrophage-derived cytokines including lymphocyteactivating factors (LAFs) play a critical role in lung granuloma formation in mice and that granulomas sizes correlated with LAF activity in the lesions. In the present study, we examined the effects ofd-penicillamine (d-Pc), 2-acetylthiomethyl-3-(4-methyl-benzoyl)propionic acid (KE-298) and dexamethasone (Dex) on dextran bead-induced lung granulomas in mice. KE-298 is a newly synthesized compound containing sulfur (S) similar tod-Pc. Large granulomas developed, which reached peak intensity within 3 days and declined in size thereafter. Aqueous lung extracts of the mice contained high levels of LAF that were correlated with granuloma sizes. The lesions and local LAF activity were inhibited by administration of these agents. The most potent inhibitor was Dex. The suppressive effect of KE-298 was similar to that ofd-Pc. These results suggest that suppression of granulomas may be attributed to inhibition of LAF activity/synthesis by these agents.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01987896
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  • 8
    Electronic Resource
    Electronic Resource
    Characteristics of binding of [3H]NE-100, a novel sigma-receptor ligand, to guinea-pig brain membranes (1995)
    Springer
    Naunyn-Schmiedeberg's archives of pharmacology 351 (1995), S. 244-251 
    Details
    ISSN: 1432-1912
    Keywords: Key words Sigma binding sites ; NE-100 ; (N ; N-dipropyl-2-[4-methoxy-3-(2-phenylethoxy) phenyl]-ethylamine monohydrochloride) ; Radiolabeled ligand binding ; Brain ; Guinea-pig
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract  We examined the characteristics of binding of radiolabeled N,N-dipropyl-2-[4-methoxy-3-(2-phenyl- ethoxy)phenyl]-ethylamine monohydrochloride ([3H] NE-100), a highly potent and selective sigma-receptor ligand, to guinea-pig brain membranes. [3H]NE-100 showed saturable and reversible binding to sigma binding sites. A dissociation constant (Kd) and maximal numbers of binding sites (B max) obtained from Scatchard plot analysis were 1.2±0.1 nM and 1049.3±115.1 fmol/mg protein (n=3), respectively. NE-100 was the most potent inhibitor of [3H]NE-100 binding among several structurally dissimilar sigma-receptor ligands, including haloperidol and (+)-pentazocine. (+)-Benzomorphanes had more than a 10-fold potent inhibitory activity over (−)-benzomorphanes, with regard to [3H]NE-100 binding. The binding of [3H]NE-100 was not influenced by histaminergic, dopaminergic, adrenergic, serotonergic cholinergic or glutaminergic agents at 10-7 M. GTP-γ-S and phenytoin also did not affect the binding of [3H]NE-100. A higher [3H]NE-100 binding was observed in the cerbellum and medulla oblongata. Except for the nuclear fraction, the highest level of [3H]NE-100 binding to subcellular fractions was observed in microsomal fractions. These results suggest that NE-100 selectively binds, with a high affinity, to sigma-1 binding sites in guinea-pig brain membranes, as an “antagonist”.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00233243
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  • 9
    Electronic Resource
    Electronic Resource
    Characteristics of binding of [3H]NE-100, a novel sigma-receptor ligand, to guinea-pig brain membranes (1995)
    Springer
    Naunyn-Schmiedeberg's archives of pharmacology 351 (1995), S. 244-251 
    Details
    ISSN: 1432-1912
    Keywords: Sigma binding sites ; NE-100 (N,N-dipropyl-2-[4-methoxy-3-(2-phenylethoxy) phenyl]-ethylamine monohydrochloride) Radiolabeled ligand binding ; Brain ; Guinea-pig
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract We examined the characteristics of binding of radiolabeled N,N-dipropyl-2-[4-methoxy-3-(2-phenylethoxy)phenyl]-ethylamine monohydrochloride ([3H] NE-100), a highly potent and selective sigma-receptor ligand, to guinea-pig brain membranes. [3H]NE-100 showed saturable and reversible binding to sigma binding sites. A dissociation constant (Kd) and maximal numbers of binding sites (B max) obtained from Scatchard plot analysis were 1.2 ± 0.1 nM and 1049.3 ± 115.1 fmol/mg protein (n = 3), respectively. NE-100 was the most potent inhibitor of [3H]NE-100 binding among several structurally dissimilar sigma-receptor ligands, including haloperidol and ( + )-pentazocine. ( + )-Benzomorphanes had more than a 10-fold potent inhibitory activity over (−)-benzomorphanes, with regard to [3H]NE-100 binding. The binding of [3H]NE-100 was not influenced by histaminergic, dopaminergic, adrenergic, serotonergic cholinergic or glutaminergic agents at 10−7 M. GTP-γ-S and phenytoin also did not affect the binding of [3H]NE-100. A higher [3H]NE-100 binding was observed in the cerbellum and medulla oblongata. Except for the nuclear fraction, the highest level of [3H]NE-100 binding to subcellular fractions was observed in microsomal fractions. These results suggest that NE-100 selectively binds, with a high affinity, to sigma-1 binding sites in guinea-pig brain membranes, as an “antagonist”.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00233243
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  • 10
    Electronic Resource
    Electronic Resource
    Studies of tetrazoles as rubber chemicals. I. Preparation and characterization of reactive antioxidants based on tetrazoles (1983)
    New York, NY [u.a.] : Wiley-Blackwell
    Journal of Applied Polymer Science 28 (1983), S. 3671-3679 
    Details
    ISSN: 0021-8995
    Keywords: Chemistry ; Polymer and Materials Science
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology , Mechanical Engineering, Materials Science, Production Engineering, Mining and Metallurgy, Traffic Engineering, Precision Mechanics , Physics
    Notes: The novel reactive antioxidants based on tetrazoles that are stable at room temperature and convertible into the highly reactive nitrileimines by pyrolysis were prepared and the reactivity for carbon-carbon double bonds was evaluated. Antioxidants, i.e., 2-substituted phenyl-5-(3′,5′-di-tert-butyl-4′-hydroxyphenyl)tetrazoles (PHPT) were prepared with the reaction of p-toluenesulfonylhydrazone of 3,5-di-tert-butyl-4-hydroxybenzaldehyde and substituted phenyl diazonium chloride in a mixed solvent of pyridine, ethanol, and water at -10°C to -20°C in 31-61% yields. To evaluate the reactivities of PHPT for carbon-carbon double bonds, m-chloro-substituted PHPT was pyrolyzed in an excess of styrene at 160-170°C for 0.5 h to give the 1-(3′-chlorophenyl)-3-(3″,5″-di-tert-butyl-4″-hydroxyphenyl)-5-phenyl-2-pyridazoline in a 44.1% yield by 1,3-dipolar addition reaction of the nitrileimine formed from the m-chloro-substituted PHPT. The thermogravimetric analysis of a mixture of proton isomer of PHPT and liquid polybutadiene showed that PHPT attached to liquid polybutadiene with an accompanying evolution of nitrogen.
    Additional Material: 3 Ill.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1002/app.1983.070281208
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