31 research outputs found

    Octopaminergic agonists for the cockroach neuronal octopamine receptor

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    The compounds 1-(2,6-diethylphenyl)imidazolidine-2-thione and 2-(2,6-diethylphenyl)imidazolidine showed the almost same activity as octopamine in stimulating adenylate cyclase of cockroach thoracic nervous system among 70 octopamine agonists, suggesting that only these compounds are full octopamine agonists and other compounds are partial octopamine agonists. The quantitative structure-activity relationship of a set of 22 octopamine agonists against receptor 2 in cockroach nervous tissue, was analyzed using receptor surface modeling. Three-dimensional energetics descriptors were calculated from receptor surface model/ligand interaction and these three-dimensional descriptors were used in quantitative structure-activity relationship analysis. A receptor surface model was generated using some subset of the most active structures and the results provided useful information in the characterization and differentiation of octopaminergic receptor. Abbreviation: / AEA: arylethanolamine AII: 2-(arylimino)imidazolidine AIO: 2-(arylimino)oxazolidine AIT: 2-(arylimino)thiazolidine APAT: 2-(α-phenylethylamino)-2-thiazoline BPAT: 2-(β-phenylethylamino)-2-thiazoline CAO: 2-(3-chlorobenzylamino)-2-oxazoline DCAO: 2-(3,5-dichlorobenzylamino)-2-oxazoline DET5: 2-(2,6-diethylphenylimino)-5-methylthiazolidine DET6: 2-(2,6-diethylphenylimino)thiazine EGTA: ethylene glycol bis(β-aminoethyl ether)-N,N,N′,N′-tetraacetic acid GFA: genetic function approximation G/PLS: genetic partial least squares IND: 2-aminomethyl-2-indanol LAH: lithium aluminum hydride MCSG: maximum common subgroup MCT6: 2-(2-methyl-4-chlorophenylimino)thiazine OA: octopamine PLS: partial least squares QSAR: quantitative structure-activity relationship SBAT: 2-(substituted benzylamino)-2-thiazoline SD: the sum of squared deviations of the dependent variable values from their mean SPIT: 3-(substituted phenyl)imidazolidine-2-thione THI: 2-amino-1-(2-thiazoyl)ethanol TMS: tetramethyl silan

    Deposition of transparent conducting Al-doped ZnO thin films by ICP-assisted sputtering

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    Aluminum-doped zinc oxide (AZO) is one of the promising transparent conductive oxide materials, which is expected to be an alternative to tin-doped indium oxide (ITO) that for long has been widely used in industry. The authors have been engaged in the development of AZO deposition process using inductively-coupled plasma assisted sputtering in a couple of years. This paper reports the results showing effectiveness of inductively coupled plasma (ICP) assisted sputtering in AZO film deposition process.2010 IEEE Region 10 Conference (TENCON 2010) : Fukuoka, 2010.11.21-2010.11.2

    トクシマ コウエン トクシマ チュウオウ コウエン ノ ゾウエン セッケイ ニツイテ : ヒビヤ コウエン オヨビ ザイファースドルフジョウ トノ ヒカク

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    Tokushima Park (originally named Tokushima Central Park) is the Japan’s second western-style park that was opened in 1906. We investigated landscape architecture of Tokushima Park based on a blueprint made in 1905 to understand its purpose and function of the park, and compared with Hibiya Park that is the Japan’s first western-style park. Tokushima Park consisted of five areas. The central area included Mt. Shiroyama (Castle Mountain), and primeval forest was protected without allowing to make a big building within the area. A commercial museum, an athletic field, and a botanical garden and a library were placed in the southern, western and eastern areas respectively, so that each area was designed to exhibit each function. Tokushima Park and Hibiya Park were designed by the same two persons Seiroku Honda and Takanori Hongo. The two parks were equipped with a wide road, an athletic field, a botanical garden and so on, and these facilities were adopted to the park made since them. Because Seiroku Honda adopted three design drawings of German parks from the book Gärtnerisches Planzeichnen into a blueprint of Hibiya Park, we investigated the book to ascertain whether any design drawing was also used in Tokushima Park. We found that Seifersdorf Castle, the castle of count Brühl that was built at Seifersdorf in Germany in 13th century, is similar to the southern area of Tokushima Park

    Biogenic Amines in Periplaneta americana

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    Inhibitors of calling behavior of Plodia interpunctella

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    Some octopamine agonists were found to suppress the calling behavior of the stored product Indian meal moth, Plodia interpunctella. Compounds were screened using a calling behavior bioassay using female P. interpunctella. Four active derivatives, with inhibitory activity at the nanomolar range, were identified in order of decreasing activity: 2-(1-phenylethylamino)-2-oxazoline > 2-(2-ethyl,6-methylanilino)oxazolidine > 2-(2-methyl benzylamino)-2-thiazoline > 2-(2,6-diethylanilino)thiazolidine. Three-dimensional pharmacophore hypotheses were built from a set of 15 compounds. Among the ten common-featured models generated by the program Catalyst/HipHop, a hypothesis including a hydrogen-bond acceptor lipid, a hydrophobic aromatic and two hydrophobic aliphatic features was considered to be essential for inhibitory activity in the calling behavior. Active compounds mapped well onto all the hydrogen-bond acceptor lipid, hydrophobic aromatic and hydrophobic aliphatic features of the hypothesis. On the other hand, less active compounds were shown not to achieve the energetically favorable conformation that is found in the active molecules in order to fit the 3D common-feature pharmacophore models. The present studies demonstrate that inhibition of calling behavior is via an octopamine receptor
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