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Comparative effects of idazoxan, efaroxan, and BU 224 on insulin secretion in the rabbit: Not only interaction with pancreatic imidazoline I2 binding sites

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Health 2010年第2期2卷 112-123页

作者： María José García-Barrado María Francisca Pastor María Carmen Iglesias-Osma Christian Carpéné Julio Moratinos 不详

The nature of the binding site(s) involved in the insulin secretory activity of imidazoline compo- unds remains unclear. An imidazoline I2 binding site (I2BS) has been neglected since the classic I2 ligand, idazoxan, does not release insulin. Using the rabbit as an appropriate model for the study of this type of binding sites, we have tried to re-evaluate the effects of idazoxan, the selective I2 compound BU 224, and efaroxan on insulin secretion. Mimicking efaroxan, idazoxan and BU 224 potentiated insulin release from perifused islets in the presence of 8 mM glucose. In static incubation, insulin secretion induced by idazoxan and BU 224 exhibited both dose and glucose dependencies. ATP-sensitive K+ (KATP) channel blockade, though at a different site from the SUR1 receptor, with subsequent Ca2+ entry, mediates the insulin releasing effect of the three ligands. However, additional MAO independent intracellular steps in stimulus- secretion coupling linked to PKA and PKC activation are only involved in the effect of BU 224. Therefore, both an I2 related binding site at the channel level shared by the three ligands and a putative I3-intracellularly located binding site stimulated by BU 224 would be mediating insulin release by these compounds. In vivo experiments reassess the abilities of idazoxan and BU 224 to enhance glucose-induced insulin secretion and to elicit a modest blood glucose lowering response.

关键词： BU 224 Efaroxan Idazoxan imidazoline Ligands Insulin Secretion IVGTT (Intravenous Glucose Tolerance Test) KATP Channel PK Activity Rabbit Pancreatic Islets

Neuroprotective effects of receptor imidazoline 2 and its endogenous ligand agmatine

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Neuroscience Bulletin 2006年第3期22卷 187-191页

作者： Wei-Wen QIU Rong-Yuan ZHENG Department of Neurology the First Affiliated Hospital of Wenzhou Medical College Wenzhou 325000 China

Receptor imidazoline 2 （I2） is one of the imidazoline receptors with high affinity for [^3H]-idazoxan. Receptor I2, being classified into I2A and I28 subtypes, is mainly localized to the outer membrane of mitochondria in liver, kidney and brain. Receptor I2, displaying high similarity of sequence with monoamine oxidase-B （MAO-B）, is structurally related to MAO-B, but the I2 imidazoline binding site （IEBS） with ligand is distinct from the catalytic site of MAO-B. Agmatine is the endogenous ligand of receptor I2. Accumulating evidence have revealed that the activation of receptors I2 may produce neuroprotective effects by increasing expression of glial fibriUary acidic protein （GFAP） in astrocytes, inhibiting activity of MAO, reducing calcium overload in cells. Agmatine exerts neuroprotection against ischemia-hypoxia, injury, glutamateinduced neurotoxicity by activating imidazoline receptors, blocking N-methyl-D-aspartate （NMDA） receptor, inhibiting all isoforms of nitric oxide synthase （NOS）, and selectively blocking the voltage-gated calcium channels （VGCC）. It would be expected that agmatine is one of the potential neuroprotective agents.

关键词： receptor imidazoline ligand agmatine neuroprotection

Construction of bicyclic imidazoline derivatives via dipolar cycloadditions from conjugate addition-proton transfer

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Construction of bicyclic imidazoline derivatives via dipolar...

New Palladium-Imidazole and imidazoline Complexes:Structures and Reactivity in Coupling Reaction

有机合成创新—产业化的新动力——中国化学会全国第三届有机合成化学与过程学术讨论会

作者： Zhang,Xiaohui~* Guo,Ming (College of Environment and Chemical Engineering,Dalian University,Dalian 116622)

Azomethine ylides,defined by Huisgen,are planar molecules composed of one nitrogen atom and terminal sp carbons and belong to a class of azomethine obtained which lead to 1,3-dipolar cycloaddition reaction. Cycloaddition reactions minimise the number of separate bond-forming steps by generating several bonds simultaneously,and 1,3-dipolar cycloadditions are an obvious way to apply this strategy to heterocycles.

关键词： imidazoline dihydroimidazolium ylide dipolar cycloaddition proton-transfer

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复旦学报（自然科学版） 2007年第5期46卷 768-页

作者： Satoshi Haneda Kazuo Eda Masahiko Hayashi Department of Chemistry Graduate School of ScienceKobe University

1 Results We have recently reported the Mizoroki-Heck reaction catalyzed by PdCl2 and imidazole ligands[1]. During the course of our study of palladium imidazole complex,we disclosed the synthesis of trans-Pd(Ln)2Cl2 by the reaction of PdCl2 with Ln (where L1=2-phenylimidazole,L2=2-phenylimidazole) in a 1∶2 molar *** single crystals of trans-Pd(L1)2Cl2·2DMF (1a) and trans-Pd(L2)2Cl2 (2a) were obtained by following slow evaporation of DMF as a solvent. The single crystal of trans-Pd(L2)2Cl2 (2b) w...

关键词： palladium complex imidazole imidazoline X-ray analysis coupling reaction Mizoroki-Heck reaction

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咪唑啉及其衍生物imidazoline

精细与专用化学品 1985年第8期 17-17页

作者：李宇乡

别名二氢咪唑(Dihydroimidazole),间二氮杂环烯。【毒性】有毒。【制法】以乙二醛、甲醛和氨为原料制得咪唑,然后氢化得二氢咪唑。【生产情况】美国齐密特(Ziminito)等公司生产。【用途】咪唑啉及其衍生物是新开发的高效有机缓蚀剂。美... 详细信息

别名二氢咪唑(Dihydroimidazole),间二氮杂环烯。【毒性】有毒。【制法】以乙二醛、甲醛和氨为原料制得咪唑,然后氢化得二氢咪唑。【生产情况】美国齐密特(Ziminito)等公司生产。【用途】咪唑啉及其衍生物是新开发的高效有机缓蚀剂。美国在油田使用的各种有机缓蚀剂中,以咪唑啉的用量最大。

关键词：有机缓蚀剂 imidazoline 衍生物

Preparation of ferrocenyl imidazolines using bis(triphenyl)oxodiphosphonium trifluoromethanesulfonate

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Science China Chemistry 2009年第9期52卷 1331-1336页

作者： WANG XueQiang XIA JiBao DAI XiaoYang YOU ShuLi State Key Laboratory of Organometallic Chemistry Shanghai Institute of Organic ChemistryChinese Academy of SciencesShanghai 200032China

An efficient synthesis of ferrocenyl imidazolines starting from ferrocenyl carboxylic acids has been developed. Bis(triphenyl)oxodiphosphonium trifluoromethanesulfonate was used to convert smoothly ferrocenyl carboxylic amides bearing an amine side chain, derived from ferrocenyl carboxylic acids and 1,2-diamines, to their corresponding ferrocenyl imidazolines.

关键词： asymmetric catalysis chiral dehydration ferrocene imidazoline

Studies of Self-assembled Monolayers Formed by Imidazofine on Iron Surface by SEM and SECM

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Chinese Chemical Letters 2006年第12期17卷 1615-1618页

作者： Xiu Yu LIU Shen Hao CHEN Shuai MIAO Su Xiang WU Li Xia SHEN Yuan Xing CAI Hong Yan ZHAI Deoartment of Chemistry Shandong University Jinan 250100 State Key Laboratory for Corrosion and Protection Shenyang 110015 Shandong Academy of Sciences Jinan 250014

The self-assembled monolayers （SAMs） of imidazoline （IM） on the iron surface were characterized by scanning electron microscope （SEM） and scanning electrochemical microscopy （SECM）. The results showed that SAM... 详细信息

关键词： imidazoline self-assembled monolayers (SAMs) SEM SECM.

The synthesis of dialdehydes from dicarboxylic acids via imidazolines

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Chinese Science Bulletin 1997年第2期42卷 130-132页

作者： Shi, Z Gu, H Xu, LL Department of Chemistry Northwest University Xi’an China

DIALDEHYDES are important chemical industrial materials, which are widely used in textile,medicine, dye, binder, coating and so on. The traditional method for preparing dialdehydes is the catalytic oxidation of glycol. We have reported the reduction ring-opening reaction of inndazoline by NaBH4.In this note, the reduction of imidazoline by sodium and ethanol is studied. A new synthetic method for the preparation of dialdehydes from dicarboxylic acids

关键词： dicarboxylic acid imidazoline dialdehyde new synthetic method.

Hydroxy- and Aminoethyl imidazolines of Cottonseed Oil Fatty Acids as Additives for Diesel Fuels

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Open Journal of Synthesis Theory and Applications 2015年第2期4卷 33-39页

作者： Vaqif Maherram Abbasov Tarana Aslan Mammadova Khayam Rahim Veliyev Khayala Hamlet Kasamanli Institute of Petrochemical Processes Named after Yu. G. Mamedaliyev of National Academy of Sciences of Azerbaijan Baku Azerbaijan Ganja State University Ganja Azerbaijan

In the research, aminoethyl imidazolines of cottonseed oil fatty acids with diethylenetriamine have been synthesized using the ultrasonic device creating the effect of cavitation. The yield of imidazolines was 90% - 95%. The influence of the synthesized imidazolines on lubricity quality of low sulfur diesel fuels having low lubricating quality was studied. The results showed that at concentrations 200 - 250 ppm the synthesized imidazolines can be applied as additives enhancing lubricity quality of diesel fuels.

关键词： Cavitation imidazoline Cottonseed Oil Fatty Acids N-Hydroxyethyl Ethylenediamine Diethylenetriamine