Acidic elements in histamine H(3) receptor antagonists.

Sander K; von Coburg Y; Camelin JC; Ligneau X; Rau O; Schubert Zsilavecz M; Schwartz JC; Stark H

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Acidic elements in histamine H(3) receptor antagonists.

机译：组胺H（3）受体拮抗剂中的酸性元素。

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Antagonists of the human histamine H(3) receptor (hH(3)R) often contain a second basic moiety, which is well known to boost affinity on this histamine receptor subtype. Here, we prepared compounds with acidic moieties of different pK(a) values to figure out that the hH(3)R tolerates these functionalities when added to a common pharmacophore blueprint. Depending on the acidic, electronic and steric features the designed ligands showed hH(3)R affinities in the nanomolar concentration range. Additionally, selected ligands were tested but failed as dual acting hH(3)R/hPPAR (human peroxisome proliferator-activated receptor) ligands.

机译：人类组胺H（3）受体（hH（3）R）的拮抗剂通常包含第二个基本部分，众所周知，它可以增强对该组胺受体亚型的亲和力。在这里，我们制备了具有不同pK（a）值的酸性部分的化合物，以弄清楚hH（3）R在添加到常见药效基团设计图时可以耐受这些功能。根据酸性，电子和空间特征，设计的配体在纳摩尔浓度范围内显示出hH（3）R亲和力。此外，测试了选定的配体，但未能作为双重作用的hH（3）R / hPPAR（人过氧化物酶体增殖物激活受体）配体。

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《Bioorganic and Medicinal Chemistry Letters》 |2010年第5期|共4页
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Sander K; von Coburg Y; Camelin JC; Ligneau X; Rau O; Schubert Zsilavecz M; Schwartz JC; Stark H;
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1. Acidic elements in histamine H(3) receptor antagonists. [J] . Sander K, von Coburg Y, Camelin JC, Bioorganic and Medicinal Chemistry Letters . 2010,第5期

机译：组胺H（3）受体拮抗剂中的酸性元素。
2. From histamine to imidazolylalkyl-sulfonamides: the design of a novel series of histamine H3-receptor antagonists. [J] . Tozer MJ, Harper EA, Kalindjian SB, Bioorganic and Medicinal Chemistry Letters . 1999,第13期

机译：从组胺到咪唑基烷基磺酰胺：一系列新的组胺H3受体拮抗剂的设计。
3. 4-Chlorobenzyl sulfonamide and sulfamide derivatives of histamine homologues: the design of potent histamine H3 receptor antagonists. [J] . Tozer MJ, Buck IM, Cooke T, Bioorganic and Medicinal Chemistry Letters . 1999,第21期

机译：组胺同系物的4-氯苄基磺酰胺和磺酰胺衍生物：有效的组胺H3受体拮抗剂的设计。
4. Active H_1 -receptors protect against the harmful effects of H_2-receptors in a histamine induced brain edema model [C] . R. De Jongh, A. Smets, R. Nuydens, European Meeting on Glial Cells in Health and Disease . 2009

机译：活跃的H_1-refeptors防止H_2-受体在组胺诱导的脑水肿模型中的有害影响
5. Design, synthesis and evaluation of subtype-selective and non-hydrolyzable lysophosphatidic acid receptor agonists and antagonists. [D] . Heasley, Brian Haid. 2005

机译：设计，合成和评估亚型选择性和不可水解的溶血磷脂酸受体激动剂和拮抗剂。
6. Histamine H1 receptors on adherent rheumatoid synovial cells in culture: demonstration by radioligand binding and inhibition of histamine-stimulated prostaglandin E production by histamine H1 antagonists. [O] . D J Taylor, D E Woolley 1987

机译：培养的类风湿性滑膜细胞上的组胺H1受体：通过放射性配体结合和组胺H1拮抗剂抑制组胺刺激的前列腺素E产生来证明。
7. Histamine H1 receptors on adherent rheumatoid synovial cells in culture: demonstration by radioligand binding and inhibition of histamine-stimulated prostaglandin E production by histamine H1 antagonists. [O] . Taylor, D J, Woolley, D E 1987

机译：培养的类风湿性滑膜细胞上的组胺H1受体：通过放射性配体结合和组胺H1拮抗剂抑制组胺刺激的前列腺素E产生来证明。
8. Hyperemia and Edema in the Monkey Spinal Cord Following Injury: Modified by Histamine Antagonists. [R] . Doyle, T. F., Kobrine, A. I., Martins, A. N. 1976

机译：组胺拮抗剂修饰猴脊髓损伤后的充血和水肿。

Acidic elements in histamine H(3) receptor antagonists.

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