A novel serie of ET_A selective antagonists

机译：Et_A选择性拮抗剂的一部小说Serie

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The endothelins (ETs) are a family of three isopeptides (ET-1, ET-2 and Et-3) with potent vasoconstrictor properties [1]. All three of these peptides are encoded in the human genome and each is composed of 21 amino acids, with disulfide linkages between cysteine residues at positions 1,15 and 3,11. The ETs elicit their effects through binding to receptors of the G-protein coupled seven-transmembrane spanning superfamily. Two receptor subtypes have thus far been fully characterized from human tissues through molecular cloning and expression. Recently, compelling data has become available using receptor specific antagonists to support a role for the ETs in disease processes. Despite extensive animal model studies, however, controversy still surrounds the optimal antagonist selectivity considered necessary for the treatment of human disorders [2] and this may also be dependent upon the disease targeted.

机译：内皮素（ETE）是三种异肽（ET-1，ET-2和ET-3）的家族，具有有效的血管电机特性[1]。这些肽中的所有三种在人类基因组中编码，每个肽由21个氨基酸组成，在1,15和3,11,111的半胱氨酸残基之间具有二硫键。 ETS通过与跨家族的G-蛋白偶联的七跨膜的受体结合来引发它们的效果。到目前为止，两种受体亚型通过分子克隆和表达完全表征了人体组织。最近，使用受体特异性拮抗剂可获得引人注目的数据，以支持疾病过程中ETS的作用。然而，尽管具有广泛的动物模型研究，但争议仍然围绕着治疗人类疾病所需的最佳拮抗剂选择性[2]，这也可能取决于靶向的疾病。

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《Chinese peptide symposium》|1998年||共4页
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J.-N.Xiang; S.T.Atkinson; D.Gaitanopoulos; D.Bryan; P.Nambi; E.H.Ohlstein; J.Weinstock; J.D.Elliott;
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中图分类抗体蛋白与干扰素蛋白;
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1. Discovery, Modeling, and Human Pharmacokinetics of N-(2-Acetyl-4,6-dimethylphenyl)-3-(3,4-dimethylisoxazol-5-ylsulfamoyl)thiophene-2-carboxamide (TBC3711), a Second Generation, ET_A Selective, and Orally Bioavailable Endothelin Antagonist [J] . Chengde Wu, E. Radford Decker, Natalie Blok, Journal of Medicinal Chemistry . 2004,第8期

机译：第二代ET_A选择性N-（2-乙酰基-4,6-二甲基苯基）-3-（3,4-二甲基异恶唑-5-基氨磺酰基）噻吩-2-羧酰胺（TBC3711）的发现，建模和人体药代动力学和口服生物利用内皮素拮抗剂
2. Effect of ABT-627(A-147627), a potent selective ET_A receptor antagonist, on the cardiopulmonary profile of newborn lambs with surgically-induced diaphragmatic hernia [J] . Melanie Kavanagh, Bruno Battistini, Sonia Jean British Journal of Pharmacology . 2001,第8期

机译：有效的选择性ET_A受体拮抗剂ABT-627（A-147627）对手术致diaphragm肌疝的新生羔羊心肺功能的影响
3. Effects of the novel selective endothelin ET_A receptor antagonist, SB 234551, on the cardiovascular responses to endotoxaemia in Conscious rats [J] . S.M.Gardiner, J.E.March, P.A.Kemp British Journal of Pharmacology . 2001,第8期

机译：新型选择性内皮素ET_A受体拮抗剂SB 234551对清醒大鼠对内毒素血症的心血管反应的影响
4. A novel serie of ET_A selective antagonists [C] . J.-N.Xiang, S.T.Atkinson, D.Gaitanopoulos, Chinese peptide symposium . 1998

机译：Et_A选择性拮抗剂的一部小说Serie
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A novel serie of ET_A selective antagonists

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