Development of a model for the delta opioid receptor pharmacophore. 1. Conformationally restricted Tyr1 replacements in the cyclic delta receptor selective tetrapeptide Tyr-c[D-Cys-Phe-D-Pen]OH (JOM-13).
Development of a model for the delta opioid receptor pharmacophore. 1. Conformationally restricted Tyr1 replacements in the cyclic delta receptor selective tetrapeptide Tyr-c[D-Cys-Phe-D-Pen]OH (JOM-13).
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开发 δ 阿片受体药效团模型。
DOI：
10.1021/jm00051a015
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发表时间：
1994
影响因子：
7.3
通讯作者：
Porreca,F
中科院分区：
文献类型：
--
作者：
Mosberg,HI;Lomize,AL;Wang,C;Kroona,H;Heyl,DL;Sobczyk-Kojiro,K;Ma,W;Mousigian,C;Porreca,F
在生物活性多肽的类似物中加入构象限制是提高受体选择性和调节效力的一种公认的方法，因为原则上产生的更刚性的类似物可能具有低能量的构象-+缩写，并且使用了IUPAC-IUB生物化学命名委员会推荐的定义。其他缩写：-MeTyr，a-甲基-Tyr；Ho-Tic，1，2，3，4，-tetrahydro-7-hydroxyisoquinoline-3-carboxyIic酸；Hai，6-羟基-2-氨基吲哚-2-羧酸；Hat，6-羟基-2-氨基四氢-2-羧酸；c-hpp和-hpp，顺式和irans-3-(4‘-羟基苯基)脯氨酸。
The incorporation of conformational constraints in analogues of biologically active peptides is a well-established approach for enhancing receptor selectivity and modulating efficacy, since, in principle, the resulting more rigid analogues may possess low-energy conforma-+ Abbreviations and definitions recommended by IUPAC-IUB Com-mission of Biochemical Nomenclature have beenused. Other abbreviations:-MeTyr, a-methyl-Tyr; HO-Tic, 1, 2, 3, 4,-tetrahydro-7-hydroxyisoquinoline-3-carboxyIic acid; Hai, 6-hydroxy-2-aminoindan-2-carboxylic acid; Hat, 6-hydroxy-2-aminotetralin-2-carboxylic acid; c-Hpp and-Hpp, cis-and irans-3-(4'-hydroxyphenyl) proline, respec-tively.