Twin and Triplet Drugs in Opioid Research

被引:38
作者
Fujii, Hideaki [1 ]
机构
[1] Kitasato Univ, Sch Pharm, Minato Ku, Tokyo 1088641, Japan
来源
CHEMISTRY OF OPIOIDS | 2011年 / 299卷
关键词
Dual action; Increment of potency; Receptor dimerization; Twin drug; Triplet drug; RECEPTOR-BINDING PROPERTIES; LINKED BIFUNCTIONAL PEPTIDES; ANTAGONIST BIVALENT LIGANDS; PROTEIN-COUPLED RECEPTORS; MESSAGE-ADDRESS CONCEPT; RAT SPINAL-CORD; SUBSTANCE-P; MORPHINE-TOLERANCE; HIGH-AFFINITY; I-2-IMIDAZOLINE RECEPTORS;
D O I
10.1007/128_2010_76
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Twin and triplet drugs are defined as compounds that contain respectively two and three pharmacophore components exerting pharmacological effects in a molecule. The twin drug bearing the same pharmacophores is a "symmetrical twin drug", whereas that possessing different pharmacophores is a "nonsymmetrical twin drug." In general, the symmetrical twin drug is expected to produce more potent and/or selective pharmacological effects, whereas the nonsymmetrical twin drug is anticipated to show both pharmacological activities stemming from the individual pharmacophores (dual action). On the other hand, nonsymmetrical triplet drugs, which have two of the same pharmacophores and one different moiety, are expected to elicit both increased pharmacological action and dual action. The two identical portions could bind the same receptor sites simultaneously while the third portion could bind a different receptor site or enzyme. This review will mainly focus on the twin and triplet drugs with an evaluation of their in vivo pharmacological effects, and will also include a description of their pharmacology and synthesis.
引用
收藏
页码:239 / 275
页数:37
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