Binding properties of dipropyltryptamine at the human 5-HT1a receptor.
Binding properties of dipropyltryptamine at the human 5-HT1a receptor.
复制标题
二丙基色胺与人类 5-HT1a 受体的结合特性。
DOI：
10.1159/000085649
复制
发表时间：
2005
期刊：
影响因子：
3.1
通讯作者：
Parker,KeithK
中科院分区：
文献类型：
--
作者：
Thiagaraj,HarishV;Russo,EthanB;Burnett,Andrea;Goldstein,Eric;Thompson,CharlesM;Parker,KeithK
二丙基色胺（Dipropyltryptamine， DPT）是20世纪60年代首次发现的一种人工合成吲哚烷基胺。自从发现多种5-羟色胺受体亚型以来，人们基本上被遗忘了，本文描述了克隆人类5-HT1a受体上DPT的一些特性。当[3H]8-OH-DPAT与受体结合时，DPT抑制相互作用，ic50为0.1µmol/l。当DPT/激动剂相互作用的双倒数图被分析时，这种相互作用被证明是竞争性的。DPT在信号转导系统中的作用是复杂的。当测定cAMP和γ-S-GTP掺入量时，DPT单独（0.1 - 1000µmol/l）激活gim，而在5-HT（0.1-10µmol/l）存在时，DPT阻断了激动剂的作用。综上所述，研究结果表明DPT是人类5-HT1a受体的中等亲和力部分激动剂。这些结果提供了证据，证明DPT有潜力作为5-HT1a受体的多功能实验工具。
Dipropyltryptamine (DPT) is a synthetic indolealkylamine first characterized in the 1960s. Largely forgotten since the discovery of multiple serotonin receptor subtypes, some of the properties of DPT at the cloned human 5-HT1a receptor are described here. When [3H]8-OH-DPAT is bound to the receptor, DPT inhibits the interaction with an IC50of 0.1 µmol/l. This interaction is shown to be competitive when double-reciprocal plots of the DPT/agonist interaction are analyzed. DPT’s effects in the signal transduction system are complex. While DPT alone (0.1–1,000 µmol/l) activates Giwhen both cAMP and γ-S-GTP incorporation are measured, in the presence of 5-HT (0.1–10 µmol/l), DPT blocks the agonist effect. In combination, the findings suggest that DPT is a moderate affinity partial agonist at the human 5-HT1a receptor. These results provide evidence that DPT has potential as a versatile experimental tool at 5-HT1a receptors.