Waeber C, Schoeffter P, Hoyer D, Palacios J M
Preclinical Research, Sandoz Pharma Ltd., Basel, Switzerland.
Neurochem Res. 1990 Jun;15(6):567-82. doi: 10.1007/BF00973745.
Most of the known neurotransmitters interact with more than one type of receptor. Some of them even dispose of receptor subtypes to exert their actions. Serotonin, far from being an exception to that, possesses at least 3 classes of receptors, which have all been reported to be heterogeneous, although convincing data only exist for the 5-HT1 class. This name has been proposed in 1979, two years before the introduction of 'A' and 'B' in the nomenclature to account for the observed heterogeneity of these sites. The 5-HT1C receptor subtype was first described in 1984 and the last member of the family, named 5-HT1D, was characterized in 1987. The pharmacological profiles, the signal transducing systems and the anatomical localizations, both at the regional and cellular levels, of all these subtypes have been investigated and possible functions have been proposed for each of them. Moreover, last and most definitive demonstration of the subtype individuality, the gene or complementary DNA coding for the 5-HT1A and 5-HT1C (and 5-HT2) receptors have been cloned and sequenced. Such data are still missing for 5-HT1D (and 5-HT1B) receptors, but will certainly be provided in the next few years. However and waiting for this decisive clue, the characterization of the 5-HT1D subtype leaves no doubt concerning its significance as a function 5-HT receptor. This review will concentrate on the characteristics of this subtype of 5-HT receptor.
大多数已知的神经递质可与不止一种类型的受体相互作用。其中一些甚至具有受体亚型以发挥其作用。血清素也绝非例外,它至少拥有3类受体,据报道所有这些受体都是异质性的,尽管仅针对5-HT1类有令人信服的数据。这个名称于1979年被提出,比在命名法中引入“A”和“B”以解释这些位点观察到的异质性早两年。5-HT1C受体亚型于1984年首次被描述,该家族的最后一个成员,即5-HT1D,于1987年被鉴定。已经对所有这些亚型在区域和细胞水平上的药理学特征、信号转导系统和解剖定位进行了研究,并针对它们各自提出了可能的功能。此外,作为亚型个体性的最后也是最确凿的证明,编码5-HT1A和5-HT1C(以及5-HT2)受体的基因或互补DNA已被克隆和测序。对于5-HT1D(和5-HT1B)受体,此类数据仍然缺失,但肯定会在未来几年内得到。然而,在等待这一决定性线索的过程中,5-HT1D亚型的特征无疑表明了其作为5-HT功能受体的重要性。本综述将集中讨论5-HT受体这一亚型的特征。