Hynie S
Farmakologický ústav 1. LF UK, Praha.
Cesk Fysiol. 1995 Sep;44(3):135-8.
5-HT receptors represent a superfamily of receptors with the largest known number of receptor subtypes. At present 15 receptor subtypes of three groups has been recognized. The 5-HT1 subfamily of receptors contains subtypes 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, and 5-HT1F; activation of all of them results in the inhibition of adenylylcyclase. The subfamily of 5-HT2 contains subtypes 5-HT2A, 5-HT2B, and 5-HT2C; their activation leads to the stimulation of PLC. Finally, subfamily of miscellaneous 5-HT receptors contains subtypes 5-HT3, 5-HT4, 5-HT5, 5-HT6, and 5-HT7; some of them has been cloned, however, our knowledge on their function is still minimal. 5-HT receptors participate in many physiological functions and a disturbance in serotonergic neurotransmission might cause several types of disease. 5-HT plays an important role in depression; to cure this disease, drugs which increase levels of this neurotransmitter are used. A new drug group called Selective Serotonin Reuptake Inhibitors (SSRI) has been recently discovered. These drugs block the reuptake of 5-HT into nerve endings. There is an intensive search for new selective agonists as well as antagonists which could be use not only in the classification of receptor subtypes but which also possess certain therapeutic potential.
5-羟色胺(5-HT)受体代表了一个受体超家族,其已知的受体亚型数量最多。目前已识别出三组共15种受体亚型。5-HT1受体亚家族包含5-HT1A、5-HT1B、5-HT1D、5-HT1E和5-HT1F亚型;它们的激活均导致腺苷酸环化酶的抑制。5-HT2亚家族包含5-HT2A、5-HT2B和5-HT2C亚型;它们的激活会刺激磷脂酶C(PLC)。最后,其他5-HT受体亚家族包含5-HT3、5-HT4、5-HT5、5-HT6和5-HT7亚型;其中一些已被克隆,然而,我们对它们功能的了解仍然很少。5-HT受体参与许多生理功能,血清素能神经传递的紊乱可能会导致多种疾病。5-HT在抑郁症中起重要作用;为了治疗这种疾病,人们使用能增加这种神经递质水平的药物。最近发现了一种名为选择性5-羟色胺再摄取抑制剂(SSRI)的新药组。这些药物可阻止5-HT重新摄取到神经末梢中。人们正在积极寻找新的选择性激动剂和拮抗剂,它们不仅可用于受体亚型的分类,还具有一定的治疗潜力。