别名 血清素质膜转运蛋白、5-HTT、5-hydroxytryptamine (serotonin) transporter + [13] |
简介 Serotonin transporter that cotransports serotonin with one Na(+) ion in exchange for one K(+) ion and possibly one proton in an overall electroneutral transport cycle. Transports serotonin across the plasma membrane from the extracellular compartment to the cytosol thus limiting serotonin intercellular signaling (PubMed:27756841, PubMed:34851672, PubMed:21730057, PubMed:10407194, PubMed:27049939, PubMed:12869649). Essential for serotonin homeostasis in the central nervous system. In the developing somatosensory cortex, acts in glutamatergic neurons to control serotonin uptake and its trophic functions accounting for proper spatial organization of cortical neurons and elaboration of sensory circuits. In the mature cortex, acts primarily in brainstem raphe neurons to mediate serotonin uptake from the synaptic cleft back into the pre-synaptic terminal thus terminating serotonin signaling at the synapse (By similarity). Modulates mucosal serotonin levels in the gastrointestinal tract through uptake and clearance of serotonin in enterocytes. Required for enteric neurogenesis and gastrointestinal reflexes (By similarity). Regulates blood serotonin levels by ensuring rapid high affinity uptake of serotonin from plasma to platelets, where it is further stored in dense granules via vesicular monoamine transporters and then released upon stimulation (PubMed:17506858, PubMed:18317590). Mechanistically, the transport cycle starts with an outward-open conformation having Na1(+) and Cl(-) sites occupied. The binding of a second extracellular Na2(+) ion and serotonin substrate leads to structural changes to outward-occluded to inward-occluded to inward-open, where the Na2(+) ion and serotonin are released into the cytosol. Binding of intracellular K(+) ion induces conformational transitions to inward-occluded to outward-open and completes the cycle by releasing K(+) possibly together with a proton bound to Asp-98 into the extracellular compartment. Na1(+) and Cl(-) ions remain bound throughout the transport cycle (PubMed:27756841, PubMed:34851672, PubMed:21730057, PubMed:10407194, PubMed:27049939, PubMed:12869649). Additionally, displays serotonin-induced channel-like conductance for monovalent cations, mainly Na(+) ions. The channel activity is uncoupled from the transport cycle and may contribute to the membrane resting potential or excitability (By similarity). |
作用机制 多巴胺重摄取抑制剂 [+2] |
在研机构 |
最高研发阶段批准上市 |
首次获批国家/地区 中国 |
首次获批日期2022-11-01 |
作用机制 肾上腺素能吸收抑制剂 [+1] |
非在研适应症- |
最高研发阶段批准上市 |
首次获批国家/地区 美国 |
首次获批日期2022-06-29 |
作用机制 5-HT1D receptor激动剂 [+4] |
在研机构 |
原研机构 |
在研适应症 |
非在研适应症- |
最高研发阶段批准上市 |
首次获批国家/地区 美国 |
首次获批日期2020-06-25 |
开始日期2025-10-30 |
申办/合作机构 |
开始日期2025-07-01 |
开始日期2024-12-01 |
申办/合作机构- |