GPCR/G protein - 5-HT Transporters - 5-HT7 Receptors
All GPCRs share a common seven trans-membrane structure. GPCRs are associated with heterotrimeric G-proteins which are GTP-binding proteins made of alpha, beta, and gamma subunits. When a ligand binds to GPCR, it activates the attached G-protein, the GDP is replaced with GTP. The activated G-protein then dissociates into an alpha and a beta-gamma complex which activates downstream signaling pathways. These intracellular signaling pathways include cAMP/PKA, calcium/NFAT, phospholipase C, protein tyrosine kinases, MAP kinases, PI-3-kinase, nitric oxide/cGMP, Rho, and JAK/STAT.
GPCRs are one of the most important therapeutic targets for various diseases, over 30% of all modern medicinal drugs target this family. Aberrant GPCR functions are involved in pathological conditions such as neurological, immunological and hormonal disorders. A large number of GPCRs have been identified, but whose ligands are not known, are classified as orphan receptors.
- B2236 Desvenlafaxine中文名: 去甲文拉法辛Target: 5-HT Transporters|Norepinephrine transportersSummary: 5-羟色胺(5-HT)和去甲肾上腺素(NE)再摄取抑制剂
- B2231 Amitriptyline HCl中文名: 盐酸阿米替林Target: Trk Receptors|5-HT2 Receptors|Norepinephrine transporter|5-HT TransportersSummary: 血清素/去甲肾上腺素受体/5-HT4/5-HT2抑制剂
- B1477 Lurasidone HCl中文名: 盐酸鲁拉西酮Target: 5-HT2 Receptors|D2 Receptors|5-HT1 Receptors|5-HT7 ReceptorsSummary: 多巴胺D2/5-HT2A/5-HT7/5-HT1A抑制剂
- A3926 Vortioxetine中文名: 沃替西汀Target: 5-HT1 Receptors|5-HT7 Receptors|5-HT3 Receptors|SERTSummary: 5-HT受体拮抗剂