GPCR/G protein - CysLT1 - 5-HT4 Receptors - Adenosine A2A Receptors - 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.
- B5904 Regadenoson1 Citation中文名: 类伽腺苷Target: Adenosine A2A ReceptorsSummary: A2A腺苷受体激动剂
- B8031 MK-571 sodium salt hydrate3 CitationTarget: CysLT1Summary: CysLT1受体拮抗剂
- B6995 SCH 58261Target: Adenosine A2A ReceptorsSummary: A2A腺苷受体竞争性拮抗剂
- 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
- A8454 Istradefylline (KW-6002)中文名: 伊曲茶碱Target: Adenosine A2A ReceptorsSummary: 选择性A2A受体拮抗剂
- A1334 Mosapride Citrate中文名: 莫沙必利柠檬酸盐Target: 5-HT3 Receptors|5-HT4 ReceptorsSummary: 5-HT受体激动剂
- 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
- A3885 TozadenantTarget: Adenosine A2A ReceptorsSummary: 腺苷2A受体拮抗剂
- A3735 PreladenantTarget: Adenosine A2A ReceptorsSummary: 腺苷A2A受体拮抗剂