GPCR/G protein - Purinergic (P2Y) Receptors - Adenosine A2A 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
- B6995 SCH 58261Target: Adenosine A2A ReceptorsSummary: A2A腺苷受体竞争性拮抗剂
- B4634 AZD1283Target: Purinergic (P2Y) ReceptorsSummary: P2Y12拮抗剂
- A8454 Istradefylline (KW-6002)中文名: 伊曲茶碱Target: Adenosine A2A ReceptorsSummary: 选择性A2A受体拮抗剂
- 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