GPCR/G protein - Adenosine A2A Receptors - Prostanoid Receptors - Angiotensin AT1 Receptors - Animal Experiments
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
- B7568 16,16-Dimethyl Prostaglandin E2Target: Prostanoid ReceptorsSummary: 前列腺素E2的衍生物
- B7088 L-161,982Target: Prostanoid ReceptorsSummary: EP4受体拮抗剂
- B2214 Valsartan中文名: 缬沙坦Target: Angiotensin AT1 ReceptorsSummary: 血管紧张素II AT1受体拮抗剂
- B1007 AVE 09911 CitationTarget: Angiotensin AT1 ReceptorsSummary: 血管紧张素-(1-7)受体激动剂
- B2210 Azilsartan中文名: 阿齐沙坦Target: Angiotensin AT1 ReceptorsSummary: 强效血管紧张素II 1型(AT1)受体反向激动剂
- A8454 Istradefylline (KW-6002)中文名: 伊曲茶碱Target: Adenosine A2A ReceptorsSummary: 选择性A2A受体拮抗剂
- A5970 Irbesartan中文名: 安博维,厄贝沙坦Target: Angiotensin AT1 ReceptorsSummary: 血管紧张素II抑制剂
- A3735 PreladenantTarget: Adenosine A2A ReceptorsSummary: 腺苷A2A受体拮抗剂