GPCR/G protein - Angiotensin AT2 Receptors - Angiotensin AT1 Receptors - Glutamate (Metabotropic) Group I Receptors - 5-HT1 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.
- 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
- 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
- B2206 PD123319Target: Angiotensin AT2 ReceptorsSummary: 血管紧张素AT2受体的拮抗剂
- 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
- A5294 Sumatriptan Succinate中文名: 舒马普坦琥珀酸盐Target: 5-HT1 ReceptorsSummary: 5-HT1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
- A3704 PD 123319 ditrifluoroacetateTarget: Angiotensin AT2 ReceptorsSummary: 血管紧张素AT2受体拮抗剂
- A3633 MPEP HydrochlorideTarget: Glutamate (Metabotropic) Group I ReceptorsSummary: MGlu5受体拮抗剂