GPCR/G protein - CB1 Receptors - Angiotensin AT2 Receptors - 5-HT2 Receptor
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.
- B6347 Methylergometrine maleate中文名: 马来酸甲麦角新碱Target: 5-HT1 Receptor|5-HT2 ReceptorSummary: 5-HT1/5-HT2受体拮抗剂
- B1427 AM251Target: CB1 ReceptorsSummary: 有效的CB1拮抗剂
- B1429 Rimonabant3 Citation中文名: 利莫那班Target: CB1 Receptors|CB2 ReceptorsSummary: CB1 受体拮抗剂
- B1426 Org 27569Target: CB1 ReceptorsSummary: 大麻素CB1受体别构调节剂
- B2206 PD123319Target: Angiotensin AT2 ReceptorsSummary: 血管紧张素AT2受体的拮抗剂
- A3704 PD 123319 ditrifluoroacetateTarget: Angiotensin AT2 ReceptorsSummary: 血管紧张素AT2受体拮抗剂