GPCR/G protein - Norepinephrine transporter - 5-HT6 Receptor - Angiotensin AT1 Receptors - 5-HT1 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
- B7531 WAY 208466 dihydrochlorideTarget: 5-HT6 ReceptorSummary: 5-HT6激动剂
- B2231 Amitriptyline HCl中文名: 盐酸阿米替林Target: Trk Receptors|5-HT2 Receptors|Norepinephrine transporter|5-HT TransportersSummary: 血清素/去甲肾上腺素受体/5-HT4/5-HT2抑制剂
- B2251 Naratriptan中文名: 盐酸那拉曲坦,盐酸纳拉曲坦Target: 5-HT1 ReceptorSummary: 选择性5-HT1受体亚型激动剂
- 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
- 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