GPCR/G protein - 5-HT4 Receptors - 5-HT4 Receptor - PAR receptor - Sigma 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.
- B5705 Q94 hydrochlorideTarget: PAR receptorSummary: PAR1负变构调节剂
- B6765 Rimcazole dihydrochlorideTarget: Sigma ReceptorsSummary: σ受体拮抗剂
- B6364 PRE-084 hydrochloride1 CitationTarget: Sigma ReceptorsSummary: σ1受体激动剂
- B1198 CisaprideTarget: Voltage-gated Potassium (KV) Channels|5-HT4 ReceptorSummary: 5-HT4受体激动剂
- A1334 Mosapride Citrate中文名: 莫沙必利柠檬酸盐Target: 5-HT3 Receptors|5-HT4 ReceptorsSummary: 5-HT受体激动剂