GPCR/G protein - Sigma Receptors - Sphingosine kinases (SphKs) - S1P receptors - 5-HT2 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.
- B5321 DOI hydrochlorideTarget: 5-HT2 ReceptorsSummary: 脑通透性、混合型5-HT2A/5-HT2C受体激动剂
- B7634 RP 001 hydrochlorideTarget: S1P receptorsSummary: S1P1受体激动剂
- B6765 Rimcazole dihydrochlorideTarget: Sigma ReceptorsSummary: σ受体拮抗剂
- B6574 BW 723C86 hydrochlorideTarget: 5-HT2 ReceptorsSummary: 5-HT2B激动剂
- B6364 PRE-084 hydrochloride1 CitationTarget: Sigma ReceptorsSummary: σ1受体激动剂
- B2248 Ketanserin中文名: 酮色林Target: 5-HT2 ReceptorsSummary: 特异性5-HT2A受体拮抗剂
- 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
- B2007 Pizotifen Malate中文名: 苹果酸苯噻Target: 5-HT2 Receptors|D2 ReceptorsSummary: 5-HT受体拮抗剂
- B1206 Pizotifen中文名: 苯噻啶Target: 5-HT2 ReceptorsSummary: 高选择性5-HT受体阻断剂
- 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