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| 1 | INN | Class | Route (list) | PK parameters= Cmax; Tmax; F: bioavailability; t1/2: half-life; VD: volume of distribution; Cl: clearance; PPB: plasma protein binding;(EQN means that the equation t1/2 = VD / Cl * 0.693 was used | Primary Target and PDB code of Protein-Drug complex | Targets from DrugCentral | Links | |||
| FOSPROPOFOL DISCONTINUED (has an active metabolite)
| FOSPROPOFOL | NERVOUS SYSTEM | INTRAVENOUS | Cmax 732.6 MICROMOLAR (18 MILLIGRAM/KG) VD 21.4 LITER (65 KILOGRAM) PPB 98 PERCENT Cl 18.2 LITER / HOUR (65 KILOGRAM) HT 0.81 HOUR (18 MILLIGRAM/KG) SOLUBILITY WATER SOLUBLE PRODRUG OF PROPOFOL | GAMMA-AMINOBUTYRIC-ACID RECEPTOR SUBUNIT ALPHA-1 (GABA(A)) BETA-ADRENOCEPTOR (BETA-AR) (PMID21793316) PDB 8YRG (CRYOEM STRUCTURE OF FOSPROPOFOL-BOUND MRGPRX4-GQ COMPLEX) LIGAND CODE = A1LZU (link to the list of PDB complexes) Download experimental 3D coordinates of A1LZU with added hydrogens | GABA-A receptor alpha-1,beta-2,gamma-2 UNIPROT P14867 GABRA1 -- GABA-A receptor alpha-1,beta-3,gamma-2 UNIPROT P14867 GABRA1 more at DrugCentral | EMA | |||
| 2 | INN | Class | Route (list) | PK parameters= Cmax; Tmax; F: bioavailability; t1/2: half-life; VD: volume of distribution; Cl: clearance; PPB: plasma protein binding;(EQN means that the equation t1/2 = VD / Cl * 0.693 was used | Primary Target and PDB code of Protein-Drug complex | Targets from DrugCentral | Links | |||
| PROPOFOL (is an active metabolite)
| PROPOFOL | NERVOUS SYSTEM | INJECTION | Cmax 21.9 MICROMOLAR (18 MILLIGRAM/KG) VD 305 LITER (65 KILOGRAM) PPB 98 PERCENT Cl 150 LITER / HOUR HT 3.2 HOUR SOLUBILITY SLIGHTLY SOLUBLE IN WATER | GAMMA-AMINOBUTYRIC-ACID RECEPTOR SUBUNIT ALPHA-1 (GABA(A)) BETA-ADRENOCEPTOR (BETA-AR) (PMID21793316) PDB 5MVN (X-RAY STRUCTURE OF THE M205W MUTANT OF GLIC IN COMPLEX WITH PROPOFOL) LIGAND CODE = PFL (link to the list of PDB complexes) Download experimental 3D coordinates of PFL with added hydrogens | GABA-A receptor alpha-1,beta-2,gamma-2 UNIPROT P14867 GABRA1 -- GABA-A receptor alpha-1,beta-3,gamma-2 UNIPROT P14867 GABRA1 more at DrugCentral | EMA | |||
