Reference

Interactions between macromolecular adjuvants and drugs

Interactions between macromolecular adjuvants and drugs. Part 9: association tendency between dextran and phenothiazine derivatives. Keipert, S.; Schultze, H. H.; Voigt, R. (Sekt. Chem., Humboldt-Univ., Berlin, E. Ger.). Pharmazie, 32(6), 339-40 (German) 1977. CODEN: PHARAT. DOCUMENT TYPE: Journal CA Section: 63 (Pharmaceuticals) The binding of chlorpromazine (I) [50-53-3] by dextran [9004-54-0] first increased linearly and then decreased, possibly due to dextran self-assocn. and steric hindrance to formation of mol. complexes. Dextran binding of several phenothiazine derivs. decreased in the order thioridazine [50-52-2] > I > promazine [58-40-2] > promethazine [60-87-7] > dioxopromethazine [13754-56-8]. The binding generally increased with increases in factors which promote micellar assocn. The binding decreased sharply with decreasing dielec. const. of the solvent medium, and also with increasing temp.

Biotransformation of 9,9-dioxopromethazine (Prothanon)

Biotransformation of 9,9-dioxopromethazine (Prothanon). Borchert, H. H. 13754-56-8 are also occured in this study.; Bornschein, Inga; Pfeifer, S.; Kraft, Regine (Sekt. Chem., Humboldt-Univ., Berlin, E.In this experiment, several chemicals are used like 13754-56-8 Ger.). Pharmazie, 32(8-9), 489-96 (German) 1977. CODEN: PHARAT. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacodynamics) 9,9-Dioxopromethazine-HCl (I) [13754-56-8] (50 mg/kg) given orally to rats was metabolized to 9,9-dioxo-10-[2'-methylamino-2'-methylethyl]phenothiazine [13839-55-9], 9,9-dioxophenothiazine [1209-66-1], and 8 other metabolites which were excreted in the urine. In vitro expts. indicated that the 9,9-dioxopromethazine N-oxide [29138-23-6] metabolite was converted to 10-allylphenothiazine sulfone [20962-93-0] which in turn formed 9,9-dioxo-10-2',3'-dihydroxypropyl)phenothiazine [60887-54-9]; isolation and characterization of the metabolites as well as the transformation schemes are presented. ..