An article Nanocrystal dispersion of DK-I-56-1, a poorly soluble pyrazoloquinolinone positive modulator of alpha 6 GABAA receptors: Formulation approach toward improved in vivo performance WOS:000555462800006 published article about CREMOPHOR-EL; ORAL BIOAVAILABILITY; DRUG; NANOSUSPENSIONS; STABILITY; PHARMACOKINETICS; STABILIZATION; DISSOLUTION; SOLUBILITY; STRATEGIES in [Mitrovic, Jelena R.; Dokovic, Jelena B.; Calija, Bojan R.; Savic, Snezana D.] Univ Belgrade, Fac Pharm, Dept Pharmaceut Technol & Cosmetol, Vojvode Stepe 450, Belgrade 11221, Serbia; [Divovic, Branka; Savic, Miroslav M.] Univ Belgrade, Fac Pharm, Dept Pharmacol, Vojvode Stepe 450, Belgrade 11221, Serbia; [Knutson, Daniel E.; Cook, James M.] Univ Wisconsin, Dept Chem & Biochem, Milwaukee Inst Drug Discovery, 3210N Cramer St, Milwaukee, WI 53211 USA; [Vulic, Predrag J.] Univ Belgrade, Fac Min & Geol, Crystallog Lab, Dusina 7, Belgrade 11000, Serbia; [Randjelovic, Danijela V.] Univ Belgrade, Inst Chem Technol & Met, Dept Microelect Technol, Njegoseva 12, Belgrade 11000, Serbia; [Dobricic, Vladimir D.] Univ Belgrade, Fac Pharm, Dept Pharmaceut Chem, Vojvode Stepe 450, Belgrade 11221, Serbia in 2020.0, Cited 58.0. The Name is Benzyl Alcohol. Through research, I have a further understanding and discovery of 100-51-6. SDS of cas: 100-51-6
DK-I-56-1 (7-methoxy-2-(4-methoxy-d(3)-phenyl)-2,5-dihydro-3H-pyrazolo[4,3-c]quinolin-3-one), a recently de-veloped deuterated pyrazoloquinolinone, has been recognized as a lead candidate for treatment of various neuropsychiatric disorders. During preclinical investigation of poorly water-soluble compounds such as DK-I-56-1, the application of nanotechnology could be advantageous due to improved safety and possibly increased bioavailability of nanosized formulation. DK-I-56-1 nanosuspensions stabilized by polysorbate 80, alone or in combination with poloxamers 188 i.e. 407 or D-alpha-tocopheryl polyethylene glycol 1000 succinate, were prepared using a small-scale media milling device. With particle size 208.7-250.6 nm and polydispersity index <0.250, selected nanodiseprsions were stable for three weeks. Pharmacokinetic and biodistribution studies following intraperitoneal administration of three types of formulation in mice indicated high plasma DK-I-56-1 levels after solution (10,228.6 +/- 1037.2 ngh/ml) and nanosuspension (6770.4 +/- 770.7 ngh/ml) but not suspension ad-ministration (966.0 +/- 58.1 ngh/ml). However, distribution of DK-I-56-1 after solution was heavily influenced by its composition, and brain availability of nanosuspension was superior to that of solution formulation. In spontaneous locomotor activity test, the expected hyperlocomotor effect was observed after nanosuspension administration, without compromising impact of the vehicle/excipients used. Therefore, nanonization of drug compound assembled with proper selection of stabilizers may seemingly contribute further thorough testing of DK-I-56-1 preclinical efficacy. SDS of cas: 100-51-6. About Benzyl Alcohol, If you have any questions, you can contact Mitrovic, JR; Divovic, B; Knutson, DE; Dokovic, JB; Predrag, J; Randjelovic, DV; Dobricic, VD; Calija, BR; Cook, JM; Savic, MM; Snezana, D or concate me.
Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles