The pharmacokinetics and bioavailability of a derivative of 3,7-diazabicyclo[3.3.1]nonane exhibiting a nootropic effect, were studied after a single dose to rats. The pharmacokinetics of the compound was studied after oral and intravenous administration to 270 male rats Sprague Dawley at doses of 2.5 mg/kg, 13 mg/kg and 25 mg/kg. Its distribution in organs and tissues (brain, thymus, heart, lungs, liver, kidneys, and spleen) was also investigated. It was found that after a single intravenous administration, the investigated substance was determined in the blood of animals for 24 h; the half-life was 4.69 h. The relative bioavailability of the 3,7-diazabicyclo[3.3.1]nonane derivative after oral administration was 42.3%, thus suggesting the prospect of creating dosage forms for oral administration. After a single oral administration, the dose dependence of AUC0-t was exponential. The substance is characterized by heterogeneous distribution in the body with preferential accumulation mainly in well-vascularized tissues.
Brkich G.E. et al. Pharmacokinetic properties of an innovative nootropic agent based on a derivative of 3,7-diazabicyclo[3.3.1]nonane // Biomeditsinskaya khimiya. - 2020. - V. 66. -N 1. - P. 71-76.
Brkich G.E. et al., "Pharmacokinetic properties of an innovative nootropic agent based on a derivative of 3,7-diazabicyclo[3.3.1]nonane." Biomeditsinskaya khimiya 66.1 (2020): 71-76.
Brkich, G. E., Pyatigorskaya, N. V., Beregovykh, V. V., Nedorubov, A. A., Filippova, O. V., Zyryanov, O. A. (2020). Pharmacokinetic properties of an innovative nootropic agent based on a derivative of 3,7-diazabicyclo[3.3.1]nonane. Biomeditsinskaya khimiya, 66(1), 71-76.
Guidelines for the Early Management of Patients With Acute Ischemic Stroke: A Guideline for Healthcare Professionals From the American Heart Association (2018) American Stroke Association. Stroke. 49.3 DOI: 10.1161/STR.0000000000000158. CrossRef Scholar google search
Hui C., Tadi P., Patti L. (2019) Ischemic Stroke Last Update www.ncbi.nlm.nih.gov/books/NBK499997/. Scholar google search
Zefirov N.S., Palyulin V.A., Lavrov M.I., Zapolsky M.E. (2013) patent RF No. 2480470. Appl. 2011113043 from 06.04.2011; publ. 27.04.2013 in BI No. 12. Scholar google search
Lavrov M.I. (2011) Novel AMPA receptor modulators: design and assessment. Diss. kand. nauk, Lomonosov Moscow State University, Moscow]. Scholar google search
State Pharmacopoeia of the Russian Federation XIV edition of OFS.1.1.0012.15 “Validation of analytical methods”. Scholar google search
Decision of the Board of the Eurasian Economic Commission of July 17, 2018 N 113 “On approval of the Guidelines for the validation of analytical methodsfor testing drugs”. Режим доступа: https://www.alta.ru/tamdoc/18kr0113/ Дата обращения: 28.11.2019. Scholar google search
Guidelines for preclinical studies of drugs. (2012) Part One (Mironov A.N., ed. ). M. Grif and K, 2012. 944. Scholar google search