Pharmacokinetic properties of an innovative nootropic agent based on a derivative of 3,7-diazabicyclo[3.3.1]nonane

   
Brkich G.E.1, Pyatigorskaya N.V.1, Beregovykh V.V.1, Nedorubov A.A.1, Filippova O.V.1, Zyryanov O.A.1

1. Sechenov First Moscow State Medical University, Moscow, Russia
Section: Experimental Study
DOI: 10.18097/PBMC20206601071      PubMed Id: 32116228
Year: 2020  Volume: 66  Issue: 1  Pages: 71-76
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.
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Keywords: derivative of 3,7-diazabicyclo[3.3.1]nonane, pharmacokinetics, nootropic effect, AMPA receptors, tissue accessibility, rats
Citation:

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.
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