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

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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