Pharmacokinetics and brain entry of alaptide, a novel nootropic agent, in mice, rats and rabbits.
Pharmacokinetics of a novel nootropic agent, alaptide, have been examined in plasma and brain of mice, rats and rabbits following an intravenous dose (1 mg kg-1). First-order equilibration rate constants between plasma and brain (kBO) were calculated by a two-compartment model with a linked compartment (brain). Brain alaptide equilibrates rapidly with the central compartment in mice and rats due to the high kBO/beta ratio. In rabbits the equilibration is much slower (kBO/beta approximately 1). Partition coefficients between brain and plasma calculated from areas under the brain and plasma concentration-time curves, are 0.479, 0.549 and 0.864, in mice, rats and rabbits, respectively.
Research Institute for Pharmacy and Biochemistry, Prague, Czechoslovakia.
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D000818:Animals; D001921:Brain / Q000378:metabolism; D002682:Chinchilla; D002855:Chromatography, Thin Layer; D066298:In Vitro Techniques; D008297:Male; D051379:Mice; D008954:Models, Biological; D009479:Neuropeptides / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics* / Q000652:urine; D010456:Peptides, Cyclic / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics* / Q000652:urine; D011485:Protein Binding; D011619:Psychotropic Drugs / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics* / Q000652:urine; D011817:Rabbits; D051381:Rats; D011919:Rats, Inbred Strains; D012710:Serum Albumin, Bovine
D009479:Neuropeptides; D010456:Peptides, Cyclic; D011619:Psychotropic Drugs; D012710:Serum Albumin, Bovine; C049178:cyclo(alanine-(1-amino-1-cyclopentane)carbonyl)