Brain transfer of a new neuromodulating ACTH analog, ebiratide, in rats.
The transfer of ebiratide into the brain was examined in rats. Its brain levels after intravenous administration (2-20 mg/kg), determined by radioimmunoassay, peaked at 5 min and declined almost in parallel with the plasma levels. Brain/plasma ratios (B/P) were constantly about 0.05 ml/g at all doses. Brain distribution study at 5 min after 125I-ebiratide at an effective dose (0.4 microgram/kg) revealed that unchanged ebiratide had larger B/P than the metabolites and region selectivity. The combined use with unlabeled ebiratide resulted in marked decreases in B/P, particularly in the hippocampus, suggesting a specific uptake of this peptide.
Pharma Research Laboratories, Hoechst Japan Limited, Saitama-ken.
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Shimura
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Tabata
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Hayashi
D000324:Adrenocorticotropic Hormone / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000097:blood / Q000493:pharmacokinetics; D000818:Animals; D001693:Biological Transport, Active; D001812:Blood-Brain Barrier; D001921:Brain / Q000378:metabolism*; D006624:Hippocampus / Q000378:metabolism; D007275:Injections, Intravenous; D008297:Male; D018377:Neurotransmitter Agents / Q000008:administration & dosage / Q000493:pharmacokinetics; D010446:Peptide Fragments / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D051381:Rats; D011919:Rats, Inbred Strains; D014018:Tissue Distribution
D018377:Neurotransmitter Agents; D010446:Peptide Fragments; D000324:Adrenocorticotropic Hormone; C057139:ebiratide