Pharmacokinetics of repinotan in healthy and brain injured animals

@article{Schwarz2005PharmacokineticsOR,
  title={Pharmacokinetics of repinotan in healthy and brain injured animals},
  author={Thomas Schwarz and Bernhard Beckermann and Klaus Buehner and Frank Mauler and Joachim Schuhmacher and Dietrich Seidel and Wolfram Steinke and Corinna Weinz and Dieter Zimmerd},
  journal={Biopharmaceutics \& Drug Disposition},
  year={2005},
  volume={26}
}
Repinotan hydrochloride (repinotan) is a highly potent and selective 5‐HT1A full receptor agonist. The ability of repinotan to cross the blood–brain barrier (BBB) and penetrate into rat brain tissue was investigated, because rapid penetration into brain tissue is thought to be essential for neuroprotective efficacy. Intravenous (i.v.) repinotan was rapidly distributed into brain, and the distribution equilibrium between blood and brain was reached immediately after the start of infusion. Free… 
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TLDR
The dose- and time-dependent neuroprotective efficacy of repinotan indicates that the drug is a promising candidate for prevention of secondary brain damage in brain-injured patients suffering from acute ischemic stroke, however, the first, randomized, double blind, placebo-controlled clinical trial did not demonstrate the efficacy of the drug.
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TLDR
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TLDR
Findings highlight the differential role of these 5-HTRs in cognitive/emotional domains of behavior and indicate that tonic and phasic 5-HT release can exert different and potentially opposing effects on emotional memory, depending on the states of5-HT1ARs and 5- HT7Rs and their interaction.

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