Design, synthesis, and characterization of high-affinity, systemically-active galanin analogues with potent anticonvulsant activities.

@article{Bulaj2008DesignSA,
  title={Design, synthesis, and characterization of high-affinity, systemically-active galanin analogues with potent anticonvulsant activities.},
  author={Grzegorz Bulaj and Brad Reed Green and Hee-Kyoung Lee and Charles Ray Robertson and Karen White and Liuyin Zhang and Marianna Sochanska and Sean Patrick Flynn and Erika Adkins Scholl and Timothy H. Pruess and Misty D. Smith and Henry S White},
  journal={Journal of medicinal chemistry},
  year={2008},
  volume={51 24},
  pages={
          8038-47
        }
}
Galanin is an endogenous neuropeptide that modulates seizures in the brain. Because this neuropeptide does not penetrate the blood-brain barrier, we designed truncated galanin analogues in which nonessential amino acid residues were replaced by cationic and/or lipoamino acid residues. The analogues prevented seizures in the 6 Hz mouse model of epilepsy following intraperitoneal administration. The most active analogue, Gal-B2 (NAX 5055), contained the -Lys-Lys-Lys(palmitoyl)-Lys-NH(2) motif and… CONTINUE READING

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