Orexin - Selective Ligands

Selective Ligands

Several drugs acting on the orexin system are under development, either orexin agonists for the treatment of conditions such as narcolepsy, or orexin antagonists for insomnia. No non-peptide agonists are yet available, although synthetic Orexin-A polypeptide has been made available as a nasal spray and tested on monkeys. Several non-peptide antagonists are in development however; SB-649,868 is under development by GlaxoSmithKline for sleep disorders and is a non-selective orexin receptor antagonist. Another OX1 and OX2 receptor antagonist (ACT-078573, almorexant) is a similar compound under development for primary insomnia by Actelion. A third entry is Merck's MK-4305.

Most ligands acting on the orexin system so far are polypeptides modified from the endogenous agonists Orexin-A and Orexin-B, however there are some subtype-selective non-peptide antagonists available for research purposes.

  • SB-334,867 - selective OX1 antagonist
  • SB-408,124 - selective OX1 antagonist
  • TCS-OX2-29 - selective OX2 antagonist
  • EMPA(drug) (N-Ethyl-2--N-pyridin-3-ylmethyl-acetamide) - selective OX2 antagonist

Read more about this topic:  Orexin

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