Zyklophin

Zyklophin
Clinical data
ATC code
  • None
Legal status
Legal status
  • In general: legal
Identifiers
PubChem CID
ChemSpider
Chemical and physical data
Formula C65H96N20O13
Molar mass 1365.584 g/mol
3D model (JSmol)

Zyklophin is a semisynthetic peptide derived from dynorphin A and a highly selective antagonist of the κ-opioid receptor (KOR).[1][2] It is systemically-active, displaying good metabolic stability and blood-brain-barrier penetration.[2] Similarly to other KOR antagonists, it has been shown to block stress-induced reinstatement of cocaine-seeking in animals.[2] The drug is currently experimental, and thus cannot be considered safe for consumption or usage.

See also

References

  1. ↑ Patkar KA, Yan X, Murray TF, Aldrich JV (July 2005). "[Nalpha-benzylTyr1,cyclo(D-Asp5,Dap8)]- dynorphin A-(1-11)NH2 cyclized in the "address" domain is a novel kappa-opioid receptor antagonist". J. Med. Chem. 48 (14): 4500–3. PMID 15999987. doi:10.1021/jm050105i.
  2. 1 2 3 Aldrich JV, Patkar KA, McLaughlin JP (October 2009). "Zyklophin, a systemically active selective kappa opioid receptor peptide antagonist with short duration of action". Proc. Natl. Acad. Sci. U.S.A. 106 (43): 18396–401. PMC 2775281 Freely accessible. PMID 19841255. doi:10.1073/pnas.0910180106.


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