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111846-43-6

111846-43-6 Structure

111846-43-6 Structure
IdentificationBack Directory
[Name]

dynorphin amide (1-13), Ala(2)-(5-F-Phe)(4)-
[CAS]

111846-43-6
[Synonyms]

Dafphedyn
dynorphin amide (1-13), Ala(2)-(5-F-Phe)(4)-
Dynorphin A (swine), 2-D-alanine-4-(2,3,4,5,6-pentafluoro-L-phenylalanine)-13-L-lysinamide-14-de-L-tryptophan-15-de-L-aspartic acid-16-de-L-asparagine-17-de-L-glutamine- (9CI)
[Molecular Formula]

C76H124F5N25O14
[MOL File]

111846-43-6.mol
[Molecular Weight]

1706.95
Chemical PropertiesBack Directory
[Sequence]

Tyr-{d-Ala}-Gly-{Phe(F5)}-Leu-Arg-Arg-Ile-Arg-Pro-Lys-Leu-Lys-NH2
Hazard InformationBack Directory
[Description]

Dafphedyn, [D-Ala2, (F5) Phe4]-dynorphin 1-13-NH2 (DAFPHEDYN) is a potent analog of dynorphin 1-13. Intracerebroventricular administration of the dynorphin analog, [D-Ala2,(F5)Phe4]-dynorphin 1-13-NH2 (DAFPHEDYN) in rats produced diuresis and profound analgesia. Both effects were antagonized by central administration of naltrexone or naloxone. Intravenous administration of 10, 25, and 50 mg/kg of DAFPHEDYN failed to induce diuresis. The increased potency of DAFPHEDYN was apparent from the failure of an equal dose of the parent compound (dynorphin 1-13) to produce diuresis and the failure of [D-Ala2]-dynorphin 1-13-NH2 to produce analgesia. Radioligand binding studies indicated the DAFPHEDYN retains the same degree of kappa selectivity as the parent compound (dynorphin 1-13) though a drop in affinity occurred. DAFPHEDYN may be of significant interest because it retains the essential pharmacology of the parent compound and exhibits marked in vivo potency.
[Uses]

Dafphedyn is an analogue of Dynorphin (1-13). Dafphedyn has diuretic and profound analgesia effects that can be antagonized by centrally administered Naltrexone (HY-76711) or Naloxone (HY-17417A)[1].
[in vivo]

Dafphedyn (5-40 μg, icv, once) induces profound analgesia in a dose-dependent manner in male Sprague-Dawley rats[1].

[References]

[1] Walker JM, et al. [D-Ala2, (F5) Phe4]-dynorphin 1-13-NH2 (DAFPHEDYN): a potent analog of dynorphin 1-13. Peptides. 1987 Sep-Oct;8(5):811-7. DOI:10.1016/0196-9781(87)90064-7
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