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

dynorphin amide (1-13), Ala(2)-(5-F-Phe)(4)- Property

Sequence

Tyr-{d-Ala}-Gly-{Phe(F5)}-Leu-Arg-Arg-Ile-Arg-Pro-Lys-Leu-Lys-NH2

Hazard and Precautionary Statements (GHS)

dynorphin amide (1-13), Ala(2)-(5-F-Phe)(4)- Chemical Properties,Usage,Production

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

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