Add time:09/01/2019         Source:sciencedirect.com

Intracerebroventricular administration of the dynorphin analog, [D-Ala2,(F5)Phe4]-dynorphin1–13-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]-dynorphin1–13-NH2 to produce analgesia. Radioligand binding studies indicated the DAFPHEDYN retains the same degree of κ 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.

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