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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.
J M Walker, and
D H Coy, and
E A Young, and
G Baldrighi, and
S F Siegel, and
W D Bowen, and
H Akil
January 1982,
Life sciences,
J M Walker, and
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E A Young, and
G Baldrighi, and
S F Siegel, and
W D Bowen, and
H Akil
September 2003,
Journal of medicinal chemistry,
J M Walker, and
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E A Young, and
G Baldrighi, and
S F Siegel, and
W D Bowen, and
H Akil
September 1980,
Life sciences,
J M Walker, and
D H Coy, and
E A Young, and
G Baldrighi, and
S F Siegel, and
W D Bowen, and
H Akil
January 1983,
Life sciences,
J M Walker, and
D H Coy, and
E A Young, and
G Baldrighi, and
S F Siegel, and
W D Bowen, and
H Akil
June 2002,
Naunyn-Schmiedeberg's archives of pharmacology,
J M Walker, and
D H Coy, and
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G Baldrighi, and
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H Akil
January 1985,
Peptides,
J M Walker, and
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G Baldrighi, and
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J M Walker, and
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E A Young, and
G Baldrighi, and
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H Akil
December 1984,
Neuropeptides,
J M Walker, and
D H Coy, and
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G Baldrighi, and
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H Akil
January 1988,
Psychopharmacology,
J M Walker, and
D H Coy, and
E A Young, and
G Baldrighi, and
S F Siegel, and
W D Bowen, and
H Akil
December 1984,
Neuropeptides,
