Send to

Choose Destination
J Pharmacol Exp Ther. 1993 May;265(2):896-902.

Agonist and antagonist profiles of [D-Ala2,Glu4]deltorphin and its [Cys4]- and [Ser4]-substituted derivatives: further evidence of opioid delta receptor multiplicity.

Author information

Department of Pharmacology, University of Arizona, Tucson.


Pharmacological evidence has suggested the presence of two supraspinal opioid delta receptor subtypes in the mouse, termed delta-1 and delta-2. [D-Pen2,D-Pen5]enkephalin (DPDPE) is thought to be primarily an agonist at the opioid delta-1 subtype, whereas H2N-Tyr-D-Ala-Phe-Glu-Val-Val-Gly-NH2 ([D-Ala2,Glu4]deltorphin) is a selective agonist at the delta-2 subtype. Based on previous reports suggesting that a receptor sulfhydryl group may be critical for ligand binding to the opioid delta receptor, the present investigation has attempted to discover whether this concept extends to the opioid delta-2 receptor. For this purpose, a cysteine-substituted deltorphin was synthesized and the potential agonist and antagonist properties of this compound, H2N-Tyr-D-Ala-Phe-Cys-Val-Val-Gly-NH2 ([D-Ala2,Cys4]deltorphin), were evaluated in an antinociceptive assay after i.c.v. administration to mice and stability in mouse brain was determined. As a control a serine-substituted deltorphin was also prepared and the potential agonist and antagonist properties of this compound, H2N-Tyr-D-Ala-Phe-Ser-Val-Val-Gly-NH2 ([D-Ala2,Ser4]deltorphin), as well as those of the parent deltorphin, [D-Ala2,Glu4]deltorphin, were evaluated. Acutely, [D-Ala2,Cys4]deltorphin, [D-Ala2,Ser4]deltorphin and [D-Ala2,Glu4]deltorphin each produced dose-related antinociceptive effects.(ABSTRACT TRUNCATED AT 250 WORDS).

[Indexed for MEDLINE]

Supplemental Content

Full text links

Icon for HighWire
Loading ...
Support Center