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Bioorg Med Chem Lett. 2000 Jan 17;10(2):167-70.

Novel Dmt-Tic dipeptide analogues as selective delta-opioid receptor antagonists.

Author information

1
Department of Chemistry, AstraZeneca R&D Montréal, Saint-Laurent, Québec, Canada. daniel.page@astrazeneca.com

Abstract

A series of Dmt-Tic analogues with substitution on the Tic aromatic ring has been synthesized and evaluated for opioid receptor affinity and activation. Incorporation of large hydrophobic groups at position 7 of Tic did not greatly alter the delta opioid receptor binding affinities of the dipeptides whereas substitution at position 6 substantially diminished their affinity. These modified Dmt-Tic peptides showed binding affinities as low as 2.5 nM with up to 500-fold selectivity for the delta versus mu opioid receptor and proved to be delta receptor antagonists.

PMID:
10673103
DOI:
10.1016/s0960-894x(99)00652-6
[Indexed for MEDLINE]

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