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

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.
AuthorsD Pagé, A McClory, T Mischki, R Schmidt, J Butterworth, S St-Onge, M Labarre, K Payza, W Brown
JournalBioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 10 Issue 2 Pg. 167-70 (Jan 17 2000) ISSN: 0960-894X [Print] ENGLAND
PMID10673103 (Publication Type: Journal Article)
Chemical References
  • Benzamides
  • Dipeptides
  • Isoquinolines
  • Piperazines
  • Receptors, Opioid, delta
  • Tetrahydroisoquinolines
  • 2',6'-dimethyltyrosine
  • 4-(alpha-(4-allyl-2,5-dimethyl-1-piperazinyl)-3-methoxybenzyl)-N,N-diethylbenzamide
  • 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid
  • Guanosine 5'-O-(3-Thiotriphosphate)
  • Tyrosine
  • Benzamides (metabolism)
  • Binding, Competitive
  • Dipeptides (chemical synthesis, pharmacology)
  • Guanosine 5'-O-(3-Thiotriphosphate) (metabolism)
  • Humans
  • Isoquinolines (chemistry)
  • Piperazines (metabolism)
  • Receptors, Opioid, delta (agonists, antagonists & inhibitors)
  • Tetrahydroisoquinolines
  • Tyrosine (analogs & derivatives, chemistry)

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