• Publications
  • Influence
kappa-Opioid receptor binding populations in rhesus monkey brain: relationship to an assay of thermal antinociception.
The binding characteristics of the kappa opioid ligands [3H]U69,593 and [3H]bremazocine, the mu opioid ligand [3H][D-ala2,N-Me-Phe4,glycol5]enkephalin and the delta opioid ligandExpand
  • 55
  • 2
Combined use of stereospecific deuteration, NMR, distance geometry, and energy minimization for the conformational analysis of the highly .delta. opioid receptor selective peptide
Comparison of 'H and "C NMR parameters for the cyclic, conformationally restricted, 6 opioid receptor selective enkephalin analogue Tyr-D-Pen-Gly-Phe-WPen ((~-Pen~,~-Pen~)enkephalin, DPDPE) inExpand
  • 54
  • 1
Activation of κ-Opioid Receptors Inhibits Pruritus Evoked by Subcutaneous or Intrathecal Administration of Morphine in Monkeys
Pruritus (itch sensation) is the most common side effect associated with spinal administration of morphine given to humans for analgesia. A variety of agents have been proposed as antipruritics withExpand
  • 93
  • 1
  • PDF
Development and in vitro characterization of a novel bifunctional μ-agonist/δ-antagonist opioid tetrapeptide.
The development of tolerance to and dependence on opioid analgesics greatly reduces their long-term usefulness. Previous studies have demonstrated that co-administration of a μ-opioid receptor (MOR)Expand
  • 30
  • 1
Development of a model for the delta opioid receptor pharmacophore. 1. Conformationally restricted Tyr1 replacements in the cyclic delta receptor selective tetrapeptide Tyr-c[D-Cys-Phe-D-Pen]OH
A series of analogues of the conformationally restricted delta opioid receptor selective tetrapeptide Tyr-c[D-Cys-Phe-D-Pen]OH (JOM 13) was prepared in which the conformationally labile Tyr residueExpand
  • 60
Development of a Bioavailable μ Opioid Receptor (MOPr) Agonist, δ Opioid Receptor (DOPr) Antagonist Peptide That Evokes Antinociception without Development of Acute Tolerance
We have previously described a cyclic tetrapeptide, 1, that displays μ opioid receptor (MOPr) agonist and δ opioid receptor (DOPr) antagonist activity, a profile associated with a reduced incidenceExpand
  • 31
Behavioral and neurobiological effects of the enkephalinase inhibitor RB101 relative to its antidepressant effects.
Nonpeptidic delta-opioid receptor agonists produce antidepressant-like effects in rodents, and compounds that inhibit the breakdown of endogenous opioid peptides have antidepressant-like effects inExpand
  • 44
Opioid peptidomimetics: leads for the design of bioavailable mixed efficacy μ opioid receptor (MOR) agonist/δ opioid receptor (DOR) antagonist ligands.
We have previously described opioid peptidomimetic, 1, employing a tetrahydroquinoline scaffold and modeled on a series of cyclic tetrapeptide opioid agonists. We have recently describedExpand
  • 31
A high affinity, mu-opioid receptor-selective enkephalin analogue lacking an N-terminal tyrosine.
We report a high affinity, mu opioid receptor selective enkephalin analogue in which the N-terminal tyrosine residue thought to be required for such high affinity is replaced by phenylalanine. TheExpand
  • 20
Single residue modifications of the delta opioid receptor selective peptide, [D-Pen2,D-Pen5]-enkephalin (DPDPE). Correlation of pharmacological effects with structural and conformational features.
Six analogs of the highly delta opioid receptor selective, conformationally restricted, cyclic peptide [D-Pen2,D-Pen5]enkephalin, Tyr-D-Pen-Gly-Phe-D-PenOH (DPDPE), were synthesized and evaluated forExpand
  • 11