• Publications
  • Influence
Constitutive activity of the δ‐opioid receptor expressed in C6 glioma cells: identification of non‐peptide δ‐inverse agonists
G‐protein coupled receptors can exhibit constitutive activity resulting in the formation of active ternary complexes in the absence of an agonist. In this study we have investigated constitutiveExpand
  • 44
  • 7
Differential binding properties of oripavines at cloned μ- and δ-opioid receptors
This study examines the possibility that oripavine opioid receptor agonists bind equally to both high and low affinity states of the μ-opioid receptor. Studies were performed in C6 cells expressingExpand
  • 95
  • 4
BU74, a complex oripavine derivative with potent kappa opioid receptor agonism and delayed opioid antagonism.
In the search for opioid agonists with delayed antagonist actions as potential treatments for substance abuse, the bridged morphinan BU74Expand
  • 27
  • 2
The delta receptor
The Delta Receptor: History of Delta Opioid Receptors, Wen-Jen Chang Cloning of Delta Opioid Receptors, Arnaud Lacoste and Christopher J. Evans Cloning and Expression of the Human Delta OpioidExpand
  • 48
  • 2
Structural analysis of thermostabilizing mutations of cocaine esterase.
Cocaine is considered to be the most addictive of all substances of abuse and mediates its effects by inhibiting monoamine transporters, primarily the dopamine transporters. There are currently noExpand
  • 46
  • 2
Characterization of the complex morphinan derivative BU72 as a high efficacy, long-lasting mu-opioid receptor agonist.
The development of buprenorphine as a treatment for opiate abuse and dependence has drawn attention to opioid ligands that have agonist actions followed by long-lasting antagonist actions. In aExpand
  • 36
  • 1
[3H]dynorphin A binding and kappa selectivity of prodynorphin peptides in rat, guinea-pig and monkey brain.
We have previously demonstrated that [3H]dynorphin A selectively labels kappa opioid receptors in guinea-pig whole brain. In these current studies, using protection from inactivation byExpand
  • 37
  • 1
Pharmacological activities of optically pure enantiomers of the κ opioid agonist, U50,488, and its cis diastereomer: evidence for three κ receptor subtypes
De Costa et al. (FEBS Lett. 223, 335; 1987) recently described the synthesis of optically pure enantiomers of (±)-trans-3,4-dichloro-N-methyl-N-[2-(1-pyrrolidinyl)-cyclohexyl]benzeneacetamideExpand
  • 37
  • 1
The Steroid 17α-Acetoxy-6-dimethylaminomethyl-21-fluoro-3-ethoxy-pregna-3,5-dien-20-one (SC17599) Is a Selective μ-Opioid Agonist: Implications for the μ-Opioid Pharmacophore
The steroid SC17599 (17α-acetoxy-6-dimethylaminomethyl-21-fluoro-3-ethoxypregna-3,5-dien-20-one) has μ-opioid actions in vivo. The ability of SC17599 to interact with opioid receptors has beenExpand
  • 5
  • 1
  • PDF
Resolution in the receptor binding of putative μ and κ opiates
Conditions for the stereospecific binding of 3H-ethylketocyclazocine and 3H-etorphine were established in membranes from rat and pigeon brain. In displacing the specific binding of the radiolabeledExpand
  • 14