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Opioid peptide receptor studies. 12. Buprenorphine is a potent and selective μ/κ antagonist in the [35S]‐GTP‐γ‐S functional binding assay
Data indicated that, in this assay system, buprenorphine is a potent μ and γ receptor antagonist, and the clinical implications remain to be elucidated. Expand
Opioid peptide receptor studies. 3. Interaction of opioid peptides and other drugs with four subtypes of the κ 2 receptor in guinea pig brain
The results indicated that [125I]IOXY, like [3H]bremazocine, selectively labels kappa 2 binding sites in rat brain membranes pretreated with BIT and FIT. Expand
Preliminary ligand binding data for subtypes of the delta opioid receptor in rat brain membranes.
Data support pharmacological studies demonstrating delta receptor subtypes which mediate antinociception, and DPDPE and [D-Ala2]deltorphin-I had high affinity for the high capacity binding site, and low affinity for a low capacitybinding site. Expand
Selective labeling of κ 2 opioid receptors in rat brain by [125I]IOXY: Interaction of opioid peptides and other drugs with multiple κ 2a binding sites
Recent studies from our laboratory resolved two subtypes of the kappa 2 binding site, termed kappa 2a and kappa 2b, using guinea pig, rat, and human brain membranes depleted of mu and delta receptors… Expand
Stereochemical requirements for pseudoirreversible inhibition of opioid mu receptor binding by the 3‐methylfentanyl congeners, RTI‐46144 and its enantiomers: Evidence for different binding domains
The present study determined the stereochemical requirements for pseudoirreversible inhibition of μ receptor binding using the methylfentanyl congeners, (±)‐cis‐N‐[1‐(2hydroxy‐2‐phenylethyl)‐3‐methyl‐4‐piperidyl]‐n‐phenylpropanamide HCI and its four resolved enantiomers, and proposed a pseudoallosteric model. Expand
Opioid peptide receptor studies. 4. Antisense oligodeoxynucleotide to the delta opioid receptor delineates opioid receptor subtypes
It is demonstrated that delta antisense DNA selectively affects the delta ncx-2 site sparing the other putative delta receptor subtypes and kappa 2 receptor sub types, suggesting a powerful approach to distinguishing between postulated receptor subtype subtypes. Expand
Resolution of two [35S]GTP-γ-S binding sites and their response to chronic morphine treatment: A binding surface analysis
The results suggest that opioid receptors in chronic morphine membranes are not normally coupled to G-proteins, corroborate earlier studies that reported changes in G-protein function in morphine tolerant animals. Expand
Libraries of opiate and anti-opiate peptidomimetics containing 2,3-methanoleucine.
- K. Burgess, W. Li, +4 authors A. Shitangkoon
- Chemistry, Medicine
- Bioorganic & medicinal chemistry
- 1 September 1997
Differences between the outcome of the screens were interpreted in terms of the position of the cyclo-Leu residue in the two sequences, which indicated any change at the Leu5 had little effect on the binding when compared with modifications to the YGGF-sequence. Expand
[3H]SNC121: A novel high affinity ligand for rat brain delta receptors: Preliminary studies
Abstract Calderon et al. (1) recently prepared the enantiomers and their methoxy precursors of the non-peptide delta agonist (±)-BW373U86 and its benzlic epimer (2). In one of these enantiomers,… Expand
Selective labeling of kappa 2 opioid receptors in rat brain by [125I]IOXY: interaction of opioid peptides and other drugs with multiple kappa 2a binding sites.
Results indicated that [125I]IOXY, like [3H]bremazocine, selectively labels kappa 2 binding sites in rat brain membranes pretreated with BIT and FIT, and provide further evidence for heterogeneity of the kappa opioid receptor. Expand