Properties of TAN-67, a nonpeptide δ-opioid receptor agonist, at cloned human δ-and μ-opioid receptors

Knapp, Richard J.; Landsman, Robert S.; Waite, Sue; Malatyńska, Ewa; Varga, Éva; Haq, Wajujahal; Hruby, Victor J.; Roeske, William R.; Nagase, Hiroshi; Yamamura, Henry I.

doi:10.1016/0922-4106(95)90134-5

Cited by 33 publications

(9 citation statements)

References 14 publications

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“…This hypothesis was tested for three conformationally constrained nonpeptide δ‐opioid ligands OMI, SIOM, and TAN‐67, which all show high affinities for the δ‐receptor, but differ in their ability to simulate a biological response. TAN‐67 is a full agonist with receptor binding properties and a profile of biological activities40 very close to those of [ p Cl‐Phe 4 ]DPDPE, one of the most potent and selective cyclic δ‐opioid peptides 41. Therefore, it was reasonable to assume that TAN‐67 and DPDPE have a similar 3D pharmacophore.…”

Section: Discussionmentioning

confidence: 95%

A three-dimensional model of the δ-opioid pharmacophore: Comparative molecular modeling of peptide and nonpeptide ligands

Shenderovich¹,

Liao²,

Qian³

et al. 2000

Biopolymers

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Section: Discussionmentioning

confidence: 95%

A three-dimensional model of the δ-opioid pharmacophore: Comparative molecular modeling of peptide and nonpeptide ligands

Shenderovich¹,

Liao²,

Qian³

et al. 2000

Biopolymers

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“…TAN-67 is a morphinan derivative with high selectivity for the delta opioid receptor (Knapp et al, 1995). Although the racemic (+/−)-TAN-67 showed no analgesic activity, its enantiomer (−)-TAN-67 is highly effective (Nagase et al, 2001).…”

Section: Introductionmentioning

confidence: 99%

The delta opioid receptor tool box

2016

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In recent years, the delta opioid receptor has attracted Increasing Interest as a target for the treatment of chronic pain and emotional disorders. Due to their therapeutic potential, numerous tools have been developed to study the delta opioid receptor from both a molecular and a functional perspective. This review summarizes the most commonly available tools, with an emphasis on their use and limitations. Here, we describe (1) the cell-based assays used to study the delta opioid receptor. (2) The features of several delta opioid receptor ligands, including peptide and non-peptide drugs. (3) The existing approaches to detect delta opioid receptors in fixed tissue, and debates that surround these techniques. (4) Behavioral assays used to study the in vivo effects of delta opioid receptor agonists; including locomotor stimulation and convulsions that are induced by some ligands, but not others. (5) The characterization of genetically modified mice used specifically to study the delta opioid receptor. Overall, this review aims to provide a guideline for the use of these tools with the final goal of increasing our understanding of delta opioid receptor physiology.

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“…As mentioned previously, the inner loop of the template is δ-specific (see Figures 10 and 15). So δ-ligands that are bond-to-bond aligned with the loop would be agonists (such as TAN-67, 22 Figure 15B) or would be the antagonists if mismatched (such as the N -CH 3 analog of NTI, 23 Figure 15C).…”

Section: Resultsmentioning

confidence: 99%

Toward a Universal μ-Agonist Template for Template-Based Alignment Modeling of Opioid Ligands

Wu¹,

Hruby

2019

ACS Omega

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Opioid ligands are a large group of G-protein-coupled receptor ligands possessing high structural diversity, along with complicated structure–activity relationships (SARs). To better understand their structural correlations as well as the related SARs, we developed the innovative template-based alignment modeling in our recent studies on a variety of opioid ligands. As previously reported, this approach showed promise but also with limitations, which was mainly attributed to the small size of morphine as a template. With this study, we set out to construct an artificial μ-agonist template to overcome this limitation. The newly constructed template contained a largely extended scaffold, along with a few special μ-features relevant to the μ-selectivity of opioid ligands. As demonstrated in this paper, the new template showed significantly improved efficacy in facilitating the alignment modeling of a wide variety of opioid ligands. This report comprises of two main parts. Part 1 discusses the general construction process and the structural features as well as a few typical examples of the template applications and Part 2 focuses on the template refinement and validation.

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Properties of TAN-67, a nonpeptide δ-opioid receptor agonist, at cloned human δ-and μ-opioid receptors

Cited by 33 publications

References 14 publications

A three-dimensional model of the δ-opioid pharmacophore: Comparative molecular modeling of peptide and nonpeptide ligands

A three-dimensional model of the δ-opioid pharmacophore: Comparative molecular modeling of peptide and nonpeptide ligands

The delta opioid receptor tool box

Toward a Universal μ-Agonist Template for Template-Based Alignment Modeling of Opioid Ligands

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