Neuroleptanalgesia in wild Asian elephants (Elephas maximus maximus)

Dangolla, Ashoka; Silva, Indira; Kuruwita, V.Y.

doi:10.1111/j.1467-2995.2004.00166.x

Cited by 6 publications

(2 citation statements)

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“…19 Other prominent orvinols are buprenorphine (BPN, Suboxone ® ), a partial agonist used to treat opioid addiction, 20 and etorphine (Immobilon ® ), a ‘super-potent’ agonist used to immobilize large animals, such as wild elephants. 21 In veterinary medicine, DPN (Revivon ® ) is employed to reverse the effects of Immobilon ® when animals need to be revived. 21 Thus, the antagonist character of DPN provides a good safety profile for clinical imaging studies.…”

Section: Introductionmentioning

confidence: 99%

“…21 In veterinary medicine, DPN (Revivon ® ) is employed to reverse the effects of Immobilon ® when animals need to be revived. 21 Thus, the antagonist character of DPN provides a good safety profile for clinical imaging studies. These three orvinols are universal opioid receptor ligands, in that they bind with high and nearly equal affinities to μ, δ and κ sites.…”

Section: Introductionmentioning

confidence: 99%

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Synthesis and opioid receptor binding of indium (III) and [111In]-labeled macrocyclic conjugates of diprenorphine: novel ligands designed for imaging studies of peripheral opioid receptors

et al. 2016

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Radiolabeled diprenorphine (DPN) and analogs are widely used ligands for non-invasive brain imaging of opioid receptors. To develop complementary radioligands optimized for studies of the peripheral opioid receptors, we prepared a pair of hydrophilic DPN derivatives, conjugated to the macrocyclic chelator DOTA (1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid), for complexation with trivalent metals. The non-radioactive indium (III) complexes, tethered to the C6-oxygen position of the DPN scaffold by 6- to 9-atom spacers, displayed high affinities for binding to μ, δ and κ opioid receptors in vitro. Use of the 9-atom linker conferred picomolar affinities equipotent to those of the parent ligand DPN. The [111In]-labeled complexes were prepared in good yield (>70%), with high radiochemical purity (~99%) and high specific radioactivity (>4000 mCi/μmol). Their log D7.4 values were −2.21 to −1.66. In comparison, DPN is lipophilic, with a log D7.4 of +2.25. Further study in vivo is warranted to assess the suitability of these [111In]-labeled DPN-DOTA conjugates for imaging trials.

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