In Good Company

Bidlack, Bede Benjamin

doi:10.1163/9789004288522

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2019

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Cited by 17 publications

(1 citation statement)

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“…Since MOR agonists cause euphoria, it has been suggested that partial MOR agonism may mitigate dysphoria associated with KOR agonism, increasing the therapeutic potential of a KOR agonist. 46,[50][51][52] This work represents progress towards the development of multifunctional KOR/MOR ligands which can be investigated for this purpose.…”

Section: Resultsmentioning

confidence: 99%

Novel Dimethyltyrosine–Tetrahydroisoquinoline Peptidomimetics with Aromatic Tetrahydroisoquinoline Substitutions Show in Vitro Kappa and Mu Opioid Receptor Agonism

Montgomery

Anand

et al. 2019

ACS Chem. Neurosci.

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The dimethyltyrosine-tetrahydroisoquinoline (Dmt-Tiq) scaffold was originally developed in the production of selective delta opioid receptor (DOR) antagonists. Installation of a 7-benzyl pendant on the tetrahydroisoquinoline core of this classic opioid scaffold introduced kappa opioid receptor (KOR) agonism. Further modification of this pendant resulted in retention of KOR agonism and the addition of mu opioid receptor (MOR) partial agonism, a bifunctional profile with potential to be used in the treatment of cocaine addiction.

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Section: Resultsmentioning

confidence: 99%