A route to the γ‐secretase inhibitor [2,3,4‐<sup>3</sup>H]BMS299897 via an α‐phenylselenide derivative

The g-secretase inhibitor dibenzazepine (DBZ) and the g-secretase modulators 1 and AZ8349 were prepared as tritium-labeled compounds with high specific activity and radiochemical purity. [ 3 H]DBZ was labeled via an iodinated precursor, [ 3 H]1 was labeled by [ 3 H]methylation of an O-desmethyl precursor, and [2-3 H]AZ8349 was labeled via a tribromoacetyl precursor by catalytic hydrogenation. [ 3 H]DBZ, [ 3 H]1, and [2-3 H]AZ8349 are promising in vitro imaging radioligands and have the potential to provide key information with regard to g-secretase expression, function, stoichiometry, and pharmacology.

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Tritium labeling of a γ‐secretase inhibitor and two modulators as in vitro imaging agents

Malmquist

Bernlind

Sandell

et al. 2012

Labelled Comp Radiopharmac

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Tritium: a coming of age for drug discovery and development ADME studies

Lockley

McEwen

Cooke

2012

Labelled Comp Radiopharmac

115

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Owing to recent developments in tritium chemistry and analysis, high‐quality tritium‐labelled drugs can now be prepared simply, cheaply and in timescales commensurate with those needed for rapid drug discovery in adsorption, distribution, metabolism and excretion (ADME) projects. Such 3H‐labelled drugs are enabling high‐quality decision‐making at key points in the drug discovery process, thus ensuring more effective research projects, a key issue in commercial success. In addition, tritium‐labelled compounds continue to play a significant role in ADME studies later in the pharmaceutical development process. This is especially so for highly potent and hence low‐dose agents, for drugs with complex structures and for those compounds that undergo molecular fragmentation as a result of metabolism.

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A route to the γ‐secretase inhibitor [2,3,4‐³H]BMS299897 via an α‐phenylselenide derivative

Cited by 2 publications

References 1 publication

Tritium labeling of a γ‐secretase inhibitor and two modulators as in vitro imaging agents

Tritium labeling of a γ‐secretase inhibitor and two modulators as in vitro imaging agents

Tritium: a coming of age for drug discovery and development ADME studies

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A route to the γ‐secretase inhibitor [2,3,4‐3H]BMS299897 via an α‐phenylselenide derivative

Cited by 2 publications

References 1 publication

Tritium labeling of a γ‐secretase inhibitor and two modulators as in vitro imaging agents

Tritium labeling of a γ‐secretase inhibitor and two modulators as in vitro imaging agents

Tritium: a coming of age for drug discovery and development ADME studies

Contact Info

Product

Resources

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A route to the γ‐secretase inhibitor [2,3,4‐³H]BMS299897 via an α‐phenylselenide derivative