Section 7
Chapter 6,188

Probes for narcotic receptor mediated phenomena 8. tritiation of irreversible mu or delta specific opioid receptor affinity ligands to high specific activity

Burke, T.R.J. ; Rice, K.C.; Jacobson, A.E.; Simonds, W.F.; Klee, W.A.

Journal of Labelled Compounds and Radiopharmaceuticals 21(8): 693-702


ISSN/ISBN: 0362-4803
DOI: 10.1002/jlcr.2580210802
Accession: 006187068

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Tritiation of the delta-specific opioid alkylating ligand FIT [fentanyl isothiocyanate], and the mu-specific opioid alkylating ligand BIT [benzimidazole isothiocyanate], to high specific activity is described. Both compounds were derived from dibrominated amino intermediates which were tritiated with H3 gas over Pd/C before conversion of the amine functions to isothiocyanates.

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