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Synthesis of a psilocin hapten and a protein-hapten conjugate

Christian Albers, Matthias Lehr, Justus Beike, Helga Köhler, Bernd Brinkmann

Journal of Pharmacy and Pharmacology September 1, 2002 DOI: 10.1211/002235702320402116 (opens in new tab)

Study at a glance

AI-extracted from the abstract
Characteristics Synthesis and characterization study Peer reviewed
Topics Psilocybin
Keywords Hapten Conjugate Indole test Moiety Mass spectrometry Bovine serum albumin Alkyl Stereochemistry Chromatography Derivative finance
Citations 7
Key points The 3-carboxypropyl psilocin derivative was stable and could be conjugated to BSA with an average incorporation ratio of 4–5 hapten molecules per protein molecule.

Abstract

Abstract Derivatives of psilocin with ω-functionalized alkyl spacers in position 1 of the indole ring were synthesized as haptens for use in a radioimmunoassay. Whereas the psilocin analogues with a 3-aminopropyl and a 4-aminobutyl moiety at the indole nitrogen decomposed during synthesis, the analogous 3-carboxypropyl psilocin derivative proved to be stable. This compound was coupled to bovine serum albumin (BSA) using the N-hydroxysuccinimide ester-mediated conjugation. The protein–hapten conjugate was characterized by matrix-assisted laser desorption ionization mass spectrometry. The mass spectrometry data indicated an average incorporation ratio of 4–5 molecules of psilocin hapten per molecule of BSA.