Preparation of carbon-11 labelled prazosin, a potent and selective alpha sub(1)-adrenoreceptor antagonist

Preparation of carbon-11 labelled prazosin, a potent and selective alpha sub(1)-adrenoreceptor antagonist

The alpha sub(1)-adrenoreceptor antagonist, Prazosin: 2-(4-(2-furoyl) piperazin-1-yl)-4-amino-6,7-dimethoxyquinazoline, has been labelled with carbon-11 for in vivo studies of alpha sub(1)-adrenoreceptors using positron emission tomography. The preparation of (2- super(11)C)furoyl chloride, from cyc...

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Veröffentlicht in:Journal of labelled compounds & radiopharmaceuticals 1988-01, Vol.25 (2), p.177-184
Hauptverfasser: Ehrin, E, Luthra, S K, Crouzel, C, Pike, V W
Format: Artikel
Sprache:eng
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Zusammenfassung:The alpha sub(1)-adrenoreceptor antagonist, Prazosin: 2-(4-(2-furoyl) piperazin-1-yl)-4-amino-6,7-dimethoxyquinazoline, has been labelled with carbon-11 for in vivo studies of alpha sub(1)-adrenoreceptors using positron emission tomography. The preparation of (2- super(11)C)furoyl chloride, from cyclotron-produced ( super(11)C)carbon dioxide, and its reaction with the secondary amine, 2-(piperazin-1-yl)-4-amino-6,7-dimethoxyquinazoline, provides a fast (35 min) route to carbon-11 labelled prazosin.
ISSN:0362-4803