Synthesis of Diazipine and [3H]Diazipine : Novel dihydropyridines as Photoaffinity Probes of Calcium Channels

Motohiko TAKI; Akihiko KUNIYASU; Hitoshi NAKAYAMA; Yuichi KANAOKA

doi:10.1248/cpb.39.1860

Synthesis of Diazipine and [³H]Diazipine : Novel dihydropyridines as Photoaffinity Probes of Calcium Channels

Motohiko TAKI, Akihiko KUNIYASU, Hitoshi NAKAYAMA, Yuichi KANAOKA

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Keywords: [³H]diazipine, 1, 4-dihydropridine, calcium channel, photoaffinity ligand

JOURNAL FREE ACCESS

1991 Volume 39 Issue 7 Pages 1860-1862

DOI https://doi.org/10.1248/cpb.39.1860

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Abstract

Diazipine and [³H]diazipine were synthesized as new 1, 4-dihydropyridine photoaffinity ligands containing a phenyldiazirine group. After simple high performance liquid chromatography separation, both compounds were purified in good overall yields. [³H]Diazipine (21.2Ci/mmol) was synthesized in two steps from commercially available [³H]ethanolamine. Diazipine competitively inhibited [³H]PN200-110 binding to the calcium channel of cardiac membranes with high affinity.

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