Synthesis of diazipine and [3H]diazipine: novel dihydropyridines as photoaffinity probes of calcium channels. |
| |
| Authors: | M Taki A Kuniyasu H Nakayama Y Kanaoka |
| |
| Institution: | Faculty of Pharmaceutical Sciences, Hokkaido University, Sapporo, Japan. |
| |
| 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 (21.2 Ci/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. |
| |
| Keywords: | |
|
|
