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Synthesis and biological activity of 7 8 di hydro batrachotoxinin derivatives interacting with fast sodium channels


, : Synthesis and biological activity of 7 8 di hydro batrachotoxinin derivatives interacting with fast sodium channels. Bioorganicheskaya Khimiya 9(7): 990-993

7,8-Dihydrobatrachotoxinin (A) (I) was synthesized from 11.alpha.-hydroxyprogesterone (III) by a 37-stage procedure. Trimethylpyrrolcarboxylate, benzoate and 2-azidobenzoate derivatives of I were obtained by mixed anhydride technique, the latter two derivatives being prepared also with tritium atoms in aromatic rings (specific radioactivity .apprx. 28 Cu/mmol). Upon interaction with rat brain synaptosomes the apparent Kd of 7,8-dihydrobatrachotoxinin A 20.alpha.-[4-3H]benzoate (IB) was .apprx. 2.5 .cntdot. 10-6 M. IB specific binding was inhibited by aconitine with K0.5 = 1.3 .cntdot. 10-4 M. Anemonia sulcata toxin II (ATX II) enhanced IB affinity for the receptor up to 7 .cntdot. 10-7 M, the maximum binding capacity being 2.5 pmol/mg of protein. Benzocaine and tetracaine competitively displaced specifically bound toxin with K0.5 = 3.1 .cntdot. 10-4 M and 5.7 .cntdot. 10-7 M, respectively, in the presence of 10-5 M ATX II. 2-Azido[5-3H]benzoate derivative was shown to be an effective probe for covalent labeling of the alkaloid toxin receptor of the Na channel.

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