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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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Smyser, T.J.; Johnson, S.R.; Stallard, M.D.; McGrew, A.K.; Page, L.Kristen.; Crider, N.; Ballweber, L.R.; Swihart, R.K.; VerCauteren, K.C., 2016: Evaluation Of Anthelmintic Fishmeal Polymer Baits For The Control Of Baylisascaris Procyonis In Free-Ranging Raccoons (Procyon Lotor). Baylisascaris procyonis is a common gastrointestinal parasite of raccoons (Procyon lotor) and is a zoonotic helminth with the potential to cause severe or fatal infection. Raccoons thrive in human-dominated landscapes, and the fecal-oral transmiss...

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Zhu, L-Ling.; Zhou, Q., 2013: Intervention for improving the appropriateness of physician orders for oral medications in geriatric VIP patients during the journey to JCI accreditation. Therapeutics and Clinical Risk Management 9: 273-275

Park, I-Nae.; Ryu, J-Sook.; Shim, T.Sun., 2007: Evaluation of therapeutic response of tuberculoma using F-18 FDG positron emission tomography. Clinical Nuclear Medicine 33(1): 1-3

Kater, E., 1983: The law in Kentucky: pay up or close down. Dental Laboratory Review 58(9): 16-18

de Wijkerslooth, T.R.; de Haan, M.C.; Stoop, E.M.; Bossuyt, P.M.; Thomeer, M.; Essink-Bot, M-Louise.; van Leerdam, M.E.; Fockens, P.; Kuipers, E.J.; Stoker, J.; Dekker, E., 2012: Burden of colonoscopy compared to non-cathartic CT-colonography in a colorectal cancer screening programme: randomised controlled trial. CT-colonography has been suggested to be less burdensome for primary colorectal cancer (CRC) screening than colonoscopy. To compare the expected and perceived burden of both in a randomised trial. 8844 Dutch citizens aged 50-74 years were randomly...

Belknap Daniel F., 1991: Preservation potential of the Delaware Atlantic coast barrier; backbarrier system. Pages 1269-1283:

Unalacak, M.; Altin, R.; Kart, L.; Tor, M.; Ornek, T.; Altunel, H., 2004: Smoking prevalence, behaviour and nicotine addiction among coal workers in Zonguldak, Turkey. Smoking Prevalence, Behaviour and Nicotine Addiction among Coal Workers in Zonguldak, Turkey: Murat UNALACAK, et al. Department of Family Medicine, Zonguldak Karaelmas University, Faculty of Medicine, Turkey-To assess the smoking status of coal wo...

Li, L.X.; Nohara, R.; Okuda, K.; Hosokawa, R.; Hata, T.; Tanaka, M.; Matsumori, A.; Fujita, M.; Tamaki, N.; Konishi, J.; Sasayama, S., 1996: Comparative study of 201Tl-scintigraphic image and myocardial pathologic findings in patients with dilated cardiomyopathy. The objective of the present study was to characterize the production of 201Tl myocardial perfusion defects, the relation between the 201Tl multiple small defects and the myocardial damage indicated by myocardial fibrosis shown histopathologically...

Shapot V.S.; Potapova G.I., 1986: On methodological approaches to the studies on the metabolism of tumors and host tissues in vitro and in vivo. Eksperimental'naya Onkologiya 8(2): 3-9