Shozo Kamiya

A monoclonal antibody to scopolamine and its use for competitive enzyme-linked immunosorbent assay.

A hybridoma clone producing a monoclonal antibody (SC78.H81) against scopolamine was established. The monoclonal antibody was an IgG1 (k) antibody with high affinity (1.6 x 10(9) M-1 for methylscopolamine). The monoclonal antibody was cross-reactive with methylscopolamine and butylscopolamine, and showed weak cross-reactivity with 6 beta- and 7 beta-hydroxyhyoscyamine. The cross-reaction with L-hyoscyamine, atropine, scopine and DL-tropic acid was very weak. A competitive enzyme-linked immunosorbent assay using SC78.H81 was established to quantify scopolamine. The sensitivity of the assay allowed detection of 20 pg assay-1 (0.2 ng ml-1) of scopolamine. The assay was applied to the estimation of scopolamine content in hairy root cultures of a Duboisia hybrid.

Synthesis of 6-azabenzo[a]pyrene

Abstract 6-Azabenzo[ a ]pyrene was synthesized from perinaphthenone and 1-indo-2-nitrobenzene.

Antitumor activity of 4-nitropyridazine 1-oxides and related compounds for AH-13.

Antitumor activity of 4-nitropyridazine 1-oxides and related compounds was tested with AH-13 system. Among these nitro compounds, 3, 6-dimethoxy-4-nitropyridazine 1-oxide (III) and 4-nitrocinnoline 1-oxide (XIII) were the most effective. 4-Nitropyridazine 1-oxide (I), 3, 6-dimethyl-4-nitropyridazine 1-oxide (II) and 3-alkoxy-4-nitro-6-chloropyridazine 1-oxides (VI, VII) were effective to some extent.

Antitumor Activity of 3-Nitroso-2-oxazolidones

2-Oxazolidones (Ia→f) were not effective against rat ascites hepatoma AH13 or mouse lymphoid leukemia, L1210. However, among 3-nitroso-2-oxazolidones (IIa→f), compounds IIa, IIb, IIc and IId were active against AH13, and compounds IIa, IIb and IIf were active against L1210. Cyclic N-nitrosocarbamates and N-nitrosoureas showed greater antitumor effects than the corresponding acyclic N-nitroso compounds. Since the reaction of compounds IIa→f with 4-(p-nitrobenzyl) pyridine gave a purple color, their antitumor mechanism presumably involves alkylation ; but there was no correlation between the antitumor activities and the color intensities.

Antitumor effect of pyridine N-oxides having 1-(2-chloroethyl)-1-nitrosoureidoalkyl and 1-methyl-1-nitrosoureidoalkyl groups.

Pyridine N-oxides having 1-(2-chloroethyl)-1-nitrosoureidoalkyl or 1-methyl-1-nitrosoureidoalkyl groups were evaluated for their antitumor activity against AH13 hepatoma and L1210 leukemia. Among them, 1-(2-chloroethyl)-1-nitroso-3-(2-pyridylmethyl)urea N-oxide (1), its tosylate (2), 1-(2-chloroethyl)-1-nitroso-3-(2-pyridylethyl)urea N-oxide (4), and 1-(2-chloroethyl)-1-nitroso-3-(3-pyridylmethyl)urea N-oxide (6) were highly active against both tumors in ip-ip system. These compounds were also active in ip-iv and ip-po systems of L1210. On the other hand, pyridine N-oxides having 1-methyl-1-nitrosoureidoalkyl group were all inactive against AH13 and weakly active against L1210. Effect on blood cells in Donryu rats bearing EDEN-5 erythroblastic leukemia cells was tested with these 1-(2-chloroethyl)-1-nitrosoureidoalkylureas. These compounds caused leucopenia and compound (4) was only slightly effective against EDEN-5.