.alpha.-glycosyl derivative of catecholamine or its salt, and it

Details .alpha.-glycosyl derivative of catecholamine or its salt, and it .alpha.-glycosyl derivative of catecholamine or its salt, and it

1995-06-07

1997-04-08

Kight, John

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Carbohydrate doai

514 53, 514 54, 536 179, 435 74, C07H 1520, A61K 3170, C12P 1944

Patent

active

056187947

ABSTRACT:
Disclosed is a novel .alpha.-glycosyl derivative of a catecholamine or its salt, said .alpha.-glycosyl derivative being prepared by allowing a saccharide-transferring enzyme together with or without glucoamylase to act on a solution containing an .alpha.-glycosyl saccharide and one of catecholamines in order to form an .alpha.-glycosyl derivative of said catecholamines, and recovering the resultant .alpha.-glycosyl derivative. The .alpha.-glycosyl derivative overcomes conventional drawbacks of catecholamines, and does not substantially exhibit or have a reducing activity and undesirable toxicity, but has a relatively-high stability and exerts the inherent physiological activities of catecholamines in vivo. Thus, the .alpha.-glycosyl derivative is advantageously used as a variety of pharmaceuticals in the form of an injection, tablet, etc.

REFERENCES:
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Seikagaku-Jikken Koza, "Metabolism of amino acids, and in vivo amines", The Japanese Biochemical Society, Part B, vol. 11, pp. 725-753 (1977).
"Denpun-Kagaku-Handbook (Handbook of Starch Science)", pp. 190 (1984), published by Asakura Shoten Publisher.
The Journal of Biological Chemistry; vol. 153, Baltimore (1944).
Ishizaki et al.; "Further studies on dopamine and N-acyldopamine during the pupal stage of papilio xuthus (lepidoptera: papiliondae)"; Comp. Biochem. Physiol., vol. 97B, No. 3, pp. 563-567, 1990.
Kebabian et al; "Dopamine-sensitive adenylate cyclase in caudate nuclus of rat brain, and its similarity to the `Dopamine Receptor`", Proc. Nat. Acad. Sci. USA, vol. 69, No. 8, pp. 2145-2149 (Aug. 1972).
Mueller, D.D. et al.; ".sup.1 H and .sup.13 C NMR of 3-0 and 4-0 conjugates of dopamine and other catecholamines", Bioconjugate Chem. 4:47-53 (1993).

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