[3h]-saxitoxin dihydrochloride highly labeled with tritium

FIELD: organic chemistry, labeled compounds.

SUBSTANCE: invention relates to a new highly labeled compound that represent an analog of the known physiologically active compound that is the strongest toxin and inhibitor of some viable important processes, for example, sodium ions transporting. [3H]-Saxitoxin dihydrochloride highly labeled with tritium corresponds to the formula: .

EFFECT: valuable properties of compound.

1 ex

 

The invention relates to the field of organic chemistry and can find application in analytical chemistry, Bioorganic chemistry, biochemistry and applied medicine.

It is known that substitution of atoms of compounds for their labeled counterparts does not change any properties of the original compound (Evans E.A. Tritium and its compounds London Butterworths, 1974, p.48).

Known dihydrochloride of saxitoxin formula:

This connection, which received the name of "STX", is a powerful toxin and an inhibitor of a number of vital processes, such as transport of sodium (G.S.Wiberg, N.R.Stephenson, Toxicol. Appl. Pharmacol. 1960. Vol.2. 607. The Merck Index, 1999, N 8533).

However, tritium-labeled analogue not described.

The technical result achieved by the present invention, is expanding the range labeled analogs of the physiologically active compounds.

Achieved the specified technical result obtaining vysokobarnogo tritium dihydrochloride of saxitoxin formula:

The following is an example implementation of the invention.

Example 1.

A solution of 0.5 mg of the dihydrochloride of saxitoxin was applied to the dispersed catalyst 5% Pd/BaSO4and liofilizirovanny. The catalyst coated with a dihydrochloride of saxitoxin, transferred to the reaction vial and kept for 7.5 min in atmosphereanalysis tritium at a pressure of 333 hPa. Excess gaseous tritium was removed by vacuum. The dihydrochloride of saxitoxin from the catalyst was extracted with methanol (5 x 2 ml) and was separated by filtration through a tube LiChroSorb C18, 30-40 um. Labile tritium was removed several times, dissolving the resulting product in methanol (5×2 ml) and pariva last. Preparative purification dihydrochloride [3H]saxitoxin was performed by HPLC on a column of Bond SB-AQ C18, 4.6*150 mm, eluent - 1% isopropanol in 50 mm ammonification buffer pH 2.8 with the addition of 2 mm pentanesulfonate sodium. Retention time dihydrochloride [3H]saxitoxin - 3.19 minutes

Re-purification was performed in the system of 15 mm NH4OAc pH5+1% iPrOH+2 mm hexanesulfonic.

Output dihydrochloride [3H]saxitoxin - 55-60%, molar radioactivity of about 20 to 25 CI/mmol, radiochemical purity 98-99%.

Viscometry tritium dihydrochloride [3H]saxitoxin formula



 

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20 cl, 5 tbl, 149 ex

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