[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.
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.
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
FIELD: organic chemistry, chemical technology, medicine, pharmacy.
SUBSTANCE: invention describes derivatives of 8-phenyl-6,9-dihydro[1,2,4]-triazolo[3,4-I]purine-5-one of the general formula:
wherein R1 means hydrogen atom, group -CH2-R6 wherein R6 means phenyl; R2 means (C1-C5)-alkyl or group -(CH2)n-R6 wherein n= 1 or 2; R6 means (C1-C4)-alkoxy-group or pyridyl group; R3 means (C1-C6)-alkyl; R4 means hydrogen atom or (C1-C4)-alkyl; R5 means -(CH2)n-R7 wherein n = 0-4; R7 means 3-7-membered ring comprising 1-3 heteroatoms taken among nitrogen atom (N) and oxygen atom (O), (C3-C7)-cycloalkyl or phenyl wherein indicated groups can be substituted with different substitutes; or R4 and R5 mean independently hydrogen atom (H), (C2-C6)-alkynyl or (C1-C6)-alkyl that can be substituted possibly; or R4 and R5 in common with nitrogen atom (N) form 4-7-membered ring comprising 1-2 heteroatoms taken among N and O and substituted possibly. Also, invention relates to their pharmaceutically acceptable salts, methods for preparing these compounds, intermediate substances, pharmaceutical composition and a to a method for treatment of different diseases mediated by activity of phosphodiesterase-5 (PDE-5). Described compounds of the formula (I) are inhibitor of PDE-5.
EFFECT: improved preparing method and treatment, valuable properties of compounds.
20 cl, 5 tbl, 149 ex
< / BR>where Z denotes a group of General formula II
< / BR>where A, B, X, Z, R1-R10have the meanings indicated in the claims, as well as the way they are received and drug based on these compounds
-,or- cyclodextrin or its alkyl - or hydroxyalkylated and (6r)- or (6s)-5,10-methylenetetrahydrofolic acid or a salt thereof, a method of stabilizing aqueous solutions and the method of obtaining stable solutions" target="_blank">
< / BR>which is one of the strongest antihypertensive compounds
FIELD: veterinary science.
SUBSTANCE: the present innovation deals with supplementing the feedstuff with mineral additive as neutralized white slime of alumina production of the following composition, weight%: aluminum oxide 25-35; silicon oxide 20-25; iron oxide 3-10; calcium oxide 3-10; sodium oxide 15-20; sulfur oxide 3-6; potassium oxide 0.5-2.0, free alkali, 0.02, not more; weight portion of moisture 15, not more, to be introduced once daily for about 5-7 d before transportation at the dosage of 200-300 g/animal/d. The innovation provides decreased level of stress and loses of meat productivity in cattle.
EFFECT: higher efficiency.