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Protection by pantethine, pantothenic acid and cystamine against carbon tetrachloride-induced hepatotoxicity in the rat.

The daily ip administration of pantethine (500 mg/kg), pantothenic acid (100 mg/kg) or cystamine (50 mg/kg) for 5 days conferred significant protection against the hepatotoxic and peroxidative actions of a 0.5 mL/kg ip dose of CCl4 in rats. All three treatments lessened the increases in serum ALT and liver TBARS values, and the reductions in serum triglyceride levels, and prevented the development of hepatic steatosis caused by the halocarbon. Pantethine was found to offer the greatest protection.

Alanine Transaminase↗

Molecular properties of the adrenergic alpha-receptor. I--Structural requirements for specific covalent occupancy by N,N'-bis--(5-aminopentyl)cystamine derivatives.

The synthesis and alpha-adrenoreceptor blocking activity of several substituted analogs of the prototype alpha-blocker N,N'-bis-(5-aminopentyl)cystamine (APC) are described. The three optical forms of the analog carrying methyl groups on the carbons alpha- to the sulfurs were synthesized and shown to be equipotent and somewhat less active than APC. The omega, omega'-bis-guanidino analog of APC was less active. Significant improvement in potency was observed only with APC analogs carrying benzyl and substituted benzyl groups on the terminal nitrogens. Linking the terminal nitrogens of APC with a p.xyledenyl group so as to give the 26-membered analog caused a sharp drop in activity. The significance of these results as regards the alpha-receptor topography is discussed.

Adrenergic alpha-Antagonists↗

[Experience in using cystamine for decreasing radiation disorders in Wistar rat embryogenesis].

In experiments on 340 primigravida Wistar rats and 1557 young rats of the first generation a study was made of toxicity and radioprotective efficiency of single subcutaneous injection of 100 mg/kg cystamine on days 3, 11 and 19 of pregnancy. In the control animals, the preparation caused different changes in the pregnancy course, delivery and postnatal development of posterity. The radioprotective properties of the preparation were only manifested when embryos were exposed to 3 Gy radiation (a lethal dose) during the preimplantation period, and it was less effective during the periods of organogenesis and fetus formation.

Animals↗

[The effect of cystamine on the level of postradiation peroxidation products in the lymph of dogs].

The experiments on irradiated dogs with a drained pectoral lymph duct revealed an early accumulation of radiotoxins (diene conjugates and malonic dialdehyde) in the lymph and blood plasmas and; simultaneously, a lowering of water-soluble antioxidants. The prophylactic application of cystamine improved the drain-detoxifying function of the lymphatic system, lowered the level of radiotoxins, and aided in the antioxidant properties of lymph and blood plasmas.

Animals↗

[Effects of cystamine on the state of peripheral blood neutrophilic granulocytes in vivo in rats].

It has been found experimentally, that decay of the intercellular energy exchange, intensification of the secretory degranulation, activation of the oxygen-dependent enzyme system and increasing the functional potential of the male-rats neutrophils took place on the height of the protective action of cystamine. On the 1-st day the tendency to restoration was noted and the normalisation of the functional and metabolical status of the neutrophils could be seen on the 5-th day after injection.

Animals↗