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At least 757 records · Page 42Linked to original sources
PubMed1979

Binding of the Cain quinolinium, NSC 113089, to rat tissue lipid extracts.

The binding characteristics of the cancer chemotherapeutic Cain's quinolinium 6-amino-1-ethyl-4-[p-[[p-[(1-ethylpyridinium-4-yl) amino] phenyl] carbamoyl]-anilino]-quinolinium dibromide (NSC 113089) to lipid extracts from rat kidney, liver, heart and skeletal muscle has been studied. Such binding is saturable with an apparent KD congruent to 1.6 microM. Drug binding to the lipid extracts is displaceable by spermine, spermidine, calcium ions and protons. Spermine is the best displacing agent, achieving half drug displacement from the lipid extracts at approximately 6.3 microM regardless of tissue. The inability of the displacing agents to displace all the NSC 113089 bound to the lipid extracts as well as differences in the amount of agent bound to as compared to amount of drug displaced from the lipid extracts indicate that a number of drug binding sites may be present in the lipid extracts. The similarities of drug binding by rat tissue lipids to similar lipids extracted from normal animal and tumor tissues is discussed.

Animals↗
PubMed1983

Evaluation of cumulative properties of three new nondepolarizing neuromuscular blocking drugs BW A444U, atracurium and vecuronium.

Comparative patterns of recovery during successive doses of three new, relatively non-cumulative, intermediate-duration non-depolarizing neuromuscular blocking drugs, BW A444U, atracurium (BW33A) and vecuronium (Org NC 45), were studied in 94 surgical patients during thiopentone in nitrous oxide and oxygen with narcotic anaesthesia. The train-of-four (TOF) pattern of nerve stimulation was used. The spontaneous 5-25% recovery time of the first twitch of TOF showed a statistically significant difference between the initial dose and the fifth incremental dose in the cases of atracurium and vecuronium, but not in the case of BW A444U. The 25-75% recovery times for the final doses were significantly longer than the corresponding times for each drug after the initial doses. The percent TOF ratio at the point of recovery of the first twitch to 95% of the control height was compared for the initial and final doses in a series of doses of each drug. The difference was significant only when the final dose of vecuronium was compared with the initial dose (TOF ratio 79.3 +/- 2.3% v. 64.3 +/- 4.4%; P less than 0.005). Analysis of variance indicates that the TOF ratio at 95% recovery of the first twitch of TOF after the final dose of vecuronium (64.3%) is significantly smaller (P less than 0.001) than that of either BW A444U (78%) or atracurium (84%), indicating that vecuronium appears to show more residual fade and greater cumulative effect after incremental doses than BW A444U or atracurium. The data suggest that the cumulative properties of the new drugs may be ranked as follows: atracurium less than BW A444U less than vecuronium.

Adult↗
PubMed1984

[Cellular mechanism of the antileukemic action of quinoline dibromide].

Autoradiography (3H-thymidine) and DNA-cytofluorometry were used to study the effect of quinoline dibromide (QD), a potential inhibitor of cobalamine-dependent methionine synthetase, on the kinetics of cell proliferation of L-1210 mouse leukemia. QD was found to produce the secondary blockade of leukemic cells in the late S-phase of the mitotic cycle. Such a mechanism of QD action promoted the potentiation of antitumor activity of the antimetabolites methotrexate, cytosine arabinoside and 5-fluorouracil during combined chemotherapy.

Animals↗
PubMed1984

Protective effect of organic cation transport inhibitors on cis-diamminedichloroplatinum-induced nephrotoxicity.

Cis-diamminedichloroplatinum (II) (cisplatin) is a frequently used cancer chemotherapeutic agent. Nephrotoxicity is a serious dose-limiting side effect. Many approaches have been studied for protective action against cisplatin-induced nephrotoxicity, but with the exception of diuretics and hydration none are in widespread use. We have used a modified Sperber technique in unanesthetized hens to examine the effect of cisplatin on renal organic cation and anion transport and on renal morphology. The effects of the organic cation transport inhibitors quinine and cyanine on cisplatin-induced toxicity also were evaluated. Administration of cisplatin (3.0 mg/kg i.v.) produced nephrotoxic and lethal effects. Four days after cisplatin administration there was a significant inhibition of renal tubular excretory transport of the organic cation tetraethylammonium and the organic anion p-aminohippuric acid. Acute multifocal tubular necrosis of the proximal tubules was present. Administration of quinine (1.5 mumol/min) and cyanine (0.122 mumol/min) protected against the lethal effects, the inhibition of renal organic cation and anion transport and the renal lesions induced by cisplatin.

Animals↗
PubMed1983

Chemotherapy of Babesia divergens in the gerbil, Meriones unguiculatus.

It was found that surprisingly low doses of four babesicides were effective against Babesia divergens in gerbils and it was concluded that this was due to the involvement of host resistance, which may be of a non-specific nature. The efficacy of the drugs relative to each other was the same in gerbils as in cattle and this host-parasite system is evidently more suitable for the screening of babesicides than are other rodent babesia systems. The prophylactic dose of imidocarb dipropionate required to provide a similar degree of protection in gerbils as in cattle was found to be much higher and was very close to toxic levels. Challenge infections resulted in sterile immunity. Acute babesiosis in gerbils could be cured with all four drugs if parasitaemias were below approximately 45 per cent and packed cell volumes above 18 per cent at treatment.

Animals↗