Insights into solute carriers: physiological functions and implications in disease and pharmacokinetics

MedChemComm ◽  
2016 ◽  
Vol 7 (8) ◽  
pp. 1462-1478 ◽  
Author(s):  
Margarida Estudante ◽  
Graça Soveral ◽  
José G. Morais ◽  
Leslie Z. Benet
Keyword(s):  
Drug Toxicity ◽  
Physiological Functions ◽  
Solute Carriers ◽  
Exogenous Compounds

SLCs transport many endogenous and exogenous compounds including drugs; SLCs dysfunction has implications in pharmacokinetics, drug toxicity or lack of efficacy.

Regulation of cytochrome P450 (CYP) genes by nuclear receptors

2000 ◽  
Vol 347 (2) ◽  
pp. 321-337 ◽  
Author(s):  
Paavo HONKAKOSKI ◽  
Masahiko NEGISHI
Keyword(s):  
Cytochrome P450 ◽  
Ligand Binding ◽  
Nuclear Receptors ◽  
Nuclear Receptor ◽  
Target Genes ◽  
Physiological Functions ◽  
Nuclear Receptor Superfamily ◽  
Cyp Isoforms ◽  
Exogenous Compounds

Members of the nuclear-receptor superfamily mediate crucial physiological functions by regulating the synthesis of their target genes. Nuclear receptors are usually activated by ligand binding. Cytochrome P450 (CYP) isoforms often catalyse both formation and degradation of these ligands. CYPs also metabolize many exogenous compounds, some of which may act as activators of nuclear receptors and disruptors of endocrine and cellular homoeostasis. This review summarizes recent findings that indicate that major classes of CYP genes are selectively regulated by certain ligand-activated nuclear receptors, thus creating tightly controlled networks.

Screening for drug toxicity by wave lengths greater than 3,100 A

1967 ◽  
Vol 95 (1) ◽  
pp. 12-15 ◽  
Author(s):  
H. I. Maibach
Keyword(s):  
Drug Toxicity

Drug Toxicity

2020 ◽  
Author(s):  
Keyword(s):  
Drug Toxicity

Kruppel-Like Factor 4: From Physiological Functions to Tumor Therapy

2016 ◽  
Vol 7 (1-2) ◽  
pp. 153-158
Author(s):  
Ruocong Zhao ◽  
Yunxin Lai ◽  
Peng Li
Keyword(s):  
Tumor Therapy ◽  
Physiological Functions

TOXICOLOGICAL PROFILE OF “BIOSOLBI” DRUG

1970 ◽  
pp. 67-69
Author(s):  
E. K. Rakhmatullin ◽  
O. D. Sklyarov
Keyword(s):  
Drug Toxicity ◽  
Probit Analysis ◽  
Laboratory Animals ◽  
Control Group ◽  
Hazard Class ◽  
Water Ingestion ◽  
White Rats ◽  
Poorly Soluble ◽  
And Behavior ◽  
Purebred Dogs

The article presents the results of a study of the "Bisolbi" drug toxicity (powder of light ash color, poorly soluble in water). When it is mixed with water it forms a suspension of particles that settle rapidly. Values of acute drug toxicity were determined on rats. We studied groups of six animals of the same sex, as well as similar control ones. The "Bisolbi" drug was injected to white rats intragastrically, males weighing 310 ... 320 g in doses of 2500 and 2740 mg / kg. Each dose was used in six animals; distilled water (3 ml) was used for the controls. The LD50 was calculated by the probit analysis method proposed by Litchfield and Wilcoxon modified by Z. Roth. When administered orally, an atraumatic metal probe was immersed in the stomach. Within 14 days monitored the overall health status and behavior of animals, the manifestation or absence of symptoms of intoxication; noted the features of feed and water ingestion, assessed the condition of the coat, physiological functions. Then groups of experimental rats were euthanized and pathomorphologically examined. We studied the effect of "Bisolbi" with repeated introduction and on not purebred dogs. Two groups of 3-4 years of age were completed with an average initial body weight of 13.63 ... 15.11 kg. Before use, the additive was thoroughly mixed with feed. The drug was injected during 31 days at a dose of 0.5 g / kg. Dogs of the control group (three) were fed wheat flour. After 15 and 31 days in laboratory animals in order to characterize the general condition in the blood, the amount of protein, urea, glucose, creatinine, cholesterol were determined. Based on studies it was found that the drug daily application by animals, is low toxic and safe, does not provoke the development of pathological reactions. According to the Hodge and Sterner classification "Bisolbi" can be attributed to the 6th class of toxicity - relatively harmless. Accordingto GOST 12.1.007-76 LD50 of the drug is more than 151 mg / kg, but less than 5000 mg / kg it is the 3rd hazard class (moderately hazardous).

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