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Toxicity of pesticides to birds; the enzymic factor.
TLDR
This paper will consider some metabolic differences between birds and mammals which are related to the selective toxicity of certain pesticides, and will focus on situations where the modulation of the activity of an enzyme by one pesticide can increase the sensitivity of birds to other pesticides.
A‐esterase activities in relation to the differential toxicity of pirimiphos‐methyl to birds and mammals
Pirimiphos-methyloxon (2-diethylamino-6-methylpyrimidin-4-yl dimethyl phosphate) the phosphate analogue of pirimiphos-methyl, and paraoxon (diethyl 4-nitrophenyl phosphate) the phosphate analogue of
Effects of Fostamatinib on the Pharmacokinetics of the CYP2C8 Substrate Pioglitazone: Results From In Vitro and Phase 1 Clinical Studies
TLDR
Data suggest that although clinical significance has not been formally evaluated, fostamatinib is unlikely to have a clinically significant effect on the pharmacokinetics of pioglitazone (which may be extrapolated to other CYP2C8 substrates).
RPR 119990, a novel alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid antagonist: synthesis, pharmacological properties, and activity in an animal model of amyotrophic lateral sclerosis.
TLDR
This compound was found active in a transgenic mouse model of familial amyotrophic lateral sclerosis where it was able to improve grip muscle strength and glutamate uptake from spinal synaptosomal preparations, and prolong survival with a daily dose of 3 mg/kg s.c. administration.
Selective endothelin A receptor antagonists. 3. Discovery and structure-activity relationships of a series of 4-phenoxybutanoic acid derivatives.
TLDR
This paper describes how a pharmacophore model for ETA receptor binding was developed which enabled these two series of compounds to be merged into a single class of 4-phenoxybutanoic acid derivatives.
Effects of Fostamatinib on the Pharmacokinetics of Oral Contraceptive, Warfarin, and the Statins Rosuvastatin and Simvastatin: Results From Phase I Clinical Studies
TLDR
Fostamatinib exhibits drug–drug interactions when co-administered with OC, simvastatin, or rosuvASTatin, with the AUC of statins almost doubling, and did not exhibit a clinically relevant DDI on warfarin.
Effects of CYP3A4 Inhibitors Ketoconazole and Verapamil and the CYP3A4 Inducer Rifampicin on the Pharmacokinetic Parameters of Fostamatinib: Results from In Vitro and Phase I Clinical Studies
TLDR
Hepatic microsomes showed time-dependent loss of R406 and formation of para-O-demethylated R406, and the oxidative metabolism of R 406 is predominantly catalyzed by CYP3A4.
Resistance mechanisms to DDT and transpermethrin in Aedes aegypti
TLDR
Transpermethrin resistance in these strains is of the kdr type, while the DDT resistance is a mixture of kdr and DDT-dehydrochlorinase, by analogy with other insect species.
Cytochrome P-450 in the housefly: induction, substrate specificity and comparison to three rat hepatic isoenzymes.
TLDR
Despite similarities in patterns of induction and catalytic function, little evidence for structural commonality between the cytochrome P-450 in rat and housefly was observed.
Effects of cyclosporin A administered into the airways against antigen-induced airway inflammation and hyperreactivity in the rat.
TLDR
The data clearly demonstrate that a novel immunosuppressant with similar anti-inflammatory properties but reduced potential for systemic effects would offer an attractive therapy for severe asthma.
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