- Apparent high CYP3A5 expression is required for significant metabolism of vincristine by human cryopreserved hepatocytes
[作者:Dennison, JB; Mohutsky, MA; Barbuch, RJ; Wrighton, SA; Hall, SD,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:248-257 , 文章类型: Article,,卷期:2008年327-1]
Vincristine is metabolized to one primary metabolite, M1, by cDNA-expressed CYP3A4 and CYP3A5 and by CYP3A enzymes in human liver microsomes. For both systems, CYP3A5 is predicted to mediate approximately 80% of the C...
- Fispemifene [Z-2-{2-[4-(4-Chloro-1,2-diphenylbut-1-enyl)phenoxy]ethoxy}-ethanol], a novel selective estrogen receptor modulator, attenuates glandular inflammation in an animal model of chronic nonbacterial prostatitis
[作者:Yatkin, E; Bernoulli, J; Lammintausta, R; Santti, R,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:58-67 , 文章类型: Article,,卷期:2008年327-1]
The anti-inflammatory and antiestrogenic action of fispemifene [Z-2-{2-[4-(4-chloro-1,2-diphenylbut-1-enyl)phenoxy]ethoxy}ethanol], a novel selective estrogen receptor modulator ( SERM), was tested on the Noble rat mo...
- K+ channel TASK-1 knockout mice show enhanced sensitivities to ataxic and hypnotic effects of GABA(A) receptor ligands
[作者:Linden, AM; Aller, MI; Leppa, E; Rosenberg, PH; Wisden, W; Korpi, ER,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:277-286 , 文章类型: Article,,卷期:2008年327-1]
TASK two-pore-domain leak K+ channels occur throughout the brain. However, TASK-1 and TASK-3 knockout (KO) mice have few neurological impairments and only mildly reduced sensitivities to inhalational anesthetics, cont...
- Phenylalanine 169 in the second extracellular loop of the human histamine H-4 receptor is responsible for the difference in agonist binding between human and mouse H-4 receptors
[作者:Lim, HD; Jongejan, A; Bakker, RA; Haaksma, E; de Esch, IJP; Leurs, R,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:88-96 , 文章类型: Article,,卷期:2008年327-1]
Using the natural variation in histamine H-4 receptor protein sequence, we tried to identify amino acids involved in the binding of H-4 receptor agonists. To this end, we constructed a variety of chimeric human-mouse ...
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