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Trifluoperazine is a dopamine D2 receptor inhibitor with IC50 of 1.1 nM.
Trifluoperazine binds to α1A- and α1B-adrenoceptor with Ki value of 27.6 nM and 19.2 nM, respectively, with α1B/α1A ratio of 0.7. [2] Trifluoperazine inhibits Mycobacterium tuberculosis (Mtb) with MICs of 7.6 μg/mL. [3]Trifluoperazine (< 14.78 mM) suppresses the activities of the mouse splenic NK cell cytotoxicity and the effector-target cell conjugation in a dose dependent manner. Trifluoperazine suppresses interferon-alpha or interleukin-2 induced augmentation of the cytolytic activity of NK cells. [4] Trifluoperazine inhibits the gene expression of voltage-dependent potassium channel Kv2.1 from human brain (hKv2.1). [5]
Trifluoperazine dose dependently decreases avoidance responses and increases response failures in rats where behavior is maintained under a discrete-trial avoidance. [6]
References
[1] Lahti RA, et al. Eur J Pharmacol, 1993, 236(3), 483-486.
[2] Cahir M, et al. Eur Neuropsychopharmacol, 2005, 15(2), 231-234.
[3] Madrid PB, et al. Bioorg Med Chem Lett, 2007, 17(11), 3014-3017.
[4] Won SJ, et al. Experientia, 1995, 51(4), 343-348.
[5] Motohashi N, et al. Curr Drug Targets, 2000, 1(3), 237-245.
[6] Shannon HE, et al. J Pharmacol Exp Ther, 1999, 290(2), 901-907.
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