trifluoperazine

Description: Trifluoperazine (TFP; SKF5019), a typical phenothiazine class of antipsychotic primarily used to treat schizophrenia, is a dopamine D2 receptor inhibitor with IC50 of 1.1 NM. Other official indications may vary country by country, but generally it is also indicated for use in agitation and patients with behavioural problems, severe nausea and vomiting as well as severe anxiety. Trials have shown a moderate benefit of this drug in patients with borderline personality disorder. Trifluoperazine binds to alpha1A- and alpha1B-adrenoceptor with Ki value of 27.6 nM and 19.2 nM, respectively, with alpha1B/alpha1A ratio of 0.7. Trifluoperazine inhibits Mycobacterium tuberculosis (Mtb) with MICs of 7.6 ug/mL. 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.

References: Eur Neuropsychopharmacol. 2005 Mar; 15(2):231-4; J Pharmacol Exp Ther. 1999 Aug; 290(2):901-7.

Related CAS#: 165602-90-4 (Trifluoperazine N-Glucuronide); 117-89-5 (free base)