Detail of "19695-21-7"

Reference

The effect of antipsychotic drugs and their clinically inactive analogs on dopamine metabolism

The effect of antipsychotic drugs and their clinically inactive analogs on dopamine metabolism. Stanley, Michael; Wilk, Sherwin (Mount Sinai Sch. Med., City Univ. New York, New York, N. Y., USA). Eur. J. Pharmacol., 44(4), 293-302 (English) 1977. CODEN: EJPHAZ. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacodynamics) Changes in dopamine (I) [51-61-6] metabolite levels in the rat striatum and tuberculum olfactorium, following the administration of 3 non-antipsychotic butyrophenones (AL-499 [19695-21-7], AHR-1900 [21492-67-1], and U-25,927 [23712-07-4]) and a non-antipsychotic benzazepine (Sch-12679 [20012-08-2]), were compared to the effects seen following the antipsychotics haloperidol [52-86-8], chlorpromazine [50-53-3], and clozapine [5786-21-0]. The non-antipsychotics, although clin. ineffective, were reported as active in a variety of animal screening tests. Haloperidol, chlorpormazine and clozapine produced a dose-dependent increase in 3,4-dihydroxyphenylacetic acid (DOPAC) [102-32-9] levels in both regions. Of the non-antipsychotic drugs only AHR-1900 significantly elevated the level of DOPAC, however, the slope of its dose-response curve was atypically flat in comparison to the dose-response curves of drugs with known antipsychotic efficacy. Moreover, the maximal effect of AHR-1900 obsd. at 40 mg/kg was less than the ED50 effect of haloperidol which occurs at a 250-fold lower dose. Thus, the dose-dependent elevation of DOPAC in the striatum and tuberculum olfactorium of the rat is a good predictor of antipsychotic efficacy. A method for the detn. of gas chromatog. I is described.