Detail of "3313-27-7"

Reference

A GC/CIMS assay for the cis and trans isomers of thiothixene in human plasma

A GC/CIMS assay for the cis and trans isomers of thiothixene in human plasma. Bombardt, Paul A.; Friedel, Robert O. (Dep. Psychiatry Behav. Sci., Univ. Washington, Seattle, Wash., USA). Commun. Psychopharmacol., 1(1), 49-59 (English) 1977. CODEN: CPSZDP. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacodynamics) A sensitive gas chromatog./chem. ionization mass spectrometry assay for the detn. of cis-thiothixene (cis-I) [3313-26-6] employing selected ion monitoring is described. Use of trideutero-cis-I as the internal std. allowed plasma levels as low as 1 ng/mL to be quantified with a high degree of precision. This assay permits, for the first time, the sepn. of pharmacol. active cis-I from the relatively inactive trans-I [3313-27-7]. Plasma drug levels from patients treated with cis-I suggest conversion in vivo to trans-I by an unknown mechanism.

Neuroleptic drugs: direct correlation between clinical potency and presynaptic action on dopamine neurons

Neuroleptic drugs: direct correlation between clinical potency and presynaptic action on dopamine neurons. Seeman, Philip; Lee, Tyrone (Pharm. Dep., Univ. Toronto, Toronto, Ont., Can.). Wenner-Gren Cent. Int. Symp. Ser., Volume Date 1974, 25(Antipsychotic Drugs: Pharmacodyn. Pharmacokinet., Proc. Int. Symp.), 183-91 (English) 1976. CODEN: WGCSAA. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacodynamics) Neuroleptic (antipsychotic) drugs inhibited the elec. stimulated release of 3H-labeled dopamine [51-61-6] from rat striatal slices. The concns. for 50% inhibition (ranging from 11.5 nM for spiroperidol [749-02-0] to 800 nM for thioridazine-HCl [130-61-0]) correlated closely with the av. daiy doses of 25 neuroleptics used clin. for schizophrenia. The correlation includes such diverse drugs as butyrophenones, phenothiazines, reserpine phosphate [1263-94-1], pimozide [2062-78-4], clozapine [5786-21-0], and (+)-butaclamol-HCl [55528-07-9]. Clin. inactive isomers (P-4657A (trans-thiothixene) [3313-27-7], .beta.-flupenthixol-2HCl [56396-47-5], and (-)-butaclamol-HCl [55528-08-0]) required 20-1000 times greater concn. than the active isomers to inhibit release. Compared to the inhibition of 3H-dopamine release, much higher neuroleptic concns. were needed to inhibit the elec. stimulated release of other neurotransmitters (3H-acetylcholine, +H-GABA). One possible mechanism for the effect is that neuroleptics partially block the presynaptic coupling between impulse and neuroscretion (ultimately leading to increased dopamine turnover by local and neuronal feedback paths).