SULFORIDAZINE BESYLATE

Possibly Marketed Outside US

Details

Stereochemistry	RACEMIC
Molecular Formula	C21H26N2O2S2.C6H6O3S
Molecular Weight	560.748
Optical Activity	( + / - )
Defined Stereocenters	0 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

SMILES

OS(=O)(=O)C1=CC=CC=C1.CN2CCCCC2CCN3C4=CC(=CC=C4SC5=C3C=CC=C5)S(C)(=O)=O

InChI

InChIKey=POTAUFBGHYTSIE-UHFFFAOYSA-N

InChI=1S/C21H26N2O2S2.C6H6O3S/c1-22-13-6-5-7-16(22)12-14-23-18-8-3-4-9-20(18)26-21-11-10-17(15-19(21)23)27(2,24)25;7-10(8,9)6-4-2-1-3-5-6/h3-4,8-11,15-16H,5-7,12-14H2,1-2H3;1-5H,(H,7,8,9)

HIDE SMILES / InChI

Molecular Formula	C6H6O3S
Molecular Weight	158.175
Charge	0
Count	MOL RATIO 1 MOL RATIO (average)

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Molecular Formula	C21H26N2O2S2
Molecular Weight	402.573
Charge	0
Count	MOL RATIO 1 MOL RATIO (average)

Stereochemistry	RACEMIC
Additional Stereochemistry	No
Defined Stereocenters	0 / 1
E/Z Centers	0
Optical Activity	( + / - )

Description

Sulforidazine (Imagotan (Sandoz); Inofal (Sandoz)) is a typical piperidine-type phenothiazine antipsychotic agent. It is dopamine receptor blocker. Being the second active metabolite of thioridazine (converted from mesoridazine), Sulforidazine is significantly more potent than the parent drug.

Approval Year

PubMed

PubMed

Title	Date	PubMed
Factors affecting drug concentrations and QT interval during thioridazine therapy.	2007 Nov	17460606

Sample Use Guides

In Vivo Use Guide

The metabolism of sulforidazine was studied in female dogs and adult male humans after oral administration of 37.5 mg and 25.0 mg, respectively.

Route of Administration: Oral

In Vitro Use Guide

Mesoridazine and sulforidazine likewise produced only small increases (5-20%) in evoked overflow of DA from slices stimulated at 0.3 Hz. At this frequency of stimulation, apomorphine (30 nM) inhibited the overflow of DA by 71.4 +/- 8.43% (n = 40). All three drugs antagonized, in a concentration-dependent fashion, the inhibitory effect of apomorphine (30 nM) on electrically evoked DA release at 0.3 Hz. The IC50 for thioridazine for antagonizing the effect of apomorphine was 130 nM, whereas that for mesoridazine was 14.4 nM and for sulforidazine was 6.1 nM.