Chlorprothixene hydrochloride

Modify Date: 2024-01-04 17:34:13

Chlorprothixene hydrochloride Structure
Chlorprothixene hydrochloride structure
Common Name Chlorprothixene hydrochloride
CAS Number 6469-93-8 Molecular Weight 352.32100
Density N/A Boiling Point 461.8ºC at 760 mmHg
Molecular Formula C18H19Cl2NS Melting Point 221ºC
MSDS Chinese USA Flash Point 233.1ºC
Symbol GHS06
GHS06
Signal Word Danger

 Use of Chlorprothixene hydrochloride


Chlorprothixene hydrochloride is a dopamine and histamine receptors antagonist with Kis of 18 nM, 2.96 nM, 4.56 nM, 9 nM and 3.75 nM for hD1, hD2, hD3, hD5 and hH1 receptors, respectively. Antipsychotic activity[1].

 Names

Name 2-Chloro-9-(3-dimethylaminopropylidene)thioxanthene hydrochloride
Synonym More Synonyms

 Chlorprothixene hydrochloride Biological Activity

Description Chlorprothixene hydrochloride is a dopamine and histamine receptors antagonist with Kis of 18 nM, 2.96 nM, 4.56 nM, 9 nM and 3.75 nM for hD1, hD2, hD3, hD5 and hH1 receptors, respectively. Antipsychotic activity[1].
Related Catalog
Target

Human D1 Receptor:18 nM (Ki)

Human D2 Receptor:2.96 nM (Ki)

Human D3 Receptor:4.56 nM (Ki)

Human D5 Receptor:9 nM (Ki)

Human H1 Receptor:3.75 nM (Ki)

In Vitro Chlorprothixene binds to 5-HT receptors with pKis of 8.3, 8.5, and 9.4 for 5-HT7, 5-HT6 and 5-HT2, respectively[2].
References

[1]. Y von Coburg, et al. Potential utility of histamine H3 receptor antagonist pharmacophore in antipsychotics. Bioorg Med Chem Lett. 2009 Jan 15;19(2):538-42.

[2]. B L Roth, et al. Binding of typical and atypical antipsychotic agents to 5-hydroxytryptamine-6 and 5-hydroxytryptamine-7 receptors. J Pharmacol Exp Ther. 1994 Mar;268(3):1403-10.

 Chemical & Physical Properties

Boiling Point 461.8ºC at 760 mmHg
Melting Point 221ºC
Molecular Formula C18H19Cl2NS
Molecular Weight 352.32100
Flash Point 233.1ºC
Exact Mass 351.06200
PSA 28.54000
LogP 5.99000
Storage condition 2-8°C
Water Solubility Soluble in water and in alcohol, slightly soluble in methylene chloride.

 Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :
XO0610000
CHEMICAL NAME :
Thioxanthene, 2-chloro-9-(3-(dimethylamino)propylidene)-, hydrochloride, (Z)-
CAS REGISTRY NUMBER :
6469-93-8
LAST UPDATED :
199709
DATA ITEMS CITED :
6
MOLECULAR FORMULA :
C18-H18-Cl-N-S.Cl-H
MOLECULAR WEIGHT :
352.34
WISWESSER LINE NOTATION :
T C666 BS IYJ FG IU3N1&1 &GH -Z

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
200 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
27ZQAG "Psychotropic Drugs and Related Compounds," 2nd ed., Usdin, E., and D.H. Efron, Washington, DC, 1972 Volume(issue)/page/year: -,65,1972
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
25 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
27ZQAG "Psychotropic Drugs and Related Compounds," 2nd ed., Usdin, E., and D.H. Efron, Washington, DC, 1972 Volume(issue)/page/year: -,65,1972
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
242 mg/kg
TOXIC EFFECTS :
Behavioral - ataxia
REFERENCE :
CCCCAK Collection of Czechoslovak Chemical Communications. (Academic Press Inc. Ltd., 24-28 Oval Rd., London NW1 7DX, UK) V.1- 1929- Volume(issue)/page/year: 45,3166,1980
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
98 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
CKFRAY Ceskoslovenska Farmacie. (PNS-Ustredni Expedice a Dovoz Tisku, Kafkova 19, 160 00 Prague 6, Czechoslovakia) V.1- 1952- Volume(issue)/page/year: 15,526,1966
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
140 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
27ZQAG "Psychotropic Drugs and Related Compounds," 2nd ed., Usdin, E., and D.H. Efron, Washington, DC, 1972 Volume(issue)/page/year: -,65,1972
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
43 mg/kg
TOXIC EFFECTS :
Autonomic Nervous System - other (direct) parasympathomimetic Behavioral - somnolence (general depressed activity) Behavioral - excitement
REFERENCE :
AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium) V.4- 1898- Volume(issue)/page/year: 144,481,1963

 Safety Information

Symbol GHS06
GHS06
Signal Word Danger
Hazard Statements H301
Precautionary Statements Missing Phrase - N15.00950417
Hazard Codes Xn: Harmful;
Risk Phrases R20/21/22
Safety Phrases 36
RIDADR UN 2811 6
WGK Germany 3
RTECS XO0610000
Packaging Group III
Hazard Class 6.1(b)

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 Synonyms

Chlorprothixene hydrochloride
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