Chlorprothixene (hydrochloride) (Synonyms: cis-Chlorprothixene,NSC 169899) |
| Catalog No.GC17656 |
dopamine D2 receptor antagonist and GABAA receptor inhibitor
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 6469-93-8
Sample solution is provided at 25 µL, 10mM.
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Chlorprothixene (hydrochloride) is an antagonist of dopamine receptor and histamine receptors [1]. Chlorprothixene is also an inhibitor of GABAA receptor [2]. All of these three receptors are implicated in many neurological processes, including motivation, pleasure, cognition, memory and learning.
In vitro: Chlorprothixene exihibited strong binding affinities to dopamine and histamine receptors, The Ki values of D1, D2, D3, D5 and H1 were 18nM, 2.96 nM, 4.56 nM, 9 nM and 3.75 nM, respectively. Chlorprothixene showed little affinity to H3 with the Ki value of >1000 nM[1]. In COS-7 cells transiently expressed rat 5-HT7 receptors and HEK-293 cells stably transfected with rat 5-HT6, the Ki values of chlorprothixene were 5.6 nM and 3 nM, respectively [3]. In Vero 76 cells, chlorprothixene treatment inhibited SARS-CoV replication, with IC50 of 16.7 μM for Urbani strain, 13.0 μM for Frankfurt-1, 18.5 μM for CHUK-W1 and 15.8 μM for Toronto-2 [4].
In vivo: In rat brain depressing the release of hypothalamic and hypophyseal hormones, chlorprothixene blocked postsynaptic mesolimbic dopaminergic D1 and D2 receptors [5]. Chlorprothixene treatment restored normal ceramide concentrations in murine bronchial epithelial cells, reduced inflammation in the lungs of mice with cystic fibrosis (CF) and prevented infection with Pseudomonas aeruginosa [6].
References:
[1] Von Coburg Y, Kottke T, Weizel L, et al. Potential utility of histamine H 3 receptor antagonist pharmacophore in antipsychotics[J]. Bioorganic & medicinal chemistry letters, 2009, 19(2): 538-542.
[2] Squires R F, Saederup E. Clozapine and several other antipsychotic/antidepressant drugs preferentially block the same ‘core’fraction of GABA A receptors[J]. Neurochemical research, 1998, 23(10): 1283-1290.
[3] Roth B L, Craigo S C, Choudhary M S, et al. Binding of typical and atypical antipsychotic agents to 5-hydroxytryptamine-6 and 5-hydroxytryptamine-7 receptors[J]. Journal of Pharmacology and Experimental Therapeutics, 1994, 268(3): 1403-1410.
[4] Barnard D L, Day C W, Bailey K, et al. Is the anti-psychotic, 10-(3-(dimethylamino) propyl) phenothiazine (promazine), a potential drug with which to treat SARS infections: Lack of efficacy of promazine on SARS-CoV replication in a mouse model[J]. Antiviral research, 2008, 79(2): 105-113.
[5] Gey K F, Pletscher A. Influence of chlorpromazine and chlorprothixene on the cerebral metabolism of 5-hydroxytryptamine, norepinephrine and dopamine[J]. Journal of Pharmacology and Experimental Therapeutics, 1961, 133(1): 18-24.
[6] Becker K A, Riethmuller J, Luth A, et al. Acid sphingomyelinase inhibitors normalize pulmonary ceramide and inflammation in cystic fibrosis[J]. American journal of respiratory cell and molecular biology, 2010, 42(6): 716-724.]
| Cas No. | 6469-93-8 | SDF | |
| Synonyms | cis-Chlorprothixene,NSC 169899 | ||
| Chemical Name | (3Z)-3-(2-chloro-9H-thioxanthen-9-ylidene)-N,N-dimethyl-1-propanamine, monohydrochloride | ||
| Canonical SMILES | ClC1=CC2=C(C=C1)SC3=CC=CC=C3/C2=C/CCN(C)C.Cl | ||
| Formula | C18H18ClNS • HCl | M.Wt | 352.3 |
| Solubility | ≥ 16.75mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.8385 mL | 14.1924 mL | 28.3849 mL |
| 5 mM | 0.5677 mL | 2.8385 mL | 5.677 mL |
| 10 mM | 0.2838 mL | 1.4192 mL | 2.8385 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 13 reference(s) in Google Scholar.)
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