Chlorprothixene (hydrochloride)
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
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.]
Storage | Store at -20°C |
M.Wt | 352.3 |
Cas No. | 6469-93-8 |
Formula | C18H18ClNS·HCl |
Synonyms | cis-Chlorprothixene,NSC 169899 |
Solubility | ≥16.75 mg/mL in DMSO; ≥18.23 mg/mL in EtOH with ultrasonic; ≥53.9 mg/mL in H2O |
Chemical Name | (3Z)-3-(2-chloro-9H-thioxanthen-9-ylidene)-N,N-dimethyl-1-propanamine, monohydrochloride |
SDF | Download SDF |
Canonical SMILES | ClC1=CC2=C(C=C1)SC3=CC=CC=C3/C2=C/CCN(C)C.Cl |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |