Clozapine - Moligand™, 10mM in DMSO , Dopamine D2 receptor antagonist, CAS No.5786-21-0, Dopamine D2 receptor antagonist

CAS: 5786-21-0 Cat. No.: C408052 Molecular Weight: 326.82 EC Number: 227-313-7

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

HF 1854, LX 100-129 | 8-​chloro-​11-​(4-​methyl-​1-​piperazinyl)​-5H-​dibenzo[b,​e]​[1,​4]​diazepine

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

Information

Clozapine (HF 1854, LX 100-129) is an atypical antipsychotic drug by acting as a5-HTantagonist, used in the treatment of schizophrenia.
In vitro

Clozapine (10, 20 mg/kg) significantly increases the number of Fos-positive neurons in the nucleus accumbens, medial prefrontal cortex and lateral septal nucleus. Clozapine induces zif268 but not c-fos mRNA in rat striatum, while Haloperidol induces c-Fos-like immunoreactivity in the caudate-putamen. Clozapine is more selective for D4 receptors compared to D2 receptors. Clozapine is a mixed but weak D1/D2 antagonist. Clozapine produces a marked facilitation (300-400%) of NMDA-evoked responses in a concentration-dependent manner with EC50 of 14 nM. Clozapine, but not haloperidol, produces bursts of excitatory postsynaptic potentials (EPSPs), which are blocked by glutamate receptor antagonists, suggesting that these EPSPs are the result of increasing release of excitatory amino acids. Clozapine is a full agonist at the muscarinic M4 receptor (EC50 = 11 nM), producing inhibition of forskolin-stimulated cAMP accumulation. Clozapine potently antagonizes agonist-induced responses at the other four muscarinic receptor subtypes.

In vivo

Clozapine\xa0exhibits an "inverted-U" shaped dose-response\xa0curve, reversing the\xa0apomorphine-induced loss of prepulse\xa0inhibition\xa0(PPI) at low doses but not at high doses in the rats.\xa0Clozapine\xa0decreases PPI independent of\xa0apomorphine\xa0treatment in the rats.\xa0
Cell Data

cell lines：LNCaP cells, PC3 cells

Concentrations：

Incubation Time：

Powder Purity:≥99%

Specifications

Synonyms

HF 1854, LX 100-129 | 8-​chloro-​11-​(4-​methyl-​1-​piperazinyl)​-5H-​dibenzo[b, ​e]​[1, ​4]​diazepine

Specifications & Purity

Moligand™, 10mM in DMSO

Biochemical and Physiological Mechanisms

Clozapine (HF 1854, LX 100-129) is an atypical antipsychotic drug by acting as a 5-HT antagonist, used in the treatment of schizophrenia.

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Grade

Moligand™

Action Type

AGONIST, ALLOSTERIC MODULATOR, ANTAGONIST, GATING INHIBITOR

Mechanism of action

Dopamine D2 receptor antagonist

Product Properties

• ALogP: 3.1

Names and Identifiers

• Isomeric SMILES: CN1CCN(CC1)C2=NC3=C(C=CC(=C3)Cl)NC4=CC=CC=C42
• WGK Germany: 3
• RTECS: HP1750000
• Molecular Weight: 326.82
• Reaxy-Rn: 764984
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=764984&ln=

Associated Targets(Human)

DRD1 Tclin D(1A) dopamine receptor (9 Activities)

Discover Target: DRD1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

DRD2 Tclin D(2) dopamine receptor (40 Activities)

Discover Target: DRD2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

DRD4 Tchem D(4) dopamine receptor (62 Activities)

Discover Target: DRD4

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

HRH4 Tchem Histamine H4 receptor (6 Activities)

Discover Target: HRH4

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

HRH1 Tclin Histamine H1 receptor (13 Activities)

Discover Target: HRH1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

SLC6A4 Tclin Sodium-dependent serotonin transporter (2 Activities)

Discover Target: SLC6A4

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

DRD3 Tclin D(3) dopamine receptor (4 Activities)

Discover Target: DRD3

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CHRM5 Tclin Muscarinic acetylcholine receptor M5 (3 Activities)

Discover Target: CHRM5

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CHRM3 Tclin Muscarinic acetylcholine receptor M3 (3 Activities)

Discover Target: CHRM3

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CHRM4 Tclin Muscarinic acetylcholine receptor M4 (4 Activities)

Discover Target: CHRM4

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ADRA2B Tclin Alpha-2B adrenergic receptor (3 Activities)

Discover Target: ADRA2B

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CHRM2 Tclin Muscarinic acetylcholine receptor M2 (1 Activities)

Discover Target: CHRM2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ADRA2C Tclin Alpha-2C adrenergic receptor (4 Activities)

Discover Target: ADRA2C

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

HTR2A Tclin 5-hydroxytryptamine receptor 2A (40 Activities)

Discover Target: HTR2A

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

HTR7 Tclin 5-hydroxytryptamine receptor 7 (28 Activities)

Discover Target: HTR7

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ADRA1B Tclin Alpha-1B adrenergic receptor (2 Activities)

Discover Target: ADRA1B

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CHRM1 Tclin Muscarinic acetylcholine receptor M1 (11 Activities)

Discover Target: CHRM1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ADRA2A Tclin Alpha-2A adrenergic receptor (3 Activities)

Discover Target: ADRA2A

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ADRA1D Tclin Alpha-1D adrenergic receptor (3 Activities)

Discover Target: ADRA1D

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ADRA1A Tclin Alpha-1A adrenergic receptor (5 Activities)

Discover Target: ADRA1A

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

HTR2C Tclin 5-hydroxytryptamine receptor 2C (28 Activities)

Discover Target: HTR2C

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

HTR1A Tclin 5-hydroxytryptamine receptor 1A (4 Activities)

Discover Target: HTR1A

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

HTR3A Tclin 5-hydroxytryptamine receptor 3A (3 Activities)

Discover Target: HTR3A

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

HTR6 Tchem 5-hydroxytryptamine receptor 6 (20 Activities)

Discover Target: HTR6

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

HTR2B Tclin 5-hydroxytryptamine receptor 2B (5 Activities)

Discover Target: HTR2B

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

H1F0 Tchem Histone H1.0 (1 Activities)

Discover Target: H1F0

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

KCNH2 Tclin Potassium voltage-gated channel subfamily H member 2 (15 Activities)

Discover Target: KCNH2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Chemical and Physical Properties

• Solubility: Solubility (25°C) In vitro DMSO: 37 mg/mL (201.53 mM); Water: 37 mg/mL (201.53 mM); Ethanol: 37 mg/mL (201.53 mM)
• Melt Point(°C): 182-184℃

References

1. Huanhuan Yang, Cong Liu, Chuanhong Zhu, Yan Zheng, Juan Li, Qianyun Zhu, Hao Wang, Xiangming Fang, Quan Liu, Man Liang, Zilong Liu.  (2023)  Determination of ten antipsychotics in blood, hair and nails: Validation of a LC–MS/MS method and forensic application of keratinized matrix analysis.  JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS,      [PMID:37406464] [10.1016/j.jpba.2023.115557]

2. Xinding Yao, Zhenwei Wang, Yue Geng, Hongkun Zhao, Elaheh Rahimpour, William E. Acree, Abolghasem Jouyban.  (2022)  Hirshfeld surface and electrostatic potential surface analysis of clozapine and its solubility and molecular interactions in aqueous blends.  JOURNAL OF MOLECULAR LIQUIDS,      [PMID:] [10.1016/j.molliq.2022.119328]

3. Jiajing Xin, Saihong Yan, Xiangsheng Hong, Huan Zhang, Jinmiao Zha.  (2021)  Environmentally relevant concentrations of clozapine induced lipotoxicity and gut microbiota dysbiosis in Chinese rare minnow (Gobiocypris rarus).  ENVIRONMENTAL POLLUTION,      [PMID:33964688] [10.1016/j.envpol.2021.117298]

4. Yi Gong, Yueru Wang, Zibo Huang, Jiao sha, Yu Li, Tao Li, Baozeng Ren.  (2021)  Solubility, solvent effect, molecular simulation and thermodynamic properties of clozapine in twelve pure solvents.  JOURNAL OF CHEMICAL THERMODYNAMICS,      [PMID:] [10.1016/j.jct.2021.106398]

5. Kai Hu, Tiantian Pang, Yanmei Shi, Jiamin Cheng, Yanjie Huang.  (2020)  Facile preparation of a magnetic porous organic frameworks for highly sensitive determination of eight alkaloids in urine samples based UHPLC-MS/MS.  MICROCHEMICAL JOURNAL,      [PMID:] [10.1016/j.microc.2020.105048]

6. Juan Cui, Huaping Wang, Zhiqiang Zheng, Qing Shi, Tao Sun, Qiang Huang, Toshio Fukuda.  (2018)  Fabrication of perfusable 3D hepatic lobule-like constructs through assembly of multiple cell type laden hydrogel microstructures.  Biofabrication,  11  (1): (015016).  [PMID:30523847] [10.1088/1758-5090/aaf3c9]

7. Danyi Lu, Qian Xie, Baojian Wu.  (2017)  N-glucuronidation catalyzed by UGT1A4 and UGT2B10 in human liver microsomes: Assay optimization and substrate identification.  JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS,      [PMID:28803208] [10.1016/j.jpba.2017.07.037]

8. Kejun Liu, Zhizhong Xu, Jianfeng Zhang, Kaining Zhang, Chunyan Wen, Jindong Chen, Qingjiang Lin, Xianhua Zhang.  (2025)  Herb-drug interaction between Dahuang-Gancao decoction and clozapine: A pharmacokinetic study in rats.  Results in Chemistry,      [PMID:] [10.1016/j.rechem.2025.102665]