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Catalog No.S2459 Synonyms: HF 1854, LX 100-129

4 publications

Clozapine  Chemical Structure

CAS No. 5786-21-0

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

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10mM (1mL in DMSO) USD 130 In stock
USD 97 In stock
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Selleck's Clozapine has been cited by 4 publications

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  • Michaelis-Menten plots illustrate the effects of PGD, individual radix paeonia (Pr) and radix glycyrrhiza (Gr) preparations, and the two individual preparations in combination on the formation of N-demethyl-clozapine (A) and clozapine-N-oxide (B) in the human liver microsomes. Serial concentration of clozapine was coincubated in the presence of herbal preparations. The absence of herbal preparations serves as control (CON).

    Drug Metab Dispos, 2015, 43(7):1147-53.. Clozapine purchased from Selleck.

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Biological Activity

Description Clozapine (HF 1854, LX 100-129) is an atypical antipsychotic drug by acting as a 5-HT antagonist, used in the treatment of schizophrenia.
5-HT2 [1]
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. [1] Clozapine induces zif268 but not c-fos mRNA in rat striatum, while Haloperidol induces c-Fos-like immunoreactivity in the caudate-putamen. [2] Clozapine is more selective for D4 receptors compared to D2 receptors. Clozapine is a mixed but weak D1/D2 antagonist. [3] 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. [4] 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. [5]

In vivo Clozapine exhibits an "inverted-U" shaped dose-response curve, reversing the apomorphine-induced loss of prepulse inhibition (PPI) at low doses but not at high doses in the rats. Clozapine decreases PPI independent of apomorphine treatment in the rats. [6]


Solubility (25°C)

In vitro DMSO 65 mg/mL (198.88 mM)
Ethanol 32 mg/mL (97.91 mM)
Water Insoluble

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Chemical Information

Molecular Weight 326.82


CAS No. 5786-21-0
Storage powder
in solvent
Synonyms HF 1854, LX 100-129
Smiles CN1CCN(CC1)C2=NC3=C(C=CC(=C3)Cl)NC4=CC=CC=C42

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04325386 Recruiting Other: Education Sessions|Other: No Education Session Schizophrenia Schizoaffective University of Maryland Baltimore October 15 2020 Not Applicable
NCT03996356 Not yet recruiting Other: No study intervention - observational study Weight Gain|Antipsychotic Agents|Pharmacogenetics Cwm Taf University Health Board (NHS) March 2020 --
NCT04074213 Recruiting Drug: Clozapine Lymphoma|Leukemia University Hospital Caen March 1 2019 --
NCT03076346 Recruiting -- Schizophrenia|Treatment-resistant Schizophrenia|Schizoaffective Disorder University of Pittsburgh September 1 2017 --

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