Home Neuronal Signaling 5-HT Receptor antagonist Clozapine For research use only.

Clozapine

Synonyms: HF 1854, LX 100-129

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

Clozapine Chemical Structure

Clozapine Chemical Structure

CAS: 5786-21-0

Selleck's Clozapine has been cited by 7 Publications

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Purity & Quality Control

Batch: Purity: 99.99%
99.99

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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.
Targets
5-HT2 [1]
In vitro
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
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]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05944510 Recruiting Treatment Resistant Schizophrenia All India Institute of Medical Sciences Bhubaneswar August 31 2023 Phase 4
NCT05919550 Completed Infections University Hospital Caen April 11 2023 --
NCT06011460 Enrolling by invitation Bipolar Disorder Medical University of Gdansk February 23 2023 --
NCT05083377 Completed Schizophrenia and Related Disorders Fundación Pública Andaluza para la gestión de la Investigación en Sevilla September 8 2020 --

Chemical lnformation & Solubility

Molecular Weight 326.82 Formula

C18H19ClN4
CAS No. 5786-21-0 SDF Download Clozapine SDF
Smiles CN1CCN(CC1)C2=NC3=C(C=CC(=C3)Cl)NC4=CC=CC=C42
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 65 mg/mL ( (198.88 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 65 mg/mL

Water : Insoluble


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In vivo
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