Clozapine

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

For research use only.

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

CAS No. 5786-21-0

Selleck's Clozapine has been cited by 5 Publications

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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

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]

Protocol (from reference)

Solubility (25°C)

In vitro

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

Chemical Information

Molecular Weight 326.82
Formula

C18H19ClN4

CAS No. 5786-21-0
Storage 3 years -20°C powder
2 years -80°C in solvent
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 Active not recruiting Other: Education Sessions|Other: No Education Session Schizophrenia Schizoaffective University of Maryland Baltimore October 15 2020 Not Applicable
NCT05083377 Completed -- Schizophrenia and Related Disorders Fundación Pública Andaluza para la gestión de la Investigación en Sevilla September 8 2020 --
NCT03996356 Unknown status 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 --

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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