Clozapine

SKU: orb1310596

Description

Clozapine is an atypical antipsychotic with a unique multi-receptor profile, acting as a potent serotonin 5-HT2A/2C antagonist with only weak D2 dopamine receptor blockade. It is widely used in research to study treatment-resistant schizophrenia mechanisms and receptor interactions in both in vitro binding assays and in vivo animal models.

Research Area

Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 5786-21-0
• MW: 326.82
• Purity: 99.93%
• Formula: C₁₈H₁₉ClN₄
• SMILES: CN1CCN(CC1)C1=NC2=C(NC3=C1C=CC=C3)C=CC(Cl)=C2
• Target: Dopamine Receptor,AChR,Adrenergic Receptor,5-HT Receptor
• Solubility: 2eq.HCl:16.3 mg/mL (49.87 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (6.12 mM);DMSO:82.5 mg/mL (252.43 mM)

Bioactivity

• Target IC50:
  α2-adrenoceptor:51 nM (Ki, inhibitor)|M1 mAChR:9.5 nM(Ki)|M4 mAChR:11 nM (EC50, agonist)|D2 Receptor:75 nM (Ki, antagonist)|5-HT2A receptor:4 nM (Ki, inhibitor)
• In Vivo:
  Clozapine significantly facilitated NMDA-evoked responses in a concentration-dependent manner (EC50: 14 nM).Clozapine produced excitatory postsynaptic potentials, which were blocked by glutamate receptor antagonists, suggesting that these excitatory postsynaptic potentials were the result of an increased release of excitatory amino acids.Clozapine is a full agonist at muscarinic M4 receptors, with an EC50=11 nM, and a -logEC50=6.52.The EC50=11 nM. Clozapine is a full agonist at muscarinic M4 receptors, with an EC50=11 nM, and inhibits forskolin-stimulated cAMP accumulation.Clozapine is a potent antagonist of agonist-induced responses at four other muscarinic receptor subtypes.
• In Vitro:
  Clozapine significantly facilitated NMDA-evoked responses in a concentration-dependent manner (EC50: 14 nM).Clozapine produced excitatory postsynaptic potentials, which were blocked by glutamate receptor antagonists, suggesting that these excitatory postsynaptic potentials were the result of an increased release of excitatory amino acids.Clozapine is a full agonist at muscarinic M4 receptors, with an EC50=11 nM, and a -logEC50=6.52.The EC50=11 nM. Clozapine is a full agonist at muscarinic M4 receptors, with an EC50=11 nM, and inhibits forskolin-stimulated cAMP accumulation.Clozapine is a potent antagonist of agonist-induced responses at four other muscarinic receptor subtypes.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Clozapine, Beta Receptor, Dopamine Receptor, DopamineReceptor, D2, antipsychotic, 5-hydroxytryptamine Receptor, Adrenergic Receptor, AdrenergicReceptor, 5-HT Receptor, HeLa, HF1854, HF-1854, HF 1854, Inhibitor, inhibit, Muscarinic acetylcholine receptor, mAChR, M1 mAChR, LX 100-129, α2-adrenoceptor, schizophrenia, psychosis, Serotonin Receptor

Compound Identifiers

PubChem CID

135398737