| Name | Clozapine |
| Description | Clozapine (HF 1854) is a tricylic dibenzodiazepine, classified as an atypical antipsychotic agent. It binds several types of central nervous system receptors, and displays a unique pharmacological profile. Clozapine is a serotonin antagonist, with strong binding to 5-HT 2A/2C receptor subtype. It also displays strong affinity to several dopaminergic receptors, but shows only weak antagonism at the dopamine D2 receptor, a receptor commonly thought to modulate neuroleptic activity. |
| 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. |
| 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. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 82.5 mg/mL (252.43 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (6.12 mM), Sonication is recommended.
2eq.HCl : 16.3 mg/mL (49.87 mM), Heating is recommended.
|
| Keywords | α2-adrenoceptor | Serotonin Receptor | schizophrenia | psychosis | Muscarinic acetylcholine receptor | mAChR | M1 mAChR | Inhibitor | inhibit | HF-1854 | HF1854 | HeLa | DopamineReceptor | Dopamine Receptor | D2 | Clozapine | Beta Receptor | antipsychotic | AdrenergicReceptor | Adrenergic Receptor | 5-hydroxytryptamine Receptor | 5-HT Receptor |
| Inhibitors Related | Adiphenine hydrochloride | Alverine citrate | Dapoxetine hydrochloride | Cefaclor monohydrate | Urethane | Hexamethonium Bromide | 1,8-Cineole | Adenine | Mitotane | N,N-Dicyclohexylcarbodiimide | Arecoline | Cinchonidine |
| Related Compound Libraries | Failed Clinical Trials Compound Library | Anti-Neurodegenerative Disease Compound Library | Bioactive Compound Library | Anti-Cancer Clinical Compound Library | Anti-Viral Compound Library | Drug Repurposing Compound Library | Inhibitor Library | FDA-Approved Drug Library | Anti-Cancer Approved Drug Library | Bioactive Compounds Library Max | GPCR Compound Library | Anti-Cancer Drug Library |
United States
