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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.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
10 mg | $30 | In Stock | |
25 mg | $44 | In Stock | |
50 mg | $64 | In Stock | |
100 mg | $97 | In Stock | |
200 mg | $173 | In Stock | |
500 mg | $318 | In Stock | |
1 g | $473 | In Stock | |
1 mL x 10 mM (in DMSO) | $39 | In Stock |
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. |
Targets&IC50 | M1 receptor:9.5 nM(ki) |
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. |
Alias | LX 100-129, HF 1854 |
Molecular Weight | 326.82 |
Formula | C18H19ClN4 |
Cas No. | 5786-21-0 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 70 mg/mL (214.19 mM), Sonication is recommended. 2eq.HCl: 16.3 mg/mL (50 mM)), Heating is recommended. | ||||||||||||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||||||||||||
2eq.HCl/DMSO
DMSO
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