Clozapine is a prototypic, atypical antipsychotic which binds to both serotonin and dopamine receptors (Ki values are 35, 83 and 22, 250 and 141 nM at D2, D3 and D4, D5, D1 and 12.6 and 13.2 nM at 5-HT2A and 5-HT2C receptors respectively) and also shows activity at other receptors.
Clozapine shows high BBB permeability and is active in vivo. It shows antisychotic, antidepression and anxiolytic activites.
Recently, clozapine (which CNO rapidly converts to) has been indicated to show high DREADD (hM3Dq and hM4Di) affinity and potency. Subthreshold clozapine injections are indicated to induce preferential DREADD-mediated behaviors.
Differential regulation of rat 5-HT2A and 5-HT2C receptors after chronic treatment with clozapine, chlorpromazine and three putative atypical antipsychotic drugs.
Kuoppamã?ki M et al (1995) Neuropsychopharmacology 13(2) : 139-50.
![Clozapine [5786-21-0] Chemical Structure](https://hellobio.com/media/catalog/product//h/b/hb1607.png "Clozapine [5786-21-0]")
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