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Clozapine, a fast-off-D2 Antipsychotic

Clozapine, a fast-off-D2 Antipsychotic

Philip Seeman

ACS Chem Neurosci. 2014 Jan 15;5(1):24-9.

PMID: 24219174

Abstract:

Ever since clozapine was first synthesized and tested, it showed the unique property of having antipsychotic action but no Parkinson-like motor side effects. The antipsychotic basis of clozapine is to transiently occupy dopamine D2 receptors in the human striatum, in contrast to haloperidol and chlorpromazine, which have a prolonged occupation of D2 receptors. The chemical structure of clozapine facilitates a relatively rapid dissociation from D2 receptors. After short-term occupation of D2 receptors, peak neural activity raises synaptic dopamine, which then displaces clozapine. While clozapine also occupies other types of receptors, they may not have a significant role in preventing parkinsonism. Clozapine's transient occupation of D2 receptors permits patients to move easily and comfortably.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP207507220	Iodomethane-13C,d2		207507-22-0	Price
IAR4244651	17-Phenyl-tri-norprostaglandin D2			Price

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