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Novartis AG

Drug Names(s): Leponex, clozapine

Description: Clozaril is an atypical antipsychotic drug in that it has a relatively low affinity for the dopamine D-2 receptor and high affinity for the serotonin 5-HT2 receptor, which produces a high 5-HT2/D-2 ratio. Though the exact mechanism is unclear (either due to a difference in affinities for such receptors or fast dissociation from the D-2 receptor), atypical antipsychotics are able to produce an antipsychotic effect (through blockade of D-2 receptors in the ventral striatum) with fewer extrapyramidal motor function side effects (or EPSs, which are caused by blockade of D-2 receptors in the dorsal striatum).

CLOZARIL also acts as an antagonist at adrenergic, cholinergic, histaminergic and serotonergicreceptors. Key receptor affinities are as follows:

D2: 125 nM;
5HT-2A: 12 nM;
5HT-2C: 8 nM;
D1: 85 nM;
M1: 2 nM;
alpha-1 adrenergic: 7 nM;
H1: 6 nM.

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