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Clozaril is a yellow, crystalline powder that is usually imbibed in pill form. The chemical substance, which is very slightly soluble in water, primarily functions within the body by binding to dopamine receptors in the limbic system of the brain. Thus, the drug helps regulate dopamine action, which is centrally involved in the perception of reality, feelings, and moods. Clozaril also is an antagonist to other binding sites in the central nervous system, including the adrenergic (weight gain, moodiness, arousal, startle response), cholinergic (memory), histaminergic (sleep and weight gain), and serotonergic (depression, anxiety, panic, aggression) receptors. Through such biochemical means, the drug is able to help reduce the characteristic symptoms of schizophrenia, but cannot cure the typically genetic disorder.

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