Classics in Chemical Neuroscience: Haloperidol

Abstract

The discovery of haloperidol catalyzed a breakthrough in our understanding of the biochemical basis of schizophrenia, improved the treatment of psychosis, and facilitated deinstitutionalization. In doing so, it solidified the role for chemical neuroscience as a means to elucidate the molecular underpinnings of complex neuropsychiatric disorders. In this Review, we will cover aspects of haloperidol's synthesis, manufacturing, metabolism, pharmacology, approved and off-label indications, and adverse effects. We will also convey the fascinating history of this classic molecule and the influence that it has had on the evolution of neuropsychopharmacology and neuroscience.

Retracted: The Manganese(I)‐Catalyzed Asymmetric Transfer Hydrogenation of Ketones: Disclosing the Macrocylic Privilege

“…In view of the versatility of 2 and of its high functionalgroup tolerance,westudied haloperidol (9), an antagonist of the dopamine D 2 receptor and antipsychotic drug, [31] which is reduced to 10 during metabolism (Scheme 5). [31] Both 10 and its derivatives are prospective anticancer drugs. [32] The catalyst 2 reduces 9 on gram scale with 97 % ee and is isolated in 85 %y ield.…”

Retracted: The Manganese(I)‐Catalyzed Asymmetric Transfer Hydrogenation of Ketones: Disclosing the Macrocylic Privilege

“…In view of the versatility of 2 and of its high functional‐group tolerance, we studied haloperidol ( 9 ), an antagonist of the dopamine D 2 receptor and antipsychotic drug, which is reduced to 10 during metabolism (Scheme ) . Both 10 and its derivatives are prospective anticancer drugs .…”

Haloperidol ameliorates androgen-induced behavioral deficits in developing male rats

“…The increased locomotor activity and grooming behavior can be suppressed by Hal treatments (Hidaka et al 2010, Taylor et al 2010. Haloperidol, a formally approved medication in the United States (Egolf & Coffey 2014), is used to treat behavioral disorders and hyperactivity (Tyler et al 2017) and to control the tics and vocal utterances associated with TS (Termine et al 2013, Tyler et al 2017. It is a high-affinity antagonist of dopamine D2 receptors (Kapur & Mamo 2003) and one of the most effective anti-DAergic agents for the reduction of tics (Silay & Jankovic 2005, Scahill et al 2006.…”

“…Haloperidol, a D2 receptor antagonist, is widely used for the treatment of schizophrenia, affective disorders and TS (Silay & Jankovic 2005, Termine et al 2013, Egolf & Coffey 2014. It can control the tics and vocal utterances associated with TS (Tyler et al 2017). Therefore, to infer the potential effects of testosterone increase in some male-based childhoodonset neuropsychiatric disorders, such as TS, the present study analyzed the alterations of neurobehaviors and neurotransmitters as well as the influence of Hal upon the neurobehavioral deficits in male rats affected with early postnatal androgen exposure.…”