L-745,870

L-745,870 is a drug that acts as a selective antagonist for the D4 dopamine receptor. It was developed by the pharmaceutical company Pfizer in the 1990s, as a potential antipsychotic medication, but was found to be ineffective for schizophrenia in human trials, despite showing promise in animal studies.

History

L-745,870 was first synthesized by Pfizer in the 1990s as part of a research program aimed at developing new antipsychotic drugs. The compound was selected for development due to its high selectivity for the D4 dopamine receptor, a subtype of dopamine receptor that had been implicated in the pathophysiology of schizophrenia.

Pharmacology

L-745,870 is a selective antagonist for the D4 dopamine receptor. This means it binds to this receptor and blocks its activation by dopamine. The D4 receptor is one of five subtypes of dopamine receptor, and is found in the brain, particularly in the prefrontal cortex, a region thought to be involved in cognitive functions like memory and attention.

Clinical trials

Despite showing promise in animal studies, L-745,870 was found to be ineffective for schizophrenia in human trials. The reasons for this are not fully understood, but it is thought that the D4 receptor may not be as important in the pathophysiology of schizophrenia as initially believed.

See also

• Dopamine receptor D4
• Pfizer
• Antipsychotic

References

L-745,870 Resources
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