CP-122,288

CP-122,288

CP-122,288 is a drug that was developed by Pfizer in the 1990s. It is a member of the triptan class of drugs which are used for the treatment of migraine headaches. CP-122,288 is a potent and selective agonist for the 5-HT1B and 5-HT1D receptors, which are a type of serotonin receptor found in the brain.

History

CP-122,288 was first synthesized by Pfizer in the early 1990s as part of a research program aimed at developing new treatments for migraine. The drug was found to be highly effective in preclinical trials, but development was halted due to adverse effects observed in animal studies.

Pharmacology

CP-122,288 is a potent agonist for the 5-HT1B and 5-HT1D receptors, with a higher affinity for the 5-HT1D receptor. These receptors are found in high concentrations in the cerebral cortex and basal ganglia, areas of the brain that are involved in the pathophysiology of migraine. Activation of these receptors by CP-122,288 leads to constriction of blood vessels in the brain, which is thought to alleviate the symptoms of migraine.

Clinical Trials

In early clinical trials, CP-122,288 was found to be highly effective in relieving the symptoms of migraine. However, the drug was also found to cause hepatotoxicity in animals, which led to the discontinuation of its development.

Current Status

Despite the discontinuation of its development, CP-122,288 remains a valuable tool for research into the pathophysiology of migraine and the role of the 5-HT1B and 5-HT1D receptors in this condition. The drug is also used as a reference compound in the development of new triptan drugs.

See Also

• Triptan
• 5-HT1B receptor
• 5-HT1D receptor
• Migraine

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