PNU-142633 is an experimental drug candidate for the treatment of
migraine
Migraine (, ) is a common neurological disorder characterized by recurrent headaches. Typically, the associated headache affects one side of the head, is pulsating in nature, may be moderate to severe in intensity, and could last from a few hou ...
. It exerts its effect as a
selective, high
affinity 5-HT1D receptor antagonist
An antagonist is a character in a story who is presented as the chief foe of the protagonist.
Etymology
The English word antagonist comes from the Greek ἀνταγωνιστής – ''antagonistēs'', "opponent, competitor, villain, enemy, ri ...
. PNU-142633 is well tolerated after oral administration.
It was an interesting candidate due to its greater affinity for
5-HT1D compared to
5-HT1B receptors (typical migraine drugs such as triptans are agonists for both receptors), but experimental results were disappointing.
The structure can be compared favorably with
Sonepiprazole.
References
Serotonin receptor antagonists
Phenylpiperazines
Benzamides
Isochromenes
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