CP-122,288 is a drug which acts as a potent and selective
agonist
An agonist is a chemical that activates a Receptor (biochemistry), receptor to produce a biological response. Receptors are Cell (biology), cellular proteins whose activation causes the cell to modify what it is currently doing. In contrast, an R ...
for the
5-HT1B,
5-HT1D and
5-HT1F serotonin receptor
5-HT receptors, 5-hydroxytryptamine receptors, or serotonin receptors, are a group of G protein-coupled receptor and ligand-gated ion channels found in multiple tissues including the central and peripheral nervous systems. They mediate both ex ...
subtypes. It is a derivative of the
migraine
Migraine (, ) is a complex neurological disorder characterized by episodes of moderate-to-severe headache, most often unilateral and generally associated with nausea, and light and sound sensitivity. Other characterizing symptoms may includ ...
medication
sumatriptan
Sumatriptan, sold under the brand name Imitrex among others, is a medication used to treat migraine headaches and cluster headaches. It is taken Oral administration, orally, Nasal administration, intranasally, or by Subcutaneous injection, su ...
, but while CP-122,288 is 40,000 times more potent than sumatriptan as an inhibitor of neurogenic inflammation and plasma protein extravasation, it is only twice as potent as a constrictor of blood vessels. In human trials, CP-122,288 was not found to be effective as a treatment for migraine, but its selectivity for neurogenic anti-inflammatory action over vasoconstriction has made it useful for research into the underlying causes of migraine.
See also
*
5-MeO-MPMI
*
CP-135807
CP-135807 is a drug which acts as a potent and selective agonist for the 5-HT1D serotonin receptor, and is used to study the function of this receptor subtype.
See also
* 4-HO-MPMI
* 5-MeO-MPMI
* Eletriptan
Eletriptan, sold under the bra ...
*
Eletriptan
Eletriptan, sold under the brand name Relpax and used in the form of eletriptan hydrobromide, is a second-generation triptan medication intended for treatment of migraine headaches. It is used as an abortive medication, blocking a migraine at ...
References
5-HT1B agonists
5-HT1D agonists
5-HT1F agonists
N,N-Dialkyltryptamines
Pyrrolidines
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