CP-122,288 is a drug which acts as a potent and selective
agonist for the
5-HT1B,
5-HT1D and
5-HT1Fserotonin receptor subtypes. It is a derivative of the
migraine medication
sumatriptan, 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.[1][2][3][4][5]
^Lee WS, Moskowitz MA (October 1993). "Conformationally restricted sumatriptan analogues, CP-122,288 and CP-122,638 exhibit enhanced potency against neurogenic inflammation in dura mater". Brain Research. 626 (1–2): 303–5.
doi:
10.1016/0006-8993(93)90591-a.
PMID8281439.
S2CID9350217.
^Beattie DT, Connor HE (April 1995). "The pre- and postjunctional activity of CP-122,288, a conformationally restricted analogue of sumatriptan". European Journal of Pharmacology. 276 (3): 271–6.
doi:
10.1016/0014-2999(95)00080-5.
PMID7601213.
^Waeber C, Moskowitz MA (September 1995). "[3H]sumatriptan labels both 5-HT1D and 5-HT1F receptor binding sites in the guinea pig brain: an autoradiographic study". Naunyn-Schmiedeberg's Archives of Pharmacology. 352 (3): 263–75.
doi:
10.1007/bf00168556.
PMID8584041.
S2CID8828017.
^Roon KI, Olesen J, Diener HC, Ellis P, Hettiarachchi J, Poole PH, Christianssen I, Kleinermans D, Kok JG, Ferrari MD (February 2000). "No acute antimigraine efficacy of CP-122,288, a highly potent inhibitor of neurogenic inflammation: results of two randomized, double-blind, placebo-controlled clinical trials". Annals of Neurology. 47 (2): 238–41.
doi:
10.1002/1531-8249(200002)47:2<238::AID-ANA15>3.0.CO;2-L.
PMID10665496.
S2CID41069269.
CP-122,288 is a drug which acts as a potent and selective
agonist for the
5-HT1B,
5-HT1D and
5-HT1Fserotonin receptor subtypes. It is a derivative of the
migraine medication
sumatriptan, 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.[1][2][3][4][5]
^Lee WS, Moskowitz MA (October 1993). "Conformationally restricted sumatriptan analogues, CP-122,288 and CP-122,638 exhibit enhanced potency against neurogenic inflammation in dura mater". Brain Research. 626 (1–2): 303–5.
doi:
10.1016/0006-8993(93)90591-a.
PMID8281439.
S2CID9350217.
^Beattie DT, Connor HE (April 1995). "The pre- and postjunctional activity of CP-122,288, a conformationally restricted analogue of sumatriptan". European Journal of Pharmacology. 276 (3): 271–6.
doi:
10.1016/0014-2999(95)00080-5.
PMID7601213.
^Waeber C, Moskowitz MA (September 1995). "[3H]sumatriptan labels both 5-HT1D and 5-HT1F receptor binding sites in the guinea pig brain: an autoradiographic study". Naunyn-Schmiedeberg's Archives of Pharmacology. 352 (3): 263–75.
doi:
10.1007/bf00168556.
PMID8584041.
S2CID8828017.
^Roon KI, Olesen J, Diener HC, Ellis P, Hettiarachchi J, Poole PH, Christianssen I, Kleinermans D, Kok JG, Ferrari MD (February 2000). "No acute antimigraine efficacy of CP-122,288, a highly potent inhibitor of neurogenic inflammation: results of two randomized, double-blind, placebo-controlled clinical trials". Annals of Neurology. 47 (2): 238–41.
doi:
10.1002/1531-8249(200002)47:2<238::AID-ANA15>3.0.CO;2-L.
PMID10665496.
S2CID41069269.