CP-122,288

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CP-122,288
CP-122288 structure.png
Identifiers
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
Chemical and physical data
FormulaC16H23N3O2S
Molar mass321.437 g/mol g·mol−1
3D model (JSmol)

CP-122,288 is a drug which acts as a potent and selective agonist for the 5-HT1B, 5-HT1D and 5-HT1F serotonin 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]

See also[edit]

References[edit]

  1. ^ Lee WS, Moskowitz MA. Conformationally restricted sumatriptan analogues, CP-122,288 and CP-122,638 exhibit enhanced potency against neurogenic inflammation in dura mater. Brain Res. 1993 Oct 29;626(1-2):303-5. PMID 8281439
  2. ^ Beattie DT, Connor HE. The pre- and postjunctional activity of CP-122,288, a conformationally restricted analogue of sumatriptan. Eur J Pharmacol. 1995 Apr 4;276(3):271-6. PMID 7601213
  3. ^ Waeber C, Moskowitz MA. [3H]sumatriptan labels both 5-HT1D and 5-HT1F receptor binding sites in the guinea pig brain: an autoradiographic study. Naunyn Schmiedebergs Arch Pharmacol. 1995 Sep;352(3):263-75. PMID 8584041
  4. ^ Gupta P, Brown D, Butler P, Ellis P, Grayson KL, Land GC, Macor JE, Robson SF, Wythes MJ, Shepperson NB. The in vivo pharmacological profile of a 5-HT1 receptor agonist, CP-122,288, a selective inhibitor of neurogenic inflammation. Br J Pharmacol. 1995 Nov;116(5):2385-90. PMID 8581273
  5. ^ Roon KI, Olesen J, Diener HC, Ellis P, Hettiarachchi J, Poole PH, Christianssen I, Kleinermans D, Kok JG, Ferrari MD. 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. Ann Neurol. 2000 Feb;47(2):238-41. PMID 10665496