| 词条 | CP-122,288 |
| 释义 |
| IUPAC_name = N-methyl-1-[3-([(2R)-1-methylpyrrolidin-2-yl]methyl)-1H-indol-5-yl]methanesulfonamide | image = CP-122288_structure.png | width = 220 | tradename = | pregnancy_AU = | pregnancy_US = | pregnancy_category = | legal_AU = | legal_CA = | legal_UK = | legal_US = | legal_status = | routes_of_administration = | bioavailability = | protein_bound = | metabolism = | elimination_half-life = | excretion = | IUPHAR_ligand = 110 | CAS_number = 143321-74-8 | ATC_prefix = | ATC_suffix = | ChEMBL = | PubChem = 132552 | ChemSpiderID = 117032 | C=16 | H=23 | N=3 | O=2 | S=1 | molecular_weight = 321.437 g/mol | smiles = CNS(=O)(=O)Cc1ccc2c(c1)c(c[nH]2)C[C@H]3CCCN3C | StdInChI = 1S/C16H23N3O2S/c1-17-22(20,21)11-12-5-6-16-15(8-12)13(10-18-16)9-14-4-3-7-19(14)2/h5-6,8,10,14,17-18H,3-4,7,9,11H2,1-2H3/t14-/m1/s1 | StdInChIKey = BWQZTHPHLITOOZ-CQSZACIVSA-N | melting_point = | melting_high = }}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
References1. ^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}} {{Serotonergics}}{{nervous-system-drug-stub}}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}} 4 : Serotonin receptor agonists|Pyrrolidines|Indoles|Amines |
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