| 词条 | SB-399885 |
| 释义 |
| Verifiedfields = changed | verifiedrevid = 449587026 | IUPAC_name = N-(3,5-Dichloro-2-methoxyphenyl)-4-methoxy-3-(1-piperazinyl)benzenesulfonamide | image = SB399885.png | width = 240 | 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 = 3241 | CAS_number_Ref = {{cascite|correct|??}} | CAS_number = 402713-80-8 | ATC_prefix = | ATC_suffix = | PubChem = 6918649 | ChEMBL_Ref = {{ebicite|changed|EBI}} | ChEMBL = 1210710 | ChemSpiderID = 5293842 | C=18 | H=21 | Cl=2 | N=3 | O=4 | S=1 | molecular_weight = 446.347 g/mol | smiles = C3CNCCN3c2cc(ccc2OC)S(=O)(=O)Nc(c1OC)cc(Cl)cc1Cl | StdInChI = 1S/C18H21Cl2N3O4S/c1-26-17-4-3-13(11-16(17)23-7-5-21-6-8-23)28(24,25)22-15-10-12(19)9-14(20)18(15)27-2/h3-4,9-11,21-22H,5-8H2,1-2H3 | StdInChIKey = ATKZKAYWARYLBW-UHFFFAOYSA-N | melting_point = | melting_high = }} SB-399885 is a drug which is used in scientific research. It acts as a potent, selective and orally active 5-HT6 receptor antagonist, with a Ki of 9.0nM. SB-399885 and other 5-HT6 antagonists show nootropic effects in animal studies,[1][2] as well as antidepressant and anxiolytic effects which are comparable to and synergistic with drugs such as imipramine and diazepam,[3][4][5] and have been proposed as potential novel treatments for cognitive disorders such as schizophrenia[6] and Alzheimer's disease. References1. ^{{cite journal | last1 = Perez-García | first1 = G | last2 = Meneses | first2 = A | title = Oral administration of the 5-HT6 receptor antagonists SB-357134 and SB-399885 improves memory formation in an autoshaping learning task | journal = Pharmacology Biochemistry and Behavior | volume = 81 | issue = 3 | pages = 673–82 | year = 2005 | pmid = 15964617 | doi = 10.1016/j.pbb.2005.05.005 }} {{Serotonergics}}{{Piperazines}}{{nervous-system-drug-stub}}2. ^{{cite journal | last1 = Hirst | first1 = WD | last2 = Stean | first2 = TO | last3 = Rogers | first3 = DC | last4 = Sunter | first4 = D | last5 = Pugh | first5 = P | last6 = Moss | first6 = SF | last7 = Bromidge | first7 = SM | last8 = Riley | first8 = G | last9 = Smith | first9 = DR | last10 = Bartlett | first10 = Sarah | last11 = Heidbreder | first11 = Christian A. | last12 = Atkins | first12 = Alan R. | last13 = Lacroix | first13 = Laurent P. | last14 = Dawson | first14 = Lee A. | last15 = Foley | first15 = Andrew G. | last16 = Regan | first16 = Ciaran M. | last17 = Upton | first17 = Neil | title = SB-399885 is a potent, selective 5-HT6 receptor antagonist with cognitive enhancing properties in aged rat water maze and novel object recognition models | journal = European Journal of Pharmacology | volume = 553 | issue = 1–3 | pages = 109–19 | year = 2006 | pmid = 17069795 | doi = 10.1016/j.ejphar.2006.09.049 | display-authors = 8 }} 3. ^{{cite journal | last1 = Wesołowska | first1 = A | last2 = Nikiforuk | first2 = A | title = Effects of the brain-penetrant and selective 5-HT6 receptor antagonist SB-399885 in animal models of anxiety and depression | journal = Neuropharmacology | volume = 52 | issue = 5 | pages = 1274–83 | year = 2007 | pmid = 17320917 | doi = 10.1016/j.neuropharm.2007.01.007 }} 4. ^{{cite journal | last1 = Wesołowska | first1 = A | title = The anxiolytic-like effect of the selective 5-HT6 receptor antagonist SB-399885: the impact of benzodiazepine receptors | journal = European Journal of Pharmacology | volume = 580 | issue = 3 | pages = 355–60 | year = 2008 | pmid = 18096153 | doi = 10.1016/j.ejphar.2007.11.022 }} 5. ^{{cite journal | last1 = Wesołowska | first1 = A | last2 = Nikiforuk | first2 = A | title = The selective 5-HT(6) receptor antagonist SB-399885 enhances anti-immobility action of antidepressants in rats | journal = European Journal of Pharmacology | volume = 582 | issue = 1–3 | pages = 88–93 | year = 2008 | pmid = 18234190 | doi = 10.1016/j.ejphar.2007.12.013 }} 6. ^{{cite journal | last1 = Li | first1 = Z | last2 = Huang | first2 = M | last3 = Prus | first3 = AJ | last4 = Dai | first4 = J | last5 = Meltzer | first5 = HY | title = 5-HT6 receptor antagonist SB-399885 potentiates haloperidol and risperidone-induced dopamine efflux in the medial prefrontal cortex or hippocampus | journal = Brain Research | volume = 1134 | issue = 1 | pages = 70–8 | year = 2007 | pmid = 17207474 | doi = 10.1016/j.brainres.2006.11.060 }} 5 : 5-HT6 antagonists|Piperazines|Phenol ethers|Sulfonamides|Chloroarenes |
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