| 词条 | SB-258719 |
| 释义 |
| Verifiedfields = changed | verifiedrevid = 477856143 | IUPAC_name = (1R)-3,N-dimethyl-N-[1-methyl-3-(4-methylpiperidin-1-yl)propyl]benzenesulfonamide | image = SB-258719_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 = 281 | CAS_number_Ref = {{cascite|changed|??}} | CAS_number = 195199-95-2 | ATC_prefix = | ATC_suffix = | ChEMBL_Ref = {{ebicite|correct|EBI}} | ChEMBL = 12264 | PubChem = 5312148 | ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}} | ChemSpiderID = 4471578 | StdInChI_Ref = {{stdinchicite|correct|chemspider}} | StdInChI = 1S/C18H30N2O2S/c1-15-8-11-20(12-9-15)13-10-17(3)19(4)23(21,22)18-7-5-6-16(2)14-18/h5-7,14-15,17H,8-13H2,1-4H3/t17-/m1/s1 | StdInChIKey_Ref = {{stdinchicite|correct|chemspider}} | StdInChIKey = AGVNHDNTFYHZNL-QGZVFWFLSA-N | C=18 | H=32 | N=2 | O=2 | S=1 | molecular_weight = 340.523 g/mol | smiles = c1ccc(C)cc1S(=O)(=O)N(C)C(C)CCN(CC2)CCC2C | melting_point = | melting_high = }}SB-258719 is a drug developed by GlaxoSmithKline which acts as a selective 5-HT7 receptor partial inverse agonist,[1] and was the first such ligand identified for 5-HT7.[2] Its use in research has mainly been in demonstrating the potential use for 5-HT7 agonists as potential novel analgesics, due to the ability of SB-258719 to block the analgesic effects of a variety of 5-HT7 agonists across several different testing models.[3][4][5][6] References1. ^{{cite journal |author1=Mahé C |author2=Loetscher E |author3=Feuerbach D |author4=Müller W |author5=Seiler MP |author6=Schoeffter P |title=Differential inverse agonist efficacies of SB-258719, SB-258741 and SB-269970 at human recombinant serotonin 5-HT7 receptors |journal=European Journal of Pharmacology |volume=495 |issue=2–3 |pages=97–102 |date=July 2004 |pmid=15249157 |doi=10.1016/j.ejphar.2004.05.033 |url=}} {{Serotonergics}}{{nervous-system-drug-stub}}2. ^{{cite journal |author1=Forbes IT |author2=Dabbs S |author3=Duckworth DM |author4=Jennings AJ |author5=King FD |author6=Lovell PJ |author7=Brown AM |author8=Collin L |author9=Hagan JJ |author10=Middlemiss DN |author11=Riley GJ |author12=Thomas DR |author13=Upton N |title=(R)-3,N-dimethyl-N-[1-methyl-3-(4-methyl-piperidin-1-yl) propyl]benzenesulfonamide: the first selective 5-HT7 receptor antagonist |journal=Journal of Medicinal Chemistry |volume=41 |issue=5 |pages=655–7 |date=February 1998 |pmid=9513592 |doi=10.1021/jm970519e |url=}} 3. ^{{cite journal |author1=Brenchat A |author2=Romero L |author3=García M |author4=Pujol M |author5=Burgueño J |author6=Torrens A |author7=Hamon M |author8=Baeyens JM |author9=Buschmann H |author10=Zamanillo D |author11=Vela JM |title=5-HT7 receptor activation inhibits mechanical hypersensitivity secondary to capsaicin sensitization in mice |journal=Pain |volume=141 |issue=3 |pages=239–47 |date=February 2009 |pmid=19118950 |doi=10.1016/j.pain.2008.11.009 |url=}} 4. ^{{cite journal |author1=Yanarates O |author2=Dogrul A |author3=Yildirim V |author4=Sahin A |author5=Sizlan A |author6=Seyrek M |author7=Akgül O |author8=Kozak O |author9=Kurt E |author10=Aypar U |title=Spinal 5-HT7 receptors play an important role in the antinociceptive and antihyperalgesic effects of tramadol and its metabolite, O-Desmethyltramadol, via activation of descending serotonergic pathways |journal=Anesthesiology |volume=112 |issue=3 |pages=696–710 |date=March 2010 |pmid=20179508 |doi=10.1097/ALN.0b013e3181cd7920 |url=}} 5. ^{{cite journal |author1=Brenchat A |author2=Nadal X |author3=Romero L |author4=Ovalle S |author5=Muro A |author6=Sánchez-Arroyos R |author7=Portillo-Salido E |author8=Pujol M |author9=Montero A |author10=Codony X |author11=Burgueño J |author12=Zamanillo D |author13=Hamon M |author14=Maldonado R |author15=Vela JM |title=Pharmacological activation of 5-HT7 receptors reduces nerve injury-induced mechanical and thermal hypersensitivity |journal=Pain |volume=149 |issue=3 |pages=483–94 |date=June 2010 |pmid=20399562 |doi=10.1016/j.pain.2010.03.007 |url=}} 6. ^{{cite journal |author1=Brenchat A |author2=Ejarque M |author3=Zamanillo D |author4=Vela JM |author5=Romero L |title=Potentiation of Morphine Analgesia by Adjuvant Activation of 5-HT(7) Receptors |journal=Journal of Pharmacological Sciences |volume=116 |issue=4 |pages=388–91 |date=August 2011 |pmid=21778664 |doi= 10.1254/jphs.11039sc|url=}} 3 : 5-HT7 antagonists|Piperidines|Sulfonamides |
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