SB-258,719

SB-258,719
IUPAC ime
(1R)-3,N-dimetil-N-[1-metil-3-(4-metilpiperidin-1-il)propil]benzenesulfonamid
Identifikatori
CAS broj195199-95-2 ДаY
ATC kodnone
PubChemCID 5312148
ChemSpider4471578 ДаY
ChEMBLCHEMBL12264 ДаY
Hemijski podaci
FormulaC18H32N2O2S
Molarna masa340,523 g/mol
  • c1ccc(C)cc1S(=O)(=O)[NH2](C)C(C)CCN(CC2)CCC2C
  • InChI=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 ДаY
  • Key:AGVNHDNTFYHZNL-QGZVFWFLSA-N ДаY

SB-258,719 je lek koji deluje kao selektivni parcijalni inverzni agonist 5-HT7 receptora.[1] On je bio prvi identifikovani antagonist 5-HT7 receptora.[2] On se uglavnom upotrebljan u istraživanjima za demonstriranje potencijalne uloge 5-HT7 agonista kao potencijalnih analgetika, usled njegove sposobnosti da blokira analgetičke efekte raznih 5-HT7 agonista u miše modela.[3][4][5][6]

Reference

[уреди | уреди извор]
  1. ^ Mahé C, Loetscher E, Feuerbach D, Müller W, Seiler MP, Schoeffter P (2004). „Differential inverse agonist efficacies of SB-258719, SB-258741 and SB-269970 at human recombinant serotonin 5-HT7 receptors”. European Journal of Pharmacology. 495 (2-3): 97—102. PMID 15249157. doi:10.1016/j.ejphar.2004.05.033. 
  2. ^ Forbes IT, Dabbs S, Duckworth DM, Jennings AJ, King FD, Lovell PJ, Brown AM, Collin L, Hagan JJ, Middlemiss DN, Riley GJ, Thomas DR, Upton N (1998). „(R)-3,N-dimethyl-N-[1-methyl-3-(4-methyl-piperidin-1-yl) propyl]benzenesulfonamide: the first selective 5-HT7 receptor antagonist”. Journal of Medicinal Chemistry. 41 (5): 655—7. PMID 9513592. doi:10.1021/jm970519e. 
  3. ^ Brenchat A, Romero L, García M, Pujol M, Burgueño J, Torrens A, Hamon M, Baeyens JM, Buschmann H, Zamanillo D, Vela JM (2009). „5-HT7 receptor activation inhibits mechanical hypersensitivity secondary to capsaicin sensitization in mice”. Pain. 141 (3): 239—47. PMID 19118950. doi:10.1016/j.pain.2008.11.009. 
  4. ^ Yanarates O, Dogrul A, Yildirim V, Sahin A, Sizlan A, Seyrek M, Akgül O, Kozak O, Kurt E, Aypar U (2010). „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”. Anesthesiology. 112 (3): 696—710. PMID 20179508. doi:10.1097/ALN.0b013e3181cd7920. 
  5. ^ Brenchat A, Nadal X, Romero L, Ovalle S, Muro A, Sánchez-Arroyos R, Portillo-Salido E, Pujol M, Montero A, Codony X, Burgueño J, Zamanillo D, Hamon M, Maldonado R, Vela JM (2010). „Pharmacological activation of 5-HT7 receptors reduces nerve injury-induced mechanical and thermal hypersensitivity”. Pain. 149 (3): 483—94. PMID 20399562. doi:10.1016/j.pain.2010.03.007. 
  6. ^ Brenchat A, Ejarque M, Zamanillo D, Vela JM, Romero L (2011). „Potentiation of Morphine Analgesia by Adjuvant Activation of 5-HT(7) Receptors”. Journal of Pharmacological Sciences. 116 (4): 388—91. PMID 21778664. 

Spoljašnje veze

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