SB-258719

SB-258719
Systematic (IUPAC) name
(1R)-3,N-dimethyl-N-[1-methyl-3-(4-methylpiperidin-1-yl)propyl]benzenesulfonamide
Identifiers
CAS Number 195199-95-2 N
PubChem CID 5312148
IUPHAR/BPS 281
ChemSpider 4471578 YesY
ChEMBL CHEMBL12264 YesY
Chemical data
Formula C18H32N2O2S
Molar mass 340.523 g/mol
 NYesY (what is this?)  (verify)

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]

References

  1. ↑ Mahé C, Loetscher E, Feuerbach D, Müller W, Seiler MP, Schoeffter P (July 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. doi:10.1016/j.ejphar.2004.05.033. PMID 15249157.
  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 (February 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. doi:10.1021/jm970519e. PMID 9513592.
  3. ↑ Brenchat A, Romero L, García M, Pujol M, Burgueño J, Torrens A, Hamon M, Baeyens JM, Buschmann H, Zamanillo D, Vela JM (February 2009). "5-HT7 receptor activation inhibits mechanical hypersensitivity secondary to capsaicin sensitization in mice". Pain 141 (3): 239–47. doi:10.1016/j.pain.2008.11.009. PMID 19118950.
  4. ↑ Yanarates O, Dogrul A, Yildirim V, Sahin A, Sizlan A, Seyrek M, Akgül O, Kozak O, Kurt E, Aypar U (March 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. doi:10.1097/ALN.0b013e3181cd7920. PMID 20179508.
  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 (June 2010). "Pharmacological activation of 5-HT7 receptors reduces nerve injury-induced mechanical and thermal hypersensitivity". Pain 149 (3): 483–94. doi:10.1016/j.pain.2010.03.007. PMID 20399562.
  6. ↑ Brenchat A, Ejarque M, Zamanillo D, Vela JM, Romero L (August 2011). "Potentiation of Morphine Analgesia by Adjuvant Activation of 5-HT(7) Receptors". Journal of Pharmacological Sciences 116 (4): 388–91. doi:10.1254/jphs.11039sc. PMID 21778664.



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