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SB-258719

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Drug

Pharmaceutical compound
SB-258719
Identifiers
IUPAC name
  • (1R)-3,N-dimethyl-N-benzenesulfonamide
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC18H30N2O2S
Molar mass338.51 g·mol
3D model (JSmol)
SMILES
  • c1ccc(C)cc1S(=O)(=O)N(C)C(C)CCN(CC2)CCC2C
InChI
  • 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
  • Key:AGVNHDNTFYHZNL-QGZVFWFLSA-N
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SB-258719 is a drug developed by GlaxoSmithKline which acts as a selective 5-HT7 receptor partial inverse agonist, and was the first such ligand identified for 5-HT7. 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.

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, et al. (February 1998). "(R)-3,N-dimethyl-N-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, et al. (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. S2CID 27144262.
  4. Yanarates O, Dogrul A, Yildirim V, Sahin A, Sizlan A, Seyrek M, et al. (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, et al. (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. S2CID 16613426.
  6. Brenchat A, Ejarque M, Zamanillo D, Vela JM, Romero L (August 2011). "Potentiation of morphine analgesia by adjuvant activation of 5-HT7 receptors". Journal of Pharmacological Sciences. 116 (4): 388–91. doi:10.1254/jphs.11039sc. PMID 21778664.
Serotonin receptor modulators
5-HT1
5-HT1A
5-HT1B
5-HT1D
5-HT1E
5-HT1F
5-HT2
5-HT2A
5-HT2B
5-HT2C
5-HT3–7
5-HT3
5-HT4
5-HT5A
5-HT6
5-HT7
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