Chemistry:SB-258719

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Short description: Drug
SB-258719
SB-258719 structure.png
Identifiers
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
ChEMBL
Chemical and physical data
FormulaC18H30N2O2S
Molar mass338.51 g·mol−1
3D model (JSmol)
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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. ↑ "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. July 2004. doi:10.1016/j.ejphar.2004.05.033. PMID 15249157. 
  2. ↑ "(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. February 1998. doi:10.1021/jm970519e. PMID 9513592. 
  3. ↑ "5-HT7 receptor activation inhibits mechanical hypersensitivity secondary to capsaicin sensitization in mice". Pain 141 (3): 239–47. February 2009. doi:10.1016/j.pain.2008.11.009. PMID 19118950. 
  4. ↑ "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. March 2010. doi:10.1097/ALN.0b013e3181cd7920. PMID 20179508. 
  5. ↑ "Pharmacological activation of 5-HT7 receptors reduces nerve injury-induced mechanical and thermal hypersensitivity". Pain 149 (3): 483–94. June 2010. doi:10.1016/j.pain.2010.03.007. PMID 20399562. 
  6. ↑ "Potentiation of morphine analgesia by adjuvant activation of 5-HT7 receptors". Journal of Pharmacological Sciences 116 (4): 388–91. August 2011. doi:10.1254/jphs.11039sc. PMID 21778664. 



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