SB-258719
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| Formula | C18H32N2O2S |
| Molar mass | 340.523 g/mol |
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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[edit]
- ^ 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.
- ^ 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.
- ^ 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.
- ^ 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.
- ^ 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.
- ^ 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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