SB-258,719

SB-258,719
(IUPAC) ime
	(1R)-3,N-dimetil-N-[1-metil-3-(4-metilpiperidin-1-il)propil]benzenesulfonamid
Klinički podaci
Identifikatori
CAS broj	195199-95-2
ATC kod	nije dodeljen
PubChem	5312148
ChemSpider	4471578
ChEMBL	CHEMBL12264
Hemijski podaci
Formula	C18H32N2O2S
Mol. masa	340,523 g/mol
SMILES	eMolekuli & PubHem
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
Farmakoinformacioni podaci
Trudnoća	?
Pravni status

SB-258,719 je lek koji deluje kao selektivni parcijalni inverzni agonist 5-HT₇ receptora.^[5] On je bio prvi identifikovani antagonist 5-HT₇ receptora.^[6] 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.^[7]^[8]^[9]^[10]

Reference

↑ Li Q, Cheng T, Wang Y, Bryant SH (2010). „PubChem as a public resource for drug discovery.”. Drug Discov Today 15 (23-24): 1052-7. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519. edit
↑ Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). „Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities”. Annual Reports in Computational Chemistry 4: 217-241. DOI:10.1016/S1574-1400(08)00012-1.
↑ Hettne KM, Williams AJ, van Mulligen EM, Kleinjans J, Tkachenko V, Kors JA. (2010). „Automatic vs. manual curation of a multi-source chemical dictionary: the impact on text mining”. J Cheminform 2 (1): 3. DOI:10.1186/1758-2946-2-3. PMID 20331846. edit
↑ Gaulton A, Bellis LJ, Bento AP, Chambers J, Davies M, Hersey A, Light Y, McGlinchey S, Michalovich D, Al-Lazikani B, Overington JP. (2012). „ChEMBL: a large-scale bioactivity database for drug discovery”. Nucleic Acids Res 40 (Database issue): D1100-7. DOI:10.1093/nar/gkr777. PMID 21948594. 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. PMID 21778664.

Spoljašnje veze

	Portal Medicina
	Portal Hemija

[1] Li Q, Cheng T, Wang Y, Bryant SH (2010). „PubChem as a public resource for drug discovery.”. Drug Discov Today 15 (23-24): 1052-7. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519. edit

[2] Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). „Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities”. Annual Reports in Computational Chemistry 4: 217-241. DOI:10.1016/S1574-1400(08)00012-1.

[3] Hettne KM, Williams AJ, van Mulligen EM, Kleinjans J, Tkachenko V, Kors JA. (2010). „Automatic vs. manual curation of a multi-source chemical dictionary: the impact on text mining”. J Cheminform 2 (1): 3. DOI:10.1186/1758-2946-2-3. PMID 20331846. edit

[4] Gaulton A, Bellis LJ, Bento AP, Chambers J, Davies M, Hersey A, Light Y, McGlinchey S, Michalovich D, Al-Lazikani B, Overington JP. (2012). „ChEMBL: a large-scale bioactivity database for drug discovery”. Nucleic Acids Res 40 (Database issue): D1100-7. DOI:10.1093/nar/gkr777. PMID 21948594. edit

[pmid15249157-5] 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.

[pmid9513592-6] 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.

[pmid19118950-7] 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.

[pmid20179508-8] 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.

[pmid20399562-9] 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.

[pmid21778664-10] 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. PMID 21778664.

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