View source for SB-269970

{{Short description|Chemical compound}}
{{Drugbox
| Verifiedfields = changed
| verifiedrevid = 407721350
| IUPAC_name = (2R)-1-[(3-Hydroxyphenyl)sulfonyl]-2 -(2-(4-methyl-1-piperidinyl)ethyl)pyrrolidine
| image = SB-269,970_structure.png
| width = 220
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<!--Identifiers-->
| IUPHAR_ligand = 3233
| CAS_number_Ref = {{cascite|correct|??}}
| CAS_number = 201038-74-6
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| PubChem = 6604889
| ChemSpiderID = 5037148
| ChEMBL = 282199
| ChEMBL_Ref = {{ebicite|changed|EBI}}
<!--Chemical data-->
| C=18 | H=28 | N=2 | O=3 | S=1
| smiles = CC2CCN(CC2)CCC1CCCN1S(=O)(=O)c(c3)cccc3O
| StdInChI = 1S/C18H28N2O3S/c1-15-7-11-19(12-8-15)13-9-16-4-3-10-20(16)24(22,23)18-6-2-5-17(21)14-18/h2,5-6,14-16,21H,3-4,7-13H2,1H3/t16-/m1/s1
| StdInChIKey = HWKROQUZSKPIKQ-MRXNPFEDSA-N
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'''SB-269970''' is a [[drug]] and research chemical developed by [[GlaxoSmithKline]] used in scientific studies. It is believed to act as a selective [[5-HT7|5-HT<sub>7</sub>]] [[receptor (biochemistry)|receptor]] [[Antagonist (pharmacology)|antagonist]] (EC<sub>50</sub> = 1.25 nM) (or possibly [[inverse agonist]]). A subsequent study in guinea pig at a concentration of 10&nbsp;μM showed that it also blocks the [[Alpha-2 adrenergic receptor|α<sub>2</sub>-adrenergic receptor]].<ref name="pmid15249157">{{cite journal | vauthors = Mahé C, Loetscher E, Feuerbach D, Müller W, Seiler MP, Schoeffter P | title = Differential inverse agonist efficacies of SB-258719, SB-258741 and SB-269970 at human recombinant serotonin 5-HT7 receptors | journal = European Journal of Pharmacology | volume = 495 | issue = 2–3 | pages = 97–102 | date = July 2004 | pmid = 15249157 | doi = 10.1016/j.ejphar.2004.05.033 }}</ref><ref name="pmid10669560">{{cite journal | vauthors = Lovell PJ, Bromidge SM, Dabbs S, Duckworth DM, Forbes IT, Jennings AJ, King FD, Middlemiss DN, Rahman SK, Saunders DV, Collin LL, Hagan JJ, Riley GJ, Thomas DR | display-authors = 6 | title = A novel, potent, and selective 5-HT(7) antagonist: (R)-3-(2-(2-(4-methylpiperidin-1-yl)ethyl)pyrrolidine-1-sulfonyl) phen ol (SB-269970) | journal = Journal of Medicinal Chemistry | volume = 43 | issue = 3 | pages = 342–5 | date = February 2000 | pmid = 10669560 | doi = 10.1021/jm991151j }}</ref><ref name="pmid19190523">{{cite journal | vauthors = Foong JP, Bornstein JC | title = 5-HT antagonists NAN-190 and SB 269970 block alpha2-adrenoceptors in the guinea pig | journal = NeuroReport | volume = 20 | issue = 3 | pages = 325–30 | date = February 2009 | pmid = 19190523 | doi = 10.1097/WNR.0b013e3283232caa | s2cid = 25499247 }}</ref> The large difference in test concentrations however confirms the selectivity of SB-269970 for the [[5-HT7|5-HT<sub>7</sub> receptor]].
SB-269970 is used to study the 5-HT<sub>7</sub> receptors which are thought to be involved in the function of several areas of the brain such as the [[hippocampus]] and [[thalamus]],<ref>{{cite journal | vauthors = Thomas DR, Hagan JJ | title = 5-HT7 receptors | journal = Current Drug Targets. CNS and Neurological Disorders | volume = 3 | issue = 1 | pages = 81–90 | date = February 2004 | pmid = 14965246 | doi = 10.2174/1568007043482633 }}</ref> and regulation of dopamine release in the [[ventral tegmental area]].<ref>{{cite journal | vauthors = Mnie-Filali O, Dahan L, Zimmer L, Haddjeri N | title = Effects of the serotonin 5-HT(7) receptor antagonist SB-269970 on the inhibition of dopamine neuronal firing induced by amphetamine | journal = European Journal of Pharmacology | volume = 570 | issue = 1–3 | pages = 72–6 | date = September 2007 | pmid = 17586491 | doi = 10.1016/j.ejphar.2007.05.037 }}</ref> Possible therapeutic uses for SB-269970 and other 5-HT<sub>7</sub> antagonists include the treatment of [[anxiety]] and [[Clinical depression|depression]],<ref>{{cite journal | vauthors = Hedlund PB, Huitron-Resendiz S, Henriksen SJ, Sutcliffe JG | title = 5-HT7 receptor inhibition and inactivation induce antidepressantlike behavior and sleep pattern | journal = Biological Psychiatry | volume = 58 | issue = 10 | pages = 831–7 | date = November 2005 | pmid = 16018977 | doi = 10.1016/j.biopsych.2005.05.012 | s2cid = 10998014 }}</ref><ref>{{cite journal | vauthors = Wesołowska A, Nikiforuk A, Stachowicz K, Tatarczyńska E | title = Effect of the selective 5-HT7 receptor antagonist SB 269970 in animal models of anxiety and depression | journal = Neuropharmacology | volume = 51 | issue = 3 | pages = 578–86 | date = September 2006 | pmid = 16828124 | doi = 10.1016/j.neuropharm.2006.04.017 | s2cid = 39928418 }}</ref> and [[nootropic]] effects have also been noted in animal studies.<ref>{{cite journal | vauthors = Gasbarri A, Cifariello A, Pompili A, Meneses A | title = Effect of 5-HT(7) antagonist SB-269970 in the modulation of working and reference memory in the rat | journal = Behavioural Brain Research | volume = 195 | issue = 1 | pages = 164–70 | date = December 2008 | pmid = 18308404 | doi = 10.1016/j.bbr.2007.12.020 | s2cid = 12910296 }}</ref><ref>{{cite journal | vauthors = Liy-Salmeron G, Meneses A | title = Effects of 5-HT drugs in prefrontal cortex during memory formation and the ketamine amnesia-model | journal = Hippocampus | volume = 18 | issue = 9 | pages = 965–74 | year = 2008 | pmid = 18570192 | doi = 10.1002/hipo.20459 | s2cid = 20937527 }}</ref>
==References==
{{Reflist}}
{{Serotonin receptor modulators}}
[[Category:5-HT7 antagonists]]
[[Category:3-Hydroxyphenyl compounds]]
[[Category:Pyrrolidines]]
[[Category:Piperidines]]
{{Antihypertensive-stub}}