SB-216641 explained

SB-216641 is a drug which is a selective antagonist for the serotonin receptor 5-HT1B, with around 25x selectivity over the closely related 5-HT1D receptor.[1] It is used in scientific research,[2] [3] [4] and has demonstrated anxiolytic effects in animal studies.[5] [6]

Notes and References

  1. Price GW, Burton MJ, Collin LJ, Duckworth M, Gaster L, Göthert M, Jones BJ, Roberts C, Watson JM, Middlemiss DN . 6 . SB-216641 and BRL-15572--compounds to pharmacologically discriminate h5-HT1B and h5-HT1D receptors . Naunyn-Schmiedeberg's Archives of Pharmacology . 356 . 3 . 312–20 . September 1997 . 9303567 . 10.1007/PL00005056 . 26760453 .
  2. Matsuoka T, Hasuo H, Akasu T . 5-Hydroxytryptamine 1B receptors mediate presynaptic inhibition of monosynaptic IPSC in the rat dorsolateral septal nucleus . Neuroscience Research . 48 . 3 . 229–38 . March 2004 . 15154669 . 10.1016/j.neures.2003.11.004 . 35850798 .
  3. Yan QS, Zheng SZ, Yan SE . Involvement of 5-HT1B receptors within the ventral tegmental area in regulation of mesolimbic dopaminergic neuronal activity via GABA mechanisms: a study with dual-probe microdialysis . Brain Research . 1021 . 1 . 82–91 . September 2004 . 15328035 . 10.1016/j.brainres.2004.06.053 . 46700479 .
  4. Lee JJ, Hahm ET, Lee CH, Cho YW . Serotonergic modulation of GABAergic and glutamatergic synaptic transmission in mechanically isolated rat medial preoptic area neurons . Neuropsychopharmacology . 33 . 2 . 340–52 . January 2008 . 17392733 . 10.1038/sj.npp.1301396 . free .
  5. Tatarczyńska E, Kłodzińska A, Stachowicz K, Chojnacka-Wójcik E . Effects of a selective 5-HT1B receptor agonist and antagonists in animal models of anxiety and depression . Behavioural Pharmacology . 15 . 8 . 523–34 . December 2004 . 15577451 . 10.1097/00008877-200412000-00001 . 6940756 .
  6. Chojnacka-Wójcik E, Kłodzińska A, Tatarczyńska E . The anxiolytic-like effect of 5-HT1B receptor ligands in rats: a possible mechanism of action . The Journal of Pharmacy and Pharmacology . 57 . 2 . 253–7 . February 2005 . 15720791 . 10.1211/0022357055399 . 20743875 .

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