ChemSpider 2D Image | SB-269970 | C18H29ClN2O3S

SB-269970

  • Molecular FormulaC18H29ClN2O3S
  • Average mass388.953 Da
  • Monoisotopic mass388.158752 Da
  • ChemSpider ID10131932

  • defined stereocentres - 1 of 1 defined stereocentres

More details:

Validated by Experts, Validated by Users, Non-Validated, Removed by Users

(R)-3-[2-[2-(4-Methylpiperidin-1-yl)ethyl]pyrrolidine-1-sulfonyl]phenol hydrochloride
201038-74-6 [RN]
261901-57-9 [RN]
3-({(2R)-2-[2-(4-Methyl-1-piperidinyl)ethyl]-1-pyrrolidinyl}sulfonyl)phenol hydrochloride (1:1) [ACD/IUPAC Name]
3-({(2R)-2-[2-(4-Méthyl-1-pipéridinyl)éthyl]-1-pyrrolidinyl}sulfonyl)phénol, chlorhydrate (1:1) [French] [ACD/IUPAC Name]
3-({(2R)-2-[2-(4-Methyl-1-piperidinyl)ethyl]-1-pyrrolidinyl}sulfonyl)phenolhydrochlorid (1:1) [German] [ACD/IUPAC Name]
3-({(2R)-2-[2-(4-Methylpiperidin-1-yl)ethyl]pyrrolidin-1-yl}sulfonyl)phenol hydrochloride (1:1)
3-[(2R)-2-[2-(4-METHYLPIPERIDIN-1-YL)ETHYL]PYRROLIDIN-1-YLSULFONYL]PHENOL HYDROCHLORIDE
3-{[(2R)-2-[2-(4-METHYLPIPERIDIN-1-YL)ETHYL]PYRROLIDIN-1-YL]SULFONYL}PHENOL HYDROCHLORIDE
MFCD03788020 [MDL number]
More...

Validated by Experts, Validated by Users, Non-Validated, Removed by Users

EU-0101059 [DBID]
S7389_SIGMA [DBID]
  • References
  • Experimental Physico-chemical Properties
  • Miscellaneous

    • Safety:

      Sold for research purposes under agreement from GlaxoSmithKline. Tocris Bioscience 1612

    • Bio Activity:

      5-HT Receptor MedChem Express HY-15370A
      5-HT Receptors Tocris Bioscience 1612
      5-HT7 Receptors Tocris Bioscience 1612
      7-TM Receptors Tocris Bioscience 1612
      Biochemicals & small molecules/Antagonists & inhibitors Hello Bio HB1684
      GPCR/G protein MedChem Express HY-15370A
      GPCR/G protein; Neuronal Signaling; MedChem Express HY-15370A
      Potent and selective 5-HT<sub>7</sub> receptor antagonist. Selective for for 5-HT<sub>7A</sub> over 5-HT<sub>5A</sub> and 5-HT<sub>1B</sub> (pK<sub>i</sub> values are 8.9, 7.2 and 6.0 respectively). Inhibits hyperactivity induced by amphetamine and ketamine. Blood-brain barrier permeable. Hello Bio HB1684
      Potent and selective 5-HT7 antagonist; brain penetrant Tocris Bioscience 1612
      Potent and selective 5-HT7 receptor antagonist (pKi values are 8.9, 7.2 and 6.0 for 5-HT7A, 5-HT5A and 5-HT1B and < 6.0 for 5-HT1A, 5-HT1D, 5-HT1E, 5-HT1F, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT4 and 5-HT6 rece ptors respectively). Brain penetrant in vivo. Tocris Bioscience 1612
      Potent and selective 5-HT7 receptor antagonist (pKi values are 8.9, 7.2 and 6.0 for 5-HT7A, 5-HT5A and 5-HT1B and < 6.0 for 5-HT1A, 5-HT1D, 5-HT1E, 5-HT1F, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT4 and 5-HT6 receptors respectively). Brain penetrant in vivo. Tocris Bioscience 1612
      Potent, selective 5-HT<sub>7</sub> receptor antagonist Hello Bio HB1684
      Receptors & Transporters/G protein coupled receptors/5-HT/5-HT<sub>7</sub> Hello Bio HB1684
      SB269970 hydrochloride is a hydrochloride salt form of SB-269970, which is a 5-HT7 receptor antagonist with pKi of 8.3, exhibits MedChem Express http://www.medchemexpress.com/oc000459.html
      SB269970 hydrochloride is a hydrochloride salt form of SB-269970, which is a 5-HT7 receptor antagonist with pKi of 8.3, exhibits >50-fold selectivity against other receptors.; IC50 Value: 8.3 (pKi for 5-HT7) [1]; Target: 5-HT7 receptor; in vitro: 5-CT-stimulated adenylyl cyclase activity in guinea-pig hippocampal membranes (pEC(50) of 8.4+/-0.2) was inhibited by SB-269970-A (0.3 microM) with a pK(B) (8.3+/-0.1) in good agreement with its antagonist potency at the human cloned 5-HT(7(a)) receptor and its binding affinity at guinea-pig cortical membranes. MedChem Express HY-15370A
      SB269970 hydrochloride is a hydrochloride salt form of SB-269970, which is a 5-HT7 receptor antagonist with pKi of 8.3, exhibits >50-fold selectivity against other receptors.;IC50 Value: 8.3 (pKi for 5-HT7) [1];Target: 5-HT7 receptor;In vitro: 5-CT-stimulated adenylyl cyclase activity in guinea-pig hippocampal membranes (pEC(50) of 8.4+/-0.2) was inhibited by SB-269970-A (0.3 microM) with a pK(B) (8.3+/-0.1) in good agreement with its antagonist potency at the human cloned 5-HT(7(a)) receptor and its binding affinity at guinea-pig cortical membranes. 5-HT(7) receptor mRNA was highly expressed in human hypothalamus, amygdala, thalamus, hippocampus and testis [1]. Cortical slices were loaded with [(3)H]-5-HT and release was evoked by electrical stimulation. 5-CT inhibited the evoked release of [(3)H]-5-HT in a concentration-dependent manner. SB-269970 had no significant effect on [(3)H]-5-HT release while the 5-HT(1B) receptor antagonist, SB-224289 significantly potentiated [(3)H]-5- MedChem Express HY-15370A

Predicted data is generated using the ACD/Labs Percepta Platform - PhysChem Module, version: 14.00

No predicted properties have been calculated for this compound.

Click to predict properties on the Chemicalize site


Advertisement