Catalog Number: 3371
Chemical Name: (2S)-1-(3,4-Dihydro-6,7-dimethoxy-2(1H)-isoquinolinyl)-3,3-dimethyl-2-[(4-pyridinylmethyl)amino]-1-butanone hydrochloride
Biological Activity
Potent and selective OX2 receptor antagonist (IC50 = 40 nM). Displays >250-fold selectivity for OX2 over OX1 and a range of receptors, ion channels and transporters. Inhibits orexin A induced IP3 accumulation and ERK1/2 phosphorylation in CHO cells transfected with the OX2 receptor.
Technical Data
  • M.Wt:
    433.97
  • Formula:
    C23H31N3O3.HCl
  • Solubility:
    Soluble to 100 mM in water and to 25 mM in DMSO
  • Purity:
    >98%
  • Storage:
    Desiccate at +4°C
  • CAS No:
    372523-75-6
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. N-acyl 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline: The first orexin-2 receptor selective non-peptidic antagonist.
    Hirose et al.
    Bioorg.Med.Chem.Lett., 2003;13:4497
  2. Binding kinetics differentiates functional antagonism of orexin-2 receptor ligands.
    Mould et al.
    Br.J.Pharmacol., 2014;171:351
Citations:

The citations listed below are publications that use Tocris products. Selected citations for TCS OX2 29 include:

4 Citations: Showing 1 - 4
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  1. Both Ox1R and Ox2R orexin receptors contribute to the cardiorespiratory response evoked from the perifornical hypothalamus.
    Authors: Beig Et al.
    Clin.Exp.Pharmacol.Physiol. 2015;42:1059
  2. A role for hypocretin/orexin receptor-1 in cue-induced reinstatement of nicotine-seeking behavior.
    Authors: Plaza-Zabala Et al.
    J Mol Neurosci 2013;38:1724
  3. Central orexin (hypocretin) 2 receptor antagonism reduces ethanol self-administration, but not cue-conditioned ethanol-seeking, in ethanol-preferring rats.
    Authors: Brown Et al.
    Int.J.Neuropsychopharmacol. 2013;16:2067
  4. Orexins/hypocretins acting at Gi protein-coupled OX 2 receptors inhibit cyclic AMP synthesis in the primary neuronal cultures.
    Authors: Urbańska Et al.
    PLoS One 2012;46:42561

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