Catalog Number: 3818
Chemical Name: N-[1,1'-Biphenyl]-2-yl-1-[2-[(1-methyl-1H-benzimidazol-2-yl)thio]acetyl-2-pyrrolidinedicarboxamide
Biological Activity
Potent, dual orexin receptor antagonist (Ki values are 0.2 and 3 nM for OX2 and OX1 receptors respectively). Inhibits ADL-orexin B-mediated locomotion following i.p. administration in vivo and blocks orexin-A (Cat.No.1455) mediated increases in feeding behaviour. Brain penetrant.
Technical Data
  • M.Wt:
    470.59
  • Formula:
    C27H26N4O2S
  • Solubility:
    Soluble to 100 mM in DMSO and to 100 mM in ethanol
  • Purity:
    >98%
  • Storage:
    Store at RT
  • CAS No:
    916141-36-1
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.
Additional Information
Licensing Caveats:
Manufactured and sold under license from Merck & Co., Inc. for use solely for preclinical research purposes (ie: not for administration to or other use in humans)
Background References
  1. Orexin receptor antagonism prevents transcriptional and behavioral plasticity resulting from stimulant exposure.
    Winrow et al.
    Neuropharmacology, 2010;58:185
  2. Proline bis-amides as potent dual orexin receptor antagonists.
    Bergman et al.
    Bioorg.Med.Chem.Letts, 2008;18:1425
  3. The dual orexin receptor antagonist TCS1102 does not affect reinstatement of nicotine-seeking.
    Khoo et al.
    PLoS One, 2017;12
Citations:

The citations listed below are publications that use Tocris products. Selected citations for TCS 1102 include:

3 Citations: Showing 1 - 3
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  1. The dual orexin receptor antagonist TCS1102 does not affect reinstatement of nicotine-seeking.
    Authors: Khoo Et al.
    PLoS One 2017;
  2. Blocking of orexin receptors in the paraventricular nucleus of the thalamus has no effect on the expression of conditioned fear in rats.
    Authors: Dong Et al.
    Front Behav Neurosci 2015;9:161
  3. Calcium affects OX1 orexin (hypocretin) receptor responses by modifying both orexin binding and the signal transduction machinery.
    Authors: Putula Et al.
    Br J Pharmacol 2014;171:5816

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